ABSTRACT

Lac (Laccifer lacca) is an Indian animal origin drug. In Unani medicine Lac is known as Luk (Arabic word). Its medicinal properties are well advocated in unani literature. That’s why its use for various ailments is commonly prevailed among unani fraternity since centuries. This drug is very famous among unani practitioner for its anti-obesity effects. Various Unani medicine formulations (compound drugs) are having Lac as a chief constituent are in market. One of its most famous and acceptable formulation “Safoofe muhazzil” is being prescribed profoundly to counter obesity. Unani Scholars like Ibn Sina (Avicena), Razi, Ibn Rushd, Rabban Tabri, Hakeem Abdul Hakeem, Najmul Ghani, Jurjani and Kabeeruddin etc., wrote extensively about the medicinal use of Lac for various diseases in their respective books and treatises. Apart from Unani System of Medicine lac is also being used as drug in other complementary and alternative medicines (CAM) system especially in Indian system of medicine namely Ayurveda and Siddha.

Keywords: Lac; Laccifer lacca; Luk; Luk Maghsool; Unani medicine; Medicinal Plants.

ABSTRACT

Viral diseases, including emerging and chronic viruses, are an increasing worldwide health concern. As a consequence, the discovery of new antiviral agents from plants has assumed more urgency than in the past. A number of native Indian medicines of plant origin are known to have antimicrobial and anti-inflammatory activity, although only a few have been studied for their antiviral properties and immunomodulating effects. The number of patients seeking alternate and herbal therapy is growing exponentially. Herbal medicines are the synthesis of therapeutic experiences of generations of practicing physicians of indigenous systems of medicine for over hundreds of years. Herbal medicines are now in great demand in the developing world for primary health care not because they are inexpensive but also for better cultural acceptability, better compatibility with the human body and minimal side effects. This review gives an overview of some important medicinal plants with antiviral activities which are traditionally used in India.

Keywords- antiviral, Herbal medicine, immunomodulating effects

ABSTRACT

Modified release dosage forms have acquired a great importance in the current pharmaceutical research. It denotes a formulation of a medicinal agent that releases the active ingredients over several hours, in order to maintain a relatively constant plasma concentration of the drug. In addition, sustained and controlled release devices are not applicable in some cases like time-programmed administration of hormones and many drugs. The living systems are predictable dynamic resonating systems which require different amounts of drug at expected times within the circadian cycle.  Pulsatile drug delivery system has fulfilled this requirement. This system is such a system where drug is released suddenly after well-defined lag time or time gap according to circadian rhythm of disease states. No drug is released from the device within this lag time. This method is good for the drugs with extensive first pass metabolism and targeted to specific site in the intestinal tract. Pulsatile drug delivery system classified as time controlled pulsatile release, stimuli induced, chemical stimuli induced pulsatile systems, external stimuli pulsatile release etc.

Keywords - lag time, pulsatile, time controlled, first pass metabolism, stimuli induced

ABSTRACT

The plant based antidiabetic remedies are gaining popularity throughout the world. There is large number of medicinal plants which are traditionally used for the management of diabetes. These plants need detailed investigation for the quality and quantity of the concerned chemical compounds. The present review has highlighted 81 plant species belonging to 12 families and 68 genera. Amongst the various plant parts of these species, leaves have been utilized in almost 50% of the total medical preparations. Other plant parts also have their utility in antidiabetic formulations. This information is useful for the herbal practitioners, biomedical researchers and pharmaceutical industries.

Keywords: Active principle, diabetes, extracts, hypoglycemia, plant species.

ABSTRACT

Presently, several targeted treatment systems including magnetic field, electric field, ultrasound, temperature, UV light and mechanical force are being used in many disease treatments (e.g. cancer, nerve damage, heart and artery, anti-diabetic, eye and other medical treatments). Among them, the magnetic targeted drug delivery system is one of the most attractive and promising strategy for delivering the drug to the specified site. The targeted systems improve therapeutic index of drug molecules by minimizing the toxic side effects on healthy cells and tissues. The use of magnetic carriers for drug delivery of chemotherapeutic agents has evolved since 1970s, when little research has developed albumin microspheres encasing the chemotherapeutic agent Adriamycin, and using magnetite as the magnetically susceptible component.

Keywords: Magnetic drug delivery, Magnetic delivery, Electric field, Magnetic field delivery, Magnetic targeted drug delivery,

ABSTRACT

Melasma is a common skin ailment that affects young women especially during pregnancy and at menopause. It is more common in Asian and Hispanic women. Studies have found that it affects about 0.25-4% of the population in South East Asia. It is characterized by symmetrical gray to brown hyperpigmented lesions over sun exposed areas of the skin and is associated with substantial psychological impacts. The management of melasma is challenging and requires a long term treatment. Although various treatment modalities including topical and systemic are available viz, Azeilic acid, Kojic acid, Glycolic acid, HQ, Retinoids, Topical steroids, Mequinol, Arbutin and Glutathione, but, prolonged treatment may lead to various noxious effects. So, there has always been search for safer alternatives. Herbs are a better option. Plant products have been used for medicinal purpose long before people could write. Various herbal preparations have been tried for treatment of melasma. These have been found to be safe and effective. The present review aims at the management of melasma with a well known herb of Unani system of medicine i.e., Khulanjaan (Alpinia galanga) and summarizes the current pharmacological activities, major bio actives, reported mechanisms of action and its possible anti melasma activity. It is considered a safe herbal medicine with fewer side effects.

Keywords: Alpinia galanga, Melasma, Unani system, Khulanjaan

ABSTRACT

By name, colonic drug delivery refers to targeted delivery of drugs into the lower GI tract, which occurs primarily in the large intestine (i.e. colon).Targeted drug delivery to the colon would therefore ensure direct treatment at the disease site, lower dosing and fewer systemic side effects. In addition to the local therapy, the colon also can be utilised as a portal for the drugs into the systemic circulation. Colon targeted drug delivery has gained recent importance for the treatment of colonic diseases and systemic delivery of therapeutic proteins and peptides. Treatment could be more effective if it is possible for drug to be directly delivered to colon. This article gives a detailed information related to colon, various approaches current and novel which are employed for delivery of drugs to the colon and advantages and limitation of colonic drug delivery over conventional drug delivery along with evaluation.

Keywords:  Colon, Target drug delivery.

ABSTRACT

Constant production of unstable molecules in the body beyond a limit result in severe damage of cell proteins, DNA, lipids etc. These set of species are free radicals which try to acquire stable configuration by snatching away the electrons from the surrounding molecules thereby resulting in a chain reaction. This leads to oxidative stress which is a starting point for various life threatening diseases. Coloured Petri-Net (CPN) on the other hand is a modelling tool which is suited and used for synchronization, concurrency and message passing as it is a graphical modelling language. This paper presents a modelling set up of reactions caused by free radicals using CPN tool.

Keywords: Free radicals, Lipid peroxidation, Coloured Petri Nets

ABSTRACT

Most demanding route of administration is oral. Several times dosing of conventional drug delivery system to achieve effective therapeutic range is always abhorred by the patient. Demanding new approach to reduce the number of intake; leading to introduction of gastric retention concept. As most of drugs are absorbed in upper intestinal tract GI retention was base to it. The floating drug delivery system is an admirable approach to gastric retention. Aim of delineating this review on Floating Drug Delivery System was to stash up the recent literature with special cogitation toward principal mechanism to attain gastric retention, also including details of Floating Drug Delivery System such as Classification, Mechanism of work, Method of preparation, Aspect of characterisation, Different factors to be taken care during process of formulation. This review is loaded with data of previous work performed on Floating Drug Delivery System, which includes desirable point to solve, the queries regarding FDDS.

Keywords: Floating microspheres, Floating Drug Delivery System, Gastro Retention, bioavailability, Hydrodynamically Balanced Systems.

ABSTRACT

Over the last few years an inclusive research has been done over provesicular approach for transdermal drug delivery. Skin has a very tough diffusion barrier inhibiting penetration of drug moiety which is rate limiting barrier for penetration of drugs. There are several approaches that deal with penetration enhancement across the skin. Vesicular and provesicular systems are promising amongst them. Vesicular systems including (niosomes, ethosomes, transfersomes and liposomes) are promising systems to cross this permeation barrier. The proniosomal approach helps to solve the problem regarding stability and provides higher entrapment efficiency over conventional system. Proniosomal gel is a liquid crystalline- compact niosomal hybrid which is prepared by dissolving surfactant in small amount of suitable solvent and least amount of aqueous phase. This compact gel can be converted to niosomes hydration. Proniosomes can entrap hydrophilic as well as lipophillic drugs. Proniosomal gel offers a versatile vesicle drug delivery concept with potential for drug delivery via transdermal rout.

Keywords: Proniosomes, Niosomes, skin penetration, stability, transdermal, coacervation.

ABSTRACT

Some of the natural macromolecules have been used to prepare NPs. These polymers include gelatin, alginate, chitosan and PLGA. They are hydrophilic natural polymers and have been used to synthesize biodegradable NPs by various method. Numerous techniques now exist for synthesizing different set of nanoparticles based on the type of drugs used, and the targeted organ and delivery mechanism selected. Depending upon the protocol of choice, the parameters can be tailored to create the best possible characteristics for the nanoparticles. In this manuscript we have reviewed a number of biodegradable nanoparticles currently in use, and the techniques of their preparation. We will also discuss advances in surface modifications, drug encapsulation and specific end applications of various types of NPs. Nanotechnology, although not a new concept, has gained significant momentum in recent years. Due to the recent advances in material science and nano-engineering in the last decade, the nanoparticles have become very attractive for their applications in the fields of biology and medicine. Nanostructured materials are materials with sizes in the 1-100 nm range, which demonstrate unique properties and functions due to their "size effect".Biodegradable nanoparticles (NPs) are gaining increased attention for their ability to serve as a viable carrier for site specific delivery of vaccines, genes, drugs and other biomolecules in the body.

Keyword: PLGA Nanoparticles, Method & Characterization, Visceral Leishmaniasis

ABSTRACT

Anticonvulsants are a diverse group of pharmaceuticals used in the treatment of epileptic seizures. The goal of an anticonvulsant is to suppress the rapid and excessive firing of neurons that start a seizure. The use of current antiepileptic drugs has been questioned due to the non selectivity of the drugs and the undesirable side effects posed by them. This lead to the search for antiepileptic compounds with more selective activity and lower toxicity continues to be an area of investigation in medicinal chemistry. Semicarbazones are compounds which are synthesized by the condensation of semicarbazide and aldehydes/ketones. The literature survey revealed that semicarbazones had been emerged as a compound with broad range of activities including anticonvulsant, antitubercular, anticancer and antimicrobial activity. In this review chemistry and anticonvulsant activity of semicarbazone analogues are discussed.

Keywords: anticonvulsants, semicarbazones, chemistry, review

ABSTRACT

The aim of this investigation was to develop and optimize Metformin HCl matrix tablets for sustained release application by response surface methodology based on two factor-three response factorial design. The effects of the amounts of polysaccharide from tamarind and polysaccharide from jackfruit in Metformin HCl matrix tablets on the properties of Metformin HCl sustained release matrix tablets drug release was analyzed and optimized. The observed responses were coincided well with the predicted values by the experimental design. The optimized Metformin HCl matrix tablets showed prolonged sustained release of Metformin HCl over 6 hours. These matrix tablets followed the first-order model with anomalous (non-Fickian) diffusion mechanism.

Keywords: Metformin, Matrix tablet, Sustained Release, Factorial, Design of experiment, Jackfruit, Tamarind, Polysaccharide

ABSTRACT

Fast dissolving tablets are the tablets which dissolves rapidly and shows higher bioavailability than conventional tablets. The concept of formulating Fast dissolving tablets of Loratadine (antiallergic drug) offer suitable and practical approach in serving the desired objective of faster disintegration and dissolution characteristic with increase bioavailability and to know the effects of three synthetic superdisintegrants (Crosscarmeloss sodium, Sodium starch glycolate and Crospovidone). In the present work two methods of solid dispersion were compared for improving the bioavailability i.e Solvent Evaporation and Fusion method with beta cyclodextrin as a carrier to increase the solubility of the drug. Comparison between these three synthetic superdisintegrants was done by taking different ratios individually and in combination. Combination of these three superdisintegrants shows synergistic effect when it is compared to individually. Prepared tablets were subjected to different evaluation parameters such as hardness, thickness, friability, weight variation, drug content uniformity, in vitro disintegration time, wetting time, in vitro dissolution studies and stability studies are carried out by using the best formulation. From all the formulations prepared and evaluated F11 was found to the best formulation.

Key words: Fast dissolving tablets, Solid dispersion, Crosscarmeloss sodium, Sodium starch glycolate, Crospovidone, Evaluation parameters.

ABSTRACT

The present report deals with the study of phytochemicals present in Padina tetrastromatica Hauck collected from the south east coast of Tamil Nadu, India. The phytochemicals of different extracts was analyzed by the standard procedure for UV-Vis spectroscopic and HPLC. The UV-Vis phytochemical profile of different extracts of Padina tetrastromatica Hauck was predicted. The qualitative HPLC fingerprint profile of methanol extract of Padina tetrastromatica Hauck was chosen at a wavelength of 660 nm due to sharpness of the peaks and suitable baseline. The profile showed one prominent peak at a retention time of 1.500 min and seven moderate peaks were also noted at the retention times of 2.220, 2.400, 2.500, 2.800, 3.000, 3.300 and 6.300 min respectively. The present study on Padina tetrastromatica Hauck fashioned a novel phytochemical marker in standardization of the quality of the drug used for medicine.

Keywords: Phytochemistry, Seaweeds, Padina tetrastromatica, UV-Vis, HPLC.

ABSTRACT

Fast dissolving tablets are the tablet which dissolves rapidly and shows higher bioavailability than conventional tablets. The concept of formulating Fast dissolving tablets of Famotidine (H2 –receptor antagonist) offer suitable and practical approach in serving the desired objective of faster disintegration and dissolution characteristic with increase bioavailability and to know the effects of two synthetic superdisintegrant (Croscarmellose sodium and Sodium starch glycolate). In the present work two methods of solid dispersion were compared for improving the bioavailability i.e. Solvent Evaporation and Fusion method with PVP K30 as a carrier to increase the solubility of the drug. Comparison between these two synthetic superdisintegrant was done by taking different ratios and in combination. Three different combination of these superdisintegrant shows synergistic effect when it is compared to individual. Prepared tablets were subjected to different evaluation parameters such as hardness (2.84±0.15 kg/cm² to 3.01±0.20 kg/cm²), friability (not more than 0.680±0.0173), weight variation (197.6±1.42 mg to 202.6±1.90 mg), drug content uniformity (97.84±0.35 to 100.23±0.71%), in vitro disintegration time (21.0±0.81 sec to 108.33±0.47 sec), wetting time (29.33±0.47 to 113.33±1.24 sec), in vitro dissolution studies and stability studies are carried out by using the best formulation. From all the formulations prepared and tested, F9 was found to the best formulation.

Keywords: Fast dissolving tablets, Solid dispersion, Croscarmellose sodium, Sodium starch glycolate.

ABSTRACT

In the present study, an attempt has been made to prepare floating microspheres of clarithromycin designed as gastroretentive dosage form for the treatment of Heliobacter pylori. The floating microspheres were  prepared using different polymers like HPMC- ethyl cellulose, HPMC, eudragit S-100, eudragit L-100, by solvent evaporation/diffusion methods which offer advantage of short processing time, lack of exposure of the ingredients to high temperature and gives high encapsulation efficiency. Formulations were characterized for their particle size, practical yield, entrapment efficiency, in vitro buoyancy, scanning electron microscopy (SEM) and in vitro drug release. Scanning electron microscopy shows that spherical microspheres with porous surface were formed. The optical microscopic studies revealed that the practical yield was more than 61.78% with a particle size range of 105.61-292.40 µm.  The percent entrapment efficiency is about 62.68% and more in larger particle as compared to smaller particle. The percent buoyancy was more than 74.10% up to 12 hours. The particle size, percent yield, percent drug entrapment and percent was increased significantly with increase in polymer concentration. The in vitro release was significantly decreased with in polymer concentration.  Hence it can be inferred that the floating microsphere of clarithromycin as a gastroretentive dosage form may prolong drug release thereby improving bioavailability and enhance opportunity of drug absorption in stomach to prevent degradation of drug under alkaline pH.

Keywords: Clarithromycin, HPMC, SEM, In- vitro buoyancy, bioavailability.

ABSTRACT

Herps zoster is a viral infection and a common disorder of the eyes. It is caused by herpes simplex virus: herpes virus type 1(HSV-1) & herpes virus type 2 (HSV-2). Topical acyclovir is currently the only and safe pharmacologic treatment of severe viral infection of the eyes. Nanoparticulate formulations have advantage of improving residence time over ocular surface, reduced size increasing permeation across corneal surface for intraocular activity. The objective of this study was to prepare and evaluate Acyclovir (Acy)  nanoparticles (NPs) for the treatment of Herps zoster infection of the eyes. So, the present study was designed with the primary aim to prepare nanoparticles by nanoprecipitation method using cationic polymer Eudragit E100 and secondly to study the effect of variables on the behaviour of nanoparticles. Preliminary study showed the compatibility of the drug with the formulation. Optimization was done using full factorial design with independent variables such as Drug to polymer ratio, Organic: aqueous phase ratio and effect of type and concentration of stabilizer. The dependent variables were determined such as particle size, drug entrapment, % drug release selected as the levels. F21 formulation was selected as the final optimized formulation.

Keywords:  Acyclovir, Eudragit E 100, nano precipitation, drug entrapment, ocular delivery.

ABSTRACT

Fast dissolving tablets are the tablets which dissolves rapidly and shows higher bioavailability than conventional tablets. The concept of formulating Fast dissolving tablets of Carvedilol (antihypertensive drug) offer suitable and practical approach in serving the desired objective of faster disintegration and dissolution characteristic with increase bioavailability and to know the effects of two natural superdisintegrants (Hibiscus Rosa, Linseed Mucilage). In the present work solid dispersion were prepared by solvent evaporation method for improving the bioavailability with beta cyclodextrin as a carrier to increase the solubility of the drug. And after compressing the tablet , heat is applied to create pores in tablet as it contain camphor as subliming agent which increase the porosity and cause faster release of drug from the tablet. Comparison between these two natural superdisintegrants was done by taking different ratios individually and in combination. Combination of these two superdisintegrants shows synergistic effect when it is compared to individually. Prepared tablets were subjected to different evaluation parameters such as hardness, friability, weight variation, drug content uniformity, in vitro disintegration time, wetting time, in vitro dissolution studies and stability studies are carried out by using the best formulation. From all the formulations prepared and tested, F11 was found to be the best formulation.

Keywords: Fast dissolving tablets, Solid dispersion, sublimation, Hibiscus Rosa, Linseed Mucilage.

ABSTRACT

The present study aims at investigating the different combinations of polymers with inclusion complex of Carvedilol (CR)-Hydroxypropyl betacyclodextrin (HPβCD) prepared in a ratio of 1:1 by use of various analytical techniques like Fourier Transformation Infrared spectroscopy (FTIR), X-ray diffraction technique (XRD), Digital scanning calorimetry (DSC), Thermo gravimetric analysis (TGA) as a part of preformulation studies. Various polymers used for the present study were Sodium alginate (SA), Hydroxy propyl beta cyclodextrin (HPBCD), Hydroxy propyl methyl cellulose LV E-15(HPMC), Pectin (P), Eudragit NE30D (EU). This study indicated that Carvedilol formed inclusion complex with the HPβCD, but in combination with other polymers, drug did not show any other interactions.

Keywords: Carvedilol, FTIR, TGA, Drug-polymer compatibility

ABSTRACT

Sublingual administration of the drug is known as placement of the drug under the tongue and drug reaches directly in to the blood stream. The concept of formulating sublingual tablets of Prochlorperazine maleate offers suitable and practical approach in serving the desired objective of faster disintegration and dissolution characteristic. Bitter taste of Prochlorperazine maleate was masked by inclusion complex with β-cyclodextrin and then sublingual tablets were prepared using various natural superdisintegrants such as hibiscus-rosa and fenugreek and synthetic superdisintegrants like Indion 414 and kyron T-314 in different concentrations by direct compression method. Prepared tablets were subjected to different evaluation parameters such as hardness, thickness, friability, weight variation, drug content uniformity, in-vitro disintegration time, water absorption ratio, wetting time, in vitro dissolution studies and stability studies are carried out by using best formulation. Overall, formulation F3 (10 mg of Indion 414) and F9 (10 mg of Hibiscus-rosa) based on disintegration time, wetting time and drug release were found to be an excellent formulations. Hence It was found that there was no significant difference between F3 and F9, which shows that natural superdisintegrants (10 mg of Hibiscus rosa) is as good as synthetic superdisintegrants (10 mg of Indion 414). Hence it proves that synthetic disintegrant can be replaced by natural disintegrants due to easy availability and compatibility.

Keywords: Prochlorperazine maleate, β-cyclodextrin, Indion414, Kyron T-314, Hibiscus rosa, Fenugreek

ABSTRACT

 Aloe vera are widely used in the cosmetics and alternative medicine industries, being marketed as variously having rejuvenating, healing, or soothing properties. There is, however, little scientific evidence of the effectiveness or safety of Aloe vera extracts for either cosmetic or medicinal purposes, and what positive evidence is available is frequently contradicted by other studies. Aloe vera has been used as a popular folk medicine. It is a colourless mucilaginous gel obtained from the parenchymatous cells in the fresh leaves of Aloe vera. It has been claimed that Aloe vera gel has the ability to cure gastric ulcers or protect against its formation in both animals and humans. This study evaluates the effect of Aloe vera gel on gastric and duodenal ulcers and determines its interaction with conventionally used antiulcer drugs; pantoprazole. The antiulcer activity of Aloe vera gel at three different doses and its interaction with Pantoprazole was evaluated in, pylorus ligation induced gastric ulcer, stress induced gastric ulcer and  indomethacin induced gastric ulcer  models. In all these models, the common parameter determined was ulcer index. All the three doses of Aloe vera gel produced marginal ulcer healing effect and augmented the ulcer healing effect of pantoprazole in stress and Indomethacin induced gastric ulcers, while in pylorus ligated rats, Aloe vera gel demonstrated gastric anti-secretory and antiulcer effect. Aloe vera gel possesses dose dependent antiulcer effect and augments the antiulcer action pantoprazole in rats.

Keywords: Aloevera gel, gastric cytoprotection, gastric ulcer, pantoprazole.

ABSTRACT

The use of chitosan (CS) is use for the encapsulation of active components has gained interest in the last years due to its mucous adhesiveness, non-toxicity, biocompatibility and biodegradability. The benefits of encapsulating active agents in such polymer matrix include their protection from the surrounding medium or processing conditions and their controlled release. In this present study Chitosan was employed for the encapsulation of caffeoyl derivatives and medicinal plants (Artemisia pallens (Tulsi), Ocimum tenuiflorum or  Ocimum  sanctum (Marikolunthu ).Encapsulation has been done with the help of ionic gelation method.  Chitosan and TPP- (Tripolyphosphate pentasodium) were mainly involved. The active components were added to the TPP solution and this was added dropwise to the chitosan solution with continuous stirring and also in this case, to investigate the anti-oxidant activity of the methonolic extract of caffeoyl derivative and medicinal plants.Anti-oxidant activity of methonolic extract was determined by DPPH -(1, 1-diphenyl 1-2 picryl hydrazyl)  free radical scavenging activity. Then the effect of encapsulating systems on the active ompound stability and its release properties was analysed.

Keywords: Artemisia pallens (Thulsi), Ocimum tenuiflorum or  Ocimum  sanctum (Marikolunthu), Chitosan, Anti-oxidant, TPP- (Tripolyphosphate pentasodium) , DPPH-(1, 1-diphenyl 1-2 picryl hydrazyl).

ABSTRACT

Lawsonia inermis (Lythraceae) commonly called as Henna or Mailanchi is known for its cosmetic properties. Henna is an important source of phytochemicals of immense medicinal and pharmaceutical significance such as alkaloids, naphthoquinone derivatives, aliphatic components, tannins, phenolic derivatives, coumarins, xanthones, flavanoids, therefore an effort to compile all the information reported on its phytochemical and pharmacological activities, so that interest could be diverted towards this dye herb, for the treatment and relief from various ailments and diseases. The resultant extracts were analyzed by thin layer chromatography (TLC), column chromatography, ultraviolet spectroscopy (UV), Infrared (IR) spectroscopy, and High performance liquid chromatography (HPLC) techniques UV analysis was done by diluting the extracts with their respective solvents. 2 to 3 peaks were observed for extracted samples at 212 nm, 238.60 nm and 283.30 nm in methanol extract, 241 nm in chloroform extract, 238 nm in chloroform: methanol extract and 272.20 nm in ethyl acetate extract respectively. In HPLC  compounds  methanol extract is carried out for HPLC separation, and mainly three peaks were observed at 2.057, 2.522, 4.133 min retention times, which is the confirmation of presence of three separated compounds.

Keywords: Lawsonia inermis, HPLC,UV, IR.

ABSTRACT

Hyponatremia is an electrolyte disturbance in which the sodium ion concentration in the serum is lower than normal. Sodium is the dominant extracellular cation (positive ion) and cannot freely cross from the interstitial space through the cell membrane, into the cell. Its homeostasis (stability of concentration) inside the cell is vital to the normal function of any cell. Normal serum sodium levels are between 135 and 145 mEq/L. Hyponatremia is defined as a serum level of less than 135 mEq/L and is considered severe when the serum level is below 125 mEq/L. In the vast majority of cases, Hyponatremia occurs as a result of excess body water diluting the serum sodium (salt level in the blood).Hyponatremia is often a complication of other medical illnesses in which excess water accumulates in the body at a higher rate than can be excreted (for example in congestive heart failure, syndrome of inappropriate antidiuretic hormone, SIADH, or polydipsia). Sometimes it may be a result of over hydration (drinking too much water).Lack of sodium (salt) is very rarely the cause of Hyponatremia, although it can promote Hyponatremia indirectly. In particular, sodium loss can lead to a state of  volume depletion (loss of blood volume in the body), with volume depletion serving as a signal for the release of ADH (anti-diuretic hormone). As a result of ADH-stimulated water retention (too much water in the body), blood sodium becomes diluted and Hyponatremia results.

Keywords: Tolvaptan, Hyponatremia, Syndrome of insufficient anti diuretic hormone (SIADH), euvolemic Hyponatremia.

ABSTRACT

A simple, specific, sensitive, precise and stability-indicating reversed phase high performance liquid chromatographic method was developed and validated for the simultaneous determination of thiocolchicoside and aceclofenac, using a RP-18 column and a mobile phase composed of 0.1% trifluoroacetic acid: acetonitrile (45:55). The retention time of thiocolchicoside and aceclofenac were found to be 2.35 and 13.2 min, respectively. Linearity was established for both thiocolchicoside and aceclofenac in the range of 0.08-0.8 and 1-10 µg/ml. Both the drugs were subjected to acid, alkali and neutral hydrolysis, oxidation, dry heat, and photolytic degradation. The degradation studies indicated that both thiocolchicoside and aceclofenac were susceptible to acid, alkaline and neutral hydrolysis. The degradation products of thiocolchicoside and aceclofenac 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 aceclofenac in bulk drugs and formulations.

Keywords: Thiocolchicoside, aceclofenac, degradation products, HPLC

ABSTRACT

The idea of formulation of controlled release drug delivery has become beneficial in the treatment of diseases. At this time, the increased understanding in the community and the significance of safe use of drugs encouraged to develop novel drug delivery system. In the present study, an attempt was made to expand the release of Cefpodoxime proxetil from matrix tablets by sintering technique. This has been an evolving one in the study of effect of heating on mechanical properties of pharmaceutical powders that is used in the formulation of sustained release matrix tablet. The tablets were formulated by direct compression method. The punched tablets were subjected to sintering process and exposed to three different durations of sintering (1.5, 3.0 and 4.5 hours). This type of system provides a important and suitable method for achieving controlled release in oral dosage forms. The release of the drug form un-sintered matrix tablets containing 100 mg polymer was 100% within 90 minutes. For a particular sintering time, the release rate decreased with increasing polymer concentration. For 1.5, 3.0, and 4.5 hours sintering durations the least retardation is offered by least polymer concentration. The highest retardation was offered by matrices with highest polymer concentration.

Keywords: Cefpodoxime proxetil, Sintering technique, Matrix tablets, Direct compression

ABSTRACT

Simple area under curve spectrophotometric method for determination of Cefixime and Linezolid in bulk and tablet formulation was developed and validated as per ICH guidelines. The lmax of Cefixime and Linezolid were found to be 289nm and 257nm respectively. The linearity range was found 2-12μg/ mL for Cefixime and 5-30μg/mL for Linezolid. In the tablets dosage form Cefixime and Linezolid were estimated as 99.92% and 99.94% respectively. The lower limit of detection (LOD) for Cefixime and Linezolid was found to be 0.039μg/ml and 1.11μg/ml respectively.and the limit of quantization (LOQ) was determined as the lowest concentration for Cefixime and Linezolid was found to be 0.118μg/mL and 3.37μg/ml respectively. The validated spectrophotometric method employed proved to be simple, economical, precise and accurate.

Keywords: Cefixime, Linezolid, UV Spectroscopy, AUC Method.

ABSTRACT

The leaves of Ocimum gratissimum (OG) and Vernonia amygdalina (VA) had been of medicinal interest mainly due to their respective antioxidant and antihyperglycaemic properties. A daily dose of 0.5gKg^-1 body weight aqueous leaf extracts of OG, VA and 50:50 (OG+VA) was orally administered to three different rabbit groups for 28 days, fed ad libitum. The control group was given only 2mlKg^-1 of normal saline daily. Fasting blood glucose concentration was monitored with a digital glucometer. From the SPSS (version 15) multivariate analysis (p=.05), results showed that the mean fasting blood glucose concentrations of normal rabbits used was 5.98±0.5 mMolL^-1. Only VA lowered fasting blood glucose within 24 hours and maintained the hypoglycaemia for 72 hours; VA potentiated OG after 72 hours and later synergistically lowered fasting blood glucose concentration. This study suggested that VA and (OG+VA) were time-dependent hypoglycaemic: while consumption of VA had acute effect, (OG+VA) could preferably be used for longer prophylaxis of diabetes. Therefore, further researches are recommended on the efficacy of this herbal combination therapy.

Keywords: Ocimum gratissimum, Vernonia amygdalina, Interactive effects, blood glucose, Rabbits

ABSTRACT

A new, simple, specific, sensitive, rapid, accurate and precise RP-HPLC method was developed for the estimation of Simvastatin in bulk and pharmaceutical formulations. Simvastatin was chromatographed on a hypersil C18 column (250x4.6mm I.D., particle size 5 μm) in a mobile phase consisting of sodium dihydrogen phosphate and Acetonitrile in the ratio 40:60 v/v. The mobile phase was pumped at a flow rate of 1.0 ml/min with detection at 239 nm. The detector response was linear in the concentration of 10-200 μg/ml. The intra and inter day variation was found to be less than 2%. The mean recovery of the drug from the solution was 99.39%. The proposed method is simple, fast, accurate, precise and reproducible hence, it can be applied for routine quality control analysis of Simvastatin in bulk and pharmaceutical formulations.

Keywords: RP-HPLC, Simvastatin, precision, accuracy and formulation.

ABSTRACT

The purpose of this study was to develop a gastroretentive controlled release drug delivery system with mucoadhesive properties of Propafenone HCl. Propafenone HCl has a short elimination half-life, a narrow absorption window and is mainly absorbed in proximal areas of gastro intestinal tract. Tablets were prepared by using controlled release polymers HPMC E5 and HPMC K100M. Mucoadhesive matrix tablet contains sodium carboxy methyl cellulose as a mucoadhesive polymer. The formulations were evaluated for pharmacopoeial quality control tests and all the physical parameters evaluated were within the acceptable limits. All formulations were evaluated for mucoadhesive strength, which showed good detachment force up to 12 h. Mucoadhesion studies via rotating paddle method and In-vitro drug release studies were conducted in 0.1 N HCl (pH 1.2) at 37 ± 0.5 ºC. Formulation M11 was proved to be good mucoadhesion, dimensional stability and drug release up to 12 h as compared to the other formulations.  Stability studies were carried out on the optimized formulation for period of 3 months at 40⁰c/75 %RH. Finally it was observed that there was no change in physiochemical and physical properties as well as in drug release profile even after storage at 45 °C and 75 % for three months.

Keywords: Propafenone HCl, dimensional stability, gastroretentive drug delivery system, mucoadhesive strength.

ABSTRACT

A novel reverse phase Ultra performance liquid chromatographic technique was developed for the determination of balofloxacin in bulk and pharmaceutical dosage forms. The method was developed using waters Acquity BEH 50mm, 2.1mm, 2μm, C 18 column with mobile phase containing a gradient mixture of 0.1% phosphoric acid and acetonitrile. Detection was carried out at wavelength 295 nm. The retention time of balofloxacin was 0.89 min. The method showed good linearity in the range 0.5, 1, 1.5,2,3 µg/ml with correlation coefficient for balofloxacin. The proposed method has been validated as per ICH guidelines and successfully applied to the estimation of balofloxacin in their tablet dosage form.

Keywords:  Balofloxacin, Ultra performance liquid chromatography, validation

ABSTRACT

Herbal medicine has become an integral part of standard healthcare based on combination of traditional usage and on-going scientific research. Gel is a semisolid system consisting of dispersion made up of either small inorganic particles or large organic molecules enclosing an interpenetrated liquid. The inorganic particles form a three dimensional structure. The gel formulation was designed by using ethanolic extract of Cassia tora seeds and evaluated for various physiological measurements; preparation involved various concentration combinations of Carbopol 934 and Sodium CMC. Containing 1.55%of Cassia tora extract, Glycerin, Methyl paraben, Propyl paraben and required amount of distilled water and neutralized by drop wise addition of tri-ethanolamine to get gel like consistency. The results of physiochemical parameters of formulations were pH (6.8 to 6.89), viscosity, spreadability, extrudability, in-vitro release respectively. Concentration and combination effect of Carbopol 934 and Sodium CMC showed increased consistency and sustained action with increase in concentration.

Keywords: Herbal gel, Cassia tora, Carbopol 934, Sodium CMC

ABSTRACT

The purpose of this research was to develop fast dissolving tablets of labetalol hydrochlorideis a phenyl ethanol amine derivative that is a competitive inhibitor at both β₁ and β₂ adrenergic receptors and at the α₁-adrenergic receptor. Labetalol is an antihypertensive drug and the dose is 50-200mg twice/day with food. From the present study, the drug content was uniform in all the labetalol FDT formulations prepared. The drug and super disintegrating agent ratio was found to influence the release of drug from the formulations. As the level of super disintegrating agent and disintegrant changed, the drug release rates were found to be increased in all formulations. The prepared tablets disintegrate within few seconds without need of water; thereby enhance the absorption leading to its increased bioavailability.

Key words:  Labetalol, antihypertensive, super disintegrating agent, fast dissolving tablets.

ABSTRACT

The aim of the work is to produce microcrystalline cellulose (MCC) from sugarcane bagasse (Saccarhum officinarum) and to characterise the MCC and compare with Avicel^®. MCC was produced from α-cellulose produced by alkaline hydrolysis from sugarcane bagasse and bleached with sodium hypochlorite. The MCC were identified by BP (2009) method and characterised in terms of pH, moisture and ash content respectively. The physico-technical properties of MCC were studied including the particle size and flowability and compared with that of Avicel^®. Also, the phytochemical properties of MCC were studied. The results of the phytochemical analysis of MCC from bagasse showed the presence of alkaloid in low concentration while, carbohydrates and glycosides were seen in very large concentrations, while flavonoids, saponin, tannin, resins, steroids, terpenoids, reducing sugars, proteins, fats and oil and acidic compounds were absent. MCC produced had a pH of 7 and moisture content of 7 % and exhibited mean particle diameter of 200.00 ± 0.05 µm. The results of the true density of the MCC showed that the differences in density between the MCC from bagasse and Avicel^® were not significant (p < 0.05). The results of angle of repose, Carr’s index and Hausner’s quotient showed that the MCC from bagasse and Avicel^® exhibited poor flow which could be improved by use of glidants. Therefore, MCC from bagasse could be used as diluents-binder in direct compression tableting and as diluents and or disintegrant in wet granulation tableting.

Keywords: Microcrystalline cellulose, sugarcane bagasse, Saccharum officinarum, phytochemical analysis

ABSTRACT

The aim of the study was to formulate colon targeted diclofenac sodium alginate beads. The beads were formulated by ionotropic gelation using sodium alginate as polymer, calcium carbonate as an internal cross linking agent and calcium chloride as an external cross linking agent. The optimized beads contained Neusilin and coated with Eudragit L100. The beads were analyzed in terms of, encapsulation efficiency (EE%), particle size and morphology. Swelling properties were studied in simulated gastric fluid (SGF, pH 1.2) and simulated intestinal fluid (SIF, pH 7.4). In vitro drug release was studied in SGF, pH 1.2, SIF, pH 6.8 and SIF, pH 7.4. The results show that the particle size of the beads ranged from 1.98 ± 0.40 to 2.80 ± 0.30 mm. The optimized batch containing Neusilin^® had the highest EE% of 72 % significantly higher than other batches (p < 0.05). The degree of swelling of the beads was zero in SGF and about 90 % in SIF at 100 min. The results of the in vitro release showed that the beads had 0 % release in SGF, pH, 1.2 at 2 h, about 3 % in SIF, pH 6.8 at 4 h and 9 % drug release in SIF, pH 7.4 at 9 h. Therefore, sodium alginate beads could be used for colon delivery of diclofenac sodium. 

Keywords: Colon targeting, Alginate beads, Diclofenac sodium, NSAIDs

ABSTRACT

The aim of the present study was to optimize carbon tetrachloride (CCl_4­) induced hepatotoxicity in the rat with respect to dose and time course. Female Sprague Dawley rats, weighing 150-200g were used in the present study. Hepatotoxicity was evaluated by measuring the activity of serum enzymes, alanine transaminase [ALT], aspartate transaminase [AST], alkaline phosphatase [ALP] and total bilirubin [TBIL] level. Experimental hepatotoxicity was induced by administering 1, 1.5, 2 ml/kg CCl₄ (dissolved in an equal volume of olive oil) intraperitonially (i.p) and observed for enzyme levels at time intervals of 0, 2, 24, 48 hours after CCl_4­ challenge. Result values are analyzed by One way ANOVA followed by Dunnett’s test. 1 ml/kg CCl₄ increased the levels of serum enzymes that reached a peak after 24 hr and showed moderate hepatitis which is ideal for development of acute hepatotoxicity. It is possible to select optimum dose of CCl₄ to induce hepatotoxicity by single i.p injection in order to study hepatoprotective activity of herb without causing death of animals.

Keywords- Carbon tetrachloride, Dose, Hepatotoxicity, Time course

ABSTRACT

Tuberculosis, due to its relentless nature, is now a major public health threat. The concomitant resurgence of TB with the MDR- or XDR-TB and HIV/AIDS pandemic has exposed the frailties of the current drug armatorium. Based on good structural similarity between BM-212, a novel antimycobacterial agent undergoing clinical trials, and 1,4,5 trisubstituted Pyrrole-3-Carbonitrile, we have designed novel 2-Amino-4,5-Diphenyl-1-(Substituted)-1H-Pyrrole-3-Carbonitrile All the compounds were screened for their antimycobacterial activity on mycobacterium tuberculosis using H37Rv strain by 1% proportion method. Some of the synthesized compounds exhibited potent antimycobacterial activity with MIC values in the range of 12.5-100 µg/mL.

Key words: Anti-tubercular, Pyrrole-3-Carbonitrile  

ABSTRACT

Drug delivery through oral route is widely accepted through all over world. Mouth dissolving tablet is most suitable tablet than conventional tablet. The main characteristic which is in the favors of mouth dissolving tablet is that there is no need of water to take it. Due to this it become more suitable dosage form for pediatric and geriatric patients. Since bioavailability of mouth dissolving tablet is high than conventional tablet, and mixing of piperine with it make them much more advance dosage form. Due to the addition of piperine in the drug, the dose size is reduced, and enhanced the onset of action. Addition of piperine with norfloxacin also increase the antibacterial activity and make them more effective.

Keywords: Mouth dissolving tablet, superdisintigrant, norfloxacin, piperine, E.coli.

ABSTRACT

In indigenous/traditional systems of medicine, the drugs are primarily dispensed as water decoction or ethanolic extract. Fresh plant parts, juice or crude powder are a rarity rather than a rule.  Total Phenolic content in the extracts measured as gallic equivalent in Ashwagandha (methanolic)  43.77 ± 1.7, aqueous = 42.52 ± 0.8, activity of Trolox by ABTS method IC₅₀ value 428.38 ± 1.90 µg /ml, Total Antioxidant activity by ABTS method in Ashwagandha (methanolic) IC₅₀ Value is 28.353 ± 0.269 mg/ml in  aqueous 32.547 ± 0.532 mg/ml , Free radical scavenging capacity by DPPH in Ashwagandha (methanolic) IC₅₀ Value 2.9  ± 0.09 mg/ml  in aqueous 3.27 ± 0.05 mg/ml. The medicinal plant examined in this study has long been used in Indian traditional medicine, Ayurveda as well as many other traditional drug practices of the rest of the world. Withania somnifera, known as ‘Ashwagandha’, has been an important herb in the Ayurvedic and indigenous medical systems for centuries in India.

Keywords:  Ashwagandha, Antioxidant, Ayurveda, traditional medicine, decoction, extract.

ABSTRACT

Cetrizine hydrochloride and Phenylephrine hydrochloride are used in combination in the treatment of allergy. The aim of this project work is to develop selective, accurate, specific and economic RP–HPLC method for simultaneous estimation of Cetrizine hydrochloride and Phenylephrine hydrochloride in Bulk and Tablet dosage form. The reverse phase C18 (250 mm × 4.6 mm i.d) column with 5 µm particle size was used. Acetonitrile: Water was taken as mobile phase was with a flow rate of 1 mL/min and detection was carried out at 222 nm. The retention time of Cetrizine hydrochloride and Phenylephrine hydrochloride was 1.956 min and 4.561 min respectively. The calibration curves were linear (>0.998) in the range of 5-25 μg/ml for Cetrizine hydrochloride and Phenylephrine hydrochloride. The Limit of Detection for Cetrizine hydrochloride and Phenylephrine hydrochloride was found to be 0.26 μg/mL and 0.51μg/mL. The Limit of Quantification was found to be 0.81μg/mL and 1.54 μg/mL respectively for Cetrizine hydrochloride and Phenylephrine hydrochloride. The developed method was simple, selective and precise and can be used for routine analysis of Cetrizine hydrochloride and Phenylephrine hydrochloride in tablet dosage form.

Keywords: Cetrizine hydrochloride (CET), Phenylephrine hydrochloride (PHE), RP-HPLC, Validation, Tablet.

ABSTRACT

Liquid chromatography-mass spectrometry (LC-MS) is sensitive technique that is affected by matrix effect. It arises due to phospholipids, proteins or metabolites present in biological fluids. It either increases or decreases the ionization of sample and affects detection limits. By careful evaluation of matrix effect on the drugs and their ionization in LC-MS the sensitivity could be improved. Evaluation of matrix effect for bio estimation of prasugrel hydrochloride is done by sample preparation methods, chromatographic conditions, internal standard and mass spectrometric conditions. A LC-MS method was developed for prasugrel hydrochloride with mobile phase consisted of ammonium formate (5mM, pH 7.5): acetonitrile (30:70, %v/v) at 1 mL/min flow rate and PDA detection at 220 nm. The mass detection method was after ionization with ESI probe, CDL temperature 230°C, detector voltage-1.5 Kv, nebulisation gas flow-1.5 L/min and column temperature was 30.5°C. The molecular ion peak was identified at m/z of 410 and product ion peak at m/z 374. The plasma spiked with prasugrel was subjected to each evaluation process and matrix effect was studied.  In sample preparation technique, the extraction efficiency and process efficiency were also calculated. The study results have shown that the matrix effect could be reduced systematically by the procedures performed and the sensitivity of LC-MS in the detection and quantification was increased to detect 20 ng/mL of Prasugrel from plasma.

Keywords: Matrix effect, Prasugrel, LC/MS, biological fluid

ABSTRACT

The present study deals with the formulation and evaluation of egg albumin based delayed release microspheres of itraconazole, which is drug of choice for systemic fungal infections. The study was undertaken in order to achieve the best possible drug-polymer (egg albumin) ratio to get delayed drug release using natural biodegradable polymer. The preparation of microsphere was done by using heat denaturation technique. The prepared microspheres were evaluated on various parameters like the size, morphology, micromeritic properties, percent drug entrapment, in-vitro dissolution studies and the scanning electron microscopy (SEM).The in vitro dissolution studies were carried out for 10 hrs. at pH 6.8 which showed that the drug release for the batch EA4 (drug: polymer ratio – 1:4) was 87.02 ± 5.89 after 10 hrs. The hypothesis of this research work i.e delayed drug release using natural biodegradable polymer was well supported by results of its evaluation.

Keywords: Itraconazole, egg albumin, delayed drug delivery systems, heat denaturation method.

ABSTRACT

Silymarin, a hepatoprotective agent has poor aqueous solubility and high permeability [class II drug]. Its absorption is dissolution rate limited. In order to improve the dissolution profile of silymarin solubility enhancement techniques were employed. Among the various techniques, solid dispersions were employed due to its feasibility. Polymers used were HPMC and PEG. Silymarin was formulated by kneading method and solvent evaporation method, where HPMC and PEG were used in different ratios of drug: polymer. Polymer characterization for the prepared solid dispersion was done using FT-IR, XRPD, SEM and DSC. In vitro dissolution studies were carried out in 0.1M HCl and phosphate buffer mixed (pH 6.8). From the in vitro studies, dissolution efficiency and drug release kinetics was also calculated. FT-IR studies revealed that there was no interaction between the drug and the polymers used. DSC, XRPD and SEM supported the existence of silymarin in amorphous state, in the prepared solid dispersions. Drug content analysis showed maximum drug release of 101.03 for solid dispersion prepared using drug: HPMC in the ratio of 1:3 [KM₂] using polysorbate 80, employing kneading method. In vitro release of KM₂ was found to be 98.87 ± 0.32 in 0.1 M HCl buffer.  Kneading method proved to be superior to solvent evaporation method. Compared to the pure drug silymarin, solid dispersions [KM₂] gave a 2.2 fold increase in the dissolution profile.

Keywords: Solubility enhancement, Solid dispersions, Kneading method.

ABSTRACT

The objective of work was to formulate, evaluate the potential of ethosomes for delivering etodolace, a potent, water insoluble non‐steroidal anti‐inflammatory drug via skin to enhance skin permeation after topical application. The effects of pH and ethanol contents on etodolac solubility were evaluated to find out the suitable dispersion medium for the ethosome preparations. Drug loaded ethosomes had been prepared using phospholipid and ethanol, were optimized and characterized  for entrapment efficiency, zeta potential, particle size and size distribution. The ethosome were prepared by using the thin film hydration method. The optimized formulation composed of 0. 4% w/v Soya lecithin and 0.1 % pluronic F127 as lipid component and 30% v/v ethanol in phosphate buffer pH 7.4 as dispersion medium. The vesicular size and zeta potential of ethosome was found to be 458.7nm,-36.6 mV respectively The entrapment efficiency was found to be 68.4±0.4%. In final phase of formulation optimized ethosome containing drug, was converted  to gel using three different carbopol 930 concentrations(0.5, 0.7 and 1% w/w).The gel of 0.7% carbopol was found to be the optimized gel  which  shown  excellent in­vitro  drug  release 

Keywords: Ethosome; Ethanol; Transdermal; Phospholipid; In vitro skin permeation, drug loading; flux.

ABSTRACT

Ophthalmic drug delivery is one of the most interesting and challenging endeavors facing the pharmaceutical scientist. The anatomy, physiology and biochemistry of the eye render this organ highly impervious to foreign substances. The poor bioavailability and therapeutic response exhibited by conventional ophthalmic solutions due to rapid pre-corneal elimination of the drug may be overcome by the use of in situ gel forming systems that are instilled as drops into the eye and then undergo a sol-gel transition in the cul-de-sac. The purpose of the present work was to develop an ophthalmic drug delivery system of Pefloxacin mesylate for in situ gelling system byusing ion sensitive gelling agent (Gelrite) and viscofying agent (HPMCK4M). Optimization by 2² factorial design using Design expert software 8.0 version was applied to the formulations. Formulation with Gelrite (gellan gum) and HPMC K4M shows percent drug content of 99.83%, viscosity of 1864 cp at 20 rpm and in-vitro drug release of 88.32% which shows formulation is good. The developed formulation was found to be stable and provided sustained release of the drug over 8 hours.

Keywords: Pefloxacin mesylate, In situ gelling system, Ophthalmic drug delivery, Gelrite (gellan gum), HPMC K4M, Factorial design.

ABSTRACT

In India. Fixed Dose Combinations(FDCs) have drawn the attention of health service providers and the service recipients. Therefore, the development of fixed dose combinations (FDCs) is becoming increasingly important from a public health  perspective. The objective was to study the prescribing pattern and to assess the rationality of fixed dose combinations using seven point criteria. During the study period a total of 100 patients were enrolled based on inclusion and exclusion criteria. The study population includes an overall 56% male with an average age of 46.15 ± 19.33 years. A total of 538 drugs were prescribed to the patient with a mean of 5.38±5.77.The major therapeutic category of drugs prescribed were antibiotics (30.03%), antihypertensives (12.63%) and others (13.01%).The study population had 130 FDCs in which again antibiotics topped the list, followed by Anti-diabetics. Among these 92 contributed to antibiotic FDCs belonging to 15 different groups. The average interaction per prescription was 1.96±3.72.The FDCs involved in drug interaction were aspirin+clopidogrel, amoxicillin+ clavulanic acid. The average length of stay for study population was found to be 5.73±2.19 days. The rationality was assessed using 7 point criteria with a maximum scoring of 14. The most commonly prescribed combination were Piperacillin + Tazobactam (25.38%) and Amoxicillin+ Clavulanic acid(16.92%).Among the combinations, 26.6% scored 13 while 66.66% scored 9-12 and 6.66%scored 7. The results indicated that majority of FDCs especially antibiotics were rational.

Keywords: Fixed Dose Combinations (FDCs), Rational Drug Use (RDU), Essential Drug List (EDL), National List Of Essential Medicines (NLEM), World Health Organization (WHO)

ABSTRACT

A series of [Alkyl or un/substituted phenyl]-2-(3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazin-2-yl)acetamide were designed and synthesized. In vitro antifungal activity assay indicates that the 1,4-Benzothiazine has good antifungal activity against most of the tested pathogenic fungi i. e. Candida albicans, Trichophyton rubrum, Epidermophyton floccosum and Malassazia furfur. Some few compounds such as BTA-43 and BTA-56 have significant antifungal activity and broader spectrum, which are promising leads for the development of novel antifungal agents. The structures of the synthesized compounds were established on the basis of IR, NMR, ¹³CNMR and Mass spectra data.

Keyword: Antifungal activity, 1,4-Benzothiazine, Dermatophytes.

ABSTRACT

Helminthes are the most common infections in man, affecting a large proportion of the world’s population. Study includes alcoholic extracts of Anacardium occidentale, Mangifera indica and combination of Anacardium occidentale and Mangifera indica leaves extracts (1:1) were evaluated for their anthelmintic activity using Pheretima posthuma model. Three concentrations (10, 20 and 50 mg/ml) of each extracts were used for this study which involved the determination of time of paralysis and time of death of the worms. Extracts obtained from both leaves not only paralyzed but also killed the earthworms. Among the two drug extracts, Mangifera indica showed maximum vermifuge and vermicidal activity at the concentration of 50 mg/ml. Combination of alcoholic extracts of Anacardium occidentale and Mangifera indica also showed a significant anthelmintic activity. Observations were comparable with the standard drug at concentration of 20 mg/ml. On the basis of the observations, it was concluded that both Anacardium occidentale and Mangifera indica leaves extracts have a potential anthelmintic property.

Keywords: Anthelmintic activity, Anacardium occidentale, Mangifera indica, Pheretima posthuma.

ABSTRACT

Two main semi-tetracycline systems were synthesized. The strategy of such synthesis depends on the transformation of aroyl-1,4-benzoquinone to aroylketal-1,4-benzoquinone causes a regiocontrol addition of cyclopentadiene and 2,3-butadiene to the unsubstituted side of the quinone. These ketal adducts were hydrolyzed using the acidic media; as a result deketalization and enolization in one step give the semi-tetracycline system. The structures of these compounds were confirmed by NMR, IR, MS and elemental analysis.

Keywords: - Diels-Alder, semi-tetracycline, Benzoquinone,Butadiene, Cyclopentadiene.