ABSTRACT

Traditional medicines have been recently recognized as a precise and knowledge for new source of anticancer drugs and new chemotherapy adjuvant to enhance the efficacy of chemotherapy and to ameliorate the side effects of cancer chemotherapies however their healing mechanisms are still largely unknown. The current available methods of treatment like chemotherapy, radiation, and surgery can induce certain side effects, so there is urge for alternate or adjuvant therapies has arisen. The natural compounds present in plants were known to inhibit or kills carcinogenic cells. In the race for the designing of new anti-cancer drugs development the phytochemical investigation of herbs has contribute new ideas in some extent. Apoptosis is the programmed cell death in which the cells activate an intracellular death program and kill themselves in a controlled way. The phytochemicals that have the anticancer property by inducing apoptosis are safe, abundantly available from dietary sources and the drugs have good immunomodulatory properties.  This attempt has been made to review plant and plant products used in the prevention and treatment of cancer by inducing apoptosis.

Keywords: Traditional medicine, Medicinal plants, Phytochemicals, Apoptosis.

ABSTRACT

Solid lipid nanoparticles (SLNs) have emerged as a forefront drug delivery system with diverse potential applications in pharmaceutical and cosmeceutical research, nanomedicine and other allied branches of science. Recently, increasing attention has been focused on these SLNs as colloidal drug carriers for incorporating hydrophilic or lipophilic drugs. Proteins and antigens intended for therapeutic purposes can also be incorporated or adsorbed onto SLNs, and further administered by parenteral route or by alternative routes such as oral, nasal and pulmonary etc. Due to their unique size dependent properties SLNs offer possibility to develop new therapeutics. The ability to incorporate drugs into these nanocarriers offers a new prototype in drug delivery that could use for drug targeting. Hence SLNs hold great promise for reaching the goal of controlled and site specific drug delivery and hence attracted wide attention of researchers. Also the problems associated with conventional chemotherapy can be overcome by encapsulating them in SLNs. The present review focuses on SLNs brief introduction, utility in terms of their advantages, production methodology, characterization and applications and their possible remedies. Further investigation and research related to SLNs may open new vistas in nanotechnology and in therapy of multifaceted diseases.

Keywords: Nanomedicine, Solid Lipid Nanoparticle, Nanocarrier, Drug Delivery.

ABSTRACT

Self nanoemulsifying drug delivery (SNEDDS) is used for drugs which exhibit low water solubility. Dissolution is the rate limiting factor for these drugs. SNEDDS are capable of improving the bioavailability substantially of such drugs. They are formulated by utilizing an oil phase, surfactant and a co-surfactant. This formulation forms nano emulsion (O/W type) on contact with aqueous body fluids i.e gastric juices when administered orally. Solid SNEDDS (s-SNEDDS) can also be formulated in the form of tablet which shows greater advantages. With recent and potential future developments, this technology will continue to enable novel applications in drug delivery and overcome limitations associated with the delivery of poorly water soluble drugs, mainly those belonging to BCS class-II and class-IV.

Keywords: Self nanoemulsifying drug delivery system (SNEDDS), oil phase, surfactants, co-surfactants, Pseudo ternary phase diagrams.  

ABSTRACT

Autism Spectrum Disorder (ASD) represents a major public health concern as a prevalent neurodevelopmental disorder with pronounced risk for failure of adaptation across social, educational, and psychological outcomes. The exact etiology of autism is unclear. However there is a lot of research work giving some insights about the possible predisposing factors that enhance chance of autism. Several lines of evidence suggest that prenatal and/or early life acetaminophen exposure may adversely affect neurodevelopment increasing incidence of autism. Since 1980 acetaminophen greatly has replaced aspirin as an analgesic and anti-pyretic following reports indicating that aspirin use was associated with Reye’s syndrome. Notably acetaminophen use has been associated with at least a 10-fold rise of autism epidemic since the early 1980s. Several mechanisms have been suggested to implicate the role of acetaminophen in pathogenesis of autism as altered immune function and impaired hepatic detoxification capacity resulting in accumulation of potentially neurotoxic metabolites. In early life, maturational compromises to the glucuronidation pathway in combination with the compromises to the sulfation pathway that typify autistic children, may lead to utilization of the suboptimal secondary metabolic routes with the potential for adverse neurological effects in susceptible individuals. Acetaminophen use during pregnancy has also been associated with altered metabolism increasing autism rates in born infants. The use of acetaminophen may also trigger autism by activating the endocannabinoid system thereby interfering with normal development. Accumulating evidence linking significantly increased rates of autism with prenatal and early life acetaminophen exposure strongly suggests its cautious use during these critical times.

Keywords: Autism, acetaminophen, sulfation, immunity, cannabinoid system.

ABSTRACT

The essay is a short overview of the chemistry, pharmacology, pharmacokinetics, clinical uses and the delivery aspects of calcitonin. It will deal with different routes of delivery of calcitonin with the focus lying primarily on the intra-nasal delivery and oral delivery of the hormone.  Calcitonin was initially administered as a subcutaneous/ intra-muscular injection and to overcome certain problems associated with these delivery routes such as patient compliance, inflammation at the site of injection, hypersensitivity reactions and stability of the formulation other routes of delivery are being explored and the most successful route of administration so far is the intra-nasal route. The essay will also give brief information of the nasal spray available in the market currently and the pump-system used for the intra-nasal delivery. The oral route of administration is also being dealt with in some detail as it is one of the most promising routes for delivery of calcitonin and other such peptide molecules and has a bright future. In vitro and in vivo research towards making a successful oral delivery formulation is being carried out and this essay gives a brief overview of some important areas studied so far.

Keywords: Calcitonin, Hormone, drug delivery.

ABSTRACT

Thiophene a five member heterocycles had been found with enormous biological activities with the suitable modifications in the structure. The present review is an attempt made to direct the attention of the researchers towards the thiopene ring for the development of newer chemical entities which are quite useful in the treatment of various life threatening diseases and disorders This review article covers the most active thiopene derivatives that have shown considerable biological actions such as antimicrobial, anti-inflammatory. This review also discusses the structure-activity relationship of the most potent compounds. It can act as an important tool for medicinal chemists to develop newer compounds possessing thiopene moiety that could be better agents in terms of efficacy and safety

Keywords: Thiophene, Biological activities, method of synthesis.

ABSTRACT

Focal ischemia, a ischemia of specific area of the brain, is responsible for many deaths and disabilities across the globe that may be due to clot formation or accidental collapse of arteries in either case treatment is required to treat ischemic insult and further deterioration of neurons in the brain. To know exact pathophysiology and biochemical events it becomes necessary to study those conditions in vivo. Furthermore to check drug moieties for the treatment of ischemic conditions and its prognosis, animal models are required to mimic those conditions artificially. There are many factors on which choice of animal for animal model is depend like age, species and genetics. The species which would be near to humans in evolution hierarchy should exhibit almost similar physiological as well as pathological architecture of vascularity and ischemic condition. But other factors cannot be ignored in this regard like finances, survival and labour intensiveness. During literature survey, out of many available models of ischemia, rodent models are found to be used mostly in preclinical research so this review is a collaborative approach contains methods and types to select animal and animal models along with the mechanisms and assessment of ischemic conditions.

Keywords: Focal Ischemia, MCAO, animal models, ischemia, choice of animal models

ABSTRACT

Pain in orofacial region is frequently observed in dentistry due to dryness of mouth (Xerostomia).  The commonly used drugs like antihistamines, antihypertensives etc and disease like diabetes may induce dryness of mouth. Treatment with conventional drugs has side effects. Hence, natural remedy with herbal drugs mainly Zingiber officinale a well known hepatoprotective, antiemetic and antiarthritic drug as a possible alternative in treatment of Xerostomia has been viewed in this paper.

Key words:  Dryness of mouth, Zingiber officinale, salivary secretion

ABSTRACT

One of the most critical problems of throughout the world especially in developing and underdeveloped countries is the increase in human population. Fertility control is an issue of global and national public health concern. Sexual and reproductive health is a prerequisite of all goals because it has a direct link to social, economic and human development. Family planning has been prompted through several methods of contraception, but due to adverse effects produced by synthetic steroidal contraceptives attention has now been focused in indigenous plants for possible contraceptive effect. Contraceptive ability of plants has been reported in several animal models. The reversibility of the anti-fertility effects of plants and its active compounds are of potential clinical relevance in the development of contraceptive. This review attempts to focus on the potential of medicinal plants as the source of new contraceptive principles.

Keywords: Contraceptive, medicinal plants, Fertility, adverse effects.

ABSTRACT

Mouth dissolving tablets (MDTs) prepared by the crystalline / phase transition method has focused on decreasing the dissolution (or disintegration) time of the tablets in the mouth, while maintaining sufficiently high mechanical strength to withstand handling during manufacturing, packaging, and transportation. The key to developing a successful MDTs formulation by the phase transition method is to select the right excipients. In general, MDTs are made of highly hydrophilic materials and possess highly porous structures for fast water absorption into the tablet. After heating MDTs, the median pore size of the tablets was increased and tablet hardness was also increased due to phase conversion into the tablets. It is concluded that a combination of low and high melting point sugar alcohols, as well as a phase transition in the manufacturing process, are important for making MDTs without any special apparatus.

Keywords: Mouth dissolving tablets; Phase transition; crystalline transition; Sugar alcohol.

ABSTRACT

Plant derived medicines are popularly used nowadays considering their natural origin and low side effects. Phytochemical compounds are responsible for their various biological activities. Qualitative evaluation of such formulations is a challenging task due to high variability of their chemical components. This work aimed at preparing and evaluating a polyherbal anti-stress medicine, formulated using four potent Ayurvedic drugs namely Withania somnifera, Valeriana wallichii, Bacopa monnieri and Piper longum and also isolating a bioactive marker compound from the same.The formulation was prepared as per classical methods of Ayurveda and analysed for physicochemical characters like loss on drying, total ash content, acid insoluble ash, water soluble extractive value and alcohol soluble extractive value by standard methods. Phytochemical analysis was performed for detecting presence of carbohydrates, phenols, flavonoids, tannins, alkaloids, steroids, Terpenoids, glycosides and saponins and for estimating active groups like total phenolic content, flavonoids, tannins and saponins. High Performance Thin Layer Chromatography fingerprint profiling was performed to confirm the presence of various phytocompounds. The biomarker compound was isolated by column chromatography method and characterized by UV-Visible, H¹-NMR, C¹³-NMR and Mass spectroscopy methods. Physicochemical analysis showed presence of about 18% water soluble components and about 14% alcohol soluble components. Preliminary phytochemical analysis confirmed presence of carbohydrate, phenols, flavonoids, tannins, alkaloids, steroids, glycosides, phytosterols and saponins. Quantitative analysis showed presence of about 7.6% phenols, 1.3% flavonoids, 1.1% tannins and 3.5% saponins. Spectroscopic study indicated isolated compound is a phenolic compound 3, 4, 5-tri hydroxybenzoic acid.

Keywords: Antioxidants, bioactive compound, phenolic compound, flavonoid, memory, anti-stress, Withania somnifera, Valeriana wallichii, Bacopa monnieri, Piper longum

ABSTRACT

A new validated RP – HPLC method was developed for the simultaneous determination of Thiocolchicoside and Ketoprofen in combined dosage form. The method developed produced high sensitivity, precision and accuracy. An isocratic C18 (Inertsil ODS, 250 x 4.6 mm, 5µ) column was used with mobile phase of composition Acetonitrile: Phosphate buffer (70: 30 at pH 4.6) at a flow rate of 1.0 mL/min with UV detection at 258.2 nm for separating Thiocolchicoside and Ketoprofen. The retention time of Thiocolchicoside and Ketoprofen were 2.4 min and 3.5 min respectively. The developed method was validated for specificity, linearity, precision, accuracy, limit of detection (LOD), limit of quantification (LOQ) and robustness as per ICH guidelines. Linearity for Thiocolchicoside and Ketoprofen were found in the range of 2.0 – 12.0 µg/ml and 6.2-38.75 µg/ml, respectively. The percentage recoveries for Thiocolchicoside and Ketoprofen ranged from 99.35- 100.21% and 98.66-99.29 %, respectively. The proposed method could be used for routine analysis of Thiocolchicoside and Ketoprofen in their combined dosage forms. All the proposed methods for Thiocolchicoside and ketoprofenare simple, selective, reproducible and specific with good precision and accuracy. The method was proved to be superior to most of the reported methods. These proposed methods for estimation of selected drugs were successfully applied either in tablet dosage form. More over the low solvent consumption along with short retention time of 2.4 and 3.5 for both Thiocolchicoside and Ketoprofen to be cost effective when compared to other developed method shown in literature reviews. The proposed method can be used as alternative methods to the reported ones for the routine determination of selected drugs under the study in tablet dosage form

Keywords: Liquid Chromatography; Thiocolchicoside, Ketoprofen, Combined dosage forms; Simultaneous estimation, Validation

ABSTRACT

The main objective of this research work was to formulate and evaluate the bi layer tablets of chlorzoxazone by using different polymers. Chlorzoxazone is centrally acting skeletal muscle relaxant. The tablets containing immediate releasing layer and sustained release layer. The polymers used are microcrystalline cellulose pH 102, sodium starch glycol ate, croscarmellose, povidone for immediate releasing layer, HPMC K 100 cps, K4cps, E15cps, carbomer 971P, and natural gums like guar gum, Xanthan gum for sustained drug release layer. The matrix tablets were prepared by direct compression and wet granulation methods. All the excipients are tested for compatibility with drug, which revealed that there was no physical and chemical interaction occurred. The Pre formulation parameters such as bulk density, tapped density, compressibility index and Hausner’s ratio were analyzed. The In-Vitro drug release studied were Performed in the USP dissolution apparatus- (paddle) using pH 1.2 HCL buffer and pH 6.8 phosphate buffer as dissolution media at 100rpm speed and temperature of 37^oC ± 5^oC. The sampling was done at periodic time intervals of 1.5, 3, 4, 6, 8, 10 and 12 hours and was replaced by equal volume of dissolution media after each withdrawal. The cumulative amount of drug release at different intervals is estimated using UV method. Based on the evaluation result the formulations F6 was selected as best formulation among immediate release and is used to compress with sustained release layer. Among all formulation FB8 formulation (HPMC K100m 88%) shown maximum release of 98.84% drug in 12^th hour.

Keywords: Chlorzoxazone, sodium starch glycolate, HPMC K100m, K4M, dissolution studies, sustained release.

ABSTRACT

Two simple, sensitive and precise HPTLC and RP-HPLC methods were developed for the estimation of berberine from Coscinium fenestratum, and its formulation. For the determination of berberine by HPTLC method, precoated silicagel 60F₂₅₄ on aluminium sheets and a mobile phase system comprising of n-butanol: glacial acetic acid : water (8:1:1 % v/v/v ) was selected. After development the plate was scanned and quantified at 350 nm. Linearity was found in the concentration range of 10 to 50 ng/spot (r=0.9992). Limit of detection was found to be 5 ng/spot and limit of quantification was found to be 10 ng/spot. In RP-HPLC method, separation was achieved on a Phenomenex, Luna, C₁₈ column (150 x 4.6mm internal diameter, 5µ particle size) using a mobile phase consisting of potassium dihydrogen phosphate (pH - 2.5) (A)  : acetonitrile (B), where B was run in gradient programme (20% for 0.01-20min, 50% for 20-25min, 50% for 25-26min, 20% for 26-30min), at a flow rate of 1ml/min and the elute was monitored at 220nm. The calibration curve was obtained in the range of 100 - 500 µg/mL. The slope, intercept and correlation coefficient values were found to be 57588, 6041and 0.9959, respectively. The method was validated in compliance with ICH guidelines. Low relative standard deviation and good % recovery values of both the methods showed that the developed methods were highly precise, accurate and can be employed for the routine analysis of formulations containing berberine.

Keywords: Coscinium fenestratum, Berberine, HPTLC, RP-HPLC, Frok capsules, Validation.

ABSTRACT

Extended spectrum -lactamases are plasmid mediated. These plasmids produce enzymes that hydrolyze broad spectrum cephalosporins and monobactams. They acquire resistance prevalently through plasmid encoded. Study determines plasmids and their correlation with drug resistance against many antibiotics that limits their therapeutic implications. Bacteriological analysis of 50 samples susceptible for ESBL was conducted. The samples subjected to susceptibility tests and detection of ESBL. Plasmid DNA isolation of all the ESBL positive strains of E. coli was done by alkali-lysis method. Finally the presence of plasmid was correlated with susceptibility to beta lactam drugs. ESBL was detected in 56% (28 out of 50 isolates). Maximum ESBL incidence recorded of E. coli (30 %) followed by Klebseilla pnemoniae (18%) and Pseudomonas aeruginosa (8 %). ESBL exhibited high-level resistance to beta lactam antimicrobial agents like  Amoxiclave (56%), Cefuroxime (54%), Cephotaxime (54%), Ceftriaxon (50%), Ceftazidime (46%) and Cefixime (36%). During plasmid profiling of eight isolates of ESBL E. coli showed one to four definite bands indicating the presence of different plasmids. ESBL’s constitute a growing class of plasmid-mediated -lactamases which confer resistance to broad spectrum β-lactam antibiotics. Incidence of ESBL is continuously increasing globally with limited treatment alternatives and formulates treatment policy. Moreover, restricted use of the third generation cephalosporins lead to withdrawal of selective pressure and use of lactam and -lactamase inhibitor combinations may exert reverse mutation on these enzymes. There is a strong correlation between the number of plasmids harbored by an isolate and drug resistance.

Keywords: Prevalence, Extended Spectrum β-Lactamase (ESBL), Clinical Infections and Plasmid profiling

ABSTRACT

Clerodendrum indicum.(L.)Kuntze is commonly known as bharangi, roots and leaves are used in skin and digestive disorders by folk people. In Ayurvedic medicine same is used as cough and pitta suppressant. However, very less work is reported from this plant. The aim of the study in this paper was to evaluate its cytotoxic and antioxidant activity of leaf and bark extracts. Cytotoxic potential was explored using brine shrimp mortality assay and antioxidant potential of the extracts was explored using quantitative TLC based DPPH assay and Qualitative Radical scavenging DPPH assay. An attempt was made to isolate the active fraction of the plant from leaf extract. Out of four extracts   Methanol extracts of leaf (C.indicum) showed significant cytotoxic activity of 90% at the dose of 200µg/ml.  Maximum number of antioxidant bands were obtained in chloroform extract of the leaf sample. Methanol extract of leaf gave a flavonoids fraction which showed promising cytotoxic activity. Thus, study has provided lead and needs elaborate experimentation.

Keywords: Brine shrimp, DPPH, Cytotoxic, Antioxidant, Clerodendrum indicum, TLC.

ABSTRACT

The present investigation focuses on the Optimization and formulation of medicated nail lacquer containing Fluconazole for transungual drug delivery system using ethyl cellulose as polymer and two different penetration enhancers. Fluconazole is a tri azole antifungal drug having broad spectrum activity. It acts by inhibiting 14 – α demethylase, a cytochrome P450 enzyme which converts lanosterol to ergosterol. Ergosterol inhibition causes increase in permeability of cellular membrane of fungi and hence leakage of cellular components. In present study Formulations were designed according by the design expert software 8.0.7.1 and the central composite design was selected for designing of experiments. The prepared formulations were evaluated for the different parameters such as drying time, smoothness of flow, gloss, water resistance, non – volatile content, drug content, in – vitro diffusion studies, in – vitro permeation studies, drug release kinetic studies. By applying the available information from the evaluation of nail lacquer 35 optimized formulations were obtained and out of which three were selected for further studies. Three optimized products were subjected to different evaluation parameters, drug release kinetics, anti – fungal testing and stability studies.

Key words: transungual drug delivery, Fluconazole, optimization, penetration enhancers, in – vitro permeation studies, ethyl cellulose.

ABSTRACT

Plant polyphenols are gaining increasing attention due to their potent antioxidant properties and marked effects in the prevention of various oxidative stress associated diseases. Identification and extraction of phenolic compounds from different plants has become a major area of health and medical research. In the present study, antioxidant activity of methanolic extracts of vegetative and reproductive parts of Moringa oleifera Lam. were tested for its free radical scavenging activity by spectrophotometric methods. Total phenolic and total flavonoid content were assayed spectrophotometrically. We observed high amount of total phenolic and flavonoid content in leaves and flowers of Moringa oleifera and this may be responsible for increased antioxidant activity in the plant. Antioxidant enzymes like ascorbate and ascorbate peroxidase (APX) were also found to be higher in vegetative and reproductive parts of Moringa oleifera. Our study reveals that M. oleifera leaves and flowers are potent source of natural antioxidants and the plant is valuable in pharmaceutical industry.

Keywords: Antioxidant enzymes, flavanoids, phenolics, reducing power, scavenging activity, Moringa oleifera.

ABSTRACT

In the present investigation an attempt has been made to prepare and evaluate medicated lollipop of mebendazole. One of the major health problems faced by hundreds of millions of school-age children is infection by helminths, more commonly known as worms. Mebendazole is used as a broad-spectrum anthelmintic. The conventional dosage forms like tablets, capsules, syrups etc are inconvenient for paediatric patients because of difficult to swallow tablets and capsules or unpleasant taste of drug. As a result, the demand for developing new technologies has been increasing day by day. Lollipops or lozenges are flavored medicated dosage forms intended to be sucked and held in the mouth or pharynx containing one or more medicaments usually in the sweetened base. Medicated lollipop is designed to improve patient compliance, acceptability and increase oral retention time. The lollipops were prepared by heating and congealing method using methylcellulose as polymer. Drug-excipient compatibility study was carried out using FT-IR. All the formulations were subjected to various physicochemical evaluations like weight variation, hardness, drug content, friability etc. The in-vitro dissolution study of F0 was found to be 96.14% at 15min whereas F1 was found to be 99.33% at 25min. Stability study was carried out as per ICH-Guidelines (Q1A) at 30^oC and 65% RH. From the present study it can be concluded that addition of hydrophilic polymers yield good result to prolong oral retention time of lollipop. Medicated lollipop can provide an attractive alternative formulation in the treatment of paediatric patients.

Keywords: Medicated lollipop, Mebendazole, methylcellulose (MC)

ABSTRACT

Garcinia pedunculata is a medicinal plant commonly known as Amlavetasa, belonging to the family Clusiaceae. The fruit of Garcinia pedunculata were used in the diet as a spice. It has been used as folk remedy in different ailments such as chronic catarrh, asthma, cough, bronchitis, cardiotonicand fever. The present study has been carried out to evaluate the anti inflammatory activity of aqueous extract of fruits of Garcinea pedunculata by carrageenan induced paw edema method. Eighteen healthy wistar albino rats were divided into three different groups of six rats each. Group I administered with normal tap water (5ml/kg) served as normal control. Group II administered with Ibuprofen 100mg/kg served as reference standard and group III administered with aqueous extract of fruits of Garcinea pedunculata(400mg/kg). In Acute oral toxicity study there was no mortality in any dose up to 2000mg/kg. The aqueous extract of fruits of Garcinea pedunculata has shown significant anti inflammatory activity by significantly decrease in the paw volume recorded at three different time interval compared with control group (**p< 0.01). It can be concluded that aqueous extract of fruits of Garcinea pedunculatahas potent anti inflammatory activity and there is a need for further scientific investigation to explore its anti inflammatory activity.

Keywords: Garcinia pedunculata, Amlavetasa, Ibuprofen, Bronchitis, Anti- inflammatory, Carrageenan.

ABSTRACT

Recurrent Aphthous Ulcer is the most common mouth ulcer disorder; found upto 25% in general population. It causes significant morbidity through pain and interference with eating. Ayurved provides a cure and prevents recurrences. For the present study , 30 patients were registered and treated into single group under the trial of combined effect of two formulations named Karpooraadi vati and Chitrakaadi Gutika  for 15 days. An analysis based on subjective & objective parameters  revealed that combination of two formulations provided significant improvement & relief in the patients. No recurrence and side effect were noted during trial and follow up.

Keywords-Karpooraadi vati, Mukhapaka ,RAU (Recurrent Aphthous Ulcer), SarvasarRoga

ABSTRACT

The aim of the current study was to assess the antioxidant potential, total phenolic and flavonoid contents of crude extracts of Artabotrys crassifolius. The leaves and barks of Artabotrys crassifolius were extracted sequentially with hexane, chloroform and ethanol. The corresponding crude extracts obtained were then subjected to TPC, TFC, ABTS, DPPH and FRAP assays. Among the extracts tested, ethanol extracts of barks and leaves showed promising radical scavenging activity which necessitates further isolation and characterisation of the bioactive compounds present in the respective extracts.

Keywords: Antioxidant, Phenolic, Flavonoid, Artabotrys crassifolius

ABSTRACT

A clinical bacterial isolate from a patient urine sample in Kasr El-Aini was identified by biochemical and molecular means to be E. coli . This isolate was optimized for production of L-asparaginase (L-asparagine amidohydrolase), a relatively widespread enzyme found in bacteria, eukaryote and mammals but not man. This enzyme catalyzes the deamidation of L-asparagine to L-aspartic acid and ammonia. The production of L-asparaginase was achieved through optimization of fermentation parameters and it showed 6.05 IU of enzyme activity. The produced L-asparaginase was then purified by means of chromatography techniques and tested against three different cell lines for its anticancerous activity, human colon cancer CACO-2, Human breast Cancer MCF-7 and Human cancer prostate PC-3. The expression for the regulatory genes BAX, P53 and BCL2, was analyzed by RT-PCR and it was clear that L-Asparaginase enzyme shows anticancer activity against (MCF-7) and (PC-3), where it was non-effective to the cell line (CACO-2). It was also noticed that BAX and P53 genes were upregulated under the effect of Asparaginase enzyme and that BcL2 gene was down-regulated in Human Breast and prostate Cancer cell line while Human colon cell line was not.

Keywords: L-asparaginase, Purification, E.coli, Antitumor activity, Expression genes

ABSTRACT

A simple, selective, linear, precise and accurate UPLC Method was developed and validated for rapid assay of Nordette in tablet Formulation. Isocratic elution at a flow rate of 0.4ml/min was employed on C8 1.7 µm (2.1 mm x 100 mm) Column at ambient temperature40 °C. Injection Volume was found to be 5.0 µl. The mobile phase consisted of Acetonitrile : Water  60:40 v/v which is filter through a 0.2 µm filter The UV detection wavelength was 220nm and 2µl sample was injected. The retention time for Ethinylestradiol, Levonorgestrel is found to be ± 1.4 minutes and ± 2.1 minutes respectively. A linear regression curve was constructed, and the correlation coefficients (R²) and assessment values calculated. The percentage RSD for both Ethinylestradiol, Levonorgestrel was found to be 1.5%.The Accuracy of method ranges between 97.0 – 102.8%.  The method was validated as per the ICH guidelines. The method was successfully applied for routine quality control analysis of pharmaceutical formulation.

Keywords: Nordette, Ethinylestradiol, Levonorgestrel, UPLC, Recovery, Precise.

ABSTRACT

A study of 90 cases of urinary tract infection in patients with diabetes mellitus has been presented with special reference to epidemiological aspects. A Prospective study was conducted in diabetes mellitus patients with symptomatic Urinary tract infection. This study revealed the incidence of urinary tract infection to be more common in females underlining the fact that females are more prone to infection (Male: Female — 1:2.3).The incidence of urinary infection was progressively higher with the duration of diabetes mellitus, with most infections occurring beyond 10 years of diabetes. Patients most commonly presented with fever, increased frequency of micturation and dysuria and were found to have pyrexia, dehydration and suprapubic tenderness as the commonest clinical signs.

Keywords:  DM-Diabetes mellitus, UTI-Urinary tract infection.

ABSTRACT

A simple, precise and sensitive reverse-phase high performance liquid chromatographic method was developed and validated for the simultaneous estimation of Ramipril and Metoprolol tartarate in pharmaceutical formulations. Chromatographic separation was performed on a High performance liquid chromatography equipped with auto sampler and UV detector. Good sensitivity for all analyte was observed with UV detection at wavelength of 218 nm, Separation was performed on a BDS Hypersil C₁₈ (250 X 4.6mm) 5µm, using a mixture of 0.1% Triethylamine buffer pH 3.5 and Acetonitrile in the ratio of (10:90, v/v). The method results in excellent separation with good resolution between the two analytes. The within day variation %RSD values between Ramipril and Metoprolol tartarate were 0.55 and 0.82. The recovery was greater than 98% with %RSD less than 1.00. The method was validated according to ICH guidelines by performing linearity, accuracy, precision, limits of quantitation and selectivity. The results show the method is suitable for its intended use.

Keywords: Ramipril (RAM), Metoprolol tartarate (MTP), HPLC, Simultaneous determination, Relative standard deviation (RSD), Validation.

ABSTRACT

In the present paper an effort was made to isolate a biomaterial from the fruit pulp of Annona squamosa and evaluate its film forming capacity. Annona squamosa was isolated by an economic method and subjected to various physical evaluation parameters. The biomaterial was subjected to spectral studies like IR, ¹H NMR and DSC analyses. Phenytoin loaded biofilms were prepared using the isolated biomaterial and other co- processing agents. The prepared biofilms were evaluated for their film parameters and subjected to in-vitro drug release studies using static MS diffusion apparatus. The results were compared with the standard HPMC film. The experimental results revealed that the prepared biofilms possessed good folding endurance with appreciable release characteristics. The best film formulation was PS6 with percentage cumulative release of 91.85% over 36 hours. Hence it clearly indicated that the isolated biomaterial possessed inbuilt filmability.

Keywords: Biofilms, Biopolymers, Annona squamosa, Phenytoin.

ABSTRACT

In the last two decades, antibiotic resistance has become a severe problem worldwide. Herbal antimicrobials have enormous potential as they can serve purpose with lesser side effects than synthetic antimicrobials. Weeds release different allelochemicals which can act as antimicrobials or herbicides. Leaves of two important Indian weeds viz. Heliotropium indicum L. (Boraginaceae) and Synedrella nodiflora (L.) Gaertn. (Asteraceae) were taken in this allelopathic and antimicrobial study.  Seed germination is considered to be the most significant stage especially under stress conditions and thus acts as an excellent model bioassay technique. Aqueous and ethanolic leaves extract of both plants progressively affected germination parameters of tested plants. But it affected seeds of Lactuca sativa more than those of Vigna mungo.  Lactuca sativa Germination % declined to 40%-52% in case of ethanolic extract of these weeds. Ethanolic extracts are more effective in inhibiting germination in both indicator plants. The weed extracts were very effective against Escherichia coli, Staphylococcus aureus and fungus Aspergillus niger. Salmonella enterica is the most resistant strain tested against these extracts. Heliotropium indicum L. was found to have tannin, alkaloid, and saponin and glycoside in both types of extracts. Synedrella nodiflora L. contain phenols, alkaloids and flavonoids in both aqueous and ethanolic extracts. Terpenoids and tannin were found in ethanolic extract of Synedrella nodiflora. The present study concludes that both plants contain herbicidal and antimicrobial constituents. Further studies regarding the isolation and identification of these antimicrobial and herbicidal constituents are necessary.

Keywords: Heliotropium indicum, Synedrella nodiflora, weed, allelopathy, antimicrobial, herbicide, Phytochemical

ABSTRACT

Some new 3-chloro-(4-substituted aryl)-1-(8-methoxy-[1,3,4]thiadiazino[6,5-b]indol-3-yl)azetidinones (4a-4g) have been synthesized from N-(substituted benzylidene)-8-methoxy-[1,3,4]thiadiazino[6,5-b]indol-3-amine (3a-3g). These newly synthesized compounds were characterized by elemental (C, H, N) and spectral (IR, ¹HNMR mass) analysis. Compounds 3a-3g and compounds 4a-4g of the present series have screened for their antibacterial and antifungal activities. Compounds 4f and 4g were found to be the most potent members of the present series; they showed maximum antibacterial and antifungal properties much better than the standard drug. In this series Chloroamphenicol was used as standard drug for antibacterial activity and Fluconazole was used as standard drug for antifungal activity.

Keywords: Indole, thiadiazine, Azetidinone, Antibacterial activity, Antifungal activity

ABSTRACT

Steroids are widely prescribed in modern medicine, because steroid hormones are crucial for proper functioning of the body. Steroid prolonged use is associated with serious AEs. Hence this study was carried out to assess the prescribing pattern and appropriateness of steroids. A prospective observational study was conducted to analyze for the pattern of prescribed steroids and also analyzed to that of the recommended therapeutic guidelines. Out of 1084, 14.5% (157) were steroid therapy. Maximum use of steroids was prescribed for patients above 50 years of age. Almost 38.8% of reasons were related to RTI. The average number of drugs prescribed for each prescription was 9.82±3.7.  The drugs prescribed in the study population includes 13.29% of steroids and 54.1% were commonly given through nebulization at the time of admission and tablets was most common dosage form at the time of discharge. 2.5±8.23 average numbers of drug interactions, 21.66% had moderate drug interactions involving steroids. There were 4 adverse drug reactions observed and none of the steroids were involved in precipitating the ADRs.  As per therapeutic guidelines, 38.85% of steroids were inappropriately prescribed and Rs. 495±39.49 was the average cost increased (drugs cost alone) for patients for whom the steroids were inappropriately prescribed. This study may be concluded that use of therapeutic guidelines while prescribing corticosteroids will benefit the patients because of lesser side effects, and it also may reduce the cost of treatment and improve therapeutic outcome.

Keywords:  Steroids, Appropriateness, Therapeutic Guidelines, Outcome.

ABSTRACT

Microorganisms play a very important role in the eco-friendly and green synthesis of metal nanoparticles. The inherent, clean, nontoxic and environment friendly. The present study focuses on the rapid synthesis of titanium nanoparticles by Iraqi Lactobacillus isolates. Seventy five isolates  from(120) samples included35vaginal swabs from healthy women, 45 infant stools and 40 yoghurt were isolated and identified to species, then tested for TINPs production. Results showed that only six(8%) isolates produced titanium nanoparticles ,titanium nanoparticles were characterized with Atomic Force Microscopy (AFM) and found the average size ranges from 70.98 to 105.37  nm. The best of our study, this is the first report on synthesis of titanium nanoparticles by Iraqi Lactobacillus isolates from different sources.

Keywords: Lactobacillus, Atomic Force Microscopy

ABSTRACT

Use of herbal medicines is increasing day by day. Herbal medicine has become popular form of healthcare. The consumption of plant based medicines and other botanicals in the west have increased manifold in recent years. Application of modern scientific knowledge coupled with sensitive analytical technique is important for the quality evaluation and standardization of polyherbal formulations. Mucuna pruriens, an important medicinal plant with wide medicinal properties, is frequently used in a large number of traditional herbal preparations. The present study deals with development and validation of RP-HPLC method for the quantitative estimation of L-DOPA from polyherbal formulations. The method involves Chromatographic separation was performed with SHIMADZU HPLC (Model no. LC- 20 AD) equipped with isocratic pump and manual injector (20μl). Spinchrom chromatographic software was used for data acquisition. RP- C18 (250 mm X 4.6 mm X 5 micron) column was used for analysis. Mobile phase comprising of methanol and water in ratio of 20:80 v/v was filtered through 0.45 micron in membrane filter (Millipore) and degassed by sonication; flow rate of 1ml/min was maintained throughout the run. Column effluent was monitored at 280 nm with variable wavelength UV detector. Thus this developed HPLC method could be further used for the determination of L-dopa in the polyherbal formulations.

Keywords: Polyherbal formulation, HPLC analytical method, M. pruriens, L-dopa, Validation. 

ABSTRACT

Leaves of Balanites aegyptiaca have been used in Africa as traditional medicine in the form of juice to treat diarrhea, dysentery, cuts and wounds. So this study is intended to discover the antioxidant and antibacterial activity of Balanites aegyptiaca leaves. Leaves were macerated using methanol to get a crude extract. Antioxidant activity of methanol extract was found to be 89.6 % at 1 mg/mL with IC₅₀ value of 182.02 μg/mL (r² = 0.9883) using DPPH (2, 2-Diphenyl-1-picryl hydrazyl) free radical scavenging method. In addition, the antibacterial activity of the methanolic leaf extracts was assessed on one gram-positive and one gram-negative bacterium using the disc diffusion assay. Antibacterial activity of methanol extract was higher for Escherichia coli with 8.15 ± 1.22 mm zone of inhibition and for Staphylococcus aureus methanol extract was not effective with the zone of inhibition of 0.00 ± 0.00 mm. The methanolic leaves extract of B. aegyptiaca revealed potential antioxidant activity but antibacterial activity was found to be relatively lower to that of the standard antibiotics used.

Keywords: Balanites aegyptiaca, DPPH, antioxidant activity and antibacterial activity. 

ABSTRACT

A simple, rapid, precise LC-MS compatible method for the degradation impurities if any UHPLC method was developed for the determination of 1-deoxynojirimycin (DNJ) in Mulberry leaves. The DNJ in 200 mg dried leaves was extracted twice with 50 mL aqueous 0.05 mol/L HCl, then derivatized by 9 fluorenylmethyl chloroformate (9 FMOC-Cl) in Potassium Borate buffer, and analyzed using a high performance liquid chromatograph equipped with a fluorescence detector. Chromatographic separation of the same was performed by using a Shimpack XR ODS-III (150*3.0mm) 2.1µm as stationary phase with a mobile phase of 0.1% Acetic acid in water: Acetonitrile (60: 40, v/v) at the rate of 0.5 mL/min. Wavelengths used were 254 nm for excitation and 322 nm for emission, which were suitable for detecting the native fluorescence of all the pigments assayed. The derivatized DNJ was well dissolved from the hydrolysis products of 9 FMOC-Cl. The linearity ranged from 0.45 to 66 mg/L, and the detection limit was 0.2 mg/L (S/N = 3). The content of DNJ in Mulberry leaves was 0.09%, the recovery was 90.0%-110.0%.

Keywords:  UPLC, Method development, Method Validation, 1-deoxynojirimycin and Mulberry leave

ABSTRACT

In Indian traditional system of medicine, herbal remedies are prescribed for the treatment of various diseases including liver diseases. The present study aims to carry out a systematic investigation of the protective influences of the ethyl acetate and ethanolic extract of R.tuberosa against N-Nitrosodiethylamine-induced hepato-carcinogenesis in wistar albino rats. Liver function was assessed by the determination of AST, ALT and ALP levels along with histopathological examinations. The serum biochemical analysis suggests that the use of ethanolic extract of R.tuberosa exhibited significant protective effect from hepatic damage in N-Nitrosodiethylamine induced hepato-toxicity model. Hepatic enzyme induction is generally an adaptive response associated with increases in liver weight, induction of gene expression, and morphological changes in hepatocytes. Histopathological studies revealed further evidence for its hepatoprotective activity.

Keywords: Ruellia tuberosa; N-Nitrosodiethylamine; Hepato carcinogenesis; Hepato toxicity.

ABSTRACT

The present work aims at evaluating the wound healing potential of a traditional plant Piper betle (PB) of both leaves and stem. The ethanolic extract of both Piper betle leaves and stem were investigated to evaluate the rate of wound healing enclosure and the histology of healed wounds in rats. Four groups of adult female albino wisttar rats were experimentally wounded at the dorsal region of the rats. Group 1 animals were left with untreated and set as negative control. Group 2 animals were treated with 10% Povidone Iodine, and set as positive control. Group 3 and 4 treated with ointment formulation containing 10% Piper betle leaves and 10% Piper betle stem leaves extract respectively. All the four groups are treated with for 21 days. Wound healing was assessed by rate of wound closure estimation and histology studies on the 21^st day of post wounding. 10% Piper betle stem enhanced the wound healing process by increasing rate of wound closure compared to negative control group. Histological observation also showed better organized tissue and more collagen fibers in 10% Piper betle stem treated group. These results strongly document the significant effect of 10% Piper betle stem extract to accelerates the rate of wound healing and closure in the experimentally induced wound rats.

Keywords: Piper betle, Wound healing, Hematoxylin & Eosin stain and Massion Trichrome stain the rate of wound healing and closure in the experimentally induced wound rats.

ABSTRACT

Fast dissolving oral films (FDOFs) are the most advanced form of oral solid dosage form due to more flexibility and comfort. Fast dissolving film is a dosage form which when placed in the oral cavity, quickly gets hydrated, sticks onto the site of application and then disintegrates to release the drug. Fast dissolving oral films of isosorbide mononitrate were prepared by solvent casting method. Optimization was carried out to study the effect of independent variables (different polymer and plasticizer concentration) such as HPMC E5 and HPMC E50 as polymer and PEG 400 as a plasticizer on the dependent variables like T90% (sec), in-vitro disintegration time (sec) & % moisture absorption (%). Design expert software (version 8.0.1.6) was used to optimize the formulation. Prepared films were subjected to different evaluation parameters such as surface pH, weight uniformity, thickness of strip, % moisture absorption, % moisture loss, swelling index, drug content, in-vitro disintegration time, in-vitro drug release, stability studies and mechanical properties like folding endurance, tensile strength.

Keywords: Fast dissolving oral films, Optimization, Isosorbide mononitrate, Anova, PEG, HPMC.

ABSTRACT

Gestational diabetes mellitus is considered as one of the most common medical complications of pregnancy as it has implications on both the mother and the child. It is caused by reduced pancreatic β-cells function as they don’t produce enough insulin to meet the requirements of pregnancy. Internationally, it is recommended to screen all pregnant women by measuring their glucose between 24 and 28 weeks of pregnancy. It can be managed either non-pharmacologically or pharmacologically depending on the severity of hyperglycemia. The present  study was intended to measure the prevalence of gestational diabetes mellitus in Oman and to explore the available treatment options in both governmental and private hospitals. Out of 1792 patients who attended the Gynecological department between the study period, a total of 219 patients visited gestational diabetes clinic at Sohar Hospital, Saham Polyclinic and a private hospital. Of the total number of participants from all the clinics, 103 had a family history of diabetes mellitus whereas 17 had no family history. 120 patients agreed to participate in questionnaire interview and were informed about the purpose of the study. A good response from patients is a good indication for a future national study.  

Keywords: Gestational diabetes, Sohar hospital, congenital anomalies 

ABSTRACT

The synthesis, characterization and application of biologically synthesized nanomaterials are an important aspect in nanotechnology. Biological synthesis of silver nanoparticles has received a tremendous attention and has been a focus of research due to their high chemical, thermal stability and promising applications in medicinal field due to its environmental friendly approach and also low cost techniques. In the present study silver nanoparticles were synthesized using the aqueous extract of red seaweed Gracilaria dura (Ag.) J.Ag. as the reducing agent. The formation of silver nanoparticles was confirmed by colour change, UV-Visible Spectroscopy, FT-IR and X-Ray Diffraction Method (XRD). The nanoparticles showed an absorbance at 446nm on UV-Vis spectroscopy. The presence of proteins was identified by Fourier Transform-Infra Red spectroscopy (FT-IR).The presence of elemental silver was characterized by X-Ray Diffraction Method (XRD).These results not only provide a green approach for the synthesis of nanoparticles but also open a door for new pharmaceutical leads.

Keywords: Nanotechnology, Seaweeds, Gracilaria dura, silver nanoparticles. 

ABSTRACT

A simple, accurate, reliable and reproducible first order derivative method was developed for the simultaneous determination of Cefoperazone sodium (CEFO) and Tazobactam sodium (TAZO) in pharmaceutical formulation. The linearity was carried out by using the concentration range 5-50 µg/ml for CEFO (275.2 nm ZCP of TAZO) and 2-50 µg/ml for TAZO (225 nm ZCP of CEFO) respectively. The correlation coefficient of CEFO and TAZO was found to be 0.999 and 0.998 respectively. At zero crossing point (ZCP) of CEFO (225nm) TAZO showed a measurable derivative absorbance, whereas at zero crossing point (ZCP) of TAZO (275.20nm) CEFO showed a appreciable derivative absorbance value. Precision study showed that %RSD was within range of acceptable limits (< 2%). The % recovery for CEFO and TAZO was found to be within range of 98-101% and 98-102%respectively. The percentage assay was found to be 101.05% and 99.41% for CEFO and TAZO. The result of analysis has been validated as per ICH guideline. This method has applied successfully for determination of CEFO and TAZO in its pharmaceutical formulation. 

Keywords: Cefoperazone sodium, Tazobactam sodium, UV Spectrophotometry, First order derivative Spectrophotometry.

ABSTRACT

The purpose of research was to study process validation of Azithromycin 250 mg tablet dosage formulation. Tablets were manufactured by wet granulation method. The critical parameters involved in sifting, dry mixing, wet granulation, drying, dry milling, lubrication, compression and coating stages were identified and evaluated as per validation master plan. Uniformity of dry mixing was found to be satisfactory in 15min. For suitable wet mass consistency, slow speed of impeller was maintained during the addition of binder solution for 10 min which was followed by high speed of impeller for 20 min. Drying time of 1 hour was sufficient to achieve % Loss on drying up to 1.5-2%w/w. Uncoated azithromycin tablets were collected at different speeds and different stages and evaluated for their appearance, average weight, diameter, thickness, disintegration time, hardness, friability and assay. Film coating was performed in auto coater and film coated tablets were evaluated for appearance, average weight, diameter, thickness, disintegration time, hardness, friability, dissolution test and assay. Based on results, it can be concluded that Azithromycin tablets can be effectively prepared with the desired specifications and reproducible quality standards.  The outcome indicated that process validation data provides high degree of assurance that manufacturing process produces product meeting its predetermined specifications and quality attributes.

Keywords: Process validation, Azithromycin film coated tablet, Control variables 

ABSTRACT

A simple, rapid reverse phase high performance liquid chromatographic method (RP- HPLC) has been developed and validated for simultaneous estimation of Aceclofenac and Pregabalin in tablet dosage form. Chromatographic separation was achieved C-18 (250 mm × 4.6 mm, 5.0μ) as stationary phase and mobile phase containing phosphate (pH adjusted to 5.0 ± 0.05 using NaOH.) Buffer: Acetonitrile (30:70 v/v) at flow rate of 1 ml/min using UV detection at 210 nm. The retention time for Aceclofenac and Pregabalin was found to be 3.177 and 5.530 min respectively. The method was validated as per International Conference on Harmonization guideline and successfully used for the quantitative analysis of commercially available tablet. The calibration curve was linear over the concentration range of 20-60μg/ml for Aceclofenac and 15-45μg/ml for Pregabalin.. Lower values of Limit of Detection (0.60μg/ml for Aceclofenac and 0.88μg/ml for Pregabalin) and Limit of Quantification (1.84μg/ml for Aceclofenac and 2.68μg/ml for Pregabalin ) indicated good sensitivity of the method. The method was validate with respect to linearity, robustness, precision and accuracy and was successfully applied for the simultaneous determination of aceclofenac and pregabalin from the combined dosage formulation. The percent amount for both the drugs were found to be within limits in the tablet dosage form for both the methods.

Keywords: Aceclofenac, Pregabalin, RP-HPLC, validation.

ABSTRACT

A new RP – HPLC method was developed for the simultaneous determination of  Montelukast and Rupatadine fumerate in combined dosage form. An Inertsil C18 column(100 x 4.6, 5µm) was used with mobile phase of composition Methanol : Buffer(0.1% triethyl amine in water with pH adjusted to 3.0 (70:30v/v at pH 4.6) at a flow rate of 1.0 mL/min and injection volume of 20µL with UV detection at 266 nm for separating Montelukast and Rupatadine fumerate. The retention time of Rupatadine fumerate and Montelukast were 5.76 min and 2.86 min respectively. The runtime of the analysis was 6 minutes. The specificity, linearity, precision, accuracy, limit of detection (LOD), limit of quantification (LOQ), ruggedness and robustness of the developed method were studied to validate as per ICH guidelines. The Linearity range for Montelukast and Rupatadine fumerate were 5.0 – 30.0 µg/ml and 5.0 – 30.0 µg/ml, respectively. The percentage recoveries were in the range for Montelukast and Rupatadine fumerate98.80-100.11 % and 99.06-99.44 %, respectively. The developed  method could be used for routine analysis of Montelukast and Rupatadine fumeratein their combined dosage forms.

Keywords: Liquid Chromatography; Montelukast, Rupatadine fumerate, Simultaneous estimation, Validation

ABSTRACT

Cyperus rotundus Linn. (Family: Cyperaceae), commonly known as Mothais a multivalent plant widely used in traditional medicine around the world for treatment of various diseases (fever, dysentery, malaria, skin disease, diarrhoea etc.). The present study was carried out to investigate the phytochemical profile of leaves of Cyperus rotundus. The powder of the leaves of Cyperus rotundus was successively extracted with acetone, aqueous, benzene, chloroform, cyclohexane, ethylacetate and methanol. A number of biologically active compounds have been isolated from the plant. Phytochemical analysis shows the presence of carbohydrates, glycosides, proteins, amino acids, phenolic compounds, tannins, steroids, anthraquinone, anthocyanin, flavonoid, saponins and alkaloid. Our findings provided evidence that crude aqueous and organic solvent extracts of these tested plants contain medicinally important bioactive compounds and it justifies their use in the traditional medicines for the treatment of different diseases. The result of the study could be useful to description and foundation of monograph of the plant.

Key words:  Phytochemical analysis, Saponins, Flavonoids and Cyperus rotundus.

ABSTRACT

An attempt was made to formulate and evaluate the Nebivolol HCl transdermal drug delivery system. The matrix type films were prepared by using solvent casting technique with polymers HPMC 15cps,PVP K-30,Eudragit RL100 and Methyl cellulose 15cps.Propylene glycol was used as plasticizer. The prepared films were evaluated for physicochemical characteristics such as thickness, weight variation, folding endurance, % moisture uptake and % moisture loss. The drug excipient compatibility was determined by Fourier Transform Infra red Spectroscopy. The results revealed that there were no interaction between drug and selected polymers. In vitro permeation studies were performed in Franz diffusion cell using commercial semi permeable membrane. Ex vivo studies were performed using skin of albino rats. Biological studies such as skin irritation test and % drug diffusion studies were carried out by using rabbits. Drug content varied from 73.72 ± 0.1to 95.4±0.15%. Moisture content and moisture uptake were increased for patches containing higher amount of HPMC due to its hydrophilic nature. The batch F4 (HPMC 1.5%, PVP 0.5%) had shown drug release for 24 h to the extent of 86.87% and drug release followed zero order release kinetics which was of non-Fickaian type of diffusion. The results of ex vivo and in vivo studies were well correlated with in vitro diffusion studies

Keywords: Nebivolol, HPMC, PVP, Eudragit RL100, MC, Transdermal matrix films

ABSTRACT

Cyclodextrin nanosponges are solid, porous, bio-compatible, nano-particulate three dimensional structures which form inclusion complexes with different types of lipophilic or hydrophilic drug molecules and have been used as drug carrier for different drugs. In this present work, new cyclodextrin-based nanosponges of atorvastatin were prepared by condensation polymerization and interfacial polymerization to release Atorvastatin in expected manner in the treatment of dyslipidaemia as novel carriers. Results of encapsulation efficiencies of all formulation trials revealed that condensation polymerization is the best method for nanosponges formation and that is considered as best selected method for preparation. For the selected condensation polymerization, encapsulation efficiencies of atorvastatin in nanosponge formulations were found to be 72 to 86%. SEM images revealed their porous nature and cavity was of β-cyclodextrin. The mean particle size of nanosponges was about 328 nm and Zeta potentials of the nanosponges were sufficient enough (-10 to -15mv) due to presence of carboxylic group and inclusion complex formation which assured stability of formulations. The results of FTIR and DSC confirmed that atorvastatin was compatible with β-cyclodextrin and completely encapsulated in nanosponges structure respectively. The selected formulation produces good dissolution profile (release more than 75% atorvastatin within 60 mins in 0.1 N HCL) which indicated that the solubility of atorvastatin was improved by forming nanosponges. In accelerated stability studies, no significant changes occurred in physical appearance and drug content of atorvastatin nanopsonges formulation during 3 months stability studies. Atorvastatin nanosponges confirmed by insolubility in water and organic solvents like dimethyl formamide, dichloromethane.

Keywords: Atorvastatin, β-cyclodextrin, nanosponges, cross-linker, inclusion complex, solubility.

ABSTRACT

The present work reports on the preparation of ethyl cellulose (EC)-pluronic F127 (PF127)-based tableted floating microspheres by the oil-in-water emulsion solvent evaporation method for the controlled release of acyclovir (ACV). Microspheres of this study were characterized by Fourier transform infrared (FTIR) spectroscopy to investigate the chemical interactions of ACV with the polymer, floating behavior, scanning electron microscopy (SEM) for morphology of the microspheres, differential scanning calorimetry (DSC) for investigating their thermal properties  and X-ray diffraction (XRD) as well as. In vitro release experiments of microspheres were performed in acidic pH 1.2 media to understand the release profiles of ACV. The selected sets of microspheres were compressed into tablets using the compressible excipients and their in vitro release performances were evaluated in pH 1.2 media.

Keywords: Floating microspheres, tablets, ethyl cellulose, pluronic F127, Acyclovir.

ABSTRACT

1,3,4 – thiadiazole derivatives derived from various reaction sequences with slight modifications in the side chain with primary amine group at 5^th position in the thiadiazole ring. The docking studies were done by using scroodinger software version against the enzyme protein kinase. The structures of all the compounds were drawn using chemdraw software version 8.0. All the thiadiazole derivatives showed satisfactory ligand binding energy between -2.70 to -5.60 k.cal /mole. Compounds A₃, A₂₁,M₃₄&M₃₆ showed better glide score with -5.4, -4.9, -4.7 and-4.00 respectively.

Keywords: Thiadiazole derivatives, molecular docking, Schroodinger software, ligand binding energy, protein kinase enzyme, mycobacterium tuberculosis.

ABSTRACT

Green beans contain high concentration of polyphenols, carotenoids, ascorbic acids, tocopherol and flavonoids which fight against oxidative damage. Free radicals have been implicated in the pathogenesis of most diseases. Thus, the consumption of dietary antioxidants from vegetables and fruits is beneficial in preventing these diseases. The present study was undertaken to evaluate antioxidant potential of ethanolic extracts of four different species of green beans. Ethanolic extract of Phaseolus vulgaris (french bean), Vicia faba (broad bean), Cyamopsis tetragonoloba (cluster bean) and Vigna unguiculata (cowpea) were studied for antioxidant properties by 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging assay, H₂O₂ decomposition, reducing power ability assay. Total phenolic content was measured by Folin Coilteau reaction and flavonoid contents were determined by AlCl₃ assay. Efforts were made to study the iron chelation. Total phenol content ranged from 17.00 ± 0.004 to 53± 0.007 µg GAE/mg while total flavonoid ranged 22 ± 0.003 to 36 ± 0.006 µg QE/ mg. All the extracts scavenged DPPH radical, decomposed H₂O₂ and had significant reducing potential. The IC₅₀ for DPPH scavenging activity was highest for Vigna unguiculata as 2.27 ± 0.19 mg/ml while lowest for Vicia faba as 0.18± 0.02 mg/ml. All the extracts chelated Fe²⁺ form of iron but not Fe³⁺. A positive and strong correlation (r² = 0.9) between total phenolic content & antioxidant activity suggests that green beans have enormous potential to enhance antioxidant capacity of our daily food supply and may provide health benefits in oxidative stress as neutraceuticals.

Keywords: Biological properties, phytochemicals, neutraceutical, oxidative stress, DPPH scavenging, green beans.

ABSTRACT

In this paper the authors proposed a simple, sensitive and selective liquid chromatography–tandem mass spectrometry (LC–MS/MS) assay method for the determination of mosapride in human plasma. This method employed mosapride–d5 as an internal standard (IS). Analyte and the IS were extracted form 100 µL of human plasma using solid–phase extraction with no drying, evaporation and reconstitution steps. The chromatographic separation was achieved on a C₁₈ column by using a mixture of methanol and 5mM ammonium acetate (80:20, v/v) as the mobile phase at a flow rate of 1.0 mL/min. The linearity of the method was established in the concentration range 0.18–60.0 ng/mL with r² ³ 0.99. The intra–day and inter–day precision (%CV) and accuracy results in five validation batches across five concentration levels were well within the acceptance limits. The validated method was found to be applicable to clinical studies.

Keywords: Mosapride, Human plasma, Solid–phase extraction (SPE), LC–MS/MS, Pharmacokinetics

ABSTRACT

A simple, rapid, precise and highly selective spectrophotometric method was developed for simultaneous estimation of Norfloxacin and metronidazole in tablet dosage form. This method involves the measurement of absorbances of Norfloxacin and Metronidazole at the wavelength of 272nm (λmax of Norfloxacin) and 334nm (λmax Metronidazole) .0.1 N NaOH was used as solvent. Linearity was observed in the concentration range of 1-10 µg/ml for Norfloxacin and 1- 19µg/ml for Metronidazole. The accuracy of the method was confirmed by recovery studies of tablet dosage forms and was found to be 101 and 102% for Norfloxacin and metronidazole respectively. The method showed good reproducibility and recovery with % RSD less than 2. The LOD of Norfloxacin and metronidazole and LOQ of Norfloxacin and metronidazole   was found to be 0.3μg/ml and 1.16μg/ml and 0.79μg/ml and 2.4μg/ml respectively. The developed method was free from interferences due to excipients present in tablets .Thus the proposed method was found to be rapid, specific, precise, accurate and cost effective quality control tool for the routine analysis of Norfloxacin and metronidazole in bulk and combined dosage form.

Keywords: Norfloxacin (Nor); Metronidazole(MTZ), UV spectrophotometric method; simultaneous equation method

ABSTRACT

An efficient and convenient multi component reaction for the synthesis of 2-Imino-4,6-diaryldihydropyrimidines scaffolds have been accomplished from chalcones and guanidine hydrochloride in the presence of a catalytic amount of an alkali under solvent-free conditions using microwave irradiation.  The synthesized pyrimidines have been characterized on the basis of their chemical properties and spectroscopic data.  Operational simplicity, short reaction times, excellent yields and environmentally-benign conditions are the other advantages of this protocol. Using this method, we have synthesized some new pyrimidines with antimicrobial properties and high chemical yields in much short reaction times.

Keywords: Solvent- free, Antibacterial, Chalcones, Biological activity, Green Chemistry

ABSTRACT

The objective of this present study is to formulate and evaluate the floating drug delivery system of Bambuterol HCl prepared by using synthetic polymers. Formulations were prepared by direct compression technique and sodium bicarbonate was incorporated as gas generating agent. Using different polymers of hydroxyl propyl methylcellulose (HPMC) such as, HPMC K100M, HPMC K4M and HPMC K100M for their gel-forming properties. The compressed Bambuterol HCl floating tablets were evaluated for physical parameters like Tablet Thickness, Hardness, % Friability, Weight variation, Content uniformity, In vitro buoyancy, Swelling index and In vitro dissolution study. Its bioavailability was reported about 20%. As the concentration of the polymers in the formulations increased the drug release decreased. Hence it was considered suitable candidate for formulation as gastro-retentive floating drug delivery system. Floating tablets has been accepted as a process to achieve controlled drug delivery by prolonging the residence time of the dosage form at the site of absorption, thereby improving and enhancing the bioavailability of drug.

Keywords: Bambuterol HCl, Floating drug delivery system, Hydroxyl propyl methylcellulose.

ABSTRACT

In the present study, Flurbiprofen was used for preparing Floating dosage form that are designed to retain in stomach for a long time and have developed as a Floating drug delivery system by using various polymers like Carbopol 940 and HPMC K4M to enhance the bioavailability and therapeutic efficacy of Flurbiprofen. The mechanism of action of Flurbiprofen is Non selective COX inhibitor which inhibits the prostaglandin synthesis. Sodium bicarbonate and citric acid was incorporated as a gas generating agent. The direct compression method is used in present work. The formulation was optimized on basis of acceptable tablet properties like optimum hardness, uniform thickness, consistent weight uniformity and low friability. The prepared formulation shows better and significant result all the evaluated parameter. 

Keywords: Flurbiprofen, Floating drug delivery system, HPMC K4M, Carbopol 940.

ABSTRACT

There is an increasing commercial demand for nanoparticles due to their wide applicability in various areas such as electronics; catalysis, chemistry, energy, and medicine Nanoparticles are prepared by a variety of chemical methods which are not environmentally friendly. We report a rapid and convenient method to reductively prepare silver nanoparticles using silver nitrate In this report we use aqueous extracts from plants namely Morinda tinctoria, Michelia champaca. The extracts template the reductive preparation of silver nano particles which are found to be < 100 nm in size. The synthesized compounds are characterized by FT-IR, UV_VIS and XRD data.  Green synthesized silver nanoparticles showed antibacterial activity against two Gram-positive bacteria Staphylococcus aureus, Bacillus subtilis and two Gram-negative bacteria Pseudomonas aeruginosa, Escherichia coli and antifungal activity against Candida albicans, Aspergillus niger and Cryptococcus neoformans.  The synthesized nano particles were found to be highly toxic against different multi drug resistant human pathogens

Keywords: Morinda tinctoria, Michelia champaca. silver nanoparticles

ABSTRACT

The purpose of present work was to prepare a nimesulide-loaded liquid suppository using menthol and to study the effects of various penetration enhancers such as neem oil, tulsi oil and ethanol on the cumulative percentage release of nimesulide. The physicochemical properties such as gelation temperature and gel strength of various formulations composed of nimesulide, menthol and poloxamer 188 were investigated. The in vitro study of nimesulide delivered by the liquid suppositories composed of poloxamer 188, menthol and various concentrations of penetration enhancers were performed. The in vitro studies were performed using Keshary-Chein diffusion cell and Small wonder (Lyzer apparatus). The cumulative percentage release of nimesulide of each formulation were calculated and compared with the other formulations. The liquid suppository formulations containing neem oil 2% and tulsi oil 2% showed excellent release rate as compared to other formulations.

Keywords: Nimesulide, Neem oil, Tulsi oil, Ethanol, Liquid Suppository, In vitro release studies.

ABSTRACT

Drug utilization review can be defined as review of drugs used in a population to determine effectiveness, potential dangers faced by the patients, problems arised due to drug interaction and also promotes rational use of drugs. Rational use of drugs minimizes polypharmacy , drug interactions minimizing the hospital stay. Our objective was to understand the pattern of occurrence of various cancerous disorders and promote rational use of drugs. It was a prospective observational study which was undertaken in Yashoda Cancer Institute, Hyderabad under the guidance of Dr. N. Bethune for a period of 6months. A total of 100 prescriptions were included in the study. The study criterion were the inpatients upto 90 yrs of age of either gender. Patient data relevant to the study was obtained from patient case records. According to the data collected we found that males (54%) predominated females (46%) and patients were more prominent in 41-60 age group. The use of anti cancer drugs in this hospital was found to be rational and more than 50% of the drugs prescribed are from National list of essential drugs. In conclusion, the use of anti cancer drugs was found to be rational. Pharmacist is the key person for better management of therapy based on stage and condition of patient and also manage the increased cost of therapy and increased risk of unwanted reactions. It has been our sincere effort to minimize the anticipated untoward events (atleast to some extent) by our dissertation

Keywords: Drug utilization review, effectiveness, drug interaction

ABSTRACT

Synthesis of coumarin based random copolyester was prepared by the reaction of biscoumarin monomer 1 and anthroquinone3 with azeloyl chloride through interfacial polycondensation technique by using phase transfer catalyst. The chemical structure of the copolyester was investigated by Fourier-transform infrared spectroscopy (FTIR) and proton nuclear magnetic resonance (¹H-NMR) spectroscopy. Disc diffusion method was employed to investigate the antifungal activity of the synthesized copolyester.

Keywords: Coumarin, Antifungal, Copolyester, Condensation.

ABSTRACT

Cassytha filiformis (Common name: love-vine, Vernacular name: Kothan) is a creeper plant in the family Lauraceae, traditionally used in treatment of several diseases (cancers, human birthing issues, hypertension, pains and fever). The present study was carried out to investigate the phytochemical profile of whole plant (except root) of Cassytha filiformis.L. The powder of the cassytha filiformis.L was successively extracted with acetone, aqueous, benzene, chloroform, cyclohexane, ethanol, ethyl acetate and methanol. Phytochemical analysis shows the presence of carbohydrates, glycosides, proteins, amino acids, phenolic compounds, tannins, steroids, anthraquinone, anthocyanin, flavonoid, and alkaloid. The result of the study could be useful to description and foundation of monograph of the plant.

Keywords: Cassytha filiformis, Flavonoid, Phytochemical, Anthocyanin, Alkaloids and Glycosides.

ABSTRACT

Gastroretentive systems have the unique quality to remain in the gastric region for several hours. Due to this they prolong the gastric residence time of the drug significantly. Floating microspheres possess the advantage of better flowing properties attributed to the use of low density polymers. Clarithromycin is a broad-spectrum antibiotic and extensively absorbed orally. It is used in the eradication of H. Pylori infection combined with an acid suppressing agent. Clarithromycin floating microspheres were prepared using polymer Ethyl Cellulose in different concentrations by solvent evaporation method. The FTIR studies showed no interaction between drug and polymers. The floating microspheres were evaluated for angle of repose, percentage yield, particle size, SEM, buoyancy percentage, drug content, percentage drug entrapment, in-vitro dissolution studies, kinetics of drug release and stability studies. Formulation F3 was found to be the best formulation showing the highest degree of sustained release that is 73.86% at the end of 12 hours. Formulations were seen to follow zero order release profile and Korsemeyer-Peppas model was the best fitting model. Marginal changes were observed in the drug content, buoyancy time and In-vitro dissolution studies which are insignificant. Storage conditions were carried out at 40±2⁰C/75±5%RH for 6 months.

Keywords: Gastroretentive, Clarithromycin, H. Pylori, Korsemeyer-Peppas

ABSTRACT

A novel, simple, rapid and stability-indicating reversed-phase ultra performance liquid chromatographic and mass spectrometric method was developed and subsequently validated for quantitation of Efavirenz (EFV) from drug substance matrix. The separation was achieved in 2.5 minutes on Waters ACQUITY UPLC BEH C₁₈ (50 x 2.1) mm, 1.7µm column in isocratic mode with flow rate 0.4 mL/min. Mobile phase used was 0.01 M ammonium acetate buffer pH 7.5 and acetonitrile in ratio 50:50 v/v. Detection was carried out at the maximum wavelength of 247 nm using a photodiode array detector. The retention time of Efavirenz was found 1.8 minutes. Specificity of the method was established on drug substance by hydrolytic and oxidative stress conditions. Validation of analytical method was carried out as per the current ICH guidelines for linearity, recovery, precision, limit of detection, limit of quantification and robustness parameters.

Keywords: Efavirenz (EFV), UPLC, Antiretroviral, Stability indicating, ICH

ABSTRACT

A simple, rapid, sensitive and precise UV spectrophotometric method has been developed for the estimation of rupatadine fumarate from bulk drug and pharmaceutical formulation. In this method rupatadine fumarate showed maximum absorbance at about 250 nm in absolute alcohol. Beer’s law was followed in the concentration range of 1 to 30 μg/ ml. Regression equation was found to be y = 0.0257- 3x 10^-5  and coefficient of correlation was 0.9999 . The proposed method is accurate, sensitive, reproducible and useful for the estimation of   rupatadine fumarate from bulk drug and pharmaceutical formulation.

Keywords: Rupatadine fumarate, Absolute alcohol 

ABSTRACT

Dermatophytosis is currently treated with the commercially available topical and oral antifungal agents in spite of the existing side effects. Treatment of these cutaneous infections with secondary metabolites produced by wild plant is considered as an alternative approach. Exploring the unexplored aspect of the wild plants for developing antidermatophytic drugs is a novel attempt which needs further investigation. Study aims to screen eleven wild medicinal plants possessing antifungal activity against the clinical fungal isolates from dermatophytic patients. The methanolic plant extract were analyzed by well diffusion assay and phytochemical characterization of the active ingredient were determined possessing mycocidal activity. Aspergillus sp. was effectively controlled by the extracts of C.roseus , R.communis, T. cordifolia, J. curcas, C. longa; Curvularia sp. by T. cordifolia, R. communis , T. erectus , C. longa; Cladosporium sp. C. roseus  , R. communis , L. inermis , T. erectus, A. nilotica; Microsporium sp. by C. roseus, R. communis, J. curcas, L. inermis, A. nilotica  and Penicillium sp. by A. nilotica, R. communis, C. longa, T. occidentalis and T. erectus . Maximum Alkaloid was recovered from T. peruviana, Saponin in R. communis and C. roseus, Flavanoid from R. communis, Tannin in T. erectus and C.  roseus and phenols from L. inermis. Methanolic plants extracts of Catherenthus reseus, Riccinus communis, Tagetus erectus, Acacia nilotica, Lawsonia inermis and Thuja occidentalis were found to be significantly controlling the test fungi.  Data revealed that plants possessing higher phenol, tannin and saponin show antifungal activity.

Keywords: Antifungal and Phytochemical screening; Clinical fungal isolates; fungal dermatophytosis; Wild Medicinal plant

ABSTRACT

The ground water is one of the major component to be environmentally protected. It is still neglected to some extent and is not given much consideration in the existing environment protection legislation in most of the developing nations. An important issue for the benefit of society is to find out the extent of impurity of water due to the pathogenic infections in the potable upper level ground water resource which is being consumed by the millions of habitants in the wide Himalayan foothill (plains) region of India. The region consists of alluvial flood effected plains with water table at shallow depth. This research paper pertains to investigation of pathogenic infections in potable first level water table at shallow depths. The samples were collected from the hand pumps of critically located village clusters in the region and tested during the pre-monsoon, monsoon and post-monsoon seasons of the year- 2011-2012. The tests for few common bacteria have been performed, e.g. -  E. coli, S. aureus, P. aeruginosa and S. typhie. The results found are positive Research Highlight; A wide scope for further research does exist for the societal issue, by  investigating complete range of pathogens in the similar geological structure/topography existing anywhere in world to solve health related problems. Also to check suffering and mortality due to water borne diseases and measures to protect and isolate the ground water pollution..

Keywords Ground Water, Surface Water Level, Potable Water, Ground Water Pollution, Pathogens and Bacteria.

ABSTRACT

The aim of the present investigation was to evaluate the effect of mucilage on the material and physico-chemical properties of native and modified starches obtained from Ipomoea batatas. Ipomoea batatas starch were pregelatinized and acid modified, subsequently, dispersions of mucilage with native, pregelatinized and acid modified starches in a ratio of 1:20, 1:10, 2:10, 3:10 and 4:10 respectively were produced. The order of magnitude pregelatinized starch > acid modified starch > native starch were seen for parameters such as moisture sorption, hydration capacity and swelling capacity, while native starch > pregelatinized starch > acid modified starch for porosity and angle of repose. These orders were also observed respectively with the dispersion of the various starches in mucilage. Generally an increase in particle size, flow properties, moisture sorption capacity, true densities and a decrease in hydration capacity, swelling capacity and porosity were observed as the mucilage concentration increased.

Keywords: Ipomoea batatas starch, pregelatinized, acid modified, dispersion, mucilage

ABSTRACT

Exposure to pesticides both occupationally and environmentally causes a range of human health problems. A vast majority of the population in India are engaged in agriculture and are therefore exposed to the pesticides used in agriculture. Endosulfan formulations are used in commercial agriculture and home gardening. Endosulfan causes degeneration of spermatozoa of mice as well as declined testosterone level. Endosulfan exposure lead to ovarian nuclear degeneration. It also causes altered liver function and hepatomegaly. Thus present study is designed to evaluate nephrotoxic effect of on biochemical and histological parameters of kidney of mice. The ‘treatment’ groups received Endosulfan 2 mg/kg b.w daily by gavage method for four and eight weeks. Animals were sacrificed after the scheduled treatment. Urea, uric acid and creatinine was increased many folds in endosulfan administered group of guinea pig. Degeneration was observed in glomerulus and bowmen’s capsule. Tubular system of nephron show more degenerative changes. It is evident from study that endosulfan exposure causes elevated biochemical parameters of kidney and degenerative changes in tubular system of nephrons of guinea pig leading impaired nephrotoxicity in kidney.

Key words: Nephron, Hepatomegly, Glomerulus, Bowmen’s Capsule

ABSTRACT

Atorvastatin Tablet is one of the best selling drugs in the world, but still it suffers inadequate bioavailability problem from oral dosage. An attempt was taken to evaluate the floating drug delivery system for Atorvastatin by incorporating it in different grades of Carbomer matrix. Direct compression technique was selected and different once daily formulations were designed. The tablets were successfully floated over prolonged time and released the drug at a controlled fashion depending on the grade and quantity of Carbomer used. The tablets were evaluated for different physical tests including weight variation, friability, hardness, diameter and thickness. The compatibility between drug and polymers were confirmed by FT-IR spectra. Buoyancy characteristics of the tablets were determined by observing lag time, swelling index and total buoyancy period. The mechanism of drug release from the matrixes was assumed by fitting the release profile with different mathematical equations. Formulation F-5 and F-10 were found to release the drug at most sustaining manner and also had the longest total floating time. 

Keywords: Gastro-retentive, buoyancy, compatibility, swelling index and kinetics.