ABSTRACT

The idea that led to this review was conceived after some investigations we carried out showed that solid lipid microparticles (SLMs) have very good prospects as a good and an effective alternative to the traditional colloidal carrier systems like liposomes, emulsions and polymeric microparticles, for the encapsulation, targeting and controlled delivery of drugs and other actives. This was corroborated by reports from several researchers working in other laboratories. Hence, the review aims at showing that SLMs are at the forefront of the rapidly developing field of lipid-based drug delivery and technology with several potential applications in drug delivery, clinical medicine and research. This review presents the various formulation techniques applied as well as relevant issues such as factors considered in drug encapsulation and loading capacity of SLMs, and methods of characterization of SLMs are treated. The important routes of administration of SLMs and examples of candidate drugs incorporated and administered through such routes as well as the various ways SLMs have been applied in drug delivery and clinical medicine. Future areas of research interest are also highlighted. From reported evidences available, SLMs could serve as a good alternative and acceptable method for the controlled delivery of various drug candidates for therapeutic and diagnostic (theranostic) purposes.

Keywords: Solid lipid Microparticles, Drug Delivery, Lipid-based, Drug Encapsulation, Loading Capacity, Drug Entrapment.

ABSTRACT

This review highlights the recent development and achievements made for the micropropagation of Stevia rebaudiana Bertoni (an antidiabatic sweetener herb) in Hadoti region of south-east Rajasthan. Shootlets were regenerated from nodal explants of stem through auxiliary shoot proliferation. The induction of multiple shoots from nodal segments was the highest in MS medium supplemented with 0.5 mg/l BAP+0.5 mg/l Kn. For rooting different concentration of IBA were used and highest rooting was recorded on MS medium with 0.5 mg/l IBA. The rooted Plantlets were hardened initially in culture room conditions and then transferred to misthouse. Leaf petiole explants were used for the purpose of callus induction. Best growth was observed in MS medium supplemented with 0.25 mg/l 2, 4-D+ 0.5 mg/l Kn and 0.25 mg/l 2,4-D+ 0.5mg/l BAP.

Keywords: - Anti diabetic, micropropagation, shoot multiplication sweetener. 

ABSTRACT

Osteoarthritis (OA) is a group of chronic, painful, disabling condition affecting synovial joints. OA is the most common among elderly people. Approximately 80% of population above 65 years of age suffers from OA and this value reaches near to 100% with increasing age. Currently available treatments of OA provide symptomatic relief or slow the progression of disease. The oral or parenteral administration of these drugs causes serious systemic side effects leading to even withdrawal of certain drugs from market. To overcome these problems, localized IA drug delivery presents a new hope. A number of drugs have been investigated for their local effect after IA administration. A number of novel drug delivery systems are available for their own merits and demerits. This review discusses the pathophysiology of OA and formulation consideration of IA injections along with details of current and novel drug formulation for OA treatments.

Keywords: Osteoarthritis, Intraarticular, Microparticles, Liposomes, Nanoscaffolds

ABSTRACT

Buccal administration of drug provides a convenient route of administration for both systemic and local drug actions. The preferred site for retentive oral transmucosal delivery systems and for sustained and controlled release delivery device is the buccal mucosa. Rapid developments in the field of molecular biology and gene technology resulted in generation of many macromolecular drugs including peptides, proteins, polysaccharides and nucleic acids in great number possessing superior pharmacological efficacy with site specificity and devoid of untoward and toxic effects. However, the main impediment for the oral delivery of such drugs as potential therapeutic agents is their extensive presystemic metabolism, instability in acidic environment resulting into inadequate and erratic oral absorption. Direct access to the systemic circulation through the internal jugular vein bypasses drug from the hepatic first pass metabolism leading to high bioavailability. The objective of this article is to review the developments in buccal adhesive drug delivery system as patches.

Keywords: Buccal mucosa, buccal patches, mucoadhesion, permeation.

ABSTRACT

Men spend about one-third of their lives asleep and sleep is responsible for memory, emotion, perception, thought, judgement and even consciousness. Sleep is not only responsible for maintenance of healthy life but also for establishment of homeostasis in biological system. Sleep deprivation is a stressor affecting the brain as well as many body systems and researchers are continuously working to understand the sleep architecture and various substances which affect sleep. Wakefulness and sleep-wake-regulation are complex states, a lot of different components and regulatory mechanisms contribute to these functions. One of the factors involved in sleep wake regulation is the immune system particularly cytokines. Interleukin-1 is a pleotrophic cytokine, serving both physiological and pathological functions including modulation of memory, mood, inflammation, appetite, brain development and sleep. This article reviews and try to elaborate various downstream pathways and mediators involved in influence of cytokines on sleep architecture.

Keywords: Sleep, cytokines, Interleukin-1, REM and NREM

ABSTRACT

Leeches are blood sucking worms that have been used in medicine as far back as 2500 years ago. The word leech comes from an old English word ‘laece’ meaning ‘physician’. The spelling later became leech.  In medieval England, leeches were linked with healing because of the etymology of the word. In old English the word “lacian” meant to heal and physicians were known as “leche”. Leeches are annelids or segmented worms. All leeches have 34 body segments. In medieval and early modern medicine, the medicinal leech- Hirudo medicinalis and its congeners was used to remove blood from a patient as part of a process to “balance” the “humours”. Hirudotherapy was introduced by Ibne Sina in the Canon of Medicine (1020s). He considered the application of leech to be more useful than cupping in “letting of the blood from deeper parts of the body”. The secretion of leech saliva contains like Hirudine, Histamine, Hyluronidase, Collgenase, Fibrinases, Hementin, Bdellin, Eglins, Elastase, Cathepsin, Inhibitor of Kellikerin, Anesthetics, Protinase inhibitor, Tryptase inhibitor, Antibacterial.

Key words: Leeches, Hirudotherapy, humours, Hirudine, Histamine, Hyluronidase

ABSTRACT

Alzheimer’s disease is the most prevalent form of dementia. Neuropathogenesis is proposed to be a result of the accumulation of amyloid β- peptides in the brain together with oxidative stress mechanisms and neuroinflammation. Drugs effective in Alzheimer’s disease (AD) should have several aims: to improve the cognitive impairment, control the behavioral and neurological symptoms, delay the progression of the disease, and prevent the onset. This review discusses the molecular mechanism of Alzheimer’s disease with a focus on the different agents those are inhibit the progression of the disease and improved patients condition and status..

Key words: Alzheimer’s disease, β-amyloid, Tacrine, Rivastigmine

ABSTRACT

Bioadhesion can be defined as the process by which a natural or a synthetic polymer can adhere to a biological substrate. When the biological substrate is a mucosal layer then the phenomena is known as mucoadhesion. The substrate possessing bioadhesive property can help in devising a delivery system capable of delivering a bioactive agent for a prolonged period of time at a specific delivery site. The current review  provides  a good insight on mucoadhesive polymers, the phenomenon of mucoadhesion and the factors which have the ability to affect the mucoadhesive properties of a polymer. This review also considers the basic mechanisms by which mucoadhesive can adhere to a mucous membrane  in terms of the nature of the adhering surfaces and the forces that may be generated to secure them together. Mucosal adhesion is backed by several theories which include electronic, adsorption, wetting, diffusion, fracture and mechanical. Stages of mucoadhesion include contact stage and consolidation stage.

Keywords: Mucosa, mucoadhesion, mucoadhesive polymers, drug delivery.

ABSTRACT

Pharmacometrics has retained its status in modern pharmacological research. Isolated tissue experiments form an important part of experimental pharmacology. Contractions of isolated tissues are very often recorded by using a recording device and a smoked paper. The key feature of having a good record is to minimize the friction between the smoked paper and the writing point of the recording device. Different types of writing points are in use despite of their disadvantages. We have developed a device to have a writing point from used refill ball point. In our experience, this simple modification improves the recordings of isolated tissue experiments.

Keywords: Pointers, isotonic contractions, recordings

ABSTRACT

Over the years, different formulation technologies for gastroretentive dosage delivery were investigated and patented. Well-designed controlled drug delivery system can overcome the problems of conventional therapy and enhance the therapeutic efficacy of a drug. There are various approaches in delivering a therapeutic substance to target site in a sustained controlled release fashion. One such approach is using multiparticulate as carriers for drugs. Such systems have advantages over single-unit dosage forms as they avoid the all-or-none gastric emptying nature of single-unit systems. However, multiparticulate dosage forms are gaining favor because of potential benefits like predictable gastric emptying, no risk of dose dumping, flexible release patterns and increased bioavailability with less inter- and intra-subject variability. The purpose of writing this review on method of prepare floating multiparticulate is to compile the recent literature with special focus on the classification and formulation aspects, principal mechanism of floatation to achieve gastric retention, characterization of floating multiparticulate system.

Keywords- multiparticulate system, design and method of preparation, floating microspheres, beads, granules.

ABSTRACT

Medicated chewing gum (MCG) is a drug delivery system that consists of an active ingredient incorporated into a chewing gum and released by the mechanical action of chewing. The first Medicated chewing gum product.‘ Aspergum’, which contained acetyl salicylic acid for headaches, was launched in 1928. Medicated chewing gum is a good vehicle for administering active ingredients in pharmaceuticals and nutraceuticals. It offers a highly convenient, patient-compliant way of dosing medications, particularly for people with swallowing difficulties such as children and the elderly. It is also an ideal dosage form for drugs that help cure or relieve oral diseases, including toothache, periodontal disease, bacterial and fungal infections, and aphthous and dental stomatitis. Medicated chewing gum containing chlorhexidine is used to treat inflammatory conditions such as gingivitis. Using the medicated chewing gum formulation, the revitalization of old products and the reformulation of new patented products will differentiate them from upcoming generics competition. Thus, the potential of Medicated chewing gum for direct systemic delivery with higher patient compliance, its fast onset of action and the opportunity for product-line extension make it a likely drug delivery system.

Keywords- Medicated chewing gum (MCG), periodontal disease, gingivitis, patient compliance

ABSTRACT

This present review is progress in selected nanotechnology topics and some possible applications. This attempt mainly focused on Different Classes of Nanoparticles (Ceramic nanoparticles, Metallic particles, Carbon nanomaterials, Quantum dots) and Applications of Nanotechnology in Pharmaceuticals (Diagnosis, Pharmacology and Therapy, Molecular Diagnosis) and Nanoparticle Drug Delivery Systems and Toxicity of Nanoparticles. Nanoparticles mainly use aims to minimize drug degradation upon administration, prevent undesirable side effects, and increase drug bioavailability and the fraction of the drug accumulated in the pathological area.

Keywords: Nanoparticles, Applications, Toxicity, Nanotechnology.

ABSTRACT

One of the challenges faced by scientific community is that of adverse and deterioting side effects of psychotropic agents, which are popularly known as neuroleptic induced extrapyramidal adverse effects. Neuroleptic induced movement disorders pose a significant burden to patients, often resulting in non-adherence, disease relapse, and decreased quality of life. Evidence indicates that drugs which potentiate or attenuate neuroleptic induced catalepsy in rodents might aggravate or reduce the extrapyramidal signs respectively in human beings. It is being appreciated that many plant drugs can be explored for their protective nature against such adverse and toxic effects on account of their ascribed effects.

Keywords: Neuroleptic, Catalepsy, Unani medicine, Extrapyramidal, Dopamine

ABSTRACT

Unique properties of Nanofibers have attracted for the designing of controlled drug delivery systems due to high surface area to volume ratio, porosity so only we can applied in advance application such as Biodegradable and controlled drug delivery systems. The benefits of the fibrous carriers are site specific delivery of drugs to the body. Nanofibers are an exciting new class of material produced using an innovative manufacturing process technology. These fibers are produced from a variety of polymers in geometrical shapes ranging from Nonwoven web, yarn, and bulk structures. The Synthetic polymer Nanofibers are made from Nylon, Acrylic, Polycarbonate, Polysulfones, and Fluro polymers among other polymers. The biological polymer nanofibers are made from materials such as Polycaprolactum, Chitosan, Polylactic acid, and Copolymer of Polylactic/glycolic acid among other biopolymers. At present, there are three techniques available for the synthesis of Nanofibers: Electro spinning, self-assembly, and phase separation, out of these Electro spinning is the most widely used technique. Mostly , the bioactive molecules like anti-cancer drugs, enzymes. Cytokines, and polysaccharides can be entrapped within the interior or physically immobilized on the surfaces of nanofiber for controlled drug delivery. The advanced approach for creating Nanofibers made of proteins developed, greatly improve drug delivery methods for the treatment of cancers, heart, and Alzheimer’s diseases, as well as aid in the regeneration of human tissue, bone and cartilage. This review paper reports on fabrication of nanofibers and its characteristics and high tech application in drug delivery, tissue engineering and filter medium.

Keywords: Electro spinning, controlled drug delivery, Fabrication, characterization, applications.

ABSTRACT

In the last few decades there has been an exponential growth in the field of herbal medicine. Herbal medicines have been the basis of treatment and cure for various diseases and physiological conditions in traditional methods of practice such as Ayurveda, Unani and Siddha. Medicinal components from plants play an important role in conventional as well as western medicine. They were the sole source of active principles capable of curing man’s ailments. Thus natural products have been a major source of drugs for centuries. Mimusops elengi, commonly called ‘Bakul’ is a medicinally important plant of family sapotaceae. All parts of the plant including stem, bark, leaves, fruit, root and seeds in all stages of their maturity have medicinal properties. Taking into consideration the medicinal importance of the plant, the present review has made to explore the phytochemical and pharmacological potential of Mimusops elengi.

Keywords: Mimusops elengi, bakul, phytochemical, pharmacological

ABSTRACT

The advent of highly active antiretroviral (ARV) agents has led to striking reduction in plasma viral load, opportunistic infection and mortality from AIDS. Unfortunately most of these drugs have poor physiochemical, metabolism or transport properties that result in poor or variable absorption and side effects, which are often related to the accumulation of the drug at inappropriate sites. Various classes of antiretroviral agents are available, though monotherapy in HIV positive individuals can develop resistance more quickly as compared to combinational therapy or fixed dose combination or highly active antiretroviral therapy. The currently available ARV drugs mostly oral formulations, which are associated with several disadvantages and inconveniences to the HIV patients. The delivery of drugs via oral route suffers from significant first-pass effect, variation of absorption and degradation in the gastrointestinal, erratic bioavailability, limited duration of drug action, metabolism/elimination and transport barriers reducing the effect of anti-HIV drugs reaching the target site. Also half-life of several ARV drugs is short, which requires frequent administration of doses leads to poor patient compliance. Therefore, the usage of novel drug delivery systems is a logical approach to circumvent these problems and effectively treat the HIV infection. Various novel drug delivery techniques were tried or on trial for ARV drugs. Among the recent approaches of novel drug delivery system for anti-HIV drugs, controlled/sustained and targeted/intracellular drug delivery are the important ones. In this review the need for novel drug delivery, advantages, and recent development in drug delivery system of antiretroviral drugs were discussed, which may useful for further research in future.

Keywords: AIDS, HIV, Antiretroviral therapy, Novel drug delivery systems

ABSTRACT

The aim of this study is to present a Quick and Easy formula for the calculations of percent spike recovery of drug samples. Currently there are several cumbersome methods used in the determination of percent spike recovery in pharmaceutical analyses performed in various laboratories including the FDA laboratories around the world and especially in USA. In this paper we have compared the Quick & Easy Method using Pal’s formula against the method suggested by ORA Manual. The efficacy of this new formula has been demonstrated by seven examples including the main example of Pilocarpine hydrochloride discussed in detail. This Quick & Easy method is very simple, efficient and convenient way of determining percent spike recoveries and RPD values of duplicate spike solutions in drug analyses by HPLC, GC or UV methods. The simplicity of the method saves time and effort when compared to the existing method

Keywords: Pal’s formula, ORA Manual

ABSTRACT

The present study was carried out to evaluate subacute toxicity of a hydroethanolic extract of Solenostemon monostachyus (Esomo) in mice. Four groups of six mice were orally treated with Esomo at 0, 500, 1000 and 2000 mg /kg b.w. for 28 days and hematological, biochemical parameters and histopathological study carried out after experimental period. The control group of mice received saline solution.Subacute administration of Esomo did not exert any significant variation on body and organs weights, on food and water intake. This treatment did not show any change in hematological parameters such as erythrocytes and leukocytes count, hemoglobin concentration, hematocrit and mean corpuscular volume. Histopathological analysis and clinical blood chemistry parameters revealed no toxic effects of the extract. However, at doses of 1000 and 2000 mg/kg b.wEsomo induced thrombocytopenia. Our results exhibit that the extract of S. monostachyus is not devoid of toxicity.

Keywords: Solenostemon monostachyus, subacute toxicity, haematological parameters, clinical blood chemistry and histopathological study.

ABSTRACT

Mixture of three compounds lupeol acetate (1), alpha amyrin acetate(2) and beta amyrin acetate(3) were isolated from the methanolic extract of the stem bark of Artocarpus lackoocha Roxb.(Family: Moraceae).The crude methanol extract as well as its petroleum ether, carbon tetrachloride; chloroform and aqueous soluble Kupchan fractions were studied for antioxidant, antimicrobial and cytotoxic activities. Among the different fractions tested for antioxidant activity, the aqueous soluble partitionate was the most potent with IC50 value of 3.47μg/ml as compared to tertbutyl-1-hydroxytoluene (IC50=27.54μg/ml). Antimicrobial screening of the different extractives was conducted by the disc diffusion method and the crude methanol extract as well as aqueous soluble fractions exhibited moderate antimicrobial activity with zone of inhibition ranging from 7-12 mm. In brine shrimp lethality bioassay, the aqueous soluble materials demonstrated the highest toxicity with LC50 of 1.6μg/ml. β-amyrin acetate is the first report of isolation of compounds from Artocarpus lackoocha.

Keywords: Artocarpus lackoocha, chemical constituents, antioxidant, antimicrobial, cytotoxicity.

ABSTRACT

Acne is a disease appearing simple but chronic in nature with multiple causative factors like bacteria, inflammation, harmones etc. The present study was conducted to formulate and evaluate the topical anti acne formulation of coriander aqueous extract. The antibacterial activity of aqueous extract against Propionibacterium acne (P. acne) and Staphylococcus epidermidis(S. epidermidis)  was investigated using disc diffusion method and minimum inhibitory concentration was determined by agar dilution method. The results showed that coriander aqueous extract showed the MIC values of 1.7 mg/ml and 2.1 mg/ml against P.acne and S. epidermidis respectively. The zone of inhibition exhibited by the aqueous extract was 21.5±1.4mm and 20.6±1.09mm against P. acne and S. epidermidis respectively. The topical formulations were developed using menthol as the penetration enhancer and tested for physical parameters, drug content uniformity, spreadibility, extrudability and in-vitro diffusion. It was reveled from the results that all the formulations showed the increased zone of inhibition for both of the bacteria. The formulations with the addition of penetration enhancer showed the increased drug content as well as the invitro release which increased with increase in the concentration of menthol. The formulation Fa₁₁ showed the drug content (97.9%), invitro- diffusion (96.8%) and maximum stability among all the formulations.

Keywords: Acne vulgaris, antibacterial activity, coriander, penetration enhancer, in-vitro activity.

ABSTRACT

The objective of this study was to develop self-emulsifying drug delivery system (SEDDS) to enhance the solubility of the poorly water-soluble drug Orlistat. Orlistat is class II molecule according to BCS (Biopharmaceutical Classification System), having low solubility and low permeability. The rate and extent of absorption of class II compounds is highly dependent on the performance of the formulated product. These drugs can be successfully formulated for oral administration, but care needs to be taken with formulation design to ensure consistent bioavailability. Solubility of Orlistat was evaluated in various nonaqueous carriers that included oils, surfactants, and cosurfactants. Pseudoternary phase diagrams were constructed to identify the self-microemulsification region. Self microemulsifying formulations were prepared using mixtures of oils, surfactants, and cosurfactants in various proportions. The self microemulsification properties, droplet size and thermodynamic stability of these formulations were studied upon dilution with water. The optimized liquid SMEDDS formulation was converted into free flowing powder by adsorbing onto a solid carrier for encapsulation. The dissolution characteristics of solid intermediates of SMEDDS filled into hard gelatin capsules were investigated and compared with pure drug and commercial formulation. The results indicated that solid intermediates showed the rate and extent of drug dissolution for solid intermediates were significantly higher than commercial formulation. The results of the study demonstrated the potential use of SMEDDS as a means of improving solubility, dissolution and concomitantly the bioavailability.

Keywords: Lipid formulations, Particle size, SMEDDS, Solubility, Orlistat

ABSTRACT

An accurate, simple, precise and sensitive HPLC method with UV detection was developed and validated to separate and detect ibuprofen in human plasma using Nimesulide as an internal standard. Ibuprofen and Nimesulide were extracted from human plasma using acetonitrile protein precipitation and HPLC analysis was performed using Waters 515 Series pumps combined with a Waters PDA 2998 series photo diode array detector (DAD). The column used was Agilent C18 column (150mm×4.6mm, particle size 5-micron Agilent, USA). Analysis was isocratic at 1.5 ml/min flow rate with ACN: Buffer (0.025M Potassium dihydrogen ortho phosphate) pH 4.5 (55:45, v/v) as mobile phase. The mobile phase was premixed, filtered through a 0.2 µm nylon membrane filter to remove any particulate matter and degassed by sonication before use. The elution was detected at 230 nm. Each solution was injected in triplicate, and the relative standard deviation (R.S.D.) was measured. The retention times of Ibuprofen 2.24 min and for I.S. 1.72 min respectively. The method was validated over the range of 0.5-8.0 μ/ml. The limit of detection was 0.06μg/ml and the limit of quantification was 0.193μg/ml for ibuprofen. Inter-day as well intra-day replicates of Ibuprofen, gave % R.S.D. below 2.07 and 2.001 respectively  The absolute recovery of ibuprofen was greater than 90% were achieved. This method of analysis for Ibuprofen determination using RP-HPLC was applied for determination of Ibuprofen in plasma.

Keywords: Bio-analytical method, Plasma Extraction, Ibuprofen, Nimesulide, HPLC, ICH.

ABSTRACT

Naproxen is a non-steroidal anti-inflammatory drug (NSAID) commonly used for the reduction of mild to moderate pain, fever, inflammation and stiffness caused by conditions such as osteoarthritis, rheumatoid arthritis, psoriatic arthritis, gout, ankylosing spondylitis, injury, menstrual cramps, tenditis, bursitis and the treatment of primary dysmenorrheal. The reason behind incorporation of Naproxen in Niosomes as this non-ionic surfactants vesicles offer several advantages over other drug carriers like liposome with respect to its biocompatibility, simple and controllable preparation, their capacity to carry large amount of drug, commercially availability, capable of entrapping hydrophilic and hydrophobic drug, cheaper in cost, any special condition not require for the use of the surfactant. The niosome system which achieves the site specific delivery of drug with controlled release kinetics of drug in predictable manner. Before this preparation, prior preparations had been made known as Pro-niosomes with Cholesterol, Surfactant, and Ethanol which later on converting to Niosomes. 

Keywords: - Cholesterol, Ethanol, Tween-80, Naproxen 

ABSTRACT

Azacitidine and its deoxy derivative are used in the treatment of myelodysplastic syndrome. These types of drugs were first synthesized in Czechoslovakia as potential chemotherapeutic agents for cancer. Conventional compositions of Azacitidine are available as powder product or as a solution of Azacitidine in water. Both these products have been associated with a number of toxicities when administered intravenously. To overcome these problems, in the present study, inclusion of Azacitidine in liposomal formulation has proved to be good approach to eliminate the toxicities and improve drug antitumor activity. We formulated Azacitidine liposomes containing Hydrogenated soy phosphatidylcholine, 1,2-Distearoyl-sn-glycero-3[Phospho-rac-(1-glycerol ) (Sodium Salt) [DSPG-Na] and Cholesterol by dried thin film hydration technique. Particle size analysis, zeta potential, %free drug are strongly affected by the different lipid concentration and result shown F5 formulation have the optimum % free drug, Particle size and F2 formulation shown highest Percent drug release when compared to the F4 & F5 formulations. The release kinetics of F2, F4 and F5 formulations were studied. All the formulations follow zero-order release kinetics and follow case-II transport when it applied to the Korsmeyer-Peppas model for the mechanism of drug release. The stability of the F2, F4 & F5 formulations were studied at 5±3^oc and at room temperature for duration of 3 months. Hence it can be concluded that the liposomes along with Hydrogenated soy phosphatidylcholine, DSPG-Na and Cholesterol are suitable carriers for the preparation of Azacitidine liposomes.

Key words: Azacitidine, Liposomes, Hydrogenated soy phosphatidylcholine, 1,2-Distearoyl-sn-glycero-3[Phospho-rac-(1-glycerol.) [DSPG-Na], cholesterol.

ABSTRACT

A simple, precise, rapid and accurate reverse phase high performance liquid chromatography method (RP-HPLC) in isocratic mode has been developed for the estimation of ranolazine in pure form and in its tablet dosage form. An Agilent Eclipse XDB C18, 150 x 4.6 mm, 5mm particle size column, with mobile phase consisting of phosphate buffer pH 3.5 and acetonitrile in the ratio of 65:35 % v/v was used. The flow rate was 1.0 mL/min and the column effluent was monitored at 272 nm. The retention time was 4.7 min. The detector response was linear for ranolazine in the concentration range of 10-150 µg/mL. The limit of detection (LOD) was found to be 0.034 μg/mL. The limit of quantification (LOQ) was 0.102 μg/mL. The method was validated by determining its accuracy, precision and system suitability. The results of the study showed that the proposed RP-HPLC method is simple, rapid, precise and accurate, which is useful for the routine determination of ranolazine in pure drug and in its tablet dosage form.

Keywords: Ranolazine, RP-HPLC estimation, tablets.

ABSTRACT

Caralluma is a succulant plant, made into pickles, curry and also eaten as raw in the treatment of diabetes. The plant also reported to have anti-inflammatory, antinocicepive, antiulcer and gastroprotective activity. Tribals use the plant as a famine food. Hence it is necessary to investigate physicochemical and quantitative phytochemical parameters of the plant. Phytochemical study revealed presence of saponin, flavonoid, carbohydrates, proteins, vit. C, hence they were quantitatively determined. Haemolytic activity, using healthy human volunteer blood, was performed. C. adscendens is a vegetable of daily use. The calorific value, determined by Bomb calorimeter. From the result of quantitative determination and higher calorific value, the plant is said to have good neutraceutical potential. Saponin content may responsible for various reported activities.

Keywords: Caralluma adscendens, Quantitative Phytochemical study, Neutraceuticals 

ABSTRACT

For evaluation of the antiemetic effects of the drugs animal models (Ferret,cat dog etc) are used. Although good guidelines may be established through the animal experiments, they may not give accurate indication of the antiemetic effect of the antiemetic drugs in patients due to species differences in pharmacokinetic and pharmacodynamic responses. Therefore, Ipecacuanha-induced emesis and flare models are used to predict more accurately the antiemetic effect of the antiemetic drugs. In ipecacuanha-induced emesis model in 10 healthy human volunteers slow intravenous injection of ondanserton -2 ml. (4 mg) was given over 5 minutes.Thirty minutes after inj. ondanserton, 30 ml. oral syrup of tincture ipecac was given with glassful of water. Then the parameters like time, number and duration of emesis were noted over 6 hour’s period. In flare model in 6 healthy human volunteers Injection Serotonin 0.05 ml of 12.98 µM was given intradermally on the flexor aspect of forearm. Resulting flare response was measured over 5 minutes. At the end of half an hour, injection ondansetron and same dose of injection serotonin was given intradermally. Resulting flare response was measured in the similar way. Out of these two models, ipecac model is technically easy and clinically relevant but its tolerability is less. Flare model has excellent tolerability but it is technically not very easy. Thus one can choose the effective model accordingly.

Key words: Antiemetic, Ipecacuanha, Ondansetron, Serotonin

ABSTRACT

A simple, specific, accurate and stability-indicating reversed phase high performance liquid chromatographic method was developed for the simultaneous determination of thiocolchicoside  and lornoxicam, using a RP-18 column and a mobile phase composed of 10mM ammonium acetate : methanol(50:50), pH7 adjusted with 1%triethyl amine. The retention time of thiocolchicoside and lornoxicam were found to be 4.6 and 10.2 min, respectively. Linearity was established for both thiocolchicoside and lornoxicam in the range of 1-10 µg/ml. The percentage recoveries of thiocolchicoside and lornoxicam were found to be 100.45±0.4489 and 100.70±0.5111, respectively. Both the drugs were subjected to acid, alkali and neutral hydrolysis, oxidation, dry heat, and photolytic degradation. The degradation studies indicated thiocolchicoside to be susceptible to acid, alkaline and neutral hydrolysis while lornoxicam showed degradation under acid and alkali. The degradation products of thiocolchicoside and lornoxicam were well resolved from the pure drugs with significant differences in the retention time values. This method can be successfully employed for simultaneous quantitative analysis of thiocolchicoside and lornoxicam in bulk drugs and formulations.

Keywords: Thiocolchicoside , lornoxicam, degradation products, stability-indicating, HPLC

ABSTRACT

Currently available drugs for diabetes mellitus pose considerable side effects. This necessitates the development of new products, particularly herbal preparations which are known to have lesser side effects. Several herbal products are used to treat diabetes; but their hypoglycemic effects are complex and few anti-diabetic plants have received proper scientific validation. The present study was undertaken to validate the use of the leaves of Nyctanthes arbor-tristis plant as anti-diabetic agent. This study was conducted on thirty healthy albino rabbits of either sex; the effect of the Nyctanthes arbor-tristis leaf extract (NALE) at doses 200mg/kg body weight and 400mg/kg body weight was evaluated for a period of 14 days on alloxan induced diabetic rabbits. The hypoglycemic effect of the leaf extract was compared with the standard Glibenclamide at dose 2.5mg/kg body weight. Results revealed that the hypoglycemic effect of the Nyctanthes arbor-tristis leaf extract at 200mg/kg body weight was not significant whereas at 400mg/kg body weight it was highly significant and comparable to Glibenclamide. However, the result of the present study can only be confirmed after evaluating Nyctanthes arbor-tristis on larger number of animals as well as clinically.

Keywords: Nyctanthes arbor-tristis, hypoglycemic effects

ABSTRACT

The objective of this work was to develop and validate simple, rapid and accurate spectrophotometric method for quantitative estimation of Benazepril in pure drug. Benazepril is used for management of hypertension, heart failure, myocardial infarction. In methanol Benazepril exhibits absorption at 242.4 nm and method obeys Beer’s law at the concentration range of 2.0-100 µg/mL. The percentage label claim was found in the range of 98-103%. The proposed method was validated statistically and by recovery studies.

Keywords: UV Spectrophotometer, Calibration curve method, Benazepril tablet

ABSTRACT

Floating dosage form for gastric retention has potential to use as controlled-release drug delivery systems which providing opportunity for both local and systemic drug action. The present work was aimed to formulate controlled release floating tablet (CRFT) of Perindopril Erbumine using gas generated low density approach. To develop CRFT, the Perindopril Erbumine was selected as a drug because it complies with the suitability criteria for the floating drug delivery system and the controlled release medication was required due to its potent action and poor bioavailability. The present investigation was suggested that the bioavailability of Perindopril Erbumine was improved due to increased gastric retention time and controlling the drug release rate using the natural polymer SFG, HPMCK15M and Acrypol 934. The CRFT of Perindopril Erbumine was developed by using wet granulation method and PVP K 30 was used as a granulating agent. The study was given the assurance that SFG had an excellent controlled drug releasing property then HPMCK15M by forming matrix in the formulation. The Acrypol 934 was added to control the drug release rate in to formulation and found good compressibility and controllable drug releasing properties in to the final formulation. All the formulation was evaluated for Weight variation, Thickness, Hardness, Diameter, Friability, Assay, FLT, TFT, Swelling Index and Dissolution study.

Key Word: CRFT, SFG, Acrypol 934, FLT, TFT, SWI, Perindopril Erbumine, DSC

ABSTRACT

The aim of this study was to investigate the performance and release behavior of drug from hydroxypropyl methylcellulose (HPMC) matrix tablets prepared using HPMC from three different manufacturers. Three various brands of HPMC used were Methocel, Novocoat, and Zhongbao. A protocol was followed to evaluate these three HPMC samples their physico-mechanical properties such as appearance, particle size distribution, bulk density, tapped density, angle of repose, compressibility index (CI), Hausner’s ratio, swelling and morphology. Formulations were prepared using Carbamazepine (CAR) as a drug molecule, by varying drug loading and polymer concentration to evaluate the physical and comparative performance characteristics. Various drug release kinetic models were evaluated for the best fit of the formulations in order to understand the underlying release mechanisms from the formulations. The best performance with respect to release kinetics was exhibited by Methocel,while Novocoat and Zhongbao were found to have similar performance.

Keywords: HPMC, Methocel, Novocoat, Zhongbao, Carbamazepine.

ABSTRACT

Iloperidone is a novel antipsychotic drug widely used to treat schizophrenia. Objective of this investigation was to develop a validated stability indicating high performance thin layer chromatographic method for the quantification of iloperidone in bulk and pharmaceutical dosage form. Aluminium backed TLC plates precoated with silica gel 60F-254 was employed as the stationary phase and n-propanol: chloroform (5:5 v/v) as the mobile phase. Densitometric analysis was performed at 275 nm in the reflectance mode. Compact spots of iloperidone with R_f value 0.36 were observed. Validation of the method as per ICH guidelines produced satisfactory results of linearity (r²>0.999), limit of detection (5.349 ng/spot), limit of quantification (16.2099 ng/spot), precision (< 2%), and accuracy (99.66 ±0.341 to 100.34±0.292%). Degradation products were found to be well separated from the pure drug with significantly different R_f values suggesting a stability indicating analysis method for the estimation of iloperidone in pharmaceutical preparations and as bulk drug. The proposed method is selective, sensitive, precise, and accurate. It is also simple, economic and time saving as compared to reported HPLC methods. 

Keywords: Iloperidone, stability indicating, HPTLC, validation, ICH guidelines, degradation

ABSTRACT

The present study revealed that, acetone among pure forms of experimental solvents and Ethyl acetate + Methanol + Water among the mixture forms could extract significantly higher (p<0.01) amount of polyphenols from all the plant leaves. The amount of polyphenols extracted in mixture forms of solvents were significantly higher (p<0.01) than those in their pure forms for majority of the plant leaves. It is concluded that, solvents in their mixture forms were better to extract phyto-phenols from leaves of the medicinal plants.

Keywords: solvents, leaves, medicinal plants, polyphenols

ABSTRACT

The present study was undertaken to evaluate the total antioxidant potential of four different varieties of green beans namely Phaseolus vulgaris (french beans), Vicia faba (broad beans), Cyamopsis tetragonoloba (cluster beans) and Vigna unguiculata (cowpea beans) in both fresh and processed condition (microwave assisted). The total phenolic and flavonoid contents were determined by Folin Coilteaus and AlCl₃ assay respectively. The antioxidant activity was determined by 1,1-diphenyl-2-picrylhydrazyl (DPPH) assay, hydrogen peroxide(H₂O₂) decomposition and reducing power assay. Efforts were also made to study the interaction of beans with metal ions. Total phenolic content ranged from 105.00 ± 0.021 to 300.00 ± 0.009 µg GAE^.g^-1  (Gallic acid equivalent) of extract and flavonoid content ranged from 55.00 ± 0.017 to 550.00 ± 0.050 µg QE^.g^-1 (Quercitin equivalent) of extract. All the extracts scavenged DPPH radical and decomposed H₂O₂. The reducing potential was found to be highest in Cyamopsis tetragonoloba followed by Vigna unguiculata, Vicia faba and Phaseolus vulgaris. Good correlation of phenolic content was observed with reducing power ability ( r² = 0.743) and DPPH radical scavenging property (r² = 0.694). The extracts chelated both the ionic forms of iron Fe²⁺ and Fe³⁺ but the affinity towards Fe³⁺ was higher. Green beans can be considered as a potential source of antioxidants. Fresh extracts were found to have higher antioxidant potential as compared to processed extracts.

Keywords: Antioxidant, Cyamopsis tetragonoloba,  Vigna unguiculata, Vicia faba, Phaseolus vulgaris, Green beans

ABSTRACT

Trigonella foenum-graecum (Fenugreek) (Leguminosae) is employed as a herbal medicine. Its seeds are known for their carminative, tonic and antidiabetic effects. A curative dose of Trigonella foenum-graecum also produces antiulcer action¹. In this study we have investigated the Ethnopharmacological activities of the aqueous extract of the seeds Trigonella foenum-graecum in normal mice using different route of administration . The methanolic extract administered through the same route produced various effect only at the dose of 1 g/kg body weight. The aqueous extract is under further investigation to determine the chemical structure of the active component. The presence of hypoglycaemic, antiflamatory, antianalgesic activity in aqueous and methanolic extract indicates that the active compounds are polar in nature. The effects of fenugreek seed extract on the alterations in serum thyroid hormone concentrations were studied in adult male mice and rats. Simultaneously, hepatic lipid peroxidation and the activities of the antioxidant enzymes, viz superoxide dismutase  and catalase were examined. Present study reports analgesic activity of petroleum ether, chloroform, ethyl acetate and methanolic extracts of leaves and seeds of Trigonella foenum-graecum Linn.

Key word: Evaluation, Ethno pharmacological Activity, methi seed.

ABSTRACT

The love affair of Asian’s with Ling zhi, the Chinese name for Ganoderma lucidum and related species can be traced back over two thousand years. Ganoderma lucidum has been used for a broad spectrum of health benefits from preventive measures and maintenance of health to the regulation or treatment of chronic as well as acute life threatening illness. The present study was done to compare the Aqueous and methanolic extract of Ganoderma lucidum for anthelmintic activity and to compare the methanolic and chloroform-acetone extract of Ganoderma lucidum for antibacterial activity. Aqueous extract of mushroom did not show any result for anthelmintic activity, while the methanolic extract (60 mg/ml) was equally effective as standard (Albendazole 20 mg/ml). For antibacterial activity both the methanolic (350 mg/ml) and chloroform-acetone (350 mg/ml) extracts showed effective results, but the results of choloroform-acetone extract were more effective than methanolic extract and standard (Gentamycin 40 mg/ml).

Key words: anthelmintic, antibacterial, methanolic extract, aqueous extract.

ABSTRACT

To evaluate the heapatoprotective activity of various extracts of Aegle Marmelos, belonging to the family Rutaceae against Carbon Tetrachloride (CCL_4­) induced hepatootxicity in wistar Female rats. Oxidative stress play important role in many diseases. Hence, Herbal drugs play crucial role in treatment of various diseases due to its antioxidant property. The toxicant was used to induce hepatotoxicity at dose of CCl₄  1.25 ml/kg of body weight as mixture of 1:1 with olive oil for 30 days. Experimental groups of were constructed: a vehicle control group received the respective vehicles; a CCl4 group received a repeated single oral dose of CCl4 at 1.25 ml/kg; and the CCl4 &AMPE, AMCL.AMAL, AMAQ received repeated oral dose of Aegel Marmelos extracts in 500 mg/kg, respectively. It was found that AMCL, AMAL & AMAQ, at a dose of 500 mg/kg body weight exhibited hepatoprotective effect by lowering the Serum Glutamate Pyruvate Transaminase (SGPT), Serum Glutamate Oxaloacetate Transaminase (SGOT), alkaline phosphate and total bilirubin to a significant extent. The groups treated with various extract of A.Marmelos & Silyamarine shows significant (P<0.001) restoration of liver weight & liver volume nearer to normal control group. Since results of biochemical studies of blood samples of Aegle Marmelos Extracts treated rats showed significant decrease in the levels of serum enzyme activities, reflecting the liver injury caused by CCL4 indicating the protection of hepatic cells against CCL4 induced hepatocellular injury. The effects of Aegel Marmelos extracts were comparable with standard drug silymarin.

Key words: Aegle Marmelos; CCl4 (Carbon Tetrachloride); Heaptotoxicity; Oxidative Stress; Protective Effects.

ABSTRACT

Chronopharmaceutics is a branch of pharmaceutics devoted to the design and evaluation of drug delivery systems that release a bioactive agent at a rhythm that ideally matches the biological requirement of a given disease therapy. A major objective of chronotherapy in the treatment of several diseases is to deliver the drug in higher concentrations during the time of greatest need according to the circadian onset of diseases or symptoms. The main objective of the present study is to develop single-unit pulsatile drug delivery system for obtaining no drug release till it reaches in colon followed by pulsed drug release in colon to achieve chronotherapeutic release of atenolol for treatment of hypertension and to improve the patient compliance. In vitro studies revealed that the tablet coated with guar gum and Eudragit S-100 have limited drug release in stomach and small intestinal environment and released maximum amount of drug in the colonic environment. Programmable pulsatile, colon-specific release has been achieved from tablet of T7 formulation (50:50) which meet demand of chronotherapeutic drug delivery.

Key Words: pulsatile, chronotherapeutic, hypertension, atenolol

ABSTRACT

An efficient and rapid synthesis of some new pyrazoles, isoxazole, benzoxazepine and benzothiazepine derivatives is described. The synthesized compounds were investigated for their anti-inflammatory and antimicrobial activities and some of them showed potent anti-inflammatory and anti-microbial activities.

Keywords: Anti-inflammatory activity, Prostaglandin, Pyrazole, Isoxazole, Benzoxazepine, Benzothiazepine, Antimicrobial activity

ABSTRACT

Two new, rapid, precise, accurate and specific chromatographic methods for the simultaneous determination of Olmesartan medoxomil and Hydrochlorothiazide in combined pharmaceutical dosage forms. The first method based on reverse phase liquid chromatography by using INERTSIL ODS C18 3V (150 x 4.6, 5μ) using mobile phase 1ml triethanolamine in one litre water and the pH was adjusted to 2.5 with orthophosphoric acid and acetonitrile using a gradient program with a flow rate of 1ml/min, throughout the gradient program with a detection wavelength of 225nm.The second method involved silica gel 60F254 high performance thin layer chromatography and densitometric detection at 270nm using chloroform : methanol(85:15) as the mobile phase

Keywords: Olmesartan medoxomil; Hydrochlorothiazide; high performance thin layer chromatography; reverse phase liquid chromatography.

ABSTRACT

A rapid, simple, sensitive, accurate, and precise UV spectrophotometric method has been developed for the simultaneous estimation of anti-retroviral agents lamivudine, didanosine and efavirenz in pharmaceutical dosage form. The absorption maxima of the drugs were found to be 271, 250 and 247 nm for lamivudine, didanosine and efavirenz respectively. Lamivudine, didanosine and efavirenz obeyed Beer’s law in the concentration range of 10-100 µg/ml, 10-100 µg/ml and 10-70 µg/ml respectively. The percentage recovery was within the range of 98% - 101%, indicating that insignificant interference from the other ingredients in the formulation. The above method was validated in terms of linearity, accuracy, precision, Limit of Detection (LOD), Limit of Quantification (LOQ) etc. in accordance with ICH guide lines. The developed method was free from interferences due to excipients present in tablets. The method was rapid, simple and suitable for routine quality control analysis.

Keywords: lamivudine; didanosine; efavirenz; UV spectrophotometric method; simultaneous equation method

ABSTRACT

This study was performed to evaluate the presence of Phytochemical, antimicrobial and antioxidant activity of Eria pseudoclavicaulis Blatt. (Orchidaceae) leaf extracts. Preliminary phytochemical analysis revealed that the ethyl acetate extract shown the maximum phytochemical constituents followed by ethanol and water. Different extracts of Eria pseudoclavicaulis were tested for antimicrobial activity of this, ethyl acetate extract shown the maximum antibacterial activity against five microorganisms. The water extract possess strong 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity (IC₅₀ 318 μg/ml), This research findings suggest that Eria pseudoclavicaulis exhibits potential antimicrobial and antioxidant properties.

Key words: phytochemical analysis, antimicrobial, antioxidant, Eria pseudoclavicaulis

ABSTRACT

Aloe gel is commonly used in herbal medicines. Many of the Aloe products available commercially, do not demonstrate beneficial effects, indicating the poor quality of the Aloe gel. Therefore, an efficient, reliable and accurate method is needed to evaluate the quality of Aloe products. The present research work discussed the development of a colorimetric and HPTLC method for the determination of Glucomannan (a marker compound for Aloe gel) in Aloe gels and its preparations. Shimadzu 1700 UV-Visible spectrophotometer was used for the colorimetric estimation. In the colorimetric method developed obeyed the Beer’s law in the concentration range of 50-90 μg-ml^-1 with r² of 0.999. CAMAG HPTLC instrument was used. The mobile phase comprised of n-butanol : ethanol : water : acetic acid (2 : 4 : 4 : 0.05 v/v) was used for the development of chromatogram. The densitometric scanning was done by TLC scanner III (CAMAG) in absorbance mode at the wavelength of 488 nm. After spraying with anisaldehyde sulfuric acid the system was found to give compact spots for glucomannan (Rf value of 0.69±0.02). The data obtained showed good linearity (r² = 0.995) with respect to peak area in the concentration range of 400-1400 ng spot^-1.

Keywords: Aloe vera, Aloe perryi, Glucomannan, Colorimetry, HPTLC

ABSTRACT

A simple, sensitive, accurate and precise simultaneous UV spectrophotometric method has been developed for the estimation of Ibuprofen, Paracetamol and Caffeine in tablet dosage form. The absorption maxima of the drugs were found to be 223, 248 and 272 nm for Ibuprofen, Paracetamol and Caffeine respectively, in methanol, using a Shimadzu UV–Visible spectrophotometer (model UV-1800). Ibuprofen, Paracetamol and Caffeine obeyed Beer’s law in the concentration range of 10-70 µg ml^-1, 10-60 µg ml^-1 and 10-70 µg ml^-1 respectively. The correlation coefficient was found to be 0.999, 0.999, and 0.999 for Ibuprofen, Paracetamol and Caffeine respectively. The method was validated for various parameters according to ICH guidelines. The low relative standard deviation values indicate good precision and high recovery values indicate accuracy of the proposed method. Assay results were in good agreement with label claim.

Keywords: Ibuprofen, Paracetamol, Caffeine, UV spectrophotometric method, simultaneous equation method.

ABSTRACT

The present manuscript describes simple, sensitive, rapid, accurate, precise and economical derivative spectroscopic method for the simultaneous determination of tolperisone hydrochloride (TOL) and diclofenac sodium (DIC) in bulk and synthetic mixture. Derivative spectroscopy offers a useful approach for the analysis of drugs in mixtures. In this study a first-derivative spectroscopic method was used for simultaneous determination of tolperisone hydrochloride and diclofenac sodium using the zero-crossing technique. The measurements were carried out at wavelengths of 250.60 and 311.20nm for tolperisone hydrochloride and diclofenac sodium respectively. The method was found to be linear (r2>0.9970) in the range of 5- 40 μg/ml for tolperisone hydrochloride at 250.60 nm. The linear correlation was obtained (r2>0.9990) in the range of 5-50 μg/ml for diclofenac sodium at 311.20 nm. The limit of determination was 0.65 and 0.55 μg/ml for tolperisone hydrochloride and diclofenac sodium respectively. The limit of quantification was 2.01 and 1.67 μg/ml. The method was successfully applied for simultaneous determination of tolperisone hydrochloride and diclofenac sodium in binary mixture.

Keywords: Diclofenac sodium, Tolperisone hydrochloride, Derivative spectroscopic method, Zero-crossing point.

ABSTRACT

Effect of nicotine on brain GABA levels in depressed rats. The present study was planned: to study effect of nicotine on brain GABA levels in depressed rats. to compare the effect of nicotine and imipramine on brain GABA levels. Isolation induced hyperactivity model was used to induce depression in rats. Five groups of 10 rats each were taken. Vehicle (D/W) treated rats before and after isolation were considered as baseline reading. Compared results of depression induced animal with results of animal without depression. Following drug treatments were administered: Rats from natural habitat was considered as before isolation. This group was used for normal GABA levels in rat brain. Vehicle (D/W) (1ml/kg) and imipramine (10mg/kg) were administered intraperitoneally. Nicotine was administered in a dose of 0.4mg/kg and 0.2mg kg by subcutaneous or inhalational route respectively. Brain GABA levels were estimated by fluorimetric method. In this model of depression, vehicle treated rats after isolation significantly reduced brain GABA levels as compared to vehicle before isolation.  Results of imipramine treated rats after isolation showing significantly increased in brain GABA levels as compared to vehicle treated rats after isolation. Nicotine administered by inhalational route showed increase in brain GABA levels as compared to vehicle treated rats after isolation. Nicotine administered subcutaneously increased brain GABA levels as compared to vehicle treated rats after isolation. Imipramine and nicotine (inhalation) showed comparable results with  normal GABA level i.e. before isolation rats. GABA level reduced in depressed rats. Imipramine, nicotine(inhalation) and nicotine(sc) increased  brain GABA level in depressed rats.

Keywords :Depression, Isolation induced hyperactivity, Brain GABA level, Nicotine

ABSTRACT

A reverse phase high performance liquid chromatographic method was developed for the determination of Mirabegron in bulk and Pharmaceutical dosage form. The separation was effected on a Waters ODS C₁₈ column (150 mm x 3.9 mm;5µ) using a mobile phase mixture of buffer and acetonitrile in a ratio of 50:50 v/v at a flow rate  of 1ml/min. The detection was made at 249 nm. The retention time of Mirabegron was found to be 2.502 min.  Calibration curve was linear over the concentration range of 6.25-37.5 µg/ml of Mirabegron. The propose method was validated as per the ICH guidelines. The method was accurate, precise, specific and rapid found to be suitable for the quantitative analysis of the drug and dosage form.

Keywords: Buffer, acetonitrile, Mirabegron, Tablets, Waters ODS C₁₈ column, RP-HPLC.

ABSTRACT

The objective of this study was to determine the phenolic content of the Sterculia foetida L. seeds methanol extract (SSME) and to evaluate the antioxidant activity of the extract. The Folin-ciocalteu procedure was used to assess the total phenolic content of the extracts as garlic acid equivalents. Antioxidant activity was evaluated using 1, 1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging, ferric reducing power and 2, 2-Azinobis-3-ethyl benzothiazoline-6-sulfonic acid (ABTS) diammonium salt methods. The seed methanol extract was yielded 9.5% crude material. The total polyphenol content was 14.32%. The antioxidant activity of extract was shown similar correlation between DPPH, ferric reducing power and ABTS.   

Keywords: Sterculia foetida, Seed, Methanol extract, Polyphenols, Antioxidant

ABSTRACT

The present study was aimed to explore the phytochemical constituents present in Turbinaria ornata (Turner) J.Ag. collected from the south east coast of Tamil Nadu, India. The phytochemical screening of different extracts was estimated using the standard procedure for UV-Vis spectroscopic and HPLC. The UV-Vis phytochemical profile of various extracts of Turbinaria ornata (Turner) J.Ag. was analyzed. The qualitative HPLC fingerprint profile of methanol extract of Turbinaria ornata (Turner) J.Ag. was selected at a wavelength of 254 nm due to sharpness of the peaks and proper baseline. The profile displayed one prominent peak at a retention time of 1.953 min and some moderate peaks were observed at a retention time of 3.000, 2.570 and 2.467 min respectively. The present study on Turbinaria ornata (Turner) J.Ag. produced novel phytochemical markers in standardization as useful analytical tools to check not only the quality of the powder but also the presence of adulterants in ayurvedic drugs.

Keywords: Phytochemistry, Seaweeds, Turbinaria ornata, UV-Vis, HPLC.

ABSTRACT

Granisetron hydrochloride is a novel serotonin 5-HT₃ receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy. It is well absorbed from the gastrointestinal tract, but its oral bioavailability is low (60%) due to extensive first-pass metabolism which makes it an ideal candidate for rapid release drug delivery system. Hence, an attempt was made to prepare and evaluate fast dissolving oral films containing Granisetron hydrochloride as a model drug by solvent casting method using natural and synthetic polymers. Various formulations were developed with varying concentration of polymers like, CMC, HPMC and Pullulan. Citric acid was used as a disintegrating agent and Propylene glycol as a plasticizer. The prepared oral films were evaluated for their physicochemical and mechanical parameters such as Physical appearance, surface texture, Weight uniformity, surface pH, ^,thickness uniformity, percentage moisture absorption, loss on drying, disintegration time, drug content uniformity, folding endurance, tensile strength, percentage elongation, in-vitro drug release, and stability studies. In-vitro release rate of Granisetron hydrochloride was studied in phosphate buffer pH 6.8. F7, F10 showed maximum release rate about 93.95% and 95.29% in 180 seconds respectively, whereas F3 showed 60.98%. The mechanism of drug release of fast dissolving oral film was found to be to be non-fickian diffusion following first order kinetics. The selected fast dissolving oral films were found to be superior to marketed conventional tablet. Short term stability studies of selected films indicated that there is no significant change with respect to physical appearance, disintegration time, drug content and in-vitro drug release.

Keywords: oral films, granisetron hydrochloride, HPMC, CMC, Pullulan

ABSTRACT

The present paper focus on the phytochemical screening and antimicrobial activity of Phyllanthus narayanaswamii (Euphorbiaceae), a critically endangered and endemic species to the East Godavari & Visakhapatnam hills of North Eastern Ghats. In the present study the alcoholic extracts of leaves, shoot and root of P. narayanaswamii were studied for their antibacterial activity by agar disc diffusion method against both Gram positive, Gram negative and one fungal strain. It was observed that, alcoholic extracts of leaf showed the highest antimicrobial activity against the pathogenic microorganisms followed by shoot and root extracts. The minimum inhibition and minimum bacterial concentrations (MIC and MBC) were determined by microdilution method using 96-well microtiter plate method. As the disc dosage level increases the inhibitory effect also increased.

Keywords: Phytochemical screening, Antimicrobial evaluation, Phyllanthus narayanaswamii, Endemic and Endangered species.

ABSTRACT

Nebivolol Hydrochloride is a third generation beta blocker used for the treatment of hypertention and heart failure. Nebivolol is rapidly absorbed following oral administration, reaching peak plasma concentrations in 0.5 – 4.0 hrs. The present study was designed to develop a suitable matrix type transdermal drug delivery system (TDDS) for Nebivolol Hydrochloride employing various ratios of hydrophilic and hydrophobic polymers by solvent casting technique. The developed patches were then evaluated for physicochemical characterization, ex-vivo permeation and skin irritation studies. The compatibility of drug with other ingredients was checked by FTIR studies. FTIR results revealed that there was no interaction between dug and other excipients. The transdermal patches obtained were transparent, smooth, uniform and flexible. The results of physicochemical properties were within the pharmacopoeial limits. All the formulations were subjected to ex-vivo skin permeation study by means of Franz’s diffusion cell in order to optimize the suitable formulation. Two formulations with the polymeric blend 3:2 (HPMC E50: ERL 100 and HPMC E15: ERL100 respectively) showed an increase in permeation of drug via skin when compared with the formulations having less proportion of hydrophilic polymer (HPMC), however the formulation with HPMC E50 : ERL 100 showed overall improvement in flux and permeation, hence it was optimized as suitable matrix system. The drug release follows zero order kinetics with diffusion mechanism. The average steady state flux obtained with HPMC E50: ERL 100 (3:2) was 43.3 µg/cm²/hr and the same was increased to 59.2 µg/cm²/hr with the incorporation of 5% v/w of DMSO as permeation enhancer. In conclusion, the present data confirm the feasibility of developing Nebivolol Hydrochloride transdermal system. The release rate of drug through patches increased when the concentration of hydrophilic polymer was increased. 

Keywords: Nebivolol Hydrochloride, HPMC E 50, HPMC E15, transdermal patches.

ABSTRACT

Effluent discharge from textile and dyestuff industries to neighbouring water bodies and wastewater treatment systems is currently causing significant health concerns to environmental regulatory agencies. Color removal, in particular, has recently become of major scientific interest, as indicated by the multitude of related research reports. Microbial decolorization and degradation of dyes is seen as a cost-effective method for removing these pollutants from the environment. In this review we have examined biological decolorization of dyes used in textile industries. A simple spectrophotometric assay method was adapted to screen for the ability of Pseudomonas aeruginosa isolates from dye industry effluent to degrade the chosen dyes. They were checked for the extent of dye decolorization [Methyl Red, Methyl Blue & Malachite green] at three different concentrations as 40, 60 & 80ppm. Visual and spec decolonization indicated that decolorization was higher in 60ppm concentration of all three dyes, indicating that to be the optimum concentration for degradation by Pseudomonas aeruginosa isolates. We suggest that the addition of bacterium to the microbial mixture indicated that decolorization was higher in case of dyes in 60 ppm concentration. It can also reduce the bulking problems of the effluent by preventing the load of the organic matter from becoming too high.

Keywords: Pseudomonas aeruginosa; Methyl Red, Methyl Blue; Malachite green; effluent; 

ABSTRACT

Phytochemical investigation of the roots of Ricinus communis L.  (Euphorbiaceae), used to cure  lumbago and toothache, led to the isolation of acyl glycosides characterized as n-octadec-9-enoyl β-D-glucopyranoside (4), n- octadecanoyl-b-D-glucopyranoside (5), n -docosany1-β-D-gluco- pyranoside (6), n-hexadecanoyl β-D-glucuranopyranoside (7) and n-octadecanoyl- β- arabinopyranosyl – (2→1″) – β- arabinopyranoside (9), a trisaccharide β-D-glucuranopyranosyl-(2→1)-β-D-arabinopyranosyl-(2→1) -β-D-arabinopyranoside (8), a tetraglycoside β- D- glucopyranosyl- (2®1)- β - D- arabinopyranosyl-(2®1)-β- D- arabinopyranosyl - (2®1)- β -D-arabinopyranoside (10), a triterpenic glucoside α-amyrin β-D-glucopyranoside (1) and two steroidal glycosides viz., stigmasterol β-L-arabinopyranoside(2) and β-sitosterol β-D-glucopyranoside(3). The structures of all these glycosides, isolated from the roots for the first time,  have been characterized on the basis of spectral data analysis and chemical reactions.

Keywords: Ricinus communis, Euphorbiaceae,  Roots, acyl glycosides, steroidal glycosides.

ABSTRACT

Guizotia abyssinica (L.f.) Cass., Syn. G. oleifera D.C., Polymnia abyssinica L.f., Suppl., Verbesina sativa Roxb., Jaegeria abyssinica Spr., commonly known as Ramtil in Hindi and Niger in English belongs to family Asteraceae (Compositae)  is native of Abyssinica (South Africa). The plant is used in the treatment of various diseases such as arthritis, microbial infections and seed oil serve as contraceptives. The leaves of Guizotia abyssinica (L.f.) Cass. (Asteraceae) are popular in Indian traditional medicine and as such provides good to develop herbal drug preparation to be used as phytomedicine. International criteria for validation and standardization of an herbal material as phytomedicine include microscopy and histological examination of raw material to guarantee its authenticity. The fresh leaves were taken to study the histology of the species. The thin section was made and treated with saffranine, chloral hydrate and iodine solution, mounted with glycerine and observed under microscope. Similarly, the dried leaves was made in to powder and was taken in glass slide, stained and mounted with glycerine, observed under microscope to reveal the powder character. The anatomical study revealed the presence of multicellular trichomes, stomata, chloroplast, conjoint and collateral vascular bundle, while powder microscopy revealed the presence of xylem vessels, parenchyma, calcium oxalate crystals etc. Thus, the present paper aims at setting the anatomical standards to establish quality control parameter for the raw material. The data obtained in present study will serve as valuable tool for identification, authentication and detection of adulterants, standardization and quality control of the plant Guizotia abyssinica (L.f.) Cass.

Keywords: Guizotia abyssinica, Leaves, Histology, Microscopy, Standards

ABSTRACT

QSAR analysis on a set of heterocyclic derivatives for antifungal activity was performed by using multiple regression procedure. The activity contribution of these compounds was determined from regression equation and the validation procedure to analyze the predictive ability of QSAR model was described. High agreement between experimental and predicted inhibitory values was obtained. The results of this study indicate that the parameter has a significant effect on antifungal activity of this class of compounds, thus simplifying design of new biologically active molecules.

Keywords: Quantitative structure-activity relationship, Antifungal activity, Multiple linear regressions

ABSTRACT

Escueltin is a coumarin derivative with wide range of biological activity. In the present study we investigated the protective effects of esculetin against cyclophosphamide induced oxidative stress and DNA damage. Following parameters were evaluated: (a) chromosomal aberration and mitotic index; (b) micronuclei formation and polychromatic erythrocyte frequency, and (c) malondialdehyde, glutathione and superoxide dismutase levels in liver homogenates. CP (50 mg/kg intraperitopeanlly) treatment significantly increased the different types of aberrant cells and micronuclei formation in bone marrow cells of mice. It also increase the lipid peroxidation and decreased glutathione and superoxide dismutase activity in liver. Whereas, pretreatment with esculetin (50, 75 and 100 mg/kg, per orally) alleviated aberrations in chromosome and lessened micronuclei formation. Esculetin pretreatment also shielded the liver of mice against cyclophosphamide induced oxidative stress as the levels of oxidative stress markers where near normal levels. Protective effect of esculetin correlated well with its genoprotective activity. It can be concluded that esculetin offsets cyclophosphamide induced oxidative stress and resulting DNA damage and can be useful as a chemopreventive agent against cyclophosphamide induced toxicity.

Keywords: Esculetin, cyclophosphamide, oxidative stress, chromosomal aberration and micronuclei formation.

ABSTRACT

The present study was performed to validate floklore claims of leaves of Corchorus trilocularis using ethanol extract for its antihyperglyceamic activity in alloxan induced diabetic rats. Ethanolic extract of C. trilocularis (EtCT) and glyburide were administered orally in alloxan induced diabetic rats. In the acute study, the serum glucose level was estimated at 0, 2, 4, 6 and 24 h after drug administration. The subacute study involved repeated administration of the drugs for 28 days, a serum glucose level estimation at 7, 14, 21 and 28 days. In the OGTT, D-glucose (2.5 g/kg) was administered in diabetic rats half an hour after pre-treatment with EtCT and glyburide. Serum glucose levels were estimated 30 min prior to glucose administration and at 0, 30, 60 and 120 min after glucose loading. In EtCT (400 mg/kg), the onset was 4 h, the peak effect was 6 h but the effect waned at 24 h. In subacute study, repeated administration (once a day for 28 days) of the glyburide and EtCT caused a significant reduction in the serum glucose level as compared to the vehicle treated group. EtCT (400 mg/kg) treatment prevented a decrease in the body weight of the diabetic rats. In the OGTT, EtCT (400 mg/kg) increased the glucose threshold at 60 min after the administration of glucose. The EtCT (400 mg/kg) showed significant antihyperglyceamic activity than EtCT (100 and 200 mg/kg).It can be concluded that ethanolic extract of C. trilocularis has antihyperglyceaamic activity.

Keywords: Corchorus trilocularis, Alloxan, OGTT, Wistar rats

ABSTRACT

A simple, specific, selective and accurate stability-indicating reversed phase high performance liquid chromatographic method was developed for simultaneous determination of Diclofenac potassium (DIC), Paracetamol (PCM) and Methocarbamol (MET). An isocratic RP-HPLC was achieved on younglin HPLC system using Varian C18 (250 Χ 4.6 mm i.d, 5 μm particle size) column with the mobile phase containing mixture of Methanol:water (80:20,v/v). The flow rate was 0.8 ml/min and the eluent was monitored at 225nm. The retention times of DIC, PCM and MET were found to be 3.51, 6.42 and 9.90 min respectively. The linearity was established for DIC, PCM and MET in the range of 10-60 µg/ml, 65-390µg/ml, 100-600µg/ml respectively. The percentage recoveries of DIC, PCM and MET were found to be in the range of 99.73%±0.109, 99.59%±0.085 and 99.50%±0.16 respectively. The LOD for DIC, PCM and MET were found to be 0.15, 2.40 and 1.82μg/ml respectively, while LOQ were 0.48, 7.29 and 5.53μg/ml respectively. All three drugs were subjected to acid, alkali, oxidation, and dry heat degradation. The degradation studies indicated DIC, PCM and MET showed degradation in acid, alkaline, H₂O₂, and in dry heat condition. The degradation products of DIC, PCM and MET were resolved well from the pure drug with significant differences in their retention time values. This method was also successfully employed for simultaneous quantitative analysis of DIC, PCM and MET in bulk drugs and formulations. The developed method is stability indicating and separate degradants and can be used to determine the stability of samples.

Keywords: DIC, PCM, MET, HPLC, LOD, LOQ

ABSTRACT

The objective of the present research work is to develop a gradient, reversed-phase liquid chromatographic (RP-UPLC) method for the determination of Dutasteride in pharmaceutical bulk drugs for assay and its related impurities. The chromatographic separation was achieved on a Waters ACQUITY ^TM UPLC C8 Column (100mm×2.1mm, 1.7µm),. The isocratic LC method employs mixture of buffer and Acetonitrile in the ratio of (50:50 v/v) solutions as mobile phase. The buffer solution contains 1.0mM potassium di hydrogen orthophosphate pH adjusted to 5.0 with dil.Potassium hydroxide solution (Buffer) .The flow rate was 0.4 ml/min and the detection wavelength was 210 nm. In the developed UPLC method, the resolution between Dutasteride and its potential impurities, namely Imp-1, Imp-2 and Imp-3 was found to be greater than 4.0. The drug was subjected to stress conditions of hydrolysis, oxidation, photolysis and thermal degradation. Considerable degradation was found to occur in Acidic medium and mild degradation observed in base hydrolysis stress conditions. Degradation product formed during acidic hydrolysis was found to be Unknown impurity. The stress samples were assayed against a qualified reference standard and the mass balance was found close to 99.5%. The developed RP-UPLC method was validated with respect to linearity, accuracy, precision and robustness. The developed method was found to be linear in the range of 2.5-15µg/mL with correlation coefficient of 0.999 for assay procedures and found to be linear in the range of 0.05-3µg/mL with correlation coefficient of 0.999 for related impurities

Keywords: RP-UPLC; Forced degradation; Validation; Dutasteride, Method development

ABSTRACT

A simple, accurate, economical and reproducible reverse phase high performance liquid chromatographic (RP-HPLC) method was developed and validated for the determination of Cetirizine hydrochloride and Ambroxol hydrochloride in bulk and pharmaceutical formulations. The separation was achieved on a phenomenex C18 column (150 × 4.6 mm i.d, particle size of 5µ) using a mixture of methanol, acetonitrile and water in the ratio of (30:30:40v/v )as mobile phase in an isocratic elution mode, at a flow rate of 1  ml/min. The detection was monitored at 230 nm. The retention time of Cetirizine hydrochloride and Ambroxol hydrochloride was found to be around 2.27 ± 0.12 min and 4.70 ± 0.14 min respectively. Excellent linearity range was found between 1-10 µg/ml for cetirizine hydrochloride and 10-100 µg/ml for Ambroxol hydrochloride. The method was validated with respect to linearity, robustness, precision and accuracy and was successfully applied for the simultaneous determination of Cetirizine hydrochloride and Ambroxol hydrochloride from the combined dosage formulation.

Key words: Cetirizine hydrochloride; Ambroxol hydrochloride; RP-HPLC method.

ABSTRACT

Treatment of myocardial infarction (MI) has undergone major advances in recent years, including reductions in mortality and hospital stays. Cardioprotective effects Ocimum gratissimum fresh leaves were evaluated in rat model having acute MI induced by Musa acuminata. Eating bananas on an empty stomach is not good to the health, because when stomach is empty, there is nearly no food in the stomach that can be digested. If this movement eats bananas, it will speed up the stomach's movement and the promotion of blood circulation, to increase the heart load. It is very easy to induce the myocardial infection. Adult male rats were divided into 4 groups. 3 groups receive Musa acuminata (banana) and 1 group Test drug. Cardio toxicity, evident from increased activities of Serum Creatine phosphokinase, Lactate Dehydrogenase, Aspartate Transaminase and Alanine Transaminase in Musa acuminata administered rats, and it was reversed by Ocimum gratissimum treatment. Musa acuminata administered rat show abnormal levels of SOD, Catalase along with high Malondialdehyde levels. The results of biochemical observation of serum and heart tissue were supplemented by histopathological examinations of rat heart sections to confirm the myocardial injury. These findings highlight the efficacy of Ocimum gratissimum as a Cytoprotectant in Musa acuminata induced cardio toxicity.

Keywords: Musa acuminate, Ocimum gratissimum, myocardial infarction

ABSTRACT

Heavy metal toxicity can result in damaged or reduced mental and central nervous function, lower energy levels and damage to several internal organs. Several bacteria have naturally developed tolerance to a wide range of toxic heavy metals. Some bacteria have also evolved mechanisms to detoxify heavy metals. Among several metals, silver has been reported to possess medicinal property and hence used as an antibacterial agent. Inspite of this few silver resistant bacteria have been reported in clinical and environmental samples. Prevalence of silver resistance among several isolated strains provided the basis of the current investigation to determine the prevalence of silver resistance in clinical isolates. The goals of this study were 1) to isolate the uropathogens 2) to investigate the presence and prevalence of silver resistance of urine isolates taken from urinary tract infected patients and 3) to obtain the antibiogram pattern and 4) to determine the maximum tolerance range of silver by the isolated uropathogens, thereby standardize the concentration of silver as antibacterial agent.

Keywords: heavy metals; silver; uropathogens

ABSTRACT

Several pharmacological activities like antitubercular, analgesic, anti-cancer, anti-inflammatory, antiasthmatic, antioxidant and antibacterial activities have been attributed to pyrazoles. The above observations prompted us to synthesize some novel pyrazole derivatives as possible antimicrobial agents. A series of novel 1,3,5-trisubstituted pyrazole derivatives (P₁-P₁₅) have been synthesized by the reaction of substituted chalcones (C₁-C₁₅) with succinichydrazide. The starting material, chalcones were prepared by claisen Schmidt condensation of acetophenone with aldehydes in the presence of sodium hydroxide in ethanol. Succinichydrazide was synthesized by condensing succinic acid with hydrazine hydrate. The cycloaddition of chalcones with succinichydrazide gives 1,3,5-trisubstituted pyrazole derivatives. The structures of synthesized derivatives were confirmed by IR, 1HNMR and Mass spectrum. The synthesized compounds were screened for their antibacterial and antifungal activity. The antibacterial activity data of the synthesized derivatives revealed that the compound P₄, P₁₃ and P₇, P₁₄ were effective against gram positive and gram negative organisms respectively. The antifungal activity data revealed that the compound P7 and P8 showed good activity against tested fungi.

Keywords: 1, 3, 5-trisubstituted Pyrazoles, Antimicrobial activity, Antifungal activity.

ABSTRACT

Quantitative estimation of temozolamide and its pharmaceutical dosage form by UV spectroscopy, RP-HPLC, HPTLC methods was developed. In the UV method (geometric method), temozolamide was quantified at 309nm, 325nm, 340nm in serum and water. The corrected absorbance was calculated. The Recovery studies was found to be 95.5-96.9%. In RP-HPLC method, the drug was resolved using a mobile phase methanol: buffer (5.0ml glacial acetic acid in 1000ml water) (70:30%v/v) on C₁₈ column in isocratic mode. The retention time of temozolamide was found to be 7.30 min. Recovery studies was found to be 99.55-100.98%.  In HPTLC method, the chromatograms were developed by using a mobile phase Chloroform: glacial acetic acid: methanol (2:3:5% v/v) on precoated plate of silica gel 60F₂₅₄ and quantified by densiometric absorbance mode at 254nm. The R_f value of Temozolamide was 0.47. Recovery studies of 98.99-100.6%, percentage relative standard deviation (%RSD less than 2%) and correlation coefficient (linearity range) that developed methods were accurate and precise. These methods can be employed for the routine analysis of capsules containing temozolamide.

Key words: Temozolamide, RP-HPLC, HPTLC, UV spectrophotometry, validation.

 ABSTRACT

In clinical practice, nonspecific antidiarrheals (allopathic and ayurvedic) are most commonly used by clinicians along with routine treatment to hasten the recovery and to give psychological reassurance. Although they are used extensively in practice, studies comparing their efficacy are few. This prospective observational study was carried out at two private clinics run by pediatricians to compare the efficacy, safety, and tolerability of racecadotril versus MEBARID, an ayurvedic polyherbal antidiarrheal formulation in the treatment of acute diarrhea. Children aged 2 y to 10 y who presented to the clinic with acute diarrhea and fulfilling selection criteria were enrolled and divided into two treatment groups viz, racecadotril and MEBARID. Data collection was done using predesigned case report forms and questionnaires. Outcome Measures used were 1)Duration of diarrhea after initiation of treatment 2)Frequency of stools until recovery 3)Time required for improvement in stool consistency. The groups were comparable clinically and demographically at enrolment. There was no significant difference in time needed for improvement in stool consistency with both racecadotril and MEBARID (17.76h vs.18.60h).Patients on racecadotril passed  3.32  ± 0.15 stools before recovery, while patients on MEBARID passed 3.13 ± 0.13 stools. The mean duration of treatment was less for racecadotril group (28.68 ± 2.18h Vs. 37.60 ± 2.18h; P = 0.005). Rapid improvement in stool consistency and frequency was found with both drugs. Thus racecadotril and MEBARID are rapid, equally effective treatments for acute diarrhea in children, but racecadotril significantly reduces the duration of diarrhea compared to MEBARID.

Keywords :Acute diarrhea,  Mebarid, Racecadotril, Nonspecific antidiarrheals, Children

ABSTRACT

Gastro retentive drug delivery is an approach to prolong gastric residence time, thereby targeting site-specific drug release in the upper gastro intestinal tract (GIT) for local and systemic effect. The present study has been a satisfactory attempt to formulate floating drug delivery system of Valacyclovir, an orally administrated antiviral drug with a view of improving its oral bioavailability and giving sustained release of the drug. In present study design expert trial 8.0.6.1 software is used for designing of experiment. In central composite design based on response surface methodology yielded nine experimental runs. These nine formulations are evaluated for precompressional parameters like bulk density, tapped density, angle of repose and carr’s index. Formulations are also evaluated for postcompressional parameters like hardness, thickness, weight variation etc. all the formulations shows results in the acceptable range. All preliminary formulations are subjected to invitrobouyancy and dissolution study. The data obtained from the in vitro release study was fit to various kinetic models to explain the release profile of the drug. Kinetic models used were zero and first-order equations, Krosmeyersand peppas and Higuchi models. Based on results obtained from the prelimimary formulations five optimized formulations are selected and validated. Short-term stability study was done for optimized formulations.

Keywords: Valacyclovir, floating drug delivery, In vitro release, kinetic models, in vitro buoyancy, optimization.

ABSTRACT

Clotrimazole (CLTZ) is a local imidazolic antifungal agent. A major problem associated with the successful formulation of effective dosage forms containing CLTZ is its poor aqueous solubility, which presents a hindrance for the local availability of CLTZ and limits the effective antifungal therapy. In the present study, the effects of various concentrations of poly(amidoamine) (PAMAM) dendrimers generation 3.5 (G3.5) and generation 4 (G4) with carboxylate (DCC), amine (DCN) and hydroxyl surface groups (DCO) on aqueous solubility, in vitro drug release studies, and for stability studies of CLTZ drug. The obtained results showed that all tested PAMAM dendrimers improved the solubility of CLTZ and the more potent were (DCC) dendrimers. The increase in solubility of CLTZ was highest at dendrimer concentration of 10 mg/ml. These observations indicate that PAMAM dendrimers enhance the solubility of CLTZ, The drug dendrimers complexes displayed the controlled release action during in vitro release studies. Formulation with amine and carboxylate were subjected to accelerated stability studies.

Key words: poly(amidoamine) dendrimers; clotrimazole; aqueous solubility; surface groups

ABSTRACT

In the current investigation, we have assessed the nephroprotective activity of the 70% ethanolic extract of Tecoma stans leaves (EETSL) against cisplatin, gentamicin and paracetamol (nephrotoxicants) induced nephrotoxicity in rats. Nephrotoxicity is confirmed by elevated kidney weight, blood urea, serum creatinine, lipid peroxidation (LPO), decreased tissue glutathione (GSH) and body weight levels at the administered doses. The ethanolic extract produced reduction in kidney weight, blood urea, serum creatinine, LPO levels and reversed the depleted GSH levels and body weight. This is further confirmed by histopathological studies. The results of the present study reveals that the ethanolic extract of Tecoma stans leaves significantly inhibited the cisplatin, gentamicin and paracetamol induced renal damage in rats and this may be attributed to its antioxidant properties.

Key words: Tecoma stans, Lipid peroxidation, GSH, Cisplatin, Gentamicin, Paracetamol, Renal injury.

ABSTRACT

A simple, accurate and precise HPLC method for the estimation of memantine in bulk and pharmaceutical dosage form has been reported. Chromatography was performed with Shimadzu HPLC equipment comprising an LC-10A VP quaternary pump, a variable-wavelength programmable UV–visible detector, an SPD-10AVP column oven, and an SCL 10AVP system controller. A Rheodyne injector fitted with a 20μL loop was also used and data were recorded and evaluated using Class-VP 5.032 software. The Compound was separated, at ambient temperature (25 ± 2°C), on a  BDS C₁₈, ( 4.6 mm i.d x 250 mm, 5μm reversed phase column with 100% methanol as mobile phase at a flow rate of 1.0mL.min⁻¹. Before use, the mobile phase was filtered through a 0.22-μm Nylon filter. UV detection was performed at 274nm. A linear response was observed in the concentration ranges of 5-25μg/ml with a regression coefficient of 0.9999. The method was then validated for different parameters as per the ICH guidelines. This method can be used for the determination of memantine in quality control of formulation without interference of the excipients.

Keywords:  Memantine, RP-HPLC, ICH.

ABSTRACT

A new reverse phase high performance liquid chromatography (RP-HPLC) method for the quantitative determination of Nimorazole was developed and validated as per ICH guidelines. The analyte was injected into an HIBER C18 column (150 mm × 4.6 mm, 5μm), maintained at ambient temperature and effluent was monitored at 297 nm. The mobile phase consisting of acetonitrile: methanol: buffer (2:3:5 v/v/v). The pH of the mobile phase was adjusted to 4.0 by using O-phosphoric acid. The flow rate was maintained at 1.0 mL/min. and retention time was observed 1.76 min. The developed method shows high specificity for Nimorazole. Calibration curve was plotted with a range from 1-5µg/ml (r²>0.999). The lower limit of quantification (LLOQ) was found to be 0.5μg/ml. The method was validated for parameters like accuracy, precision, recovery, linearity, robustness. This RP-HPLC method is suitable for determining the concentration of Nimorazole and it was applied to routine analysis for determination of the Nimorazole from its formulation during pharmacokinetic study.

Keywords: Nimorazole, RP-HPLC, Validation.

ABSTRACT

A simple, specific, accurate and precise reverse phase high performance liquid chromatographic method has been developed for determination (drug release) of Citicoline in controlled release tablet dosage form by reverse phase separation was carried out on a columns containing different stationary phases, the final choice giving satisfactory theoretical plates and tailing with good reproducibility and run time, with dimension 250 mm × 4.6 mm internal diameter, 5-μm particle; Zorbax C18 reversed-phase column. The mobile phase consisting of buffer: methanol (95:5, pH 6.0) at a flow rate of 0.8mL/min. The UV detection wavelength was set at 270nm. The retention time for Citicoline was found to be 6.4 min. and recoveries from controlled release tablet dosage form were between 99.7% and 104.4%. The method was validated for specificity, linearity, accuracy, precision and robustness. The proposed method was optimized and validated as per the ICH guidelines.

Key words: Citicoline monosodium, Reverse Phase -High performance liquid chromatography, Dissolution, Validation.

ABSTRACT

The present study was investigated the antioxidant activities of the various extracts of Aegle Marmelos (AM) belongs to family Rutaceae. The antioxidant activities of extracts have been evaluated by using a range of in vitro assays and in vivo hepatoprotective model. In vitro Antioxidant activity was evaluated by percentage inhibition in different assays  including  2, 2’-diphenyl-1-picrylhydrazyl (DPPH), hydroxyl radical scavenging assay hydrogen peroxide radical scavenging assays, reducing power capacity. The extract exhibited potent antioxidant activity compared to known antioxidant. The extracts of A.Marmelos were tested for in vivo efficacy by carbon tetrachloride (CCl4) induced liver damage rats in hepatoprotective model. The in vitro antioxidant activities of extracts showed significant activities on reducing power, DPPH, hydroxyl radical and hydrogen peroxide nearer to control group based on IC₅₀ values. Oral administration of various extracts of A.Marmelos resulted in significant improvement on the levels of malondialdehyde (MDA) and superoxide dismutase (SOD), Catalse (CAT) in liver homogenate & Significant increase in level of MDA which was intoxicated by CCl4. CCl4 produced significant alteration of serum marker enzymes, total bilirubin, total protein and liver weight. The extracts significantly restored of these values towards normal compared to control group. Due to its natural origin and potent free radical scavenging ability A.Marmelos could be used as a potential preventive intervention for free radical mediated diseases.

Key words: DPPH, SOD, CAT, MDA, In Vivo & In Vitro Antioxidant assays

ABSTRACT

The objective of the present research work is to develop a isocratic reversed-phase liquid chromatographic (RP-HPLC) method for the determination of Aspirin in pharmaceutical pharmaceutical dosage forms for its related impurities in presence of esomeprazole. The chromatographic separation was achieved on a RP 18 column (100mm×4.6mm, 5 µm). The isocratic LC method employs mixture of buffer methanol and isopropyl alcohol in the ratio of (84:13:3 v/v) solutions as mobile phase. The buffer solution contains 6.8g of Potassium dihydrogen orthophosphate adjusted to pH 2.5 with orthophosphoric acid .The flow rate was 1.5 ml/min and the detection wavelength was 275 nm. In the developed HPLC method, the resolution between Aspirin and its potential impurity salicylic acid was found to be greater than 4.0. The drug was subjected to stress conditions of hydrolysis, oxidation, photolysis and thermal degradation in presence of esomeprazole. Considerable degradation was found to occur in basic medium and mild degradation observed in acid hydrolysis stress conditions. Degradation product formed during acidic hydrolysis was salicylic acid. The stress samples were assayed against a qualified reference standard and the mass balance was found close to 99.5%. The developed RP-HPLC method was validated with respect to linearity, accuracy, precision and robustness.

Keywords: RP-HPLC; Forced degradation; Validation; Aspirin, Salicylic acid Method development

ABSTRACT

Conventional liquid ophthalmic formulations are most convenient from patient point of view. But these formulation shows low bioavailability because of a constant lachrymal drainage in the eye which leads to frequent dosing. Moreover, the absorption of the drug drained through the nasolacrymal duct may result in undesirable side effects. To overcome these limitation different approaches has been applied such as ointment, gel, cream etc. These ophthalmic formulations also fails to show desired therapeutic responses because of their own disadvantages such as ointment makes blurred vision. So two different systems was combined together as niosomes and in-situ gel by incorporating niosomes in in-situ gel formulation so that it is easy to administered and retain at the site for prolong period of time. The Ofloxacin (OFL), a second generation fluoroquinolone derivative used in eye infections needs frequent dosing in its solution form. Vesicular system reported prolonged and controlled action at corneal surface but it has again limitation of drainage along tear produced.  In this, first niosomes containing ofloxacin were prepared by applying 3² full factorial designs and evaluated for its vesicle size, percent entrapment, in-vitro drug release kinetics and their stability. Also in-situ gel formulation was prepared by dispersing the niosomes in solution of carbopol 940 and Hydroxy Propyl Methyl Cellulose (HPMC) K4M. In-vitro drug release kinetics from niosomal in-situ gel formulation indicates that the minimum inhibitory concentration (MIC) of drug (4 μg/ml) was achieved within 1-2 hrs (batch G1-G9).

Keywords: Niosomes, in-situ gel, ophthalmic, ofloxacin, factorial design

ABSTRACT

A controlled release system is designed to provide constant or nearly constant drug levels in plasma with reduced dose, frequency of administration and fluctuations in plasma concentrations via slow release over an extended period of time.One of the least complicated approaches to the manufacture of controlled release dosage forms involves the direct compression of blend of drug, retardant material and additives to formulate a tablet in which the drug is embedded in a matrix of the retardant. Gabapentin is an anti epileptic drug used for the treatment of epileptic seizures and in treatment of post therapeutic neuralgia.  In this study controlled released Gabapentin matrix tablets were prepared by using different matrix forming polymers which include hydrophilic polymers like HPMC K15M, HPMC K100M, Xanthan gum and hydrophobic polymer like Ethylcellulose in various ratios to retard the release of drug upto 12hrs. The formulations containing the combination of hydrophilic and hydrophobic polymer combinations (HPMC K100M with Ethycellulose) and the formulations prepared with the combination of two hydrophilic polymers of synthetic and natural origin (HPMC K100M with Xanthan Gum) exhibited maximum drug release(99%) upto12hrs during in vitro dissolution studies with optimum swelling characteristics.

Keywords: Gabapentin, matrix systems, HPMC K15M, HPMC K100M, EC

ABSTRACT

Anti-asthmatic activity of the alcoholic extract of Physalis angulata roots in ovalbumin induced experimental mice model. The roots were extracted with ethanol and the anti-asthmatic activity of the extract in ovalbumin-induced asthma in albino mice was evaluated. The parameters assessed were assessment of lung inflammation, OVA-specific immunoglobulin E titre by ELISA and histopathology of lung. The extract (100 and 200 mg/kg I.p) inhibited ovalbumin induced asthma by decreasing releasing of inflammatory mediators. Physalis angulata roots extract has potent anti-asthmatic activity. Its anti-asthmatic property probably acts via a reduction in inflammatory mediator’s release. The present study indicates that Physalis angulata has significant anti-asthmatic property.

Keywords: Asthma, Inflammation, Airway hyper-responsiveness and Ovalbumin Ig E.

ABSTRACT

The selective enzyme assisted extraction of curcumin was developed and optimized from Curcuma longa. When water was used as solvent, 3% of curcumin were extracted representing a search for an interesting alternative for the extraction in industrial processes. A selective extraction process after the treatment with enzymes is proposed by using 30% (v/v) methanol which releases up to 15% of the curcumin, present in the rhizome. The optimal conditions were as follows: pH value was 5.5, concentration of cellulase solution was 2.5 mg/mL, incubation time was 8 h, incubation temperature was 50 ºC and solid:solvent ratio was 1:8 . Enzyme-assisted extraction was proved to be environment-friendly and economical, and could be used in natural product extraction in large scale.

Keywords: Curcuma longa, Total curcuminoids, enzymatic extraction

ABSTRACT

Two sensitive and reproducible methods are described for the quantitative determination of zonisamide in the presence of its degradation products. The first method was based on high performance thin layer chromatographic (HPTLC) followed by densiometric measurements of their spots at 238 nm.the separation was on HPTLC aluminium sheets of silica gel 60 F₂₅₄, using toluene:ethtyl acetate (6:4 v/v), this system was found to give compact spots for zonisamide after development (R_f value 0.49.). The second method based on high performance liquid chromatographic (HPLC) of the drug from its degradation products on reversed phase Vydac column ODS (250 mm × 4.6 mm, 5.0 µ), at ambient temperature using a mobile phase consisting of methanol: water (50:50, v/v) and Retention time was (4.71 min.) Both the methods were validated as ICH guidelines no chromatographic interference from capsule excipients was found. Zonisamide was subjected to acid and alkali hydrolysis, oxidation,and dry heat. The drug was fount to be stable in neutral wet heat and photo- degradation conditions as the proposed analytical methods could effectively separated the drug from its degradation products, they can be employed as stability-indicating.

Keywords: Column liquid chromatography, Thin layer chromatography, Method validation and degradation , Zonisamide

ABSTRACT

A simple, reliable, rapid, precise, sensitive and validated RP-HPLC method has been developed to determine Acetaminophen (AI) and Prasugrel (PRA) in synthetic mixture form. Chromatographic separation achieved isocratically on Luna C₁₈ column (5 µm, 150mm x 4.60mm) and acetonitrile: 0.05M ammonium acetate buffer (pH 4.5) in the ratio of 75:25 (v/v) as the mobile phase, at a flow rate of 0.6 mL/min. Detection was carried out at 245 nm. Parameters such as linearity, precision, accuracy, recovery, specificity and ruggedness are studied as reported in the ICH guidelines. The retention times for AI and PRA was found to be 2.25 ± 0.5 and 8.72 ± 0.5 min respectively. Linearity for AI and PRA was in the range of 75-375 μg/mL and 10-50 μg/mL respectively.  The mean recoveries obtained for AI and PRA were 99.58 and 99.48% respectively and RSD was less than 2. The correlation coefficients for all components are close to 1. Developed method was found to be accurate, precise, selective and rapid for simultaneous estimation of AI and PRA.

Keywords: Acetaminophen, Prasugrel, RP-HPLC, Validation