JOURNAL OF DRUG DELIVERY AND THERAPEUTICS

8-13

Authors: Chhama Shukla, Sanchit Srivastava

As we know that, Oxadiazole is a heterocyclic compound containing an oxygen atom and two nitrogen atoms in a five-membered ring and is derived from furan by substitution of two methylene groups (=CH) with two pyridine type nitrogen (-N=) [1,2]. There are three known isomers that is 1,2,4-oxadiazole, 1,2,3-oxadiazole and 1,2,5-oxadiazole (Figure 1.0). However, 1,3,4-oxadiazole and 1,2,4-oxadiazole are better known, and more widely studied by researchers because of their many important chemical and biological properties. Among heterocyclic compounds, 1,3,4-oxadiazole has become an important construction motif for the development of new drugs. Compounds containing 1,3,4-oxadiazole cores have a broad biological activity spectrum including antibacterial, antifungal, analgesic, anti-inflammatory, antiviral, anticancer, antihypertensive, anticonvulsant, and anti-diabetic properties. They have also attracted interest in medicinal chemistry as surrogates (bioisosteres) for carboxylic acids, esters and carboxamides. The ability of 1,3,4-oxadiazole heterocyclic compounds to undergo various chemical reactions has made them important for molecule planning because of their privileged structure, which has enormous biological potential. Some examples of compounds containing the 1,3,4-oxadiazole unit currently used in clinical medicine are: Raltegravir as an antiretroviral drug and Zibotentan as an anticancer agent. They possesses various other biological activities and having various synthetic approaches, some of them are presented here in the aritcle. Keywords: Oxadiazoles synthetic approaches, biologically active ozadiazoles, oxadiazoles as anticancers etc.

18-22

Authors: A Dhulappa, K Lingappa, K G Siddalingeshwara

The main aim of the study is to enhance the biosynthesis of xylanse by incorporating nitrogen sources (both organic and inorganic). Recently, xylanases have expanded their use in many processing industries, such as pulp and paper, food and textile to newer needs such as biofuel production. .This study were taken up to the enhance the biosynthesis of xylanase by supplementation of organic nitrogen and inorganic nitrogen sources were employed in range of 0.25% to 1.25%. The organic nitrogen source were supplemented are peptone, yeast extract and beef extract and inorganic nitrogen sources are ammonium sulphate, ammonium chloride and ammonium nitrate. The yeast extract and ammonium nitrate were yielded higher xylnase production and showed 5.56 IU and 5.79 IU Key words: Xylanase, submerged fermentation, yeast extract, ammonium nitrate and assay.

31-34

Authors: Hasmukh R Jadav, Galib R, PK Prajapati

Objective: Apamarga Kshara Yoga (APK), a classical Ayurvedic formulation containing Apamarga Kshara (alkaline substance of Achyranthes aspera Linn.), Manahshila (Arsenic Disulphide) and Gomutra (cow’s urine) is effective in cases of Shvitra (vitiligo). As the formulations has short shelf life, inconvenient to patients and involve longer duration of pharmaceutical preparation; it is planned to convert into more convenient form. Design: Raw materials were authenticated and APK was prepared. Further, organoleptic and physico-chemical properties were evaluated. Results: An average 909.8 gm (90.98 %) yield after Taila Paka and 1379.6 gm ointment was observed in the process. Conclusions: As observed in present study, addition of wax to attain ointment consistency is mandate. Residue as Apamarga Kshara and Manahshila incorporated in preparation of ointment yielded more without losing its consistency.

43-55

Authors: Anshuman Keshari, Dr. PUSHPENDRA Kumar Tripathi, Arjita Srivastava, Ratan Vishwas

The aim present investigation is Formulation and Evaluation of Effervescent Floating Tablets of antidiabetic drug. Gastric retention are such systems, which increase the gastric retention time of the dosage forms at the stomach and upper part of the small intestine and suitable for the drug having site-specific absorption from the above sites. The Metformin HCl an orally administered biguanide of BCS class-3 High solubility and low permeability, which is widely use in the management of and the type-II diabetes, is an oral anti- hyperglycemic agent, shows incomplete absorption from the gastrointestinal tract and from the gastrointestinal track and absolute bioavailability is 50-60%with relatively short plasma half-life of 1.5-4.5 hours. It was using different polymers studying of deferent factors affecting the floating behavior of the prepare tablets was of our goals and important target in this part. Gastro-retentive tablets of Metformin HCl were prepared by wet granulation method using HPMC K200M (Hydroxylpropyl methyl cellulose) micro crystalline cellulose PH 101, sodium bicarbonate, HPMC K100 (LV), Magnesium stearate, colloidal silicon dioxide. In this formulation HPMC K 200 M was using different concentration. The Gastro-retentive tablet of Metformin HCl was evaluation of compression blend Angle of repose, Bulk density, tapped density, Drug compressibility study, Drug release rate, floating lag time etc. Result of our present study suggests that gastro-retentive tablets of Metformin HCl can be successfully designed to develop sustained release drug delivery which can reduce dosing frequency. Keywords: Effervescent system, gas generating system, gastro retentive drug delivery system, sustained drug release, Metformin hydrochloride

60-62

Authors: Saroj Yadav, K G Siddalingeshwara

Fibrin is a protein that forms in the blood clots after trauma or injury. This is essential to stop blood loss. There are more than twenty enzymes in the body that assist in clotting of the blood, while only one that can break the clot down. It is an endogenously produced fibrinolytic enzyme called plasmin. Streptokinase is an extracellular metallo-enzyme produced by beta-haemolytic streptococcus and is used as an effective and cheap clot-dissolving medication in some cases of myocardial infarction (heart attack) and pulmonary embolism. It belongs to a group of medications known as fibrinolytics. Fibrinolytic enzymes can be found in a variety of foods, such as Japanese Natto, Tofuyo, Korean Chungkook-Jang soy sauce, and edible honey mushroom. Fibrinolytic enzymes producing Aspergillus japonicum KSS 05 strain were screened for the production by fibrin plate assay method. The maximum zone of fibrin hydrolysis were found 6 mm diameter. Further the Aspergillus japonicum KSS 05 were employed for the production by submerged fermentation and it showed 235 IU by pH 6, temperature 300C and 1 ml inoculums size. Key words: Fermentation kinetics, effect of pH, fibrinolytic enzymes and fibrin

5-8

Authors: Pradeep Kumar Chaudhary, Subhash Goyal, Nanak Chand Mahajan, Saurabh Kansal, Priti Sinha

Cholecystitis is defined as inflammation of the gallbladder. Ninety percent of cases involve stones in the cystic duct and gall bladder, (i.e., calculus cholecystitis) with the other 10% of cases representing acalculus cholecystitis.(1) The association of gallstones with Helicobacter pylori has been investigated but not clearly demonstrated. In this study, the presence of H. pylori in the gallbladder mucosa of patients with symptomatic cholecystitis and cholelithiasis was investigated.The study included 50 cases of cholecystitis and cholelithiasis randomly selected who were admitted to the surgical wards of M.M.I.M.S.R, Mullana in last 2 years. All patients underwent cholecystectomy and gall bladder mucosa was histopathologically examined by giemsa staining (silver slide test). We concluded that no gall bladder mucosa exhibits presence of H. Pylori. Keywords: Cholelithiasis; Cholecystitis; H. pylori; Giemsa

19-25

Authors: K B Patel, J R Vyas, U M Upadhyay

The objective of this work was to prepare and evaluate oral sustained release matrix tablet of Nateglinide and to study the effect of proportion of wax and addition of release liner on in-vitro release of drug.The prepared tablets were evaluated for pre and post compression parameters. Stability study of the promising formulation was also performed. The matrix tablets were prepared by Direct compression, Co-processed & melt granulation, method using wax in concentration 25%, 35% & 45% and evaluated for on in-vitro drug release using Compritol & Precirol. No interactions were found between drug and excipients. Formulation containing 25% Precirol F13 shows releases up to 12 hours. Tablets with release characteristics offers critical advantages such as site specificity with improved absorption and efficacy etc. Keywords: Nateglinide, Sustained release, Compritol 888, Precirol ATO 5, Melt Granulation, Direct compression,

33-40

Authors: Salim Abou-Baker, T A El-Desouky, EL-Sedeek Lamyaa

Heterocyclic amines (HCAs) are a group of toxic chemicals, play an important role in the etiology of human cancer which formed at high temperature during cooking meat and fish. Antioxidants have proved to inhibit the formation of HCAs due to different mechanisms scavenging free radical, inhibits oxidative enzymes like cyochrome P450 and chelates metal ions like Fe+2 as well as protecting lipids against oxidation. Clove has potent antioxidants and antimicrobial activities standing out among the other species. Therefore current study done to show efficiency of 0.5% clove at preventing the formation of two most common HCAs: 2-amino-3,8-dimethylimidazo[4,5-f]quinoxaline (MeIQx) and 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine (PhIP) through seasoning of beef steaks before grilling and estimate antioxidant status of animals fed on the experimental diets. HCAs levels in food and blood samples were analyzed by HPLC. The results showed that content of MeIQx and PhIP in grilled beef meat steak were 23.0 ±2.87 and 15.0±2.14 ng/g, respectively. While the content of MeIQx and PhIP in seasoning grilled steak were degraded to 1.9 ± 0.31 and 1.6 ± 0.23 ng/g, respectively. On the other hand the results showed that the percentages of reduction of MeIQx and PhIP were 91.7 and 89.3% in seasoning grilled steak, respectively comparing with un- seasoning grilled steak. The levels of tested HCAs also showed significant differences among rat groups fed on the experimental diets. The highest MeIQx and PhIP concentrate in serum rats group fed on untreated grilled meat diet (positive control) were11.1±1.85 and 8.77±8.77 ng/ml, respectively, while seasoning with 0.5% clove before grilling led to decrease in MeIQx and PhIP concentrate to 0.82±0.16 and 0.51±0.09 ng/ml respectively with decreasing percent reached 92.6 % and 94.2% respectively. In addition, the results revealed that fed rats on un-seasoning grilled steak (positive control) caused high significant increased in lipid peroxide (malonaldhyde, MDA) accompanied by significant decreased in the levels of reduced glutathione content (GSH) and activities of antioxidant defense enzymes glutathione peroxidase (GHPx) and catalase (CAT), compared with basal diet group (negative control). However, clove treatment group lowered the level of lipid peroxidation and enhanced the antioxidant status of animals. Seasoning beef meat steaks before grilling with potent antioxidant clove species inhibit HCAs formation and their potential hazards to human health. This might be due to the powerful antioxidant activity of clove as strong hydrogen donating, metal chelating and scavenging of free radicals, hydrogen peroxide and superoxide. Keywords: Heterocyclic amines (HCAs), 2-amino-3,8-dimethylimidazo[4,5-f]quinoxaline (MeIQx) , 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine (PhIP), clove, grilled beef meat, antioxidant plants, lipid peroxide, antioxidant defense enzymes.

48-55

Authors: Mohammed Asadullah Jahangir, Dr MA Saleem, Mohammed Shadab Shahab, Abdul Muheem, Shakir Saleem

see pdf

64-71

Authors: Bilal Tessema, Anteneh Belete, Tsige Gebre-Mariam

D. abyssinica was partially hydrolyzed in 6% HCl solution at room temperature for different lengths of time, (2, 4, 8, 16, and 32 days), dried using oven- and spray- drying techniques and subsequently investigated as directly compressible excipient in paracetamol tablet formulations. Native dioscorea starch (NDS) and oven dried acid modified dioscorea starch (AMDS) exhibited poor flow characteristics, whereas spray dried AMDS was found to be free flowing powder with 21.37 ± 1.39° angle of repose and 13.24 ± 0.76 g/sec flow rate. Both swelling power and percent solubility of the starches were found to increase with increase in temperature; AMDS showed higher percent solubility of 68.53%. Lubricant sensitivity and dilution potential of spray dried NDS and spray dried AMDS were investigated by incorporating magnesium stearate and paracetamol, respectively. In tablet formulations, spray dried AMDS and Starch 1500® tablets were produced with acceptable tablet characteristics up to 1% and 0.5% magnesium stearate concentrations, respectively. The spray dried AMDS was able to accommodate up to 40% paracetamol with acceptable criteria. Thus, it can be concluded that AMDS can be used as an alternative directly compressible excipient in tablet formulations. Keywords: Dioscorea starch, acid modification, spray drying, directly compressible excipient.

3-8

Authors: Vijay Kaul, Shaktibala Dutta, Mirza Atif Beg, Nand Kishore Singh, Shalu Bawa, Mohammad Anjoom, Srihari Dutta

Introduction and Aim: Depression is an important global public health problem due to its relatively high lifetime prevalence and significant disability caused by it. The present study was conducted to compare improvement in functional outcome by Amisulpride and Escitalopram among depression patients using Sheehan’s Disability Scaling. Material and methods: The study was conducted in depression patients for 1 year in the Department of Neuropsychiatry, Nepalgunj Medical College & Teaching Hospital. A total of 117 depression patients were divided into 2 groups. Group I (58 patients) received Amisulpride tablet at a dose of 50 mg/day and Group II (59 patients) were given Escitalopram at a dose of 10 mg/day. The patients were required to follow up at 4, 8 and 15 weeks. The efficacy of the drugs was calculated by Hamilton depression rating scale (HAM-D). The improvement in functional outcome was compared between the two groups by using Sheehan’s Disability Scale (SDS). Appropriate statistical tools using GraphPadInstat 3.0 were used for analysis. p value < 0.05 was considered significant. Results: HAM-D score in group receiving Amisulpride at 0 and 15 weeks was 16.92±0.35 and 7.87±0.29 (p<0.0001). HAM-D score in group receiving Escitalopram at 0 and 15 weeks was 17.09±0.39 and 6.63±0.39 (p<0.0001). Sheehan’s Disability Score in group receiving Amisulpride at 0 and 15 weeks was 20.35±0.31 and 11.08±0.60 (p<0.0001). SDS score in group receiving Escitalopram at 0 and 15 weeks was 21.53±0.55 and 11.49±0.46 (p<0.0001). Intergroup comparison at 15 weeks was insignificant (p>0.05). Gastrointestinal disturbances, sexual disturbances, amenorrhea, lactation, agitation and insomnia were the commonly encountered adverse drug reactions. Conclusion: Both Amisulpride and Escitalopram showed improvement in Sheehan’s Disability Scale at the end of study period. But intergroup comparison showed no significant difference in the two groups. Key words: Depression, Amisulpride, Escitalopram, Sheehan’s Disability Scale (SDS).

14-16

Authors: Naveen Kumar Tamma, T Naga Reddy, N Radha Kishan

Objective: The objective of this study is importance of primary care physician in screening diabetic retinopahy patientsMaterial and Methods : Patients of type-2 diabetes mellitus attending diabetic clinic in melaka manipal medical college , malaysia were prospectively reviewed. Risk factors associated in study population were assessed by biochemical parameters, clinical examination , retinal photographs and referred to ophthalmology clinic. Results: The prevalence of non proliferative and proliferative diabetic retinopathy with type-2 diabetic patients was 17% and 1% with history of decreased in vision above age group of 50 years . In addition the risk factors in the study group associated with the development of diabetic retinopathy are uncontrolled HbA1c levels ( 27%) , high BMI (38% ), increased total cholesterol (9% ) , uncontrolled fasting blood sugar levels (47%), and increased duration of diabetes. Conclusion: Diabetic retinopahy is highly prevalent in patients with type-2 diabetes mellitus. Our findings indicates primary care physicians are well educated in regards to diabetic eye disease and in identification of risk factors due to number of years experience. Keywords: Proliferative and non proliferative diabetic retinopathy, risk factors, visual disability, type -2 diabetes mellitus

24-26

Authors: Ganesan Devendran, Ganesan Sivamani

The bioactive components of Costus spicatus leaves have been evaluated using GC/MS. The chemical compositions of the ethanolic extract of Costus spicatus leaves were investigated using Perkin-Elmer Gas Chromatography–Mass Spectrometry, while the mass spectra of the compounds found in the extract was matched with the National Institute of Standards and Technology (NIST) library. GC/MS analysis of ethanolic extract of Costus spicatus leaves revealed the existence of 1,2-Ethanediol, monoacetate (2.79%), 1-Tetradecanol (0.09%), Elema-1,3,11(13)-trine-12-ol (0.31%), beta-costol (0.33%), 4,7,10,13,16,19-Docosahexacnoic acid (0.57%), methyl ester (5.15%), Naphtho[1,2-6]furan-3-one (1.27%), 2,3,3a,4,5,5a,6,7,9a,9b- decahydro-3,5a-9-trimethyl-7,9a-peroxy (0.39%), Eremanthin (93.44%), 5-(ethynyl) nona-1,8-dien-5-ol (0.19%), Benzeneacetic acid (0.10%), Alpha-bergamotene (0.38%), 1,2-Benzenedicarboxylic acid, diisooctyl ester (2.55%), Isolongifolene, 4,5-dehydro- (3.68%) by GCMS analysis and the biological activity of each compound was discussed in this paper. As Costus spicatus can grow and spread easily and because of its higher biomass availability, it can prove as an effective and cheaper drug for various diseases. Key words: Costus spicatus , GCMS analysis, Bioactive components.

43-53

Authors: Mithun Bhowmick, Pratibha Bhowmick, Tamizharasi Sengodan, Sivakumar Thangavel

A simple, specific, sensitive and rapid Reverse phase high performance liquid chromatographic (RP-HPLC) method has been developed and validated for the quantification of Metoprolol Tartrate in small volumes of rabbit plasma. The method was further extended for its pharmacokinetic studies in rabbit plasma samples after transdermal and oral administration. Biological sample preparation involving simple extraction with organic solvent, followed by dilution with mobile phase was adopted to eliminate any chromatographic solvent effects. The method was proven to be linear over a plasma concentration range of 20 ng/ml to100 ng/ml with a mean correlation coefficient of 0.99. The limit of detection and the limit of quantification of the newly developed method were determined to be 5.8ng/mL and 16.1ng/mL, respectively. The method was successfully applied to assess pharmacokinetic parameters of Metoprolol Tartrate in rabbit plasma and found out the comparative bioavailability of MT following oral and transdermal dosage forms. The developed method was established as a rapid analytical tool in a pharmacokinetic study as it required short retention time, high precision, sensitivity and small volumes of plasma for analysis. Keywords: Metoprolol Tartrate, RP-HPLC, quantification, Rabbit plasma, Pharmacokinetic study, oral, transdermal.

61-70

Authors: Neha Pandit, Tanuj Josh

Objectives: A review article on novel approaches on oral insulin delivery. Data Sources: Review articles on oral insulin delivery, Books. Study selection: This review consist of importance as well as current approaches for oral insulin delivery like liposomes, nanospheres, nanocubeics, erythrocytes, thiolated chitosan tablets, chitosan microspheres etc. Summary of content article: Type 1 diabetes mellitus is a metabolic disorder which arouse as a major health problem worldwide. Clinical management of insulin is done by insulin replacement therapy and current route of its administration is through subcutaneous injection having many challenges. To overcome the problems associated with insulin injections novel approaches for insulin administration are being explored. If insulin is administered orally, in the stomach rapid enzymatic degradation of insulin occurs and in the intestine insulin is digested and hence inactivated by the action of proteolytic enzymes occurs. This review consist of importance as well as current approaches for oral insulin delivery like liposomes, nanospheres , nanocubeics, erythrocytes, thiolated chitosan tablets, chitosan microspheresetc. This review also gives the information about current market status of oral insulin5. Conclusion: The oral route is considered to be most acceptable and convenient route of administration for chronic therapy. Attempts have been made to achieve oral insulin delivery using various systems. Liposomes, microemulsions, nanocubicles, thiolated chitosan, chitosan microspheres and so forth have been prepared for the oral delivery of insulin. Keywords: oral insulin, approaches for oral insulin delivery , current market status.

5-9

Authors: Rishi Ram Parajuli, Priyanka Pokhrel, Shreekrishna Lamichane, Saroj Shrestha

Prodrugs are bioreversible derivatives of drug molecules that undergo an enzymatic and/or chemical transformation in vivo to release the active parent drug, which can then exert the desired pharmacological effect. Prodrug design is a choice of approach in solving many of the problems like stability, toxicity, solubility, permeability and drug targeting that affect drug discovery and development. Prodrug design is fruitful approach for drug targeting by changing the physiochemical, biopharmaceutical or pharmacokinetic properties of drugs. About 10-14% of drugs approved worldwide can be classified as prodrugs. The present article takes a review of introduction, classification, applications of prodrug design in various areas of drug development and basic functional groups that are amenable to prodrug design. Keywords: Prodrugs, objectives, classification, application, functional groups, limitation.

13-23

Authors: M Kadiri, A W Ojewumi, D A Agboola, M F Adekunle

An ethnobotanical survey of some plants used for management of diabetes in Abeokuta, Ogun State, Nigeria was conducted. A total of 100 questionnaires were administered; (50 herbal practitioners and 50 on patients). Investigations were carried out on the plant parts used, methods of preparation and administration including, dosage and duration of usage. The results showed that fifty (50) plant species belonging to 30 families used in herbal anti-diabetes recipes. The most frequently used plant was Vernonia amygdalina (54%), followed by Azadirachta indica (44%), Ocimum gratissimum (20%), Mormodica charantia (10%) and Citrus aurantifolia (10%). Irrespective of the plant parts (leaves, fruits, stem- barks or roots) or combinations of the plant parts, water and alcohol were the main solvents. The most frequently used plant parts was leaf (62%) and mainly by decoction. Treatment regimens were by chewing or drinking of the aqueous herbal preparations (350-400ml) daily for 6-12 weeks or until symptoms of diabetes disappear. Keywords: Anti-diabetic plants, ethnobotanical survey, herbs, plant parts.

29-36

Authors: JAY RAJNIKANT SHAH

Background: Astigmatism is a type of refractive error. Some type of it can be corrected by Cylindrical type of glasses. It is found in clinical practice commonly. This review presents an overview of research that has been carried out examining various aspects of this refractive error. Objective: The present study was aimed to examine the components of astigmatism and the research into the prevalence and natural course of astigmatic refractive errors throughout life.. Materials and Methods: Study The prevalence of astigmatism in various diseases and syndromes is also discussed. We highlight the extensive investigations that have been conducted into the possible aetiology of astigmatism, however, no single model or theory of the development of astigmatism has been proven conclusively. Discussion: Observations and evidence from the literature supporting and contradicting these hypotheses are presented. Recent advances in technology such as wavefront sensors and videokeratoscopes have led to an increased understanding of ocular astigmatism. With continued improvements in technology, our knowledge of astigmatism and its genesis should continue to grow. Conclusion: With continued improvements in technology, our knowledge of astigmatism and its genesis should continue to grow.

43-47

Authors: Navneet Kaur

Ramdass is a famous village in Punjab due to entomb of Baba Budhaa Sahab ji. It is located in tehsil Ajnala district Amritsar, Punjab. Most of the land in Punjab is used in agriculture practice, while 07 % is wasteland. Even the district Amritsar and Ramdass has a waste land, in which herbs, shrubs and trees are growing. This study was undertaken to document the floral diversity in the waste land of Ramdass village, teshil Ajnala, district Amritsar, Punjab. The study shows that 70 are easily available in wasteland in the vicinity of Ramdass village, which are belong to 65 Genus and 37 families. Keywords: Floral diversity in wasteland

55-61

Authors: Mohd. Mujahid

Aim: Reactive oxygen species (ROS) such as superoxide anion, hydrogen peroxide and hydroxyl radicals are involved in the oxidative damages resulting in pathogenesis of the various disorders and diseases. Thus, the scavenging activity of methanolic extract of Adenanthera pavonina Linn leaves (MEAP) was evaluated to find the ability to counteract oxidative damages by ROS. Materials and methods: Total phenolic and flavonoid contents were determined by colorimetric principle using gallic acid and rutin calibration curves respectively. Scavenging activity was evaluated by DPPH free radical and nitric oxide anion scavenging assays. Total reducing power was also evaluated. Results: Phytochemical analysis of MEAP showed the presence of alkaloids, glycosides, carbohydrates, phenolic compounds, tannins, flavonoids, terpenoids, saponins, sterols, proteins and resins. Total ash, acid insoluble and water soluble ash values were found to be 8.86, 2.24 and 7.18% w/w respectively. Loss on drying was found to be 1.53% w/w. Extractive value was found to be 11.2% w/w. Total phenolic and flavonoid contents in MEAP were found to be 55.43±1.07 µg/ml equivalent to gallic acid and 52.87±1.8 µg/ml equivalent to rutin. The IC50 values for the scavenging of DPPH free radical and nitric oxide anion were found to be 425 µg/ml and 352 μg/ml as compared to that of standard ascorbic acid 320 μg/ml and 280 μg/ml respectively. Total reducing power was found to be increasing with increasing doses of extract. Conclusion: Methanolic extract of Adenanthera pavonina Linn leaves is a potent scavenger of ROS and can counteract oxidative damages by ROS. Thus, MEAP can be employed as an anti-oxidant drug to counteract and treat oxidative damages by ROS. Keywords: Adenanthera pavonina, ROS, scavenging activity, Phenolics, Flavonoids.

72-75

Authors: N Santhi Priya, CH Swaroop Reddy, CH Gowtham Sai, G Madhusudana Rao, G Lakshman Reddy, M Santhosh Aruna

The present manuscript deals with the study to formulate and evaluate suppository for the successful delivery of Zidovudine through rectal administration. Zidovudine has tendency to cause gastric ulcer making it necessary to explore safer routes of its administration. Melt Fusion method was used for the preparation of suppositories using glycerogelatin and Emulsified glycerogelatin as suppository base. The prepared suppositories were evaluated for their visual characteristics, physicochemical properties like dimensions, weight variation, melting time, disintegration time, drug content and in-vitro drug release characteristics. The release was found to be greater in emulsified suppositories with satisfactory disintegration time. Keywords: suppository, Fusion method, Zidovudine

80-86

Authors: Mithilesh Kumar Dwivedi, Purushottam Das Soni, Shailja Sachan, Santosh Tiwari

QSAR analysis on a set of synthesized p-Aminosalysilic Acid derivatives analogues tested growth inhibitory antiviral activity was performed by using MLR procedure. The activity contribution of these compounds were determined from regression equation and the validation procedures to analyze the predictive ability of QSAR models were described.The results are discussed on the basis of statistical data. High agreement between experimental and predicted antiviral activity inhibitory values are obtained. The results revealed the significant roles of topological, geometrical and substituent electronic descriptor parameters on the inhibitory activitypIc50 of coumarin derivative analogues of the studied molecules Key Words: QSAR, Antiviral Activity, MLR

92-95

Authors: Mahesh Kumar Vishwanadha

The objective of the present investigation is to prepare Deacetylated Xanthan Gum, a new Xanthan Gum based polymer and to evaluate its application in controlled release (CR) and in the design of Simvastatin controlled release tablets. Deacetylated Xanthan Gum polymer was prepared by gelatinization of Xanthan Gum in the presence of sodium hydroxide. Matrix tablets each containing 40 mg of Simvastatin were formulated employing Deacetylated Xanthan Gum polymer in different proportions of drug and polymer and the tablets were evaluated. Simvastatin release from the formulated tablets was slow and spread over 12 hr and depended on percent polymer in the tablet. Release was diffusion controlled and followed zero order kinetics. Non – Fickian diffusion was the drug release mechanism from the formulated tablets. Simvastatin release from matrix tablets F1 formulated employing 37 % Deacetylated Xanthan Gum was found suitable for the design of oral controlled release tablets. Key-words: Deacetylated Xanthan Gum, Controlled release, Simvastatin, Matrix tablets.

9-16

Authors: Ganeshanand, Jeet Kamal, Ashish Baldi

Rheumatoid arthritis is an auto-immune joint disorder involving pain and inflammation. Various approaches are used for pain management and relief from arthritis with single and multiple dose therapy. In single dose therapy, use of non-steroidal anti-inflammatory drugs like diclofenac aceclofenac, celicoxib etc. reported many side effects mainly leading to decrease in production of prostaglandin and holding the ulcer. High dosing frequency of these drugs is also a major factor of risk. Recently developed novel formulations are especially suitable for achieving controlled and delayed release profile with low risk of dose dumping. These systems have received great attention of pharmaceutical industry as they deliver accurate amount of drug at the right time and location thus increasing patient compliance and economic feasibility and avoiding drug associated side effects. Present review mainly deals with the problem of ulceration in pain management, various approaches to overcome this and specifically explore the possibilities to apply novel drug delivery systems for this purpose. Keywords: Arthritis, Drug delivery systems, Gastroretentive, NSAIDs, Pain, Rheumatoid arthritis, Rheumatic pain management.

20-28

Authors: P B Dalvi, A B Gerange, P R INGALE

The solubility behavior of drugs remains one of the most exigent aspects in formulation development.With the advent of combinatorial chemistry and high throughput screening, the number of poorly water soluble compounds has dramatically increased. Among all the newly discovered chemical entities, about 40-45% drugs fail to reach market due to their poor water solubility. Because of solubility problem, bioavailability of drugs gets affected and hence solubility enhancement becomes necessary. Solid dispersions have attracted considerable interest as an efficient means of improving the dissolution rate and hence the bioavailability of drugs. This article reviews the various preparation techniques, carriers used, advantages and limitations of solid dispersions and compiles some of the recent advances. There are various methods available to improve the solubility of the new drug in which solid dispersion emerged promising. A Solid dispersion generally composed of two components- the drug and the polymer matrix. Numerous methods are existing to prepare the solid dispersions such as melting method, solvent evaporation method, fusion method, kneading method, melting method, spray drying method, co-grinding method, lyophilization technique, hot melt extrusion, melt agglomeration, supercritical fluid (SCF) technology etc. Solid dispersion technologies are particularly promising for improving the oral absorption and bioavailability of BCS Class II drugs. The experience with solid dispersions over the last 10-15 years indicates that this is a very fruitful approach in improving the release rate and oral bioavailability of poorly water soluble drugs. Hence, this approach is expected to form a basis for the commercialization of many poorly water-soluble and water-insoluble drugs in their solid-dispersion formulations in the near future. Key words: Dissolution, Solid Dispersion, Solubility, Cellulose Derivatives, Polyethylene glycol.

45-49

Authors: Mirza Atif Beg

Background: Drug utilization studies are beneficial in clinical practice for rational prescribing, as there is continuous proliferation of new drugs and the increasing recognition of their delayed adverse effects. Depression is an important global public health problem thus making such studies a must for minimizing the medication errors. Aim and objectives: Present study audits the prescribing pattern of psychiatric private practitioners (PPs) vs psychiatric practitioners of tertiary care teaching hospital (TCTH) at Dehradun, Uttarakhand. Materials and methods: A total of 371 prescriptions were analysed, 196 were from collected from PPs and 175 from TCTH at Dehradun. They were analysed using WHO drug use indicators and National List of Essential Medicines (NLEM-2013). Results: Anxiolytics 150(25.25%) were most commonly prescribed by the PPs followed by antidepressants 120(20.20%) and antipsychotics 111(18.48%), whereas antidepressants 105 (27.78%) was the major drug group prescribed by TCTH followed by anxiolytics 102(26.98%) and antipsychotics 37(9.79%). Tricyclic antidepressants(TCAs) were most frequently prescribed antidepressants followed by selective serotonin reuptake inhibitors(SSRIs) at TCTH whereas SSRIs were the major antidepressants prescribed by PPs. Anxiolytics and anticholinergics co-prescription with antidepressants and antipsychotics respectively, was a common observation among PPs and TCTH. Analysis of prescription revealed average number of drugs prescribed per prescription in teaching hospital is 2.16 vs 3.03 among the private practitioners. 18.25% Fixed drug combinations(FDCs) were prescribed by TCTH while 0% were prescribed by PPs. 55.39% and 55.56% drugs were prescribed from the NLEM-2013 by the PPs and the TCTH respectively. Conclusion: There were lesser number of drugs prescribed per prescription and more frequent use of drug combinations at TCTH while no drug combinations and greater number of drugs per prescription were prescribed by PPs. Newer class of drugs were more frequently prescribed by PPs. Key words: Drug utilization studies, antidepressants, antipsychotics, anxiolytics, Fixed drug combinations.

55-64

Authors: P B Dalvi, S S NANDAN, P R GANGURDE, S A GANGURDE

The aim of the current study was to design oral controlled release gastro-retentive drug delivery of Tinidazole. that are designed to retain in the stomach for a long time and have developed as a Local drug delivery system for better eradication of Helicobacter Pylori in peptic ulcer diseases. Tablets were prepared by direct compression and evaluated for evaluated for various physical parameters, Hardness, friability, drug Content, floating ability, Lag time, Swelling Index studies, and in vitro dissolution parameters as well as kinetics of release were assessed. Factorial design for 2 factors at 3 levels each was employed to systematically optimize drug release profile and Floating Behaviour. Sodium Alginate and Hydroxy Propyl Metheyl Celluiose (HPMC K15M) were taken as the independent variables. Response surface plots and contour plots were drawn.Compressed tablets exhibited zero order drug release kinetics, resulting in regulated and complete release until 12 hours. Polynomial mathematical models, generated for various response variables using multiple linear regression analysis, were found to be statistically significant (P < 0.05).Both the polymers had significant effect on the release profiles of the tablets, Besides unraveling the effect of the 2 factors on the various response variables, the study helped in finding the optimum Formulation ‘F4’ with Floating Lag Time (20 sec.) and having controlled release upto 12 hours (99.47%). Meanwhile, sustained profiles of drug release were also obtained. In general, these systems can float in the gastric conditions and control the drug release from the tablets.

69-72

Authors: Divya Stephy John

Introduction: Increase in research aptitude among students has resulted in a rise in the protocol numbers that get submitted to the Institutional Ethics Committee (IEC) for the purpose of recognition in dissertation, publications and forum presentations. Approval of research protocols by the IEC is considered the first barrier for most student researchers. Lack of solid concepts regarding dynamics involved in research seems to have resulted in unwarranted fear among students to pursue research. The current analysis attempts to identify areas of lacunae by retrospective reflection on the protocols submitted to the IEC in a teaching institution. Methodology: Retrospective Qualitative Analysis of 102 Protocols submitted by postgraduate medical students between January, 2013 to August, 2013 to the IEC were assessed by the following parameters: - Scientific and technical soundness of protocols, Ethical considerations and risk minimization strategies employed, Adequacy of documentation and scrutiny of Informed consent process, Temporal relationship between submission of protocols and commencement of the research procedures. Results: 79.41% of protocols were approved by the IEC. 95% of protocols were in proper format and adequate documentation.90% of the protocols were submitted for approval prior to the commencement of study. 20.59% of the submitted protocols were denied approval on the first hearing by the IEC. Discussion: We infer that majority of the postgraduate students are aware about the existence of guidelines in clinical research. The most common errors leading to non approval of research protocols are due to misjudgement regarding technical feasibility in available infrastructure, non comprehensive review of literature, non-addressal of ethical guidelines/risk minimisation strategies towards participants and inadequate documentation.

77-82

Authors: D Kapoor

see pdf

88-93

Authors: Jyoti Parkash, Kannubhai Rameshbhai Patel

Objective- Hepatoprotective activity of Chenopodium album leaves extract in CCl4 induced hepatotoxicity in rats. Method- The present study has been undertaken to evaluate hepatoprotective activity of Chenopodium album leaves extract in CCl4 induced hepatotoxicity in rats. The study was carried out by comparing SGOT, SGPT, Alkaline Phosphate, Direct Bilirubin, Total Bilirubin and Total proteins level in serum of different groups of rats. Histopathological study was also done on liver tissue of the all group of animals and compared with standard, positive control and negative control groups. Result- Rats treated with Chenopodium album leave extract caused a significant reduction in SGOT, SGPT, Alkaline phosphate, direct bilirubin, total bilirubin. Level of total proteins was found retrieving towards normalcy. Level of these enzymes was almost comparable to standard drug i.e. Silymarin. Hepatoprotective activity was confirmed by histopathological study of liver tissue of control and treated animals. Conclusion- From results it can be concluded that Chenopodium album possess hepatoprotective activity against CCl4­ induced liver toxicity in rats.

100-106

Authors: Pradeep Saha, Kanu Bhai Ramesh Bhai Patel

The hepatoprotective potential of Mahonia leschenaultii Takeda. (root wood and root bark) extract was evaluated in Country-Made Liquor (CML)-induced hepatotoxicity in Wister rats. The rats were made hepatotoxic by administering (CML) (3 ml/100g body weight/day in two divided doses) and corn oil (1 ml/100g body weight /day in a single dose) orally for 21 days. The administration of root wood and root bark of Mahonia leschenaultii Takeda. extract (200 mg/kg body weight) mixed with tween 80 (0.5% w/w) orally from day 15 to day 21 along with CML. The different biochemical parameters tested are ALAT, ASAT, ALP, LDH, TGL, total protein, total cholesterol, Albumin, total bilirubin and direct bilirubin. The results were compared with standard drugs i.e. Silymarin (70 mg/kg body weight) orally. The histopathological study was carried out and histopathological changes were observed and compared. The study showed that the extract of root wood and root bark of Mahonia leschenaultii Takeda. is definitely a hepatoprotective agent and help in reduction of liver damage. Key words: Hepatoprotective, Mahonia leschenaultii Takeda. Country-Made Liquor, Root wood, and Root bark

115-116

Authors: Mohammed Ather, P Padmavathi, D Padma Prabha, Mirza Mohammed Mohiuddin Baig, Dr Nasreen, Pallavi Gupta

Aim: To study the efficacy of Albendazole in treating Extra ocular and Orbital Myocysticercosis. Materials and Methods: This is a prospective interventional case study conducted at Department of Oculoplasty and Orbital disorder of Sarojini Devi Eye Hospital which is a tertiary care eye hospital. 6 cases of Myocysticercosis, 4 males and 2 females presented between Jan 2014 to June 2014 at department of Oculoplasty were included in the study. After clinical examination and radiological confirmation patients were given oral Albendazole 400mg bd for 3 weeks along with Tab.Prednisolone 1mg /Kg of body weight. They were evaluated clinically for control of symptoms like pain, redness and protrusion of eyeball and regression of signs like reduction in chemosis, Proptosis and tenderness. Results: All 6 cases responded to medical treatment by Albendazole and Prednisolone by total reduction in symptoms and signs thereby avoiding surgery on them. Conclusion: Ocular and Orbital Myocysticercosis respond well to medical treatment by Tab.Albendazole along with Tab. Prednisolone. Key Words: Myocysticercosis, Albendazole, Proptosis, Prednisolone.