Volume 4 - Issue 3

S.No Title & Authors Name Page
Formulation and evaluation of bilayered floating tablets of cefuroxime axetil
K. Geetha, D. Prasad, M. Sudhakar, M. Yasmin Begum
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Study aims to design a Gastro retentive Drug Delivery System of Cefuroxime axetil (CA). CA is a broad spectrum beta lactam type of antibiotic. More specifically, it is a second-generation cephalosporin. CA has site specific absorption from upper gastro intestinal tract and in intestine it undergoes hydrolysis to cefuroxime having poor absorption. Unabsorbed drug causes high concentration of antibiotic entering into colon and contributes to side effects colitis. Therefore a gastro-retentive drug delivery system is required to ensure controlled drug delivery within drug absorbable region. Bilayer tablet, each layer containing half the dose of the drug was formulated with Immediate Release Layer (IRL) and Floating Matrix Layer (FML). The present research describes formulation of bilayered floating tablets of Cefuroxime axetil using HPMC polymers like HPMC K4M, HPMC K15M, HPMC K100M and Sodium alginate. All formulations showed acceptable specifications for weight variation, thickness, hardness and friability. The formulations containing HPMC K4M, HPMC K15M provides a better option for Controlled release than HPMC K100M and Sodium alginate
Preparation of 5-florouracil microspheres for colonic drug delivery
Sangeeta Mohanty, Amit kumar Panigrahi
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5-Fluorouracil is widely used anticancer drug,which are effective during the S-phase of cellcycle. Since It has poor bioavailability so targeting of 5-Fluorouracil at site of action is of great beneficial. Attempt has been made to develop a stable microparticulate formulation of 5-Fluorouracil to be administered orally to target colon. Here, chitosan was chosen as polymer. Chitosan microspheres were coated with eudragit s-100.The Cross linked chitosan microspheres containing 5-Fluorouracil were prepared by emulsification method using glutaraldehyde as crosslinking agent and characterized for %Yield, ParticleSize, Surface properties and Morphology, Entrapment Efficiency and DSC. InVitro release studies of coated and uncoated chitosan microspheres was performed in pH progression medium at 37 ± 0.5 0C ,in simulated gastric fluid, simulated intestinal fluid. As compared to chitosan microspheres, coated microspheres(1: 5 ) showed about 7.88% drug release after 6 hours and rest of drug releases upto 24 hours. When the core:coat ratio is 1: 10 , release does not occur. Hence, we can conclude that eudragit coated chitosan microspheres prevents drug release in stomach, small intestine, targets colon only; thus avoiding systemic side-effects associated with 5-Fluorouracil.
A review on controlled drug delivery system
A Hariom Prakash Rao, V.T. Iswariya , V Lokeswara Babu and A Srinivasa Rao
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Controlled-release systems are used to control the plasma concentration of the drug after administration by various possible routes. These are the systems in which the drug is released in a predetermined pattern over a fixed period of time. The release kinetics is usually zero-order. Ideally the release rate from the dosage form should be the ratedetermining step for the absorption of the drug and in fact for the drug concentration in the plasma and target site. The controlled release formulations will reduces the dosing frequency required for daily. This article provides an ideal requirements, advantages, properties and different approaches involved in the development of controlled release formulations for the better delivery of drugs.
Analytical method development and validation of simultaneous estimation of dosulepin and methylcobalamin in tablet dosage form by RP-HPLC
Aruna P, A. Ajitha, V. Uma Maheshwar Rao
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A sensitive, selective and precise high performance liquid chromatographic method has been developed and validated for the simultaneous determination of Dosulepin and Methylcobalamin in tablet dosage form. The method employed waters xterra C8 column (150 x 4.6 mm , 5 μm particle size) as the stationary phase while Acetonitrile, 0.1 M H3PO4 (70:30,v/v) was used as mobile phase. The Retention time of Dosulepin and Methylcobalamin were observed to be 1.89and 2.85 minutes, respectively. The flow rate was found to be 1ml/min and effluents were monitored at 222 nm. The linear regression analysis data for the calibration plots showed a good linear relationship for Dosulepin and Methylcobalamin over a concentration range of 150-450 μg/ml and 3-9 μg/ml respectively with correlation co-efficient of 0.999 for Dosulepin and 0.999 for methylcobalamin. The LOQ was found to be 9.23 and 9.57 μg/ml respectively for Dosulepin and Methylcobalamin. The method was validated as per ICH guideline and it was found to be accurate, precise and robust. Marketed formulation was analyzed successfully
A review on bio-availability enhancement techniques of poorly soluble drug
Anwar Khan, Rishabha Malviya, Pramod K Sharma
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Solubility is the process of dissolution of solid in liquid phase to give a homogenous system and is one of the important parameter to achieve desired concentration of drug in systemic circulation for pharmacological response. Dissolution rate of poorly water-soluble drugs is rate limiting step for its bioavailability so increase in bioavailability is the major challenging task in drug development. Because only 8% of new drug candidates have both high solubility and permeability. For BCS class II drugs, enhancement of Solubility and hence bioavailability is important parameter before formulation of dosage form. Hydrophobic drugs often require high doses in order to reach therapeutic plasma concentrations after oral administration. Therapeutic effectiveness of a drug depends upon the bioavailability and ultimately upon the solubility of drug molecules. Various techniques are used for the improvement of the aqueous solubility, dissolution rate, and bioavailability of poorly water soluble drugs include size reduction, chemical modification, pH adjustment, solid dispersion, complexation, co‐solvency, hydrotropy etc. the main emphasis of review article is to describe the techniques of solubilisation for the attainment of effective absorption with improved bioavailability.
Qsar modeling studies on 2,4-thiazolidinediones as potential α-glucosidase inhibitors
Ch. Prasad, Bhavani Boddeda, S. Kottiah and A. Vasudeva Rao
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A linear quantitative structure-activity relationship (QSAR) model is presented for modeling and predicting the α- glucosidase inhibitory activity. The model was produced by using the multiple linear regression (MLR) technique on a twenty one compound database that consists of newly discovered 2,4-thiazolidinediones. The major conclusion of this study is that molecular weight, wiener index, andrews affinity and polar surface area affect significantly the α- glucosidase inhibitory activity by 2,4-thiazolidinediones. The selected QSAR descriptors serve as a primary guidance for the design of novel and selective α-glucosidase inhibitors.
Studies on formulation development of gastroretentive drug delivery system for pioglitazone hydrochloride
Swetha Duggi , Narendra Chary T
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Pioglitazone HCl is used for the management of type-2 diabetes. It is an absorption window limited drug, whose solubility decreases with increase in the pH and has a short half life of 3-7 h. Here an attempt is made to developed the floating matrix tablets, which design in way that after oral administration the GI resistant time is prolonged and thus to give sustained action with increase in the bioavailability of the drug. Pioglitazone HCl showed maximum absorption at wavelength 269 nm in 0.1N HCl. various formulations were developed by using release rate controlling and gel forming polymers like HPMC, Xanthan gum,guar gum & combinations by direct compression method with the incorporation of sodium bicarbonate as gas generating agent. The prepared tablets were characteristics by drug content, floating property, swelling and in vitro dissolution test using USP dissolution test apparatus Type – II (paddle method) in dissolution medium of 0.1 N HCl. The in vitro dissolution results of all tablets were computed by using dissolution software. The prepared tablets were found to be good hardness, diameter, weight variation, thickness, friability drug content, floating property and in vitro drug release. Drugpolymer compatibility studies by FTIR gave conformation about drug purity and showed no interaction between drug and selected polymers. All the formulations had floating lag time below 4 minutes and constantly floated on dissolution medium for more than 12 h. Swelling studies indicated significant water uptake and contributed in drug release. From among all the developed formulations, as F2 prolonged the drug release (95.86 %) for longer period of time (12 hrs.); they were selected as best formulations. Thus, selected formulations satisfied floating time, swelling index and in vitro drug release profile requirements for a floating drug delivery system.Tablets of Pioglitazone HCl prepared with HPMC K4M, HPMC 15M,HPMC K100M,Xanthan gum,Guar gum and Chitosan were found to be acceptable floating property, water uptake and in vitro drug release.
Effects of cyanoacrylate adhesives and their occupational hazards in prosthodontics - A review~
N. Nilofer Nisha, Jafar Abdulla Mohamed Usman
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The application of cyanoacrylate adhesives in dentistry has served a boon for many dentists, dental students and dental technicians. Cyanoacrylates have been widely used in various applications in dentistry particularly in the field of Prosthodontics as a repair adhesive and sealing glue. Its biocompatibility and histotoxicity has increased concerns regarding its potential toxic nature among the dental personals. The working room or area should be maintained with more levels of relative humidity, sufficient room airflow and appropriate ventilation to minimize the dental professionals and technicians from exposing to the volatile toxicity of cyanoacrylate adhesives. This article discusses the potential occupational hazard due to cyanoacrylates in the field of Prosthodontics.
Multi unit drug delivery system. A brief review of pelletization technique
Anwar Khan*, Rishabha Malviya, Pramod K Sharma
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At present time pharmaceutical research and development showing its interest on drug delivery. Which enhances therapeutic action while minimizing side effect. Use of multi-particulate is the gift of that research which achieve delayed or controlled release with low risk of dose dumping, flexibility of blending to attain different release pattern as well as reproducible and short gastric residence time. Pelletization is a novel approach for the formation of spherical beads or pellets from fine powder or blend in order to develop site specific drug delivery system. Different techniques of pelletization such as suspension/solution layering, extrusion and spheronisation, cryopelletization etc. can be used for the formation of multi particulate drug delivery system. In order to provide extended or delayed release formulation, thus extending the frontier of future pharmaceutical development.
Formulation and evaluation of polyherbal formulation as hair colorant
Ealumalai Vadivel and Yeshwant T. Kandolkar
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Herbal cosmetics formulated by using various coloring ingredients as the base, in which one or more coloring ingredients are used to provide defined cosmetic benefits, are termed as “Herbal Cosmetics”. The need of herbal medicines is increasing rapidly due to their lack of side effects. Herbal drugs constitute a major part in all the traditional systems of medicine. Hence, an attempt has been made to review the use of natural products obtained from plant sources to replace the synthetic dyes. The composition of natural hair dye consisting of amla, bhringraj, henna, mandara, indigo, ratanjot , sariva, curry leaves and methi seed powders are blended with urea and the mixture is soaked to obtain a dye. The plant samples have been standardized by physico-chemical parameters such as total ash, acid insoluble ash, water soluble ash and extractive value of different solvents. The formulated hair dye have been characterized by pH, microscopic study, effect of sunlight, effect of detergent, effect of three time coating and patch test. Result of the present studies shows that out of 17 hair colorant formulations four formulations, F2, IF2, BAF3 and KM2 have better activity. The studies have also shown that there is no hair damage or scalp irritation on dyeing the human hair. Hence this formulation proves to be a key alternative for modern synthetic hair dyes.
Development and validation of rp-hplc method for the estimation of fingolimod in bulk and tablet dosage form
J. Raghuram and N. Appalaraju
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A simple, precise, rapid and accurate reverse phase HPLC method was developed for the estimation of Fingolimod in tablet dosage form.ZobraxEclipseXDB-C18, 150x4.6 mm 5 μm partical size, with mobile phase consisting of water: acetonitrile in the ratio of 60:40 v/v was used. The flow rate was 0.8 ml/min and the effluents were monitored at 215 nm. The retention time& Recovery time was 20.0min&3.273. The detector response was linear in the concentration of 60-360 mcg/ml. The respective linear regression equation being Y= 41219.363x+65555.8. The limit of detection and limit of quantification was 0.15mcg and 0.45mcg/ml respectively. The percentage assay of Fingolimod was 99.72 %. The method was validated by determining its accuracy, precision and system suitability. The results of the study showed that the proposed RP-HPLC method is simple, rapid, precise and accurate, which is useful for the routine determination of Fingolimod in bulk drug and in its pharmaceutical dosage form.
Novel polymers for mucoadhesive drug delivery
Abdul Malik, Nayyar Parvez, Pramod Kumar Sharma
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The purpose of current article focuses on polymers used in mucoadhesive drug delivery system. The term “mucoadhesive” is defined as the “attachment of drug elongated with asuitable carrier like natural or synthetic polymer to mucus and/or an epithelial surface”. It is a popular novel drug delivery system because relatively permeable of mucous membranes, and mucus have higher blood flow therefore allowing rapidly uptake of a drug into the systemic circulation. It avoid the first pass metabolism. Mucoadhesive polymers are used in various dosage forms to obtained systemic delivery of therapeutics agent through the different mucosa. The dosage forms which involve in mucoadhesive drug delivery system are tablets, semisolids patches, powders, tapes and films. The mucoadhesive polymers which are used in various dosage form are PEG, Tragacanth, Guargum, HPMC, MC, sodiumCMC, CMC and Sodium alginate etc. and having mucoadhesive property. The ideal characteristics of a mucoadhesive polymer matrix is to adhere rapidly to the mucosal layer without founding any change in the physical property of the delivery matrix. The matrix have minimum interference to the release of the therapeutic agent and should be biodegradable without producing any toxic byproducts. The polymer matrix have a capability to inhibit the enzymes which is present at the delivery site and enhance the penetration of the therapeutics agent.The objective of this reviewarticle is to design improved drug delivery systems and to study about the novel mucoadhesive polymers used in mucoadhesive drug delivery system.
Formulation and evaluation of bilayered gastro retentive floating tablets containing metformin HCl and glipizide
M. Chandrakala, P. Naga Haritha
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Bilayer tablets of Metformin hydrochloride and Glipizide were formulated. Glipizide is a poor water soluble (BCS class 2) antidiabetic drug. The present study aims to increase the solubility of Glipizide by solid dispersion technique using sodium starch glycolate and crospovidone as super disintegrants. Metformin hydrochloride was formulated by using Hydroxy Propyl Methyl Cellulose as the matrix forming polymer and was directly compressed. The compressed bilayer tablets were evaluated for all required parameters. It was found that the optimized formulation showed 99% release for Metformin hydrochloride in 24 hours. However, Glipizide released 97% at the end of 60 minutes. The IR spectrum studies revealed that there is no disturbance in the principal peaks of pure drugs alone as well as with the excipients. The stability studies were carried out for the optimized batch for three months and it showed acceptable results. The kinetic studies of the formulations revealed that diffusion is the predominant mechanism of drug and release follows Korsemeyer- peppas diffusion model.
A novel drug delivery system designed for modulating the release kinetics of anti-tubercular drugs
B. Prasanthi, D. Prasanthi, B. Bhavani, J. Vijaya Ratna
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The major clinical issue with TB therapy is the poor oral bioavailability of rifampicin in the presence of isoniazid in acidic medium. The present work was undertaken to develop a novel solid dosage form (tablet and capsule in capsule) comprising a immediate release rifampicin tablet, effervescent gastro retentive rifampicin tablet and an enteric coated isoniazid capsule that can differentiately release rifampicin in a controlled manner in the stomach and isoniazid in the intestine. Rifampicin GRDDS was formulated using different concentrations of HPMCK4M and HPMCK100M as matrixing agent. Enteric coated isoniazid capsule was formulated using eudragit L100-55. Drug release and drug degradation of the novel dosage form was compared with R-Cinex. About 42% of rifampicin was degraded to 3FRSV from R-Cinex at the end of 60 mins whereas only 10% of rifampicin degraded in case of novel dosage form. Hence, the minimization of contact between rifampicin and isoniazid by sustaining the release of rifampicin can alleviate its degradation to a certain extent.
A sensitive dual-run hptlc technique for simultaneous estimation of metformin hydrochloride, glimepiride and voglibose in combined dosage form
S. M. Sandhya, U. Fathima Beevi, G. Babu
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A sensitive, selective, and precise high performance thin layer chromatography (HPTLC) based on dual-run technique has been developed for the simultaneous estimation of metformin (MET), glimepiride (GLI), and voglibose (VOG) in combined dosage form. Chromatographic separation was performed on aluminium plates precoated with silica gel 60 F254 as the stationary phase. A dual run technique was adopted for better resolution amongst all three drugs with solvent system initially toluene-methanol-ethyl acetate-formic acid (3:4:3:0.5, v/v/v/v) for separation of metformin. The plates were dried and developed again using another mobile phase system consisting of toluene-ethyl acetate-formic acid (5:5:1, v/v/v) for glimepiride and voglibose. Densitometric scanning was carried out in the absorbance mode at 254 nm. The linear regression data for calibration plots showed good linear relationship in the concentration range of 200-1200 ng/band for MET, 20-120 ng/band for GLI and VOG. The method was validated for precision, accuracy, robustness and recovery as per ICH guidelines and applied for quantification in their available combined pharmaceutical dosage form. Consider the merits of dual-run mode and sensitivity, the proposed method would be novel for the determination of MET, GLI and VOG.
Formulation and In Vitro Evaluation for Sun Protection Factor of Cosmos Sulphurus Flowers (Asteraceae) Extract Sunscreen Cream
Shantanu kale, Kapil Kulkarni, Khanderao Jadhav
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Cosmos Sulphurus(Asteraceae) flowers commonly known as Sonkusum flowers were explored to find flavonoids, so, thin layer chromatography was performed and some of the flavonoids were identified.The reported flavonoids were known to have sunscreen activity and hence SPF factor of the dried flower extract (aqueous) was incorporated in topical formulation and evaluated in vitro with the help of Optometric Model-290 SPF.. The aqueous extract prepared from flower of cosmos sulphurus was used for Thin Layer Chromatography and then into topical formulation. In vitro determination of SPF was done with the help of method specified by The Comité de Liaison de la Parfumerie in Europe (COLIPA). The SPF was found to be 1.93 and Boots Star rating as 3, indicating that Cosmos Sulphurus(Asteraceae) flower extract (aqueous) can be considered as good candidate for Sunscreen or as an additive in any other sunscreen formulation.
Role of statistics in quality by design product development for pharmaceutical industry: a review
S. A. Kale, Dr. V. H. Bajaj
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Pharmaceutical industry is showing a positive approach towards Quality by Design (QbD) for discovery, development, and commercial manufacturing of biopharmaceutical products. Regulatory agencies are providing various guidelines for pharmaceutical industry to build quality, safety and efficacy into their new biopharmaceutical products. Such concept became known as Quality by Design. To assess the Quality by Design (QbD) product development till robust quality manufacturing, several statistical tools may used. This paper outlines the role of statistics in monitoring, evaluation, optimization and improvement of Quality by Design Product Development for Pharmaceutical Industry.
Formulation & evaluation of muccoadhesive buccal patches for delivery of atenolol
Neha krishnarth, Navneet verma, Basant Sharma
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Mucoadhesive buccal patches of Atenolol for local delivery of the drug to the oral cavity were formulated by Solvent casting technique. Mucoadhesive polymer, namely sodium carboxymethyl cellulose (NaCMC) of different grade were incorporated into the patches to modify their mucoadhesive properties as well as the rate of drug release, using glycerol as plasticizer. Different concentrations of polymer were used for the preparation of patches. The patches were evaluated on the basis of their physical characteristics like surface pH, folding endurance, mucoadhesive performance, and release rate. The in-vitro drug release was carried out in Franz diffusion cell, with commercially available dialysis membrane. Formulation P-10 (10 % Sodium carboxy Methyl Cellulose (NaCMC), 5 % glycerol and 2 % Atenolol) showed sustained release upto 10 hours.
Anti-angiogenic activity of natural flavonoid myricetin on chick chorioallantoic membrane (CAM) in-vivo
Thamilarashi A.N, Mangalagowri A, Winkins Santosh
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Myricetin is a natural flavonol, it possesses anti-oxidative, anti- proliferative and anti- inflammatory effects. The anti-angiogenic activity of Myricetin was studied using Chick Chorioallantoic Membrane (CAM) in-vivo. The Chick embryos were treated with Myricetin, upto 100µM of concentration there was no morphological changes. Higher than 100µM of concentration inhibited the formation of blood vessles but the concentration of 200µM caused lethality. Myricetin inhibited the neovascularisation in a dose-dependent manner in in-vivo. Histological crosssections of Myricetin treated CAM revealed reduced large and small newly synthesized blood vessels. Treated embryos with Myricetin (100µM, 150µM and 200µM) significantly down- regulated the expression of VEGF-A with Real time PCR method. Our result showed that Myricetin inhibited the growth of newly formed blood vessels in chicken embryos and down regulated the expression of VEGF-A. This study reveals that the potential antiangiogenic effect of Myricetin proves its role as a therapeutic agent against proliferative like cancer.
Methotrexate induced hepatitis-A case report
Dinesh R, SreeNagavalli K, Moulya M.V, Languluri Reddenna, Yogananda R, Bharathi DR
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Methotrexate is a folic acid antagonist with cytotoxic and immunosuppressant activity. Drug-induced liver injury is greatly variable in the nature of reactions seen and individual patient susceptibility. Here we report a case of hepatitis which was induced by methotrexate, have been rarely implicated in the causation of hepatitis. 55 years old man was visited to dermatology with pain in the mouth, throat, and abdomen of 2 days duration leading to a diagnosis of drug induced hepatitis. The differential diagnosis (psoriasis) was found in the documents provided by the patient, he was prescribed methotrexate. Cutaneous examination showed skin lesions over the scalf, abdomen, upper & lower limbs. He was administered intravenous fluids, folic acid, antibiotic, ondansetron, paracetamol, Syp. Muconine Gel. This adverse reaction is dose-related and can be labeled as Type-A class of adverse effect. Most drug hepatotoxicity is facilitated by a phase I toxic metabolite, but glutathione depletion, barring inactivation of harmful compounds by glutathione S-transferase, can contribute as well. The magnitude of the elevations and the enzymes involved depend on the offending agent and the severity and stage of the liver damage. The most important step that can be taken in a suspected clinically significant drug-induced liver injury is discontinuation of the offending agent.
In vivo studies of (Z)-1-benzhydryl-4- cinnamylpiperazines as anti-inflammatory and analgesics
S Shivaprakash, Anaxee Burman, Latha Diwakar and G. Chandrasekara Reddy
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Benzhydryl cinnamyl piperazine drugs such as cinnarizine, flunarizine and clocinizine are being used as antihistamines and as calcium channel antagonists but possess E-geometry. The present study was designed to evaluate and compare anti-inflammatory and analgesic activities of (Z)-1-benzhydryl-4- cinnamylpiperazine derivatives (2a-c) with their E counterparts in-vivo using Swiss-albino mice. The results of the present study revealed that the Z-isomers have showed moderate to significant analgesic and anti-inflammatory action in a dose dependent manner. However, Z-counterpart of flunarizine exhibited remarkable analgesic property and also showed prolonged antiinflammatory activity compared to flunarizine.
Evaluation of antioxidant activity in fruit extracts of Avicennia Marina L and Avicennia Officinalis L
N. Sharief Mohammad, A.Srinivasulu, P. Satya Veni and Uma Maheswara Rao V
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Antioxidant activity of Avicenni marina L and Avicennia officinalis L fruit extracts in ethyl acetate, acetone, methanol and ethanol were studied by ABTS, CrO5 and FRAP method. All the extracts possessed significant amount of the antioxidant activity, extracts in methanol and ethanol was demonstrated convincingly higher antioxidant activity by all the three methods. Whereas, the ethyl acetate exhibited less antioxidant activity. The present study reveals the potential of fruit extracts of Avicennia marina L and Avicennia officinalis L with antioxidant principles.
Evaluation of Antidepressant Activity of Bacopa Monnieri in Mice
Pabba Sindhu, Mukta N. Chowta, Nishith RS, Seema Rai, Akash Gadgade, Rajeshwari S
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This study was planned with the objective of evaluating antidepressant activity Bacopa monnieri (Brahmi), a traditional Ayurvedic medicine, in two experimental models of depression in mice. Adult Albino Mice (Swiss Strain) of either sex randomly assigned to four groups of six mice each. Group 1 received distilled water and group 2 received imipramine 10mg/kg orally. Group 3 & 4 received B. monnieri extract at a dose of 50mg/kg and 100mg/kg respectively (orally). Mice were subjected to forced swim test and tail suspension test. Drugs were given one hour before the experiment in acute study whereas for chronic study drugs were given for 10 days. The decrease in immobility period in the group pretreated with imipramine as compared to control was highly significant in both acute and chronic study with forced swim test. Comparison of both the doses of Bacopa monneiri with control group also showed very high statistical significance in acute as well as chronic study. In tail suspension test, the decrease in immobility period in the group pretreated with imipramine as compared to control was significant in both acute and chronic study. Comparison of Bacopa monneiri 50mg/kg with control group did not show statistical significance in acute study, but the significant difference was demonstrated in chronic study. Comparison of Bacopa monneiri 100mg/kg with control group also showed statistical significance in acute as well as chronic study. Bacopa monneiri has demonstrated significant antidepressant activity in both the models and the effect is dose dependent. Its antidepressant effect is comparable with imipramine especially at 100mg/kg dose.
Interaction between clopidogrel and proton pump inhibitors: A clinical overview
Jinesh B. Nagavi*, B.M. Gurupadayya
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Most proton pump inhibitors inhibit the bioactivation of clopidogrel to its active metabolite. The clinical significance of this drug interaction is unknown. Over recent years there has been much debate about whether some or all proton pump inhibitors might reduce the effectiveness of clopidogrel because of a drug interaction at the cytochrome P450 2C19 enzyme. Clopidogrel is a prodrug that is metabolized to an active form, and this process occur primarily via cytochrome P450 2C19. Proton pump inhibitors inhibit cytochrome P450 enzyme to varying degrees, and the studies showed that the combined use of clopidogrel with omeprazole or lansoprazole leads to reduction in activity of clopidogrel as measured by platelet aggregation and associated biomarkers. This suggests that there is a potentially important pharmacokinetic interaction between these drugs when used at therapeutic doses. Evidence to date has been conflicting; some studies have observed an increased risk of vascular events in patients receiving clopidogrel and proton pump inhibitors, while others, including an underpowered randomized trial, found no increased risk.
Development and validation of RP-HPLC method for the simultaneous estimation of naproxen sodium and esomeprazole magnesium in pharmaceutical tablet dosage form
T. Rupini, V. Uma Maheshwara Rao and Muhammad Rafi Shaik
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A simple, rapid, specific, accurate and precise reverse phase high performance liquid chromatographic method was developed for the simultaneous estimation of Telmisartan and Indapamide in tablet dosage form. An XBridge C18 column having (100x4.6mm, 5µ) in Isocratic mode with mobile phase containing Acetonitrile:Buffer(65:35) was used. The flow rate was 1.0mL / min and eluents were monitored at 210 nm. The retention times of Telmisartan and Indapamide were 5.268min and 2.366min respectively. The calibration curves were linear over a concentration range from 100-600 ppm for Telmisartan and over a concentration range from 3.75-22.5 ppm for Indapamide. Limit of detection (LOD) and Limit of quantification (LOQ) were 2.23 and 6.77 for Telmisartan and 0.32 and 0.98 for Indapamide respectively. The developed method was fast, accurate, precise and successfully applied to estimate the amount of Telmisartan and Indapamide in bulk sample and tablet dosage form so it can be used for regular quality control of the drug..
Synthesis and evaluation of quinazolinthione derivatives as antibacterial agents
Indubhushan, Alka N. Choudhary, Preeti Kothiyal
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Quinazolinthione is a heterocyclic compound with a unique place in the field of medicinal chemistry. The comprehensive study summaries the different derivative of quinazolinthione derivative along with their chemistry, evaluated for their antibacterial activity. The structures of all newly synthesized compounds were confirmed by FTIR, Mass spectroscopy, 1HNMR spectral data. The synthesized compound were screened for antibacterial activities (500 μg,1000µg) against (both Gram +ve and Gram –ve) Escherichia coli, Pseudomonas aeruginosa.
Synthesis and evaluation of 2-substituted thiadiazole Schiff bases
Chaitanya G, Jhansi G, Susmitha B, P.V. Naveen, K. N. V. Chenchu Lakshmi, B. Anupama
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A series of 1, 3, 4-thiadiazole schiff bases were synthesized and characterized by IR and 1H NMR, 13C NMR spectral data. The compounds were evaluated for antibacterial activity against gram-positive and gram-negative bacteria. Insilico screening was carried aiming to present potential selective activities as enzyme inhibitors and kinase inhibitors. These activities were suggested by the score values using molinspiration cheminformatics program.
Formulation and evaluation of simvastatin buccal adhesive tablets
Revathy Krishnan, T.N.K Suriyaprakash, Sheron Joseph
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The objective of the study was to develop buccal adhesive tablets of Simvastatin using mucoadhesive polymers. Simvastatin has short biological half-life (3hr), high first-pass metabolism and poor oral bioavailability (5%), hence an ideal candidate for buccal delivery system. The tablets were prepared by direct compression technique using xanthan gum, guar gum, chitosan and aloe gum. Aloe gum was extracted from Aloe Barbadensis miller leaves. Formulations were evaluated for weight variation, hardness, friability, drug content, swelling studies, determination of mucoadhesive strength and in vitro release studies. FTIR studies show no evidence on interaction between drug, polymers and other excipients. In vitro drug release studies revealed that release of Simvastatin from different formulations varies with characteristics and composition of polymers. Formulation F3 selected as optimized formulation based on physicochemical parameters, and in vitro release rates and follows zero order drug release. Chitosan and guar gum were helpful for controlling the drug release in better way when used in proper combinations. The results indicate that suitable bioadhesive buccal tablets for Simvastatin with controlled drug delivery could be prepared.
Formulation and evaluation of fairness serum using polyherbal extracts
Shan Sasidharan, Pyarry Joseph, Junise
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Cosmetic Serum is a highly concentrated product based on water or oil. When using concentrates we get not only a quick cosmetic effect, but also psychological satisfaction after the treatment because the result will be seen practically immediately. Serum has a property of rapid absorption and ability to penetrate into the deeper layers of the skin, together with its non-greasy finish and intensive formula with a very high concentration of active substances. Based on these properties, the aim of this work was to formulate a fairness serum using poly herbal extracts. The objective was to carry out extraction, and to study the phyto-constituents responsible for the fairness action in the poly herbal extract and to evaluate various physicochemical and biological properties of the formulation. The fairness Serum has a super-special blend of active natural ingredients to penetrate skin‟s epidermis and color cells, resulting in fair complexion and skin tone in addition. It has skin smoothing ingredients to improve skin texture and leaves skin soft, fair and silky smooth. It is made of extracts of Glycyrrhiza glabra, Crocus sativus, Rice branand olive oil in addition. The variousphysical, chemical and biological evaluations were done. The formulationwas found to be of good spreadability and was free from heavy metals. Skin irritation studies proved that it was non-sensitizing and free to use. It is intended to provide fairness action within a week.
Development and validation of RP-HPLC method for the simultaneous estimation of naproxen sodium and esomeprazole magnesium in pharmaceutical tablet dosage form
Srinivas Ampati, SunithaLagishetti, Agaiah Goud Bairi
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An isocratic RP-HPLC method was developed and validated for the Simultaneous estimation of Naproxen sodium and Esomeprazole magnesium trihydrate in Pharmaceutical tablet dosage form. The separation was achieved by using a reversed-phase C18column(Thermo eletrole, ODS, 250mm × 4.6 mm i.d, 5μm) at ambient temperature with mobile phase consisting of Phosphate buffer (pH adjust to 3.8using OPA): Acetonitrile : Methanol (30:50:20v/v). The flow rate was 1.0 ml/min. Detection was carried out at a wavelength of 220 nm. Retention time of Naproxen sodium and Esomeprazole magnesium trihydrate were found tobe2.417 and 3.903min respectively. The proposed method was validated for selectivity, precision, linearity and accuracy. The assay method was found to be linear from 75-175µg/ml and 3-7µg/ml for Naproxen sodium and Esomeprazole magnesium trihydrate respectively. All validation parameters were within the acceptable range. The developed method was successfully applied to estimate the amount of Naproxen sodium and Esomeprazole magnesium trihydrate in Pharmaceutical tablet dosage form.
Assessment of drug prescription practice using who prescribing indicators in Felege Hiwot referral hospital (FHRH) outpatient department, North Ethiopia
Laychiluh Bantie
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Drug therapy is the most commonly used method of any disease treatment in general practice. However, the patterns of drug prescription are often inappropriate and the need for registration and evaluation of these patterns is essential in an effort to improve prescription standards. Cross sectional retrospective study was used. Prescriptions were selected by using simple random sampling technique from accumulated prescriptions over a period of six months (May 2013 to October 2013). The Data was evaluated using standardized World Health Organization prescription indicators for studies of rational drug use. Data was collected from prescriptions by using pre-prepared data collection tool. The average number of drugs per encounter was 1.83; with 97.4% drugs prescribed by generic names. 38% & 10.8% of the prescriptions contained encounters with antibiotics and injections use respectively. 100% of drugs prescribed were from the essential drugs list of Ethiopia. It is concluded from the study that the number of drugs prescribed per encounter, prescribing practices for injections, generic prescribing and prescribing from essential drug list are encouraging, whereas prescribing practices for antibiotic need to be regulated closely since study shows deviation from the standard recommended by World Health Organization guideline.
Social Networking Experiences on Facebook pertaining to Accountability and E-Professionalism: A future perspective
Wajiha Iffat, Sadia Shakeel, Saima Naseem, Abdur Rasheed
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The present study was planned to investigate students‘ Facebook activity and opinions regarding accountability and e-professionalism. A cross sectional study was conducted from Oct‘2013 till Jan‘2014. The study population includes the students enrolled in MBBS, BDS and Pharm.D program belonging to different institutes of Karachi. Descriptive statistics were determined to illustrate participant‘s characteristics and their response to the questionnaire items, following a presentation regarding potential e-professionalism issues with Facebook. Logistic regression model was used to evaluate the association of gender, institute and bachelor program of students with their response. It revealed that 84.2% of the students were aware of the privacy settings available in Face book and 81.8% uses them to limit public access to their information. Male students belonging to private sector are more likely aware of privacy settings available in Facebook. It is necessitating for young generation to be more aware of online professionalism for gearing up their careers as healthcare providers.
Antitumor activity of Moringa Oleifera leaf extract against Ehrlich solid tumor
Wagdy K. B. Khalil, Inas S. Ghaly, Kawthar A. E. Diab, Aida I. ELmakawy
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Moringa oleifera Lam (Moringaceae) is promising plant for biomedicine applications because it has an impressive range of medicinal purposes with high nutritional value. Therefore, we investigated the therapeutic effect of Moringa oleifera leaf extract (MOLE) on Ehrlich\'s solid tumor implanted mice (EST-mice). Swiss male albino mice were implanted intramuscularly with Ehrlich ascites carcinoma (EAC). Three doses of MOLE extract (125, 250 and 500mg kg-1 ) were administrated to EST-mice for 14 days. The standard drug vincristine (VCR) was i.p injected (0.1 mg kg1- ) after the implantation of EST. The antitumor activity of MOLE was assessed using several tumor markers. Modulating activity of MOLE against EST was evaluated using comet assay, micronucleus test and morphological apoptotic changes as well as DNA fragmentation assay. The expression analysis of the inducible nitric oxide synthase (iNOS), vascular endothelial growth factor (VEGF) and apoptosis related genes (p53, p21 and bcl2) were evaluated. Treatment of EST-mice with the highest dose of MOLE exhibited inhibition of tumor growth and the tumor markers in solid tumor. MOLE inhibited the apoptotic/necrotic cells, decrease of micronucleus formation and DNA damage in EST-mice. Expression of iNOS, VEGF, p53 mutation, p21 and bcl2 genes in EST-mice were significantly over-expressed compared with control group. These observations were markedly inhibited with the highest dose of extract. Moringa oleifera leaf extract revealed antitumor, antigenotoxic and anticytotoxic activities in EST-mice. The biological activities of Moringa oleifera leaf extract were discussed
Adverse drug reaction following mass drug administration during the program to eliminate lymphatic filariasis in banke district, Nepal
Upreti AR, Joshi D, Rijal B, Bharati L, Regmi BM
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This study aimed to find out types of adverse drug reaction following mass drug administration during the program to eliminate lymphatic filariasis in Banke distict of Nepal.The retrospective study of the prescription of the patient with the history of adverse drug reaction was done .The totals of 602 patient were reported to have adverse drug reactions after intake of medication against filariasis under mass drug administration program. Nausea, Vomiting, Abdominal pain, Fever, Diarrhoea, Malaise, Asthenia ,Angioedema , Dermatitis, Hydrocoel , Itching, Dyspnoea , Syncope, Convulsion, Anxiety were different types of adverse drug reactions reported during my study. Ethnic variation in adverse drug reactions was also studied which shows disadvantage non dalit terai caste group had highest reported cases of adverse drug reactions followed by religious minorities.
Evaluation of in vitro antibacterial activity of Mentha Longifolia extracts
Muhammad Ibrar, Hina Nazir, Kosar Tammana, Jehangir Khan, Palwasha, Aiman Zafar, Ume Roman, Imran Aman, Muhammad Akif, Abid Hussain, Azam Hayat, Mujaddad-ur-rehman
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The aim of the current study is to investigate the antibacterial activity of Mentha Longifolia extract against commonly encountered pathogenic bacteria. The principle focus is on naturally occurring substance and their derivatives especially flavonoids present in plants which are reported to possess good antibacterial activity. The extracts were tested for antibacterial activity against different selected bacteria by disk diffusion method. The results showed that the cold water flower extract exhibited a relatively strong antimicrobial activity against both gram positive and gram negative bacteria tested. The ethanolic extract of M. Longifolia also showed good antibacterial activity against both gram positive and gram negative. E. coli was the most sensitive bacteria among all and E. faecalis was recorded as most resistant bacteria. Present study reveals significantly higher broad-spectrum antibacterial activity of M. Longifolia and such findings could be considered a valuable support in the treatment of UTI and respiratory tract infections.
Chemical and photochemical behavior of progesterone hybrids with antiviral activity
Manal M.T. El-Saidi, Maher A. El-Hashash, Nahid Y. Khaireldin
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The reaction of progesterone 1 with different aromatic aldehydes refluxed in absolute ethanol in the presence of sodium hydroxide afforded new progesterone chalcone hybrids (2a-e). Chalcone progesterone 2b reacted with (cyclohexyl amine, o-anisidine and p-toluidine) in boiling absolute ethanol to yield the corresponding adducts (3, 4 and 5). Treatment of 2b with (2-aminothiophenol) gave the adduct 6. Hetero-aryl chalcones (2d,e) were exposed to UV lamp (125w) in the presence of benzene yielded cyclobutane derivatives (7a,b). Compound 2d,e were irradiated in ethanol a pinacol dimeric products were obtained 8a,b. The antiviral of some newly products were examined.
Investigation of essential oil of melissa officinalis for acute and sub-chronic oral toxicity
Amina Bounihi, Rachad Alnamer, Ghizlane Hajjaj, Yahia Cherrah, and Amina Zellou
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This study is aimed at determining the acute and Sub-chronic oral toxicity of Melissa officinalis essential oil and to serve as criteria to recommend the ethno pharmacological uses of the plant. In the acute toxicity test, oral administration of 300 and 2000mg/kg of the Melissa officinalis essential oil was evaluated in mice. Sub-chronic toxicity was studied by daily oral dose of 100 and 200mg/kg for three month. On day 0, 30, 60 and 90, blood samples collected from retro-orbital sinus of the eye rats were used for evaluation of serum biochemistry, hematology and histopathological examination of the heart, lungs, liver, kidney and spleen. The acute toxicity oral study revealed no observable signs of toxicity. In rats, the examination of signs, animal behavior and the changes in body and organs weights showed no abnormalities in the test groups as compared to the controls. There were no significant variations in the hematological parameters of both Melissa officinalis essential oil treated and untreated rats. However, biochemical parameters showed significant decrease in blood sugar. Melissa officinalis essential oil significantly (p<0.05) increased serum urea suggesting degenerative changes in the kidney. We can conclude that, Melissa officinalis essential oil is well tolerated in short term therapies but may have long term toxic effects on the kidney.
In-Vitro Activities of Linezolid and Co-Trimoxazole against Isolates of Diverticulitis: Breakpoint Determinations
Samiullah Burki, Zeba Gul Burki, Javeid Iqbal, Ahmad Khan, Muhammad Nadeem
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Diverticulitis is a common colon disease with pouch like projection which leads to morbidity and mortality commonly cause by E.coli and P. aeruginosa.15 isolates of MDR E.coli and P. aeruginosa derived from patient of diverticulitis were identified using biochemical tests and EMB media. Their susceptibility, resistance, and MIC values were calculated using standard agar dilution method against Linezolid (linz) and co-trimoxazole (co-tri). Results revealed that at different concentrations (conc.) 0.5, 1, 2, 4, 8, 16mgl–1, 1, 2, 4, 16, 32, and 64mgl–1 of linz and co-tri respectively. Linz and co-triMIC90 against E.coli was achieved ≥ 16mgl–1 and >64mgl–1(P<0.01)respectively while against P.aeruginosaMIC90wasachieved at 2.25mgl–1 and > 64mgl–1 respectively (P<0.01). At maximum conc. of 16mgl–1 and 64mgl–1 of linz and co-tri87.5 % and 75 % pathogens of E.coli were susceptible. P .aeruginosa at similar conc. gives 100 % and 71.42 % susceptibility (P<0.01).It is conclude that linz against current multidrug resistance (MDR) pathogens of diverticulitis was potent than co-tri.
Hypolipidemic efficacy of hyphaene thebaica (doum) in experimental nephrotic syndrome
Dawoud Fakhry Habib, Helana Naguib Michael, Josline Yehia Salib, Nadia Mohammed Ahmed, and Mervat Harvi Agaibyi
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The water extract of the fruits of Hyphaene thebaica were given orally to male albino rats for 30 days to evaluate its effect on serum cholesterol, triglycerides, lipoproteins: HDL - LDL & VLDL (high - low and very low density lipoprotein) and apolipoproteins (A-1 & B). Our findings exhibited a highly significant decrease (p < 0. 05) in all parameters except for HDL which showed insignificant decrease when compared to control group. Thus the water extract can reduce hyperlipidemia in nephrotic syndrome and leads to decrease the risk of glomerulosclerosis atherosclerosis and consequently the natural, safe and non-toxic Hyphaene thebaica fruit could be of great merit for use as hypolipidemic drug. Further, the phytochemical analysis of the potent water extract indicated the distribution of 14 polyphenolic compounds to which its activity maybe attributed. Among the isolated compounds tricin 5-O-rutinoside, kaempferol 3-O-rutinoside and rhamnazin 3-O-rutinoside were isolated, purified and identified from the fruit for the first time. The structure elucidation was based on 1H and 13C NMR.
Multidrug resistant tuberculosis (MDR-TB): A lethal risk in Benghazi City, Libya
Mohamed F. Abbar; Yousef M. Sherif; Heba J. Majbri; Makarim Elfadil M. Osman and Emadeldin Hassan E. Konozy
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Anti-tuberculosis (TB) drug resistance is a major public health problem that threatens TB treatment progress made in the inhabitants of countries in Europe, Asia, Africa, and the America. A retrospective study for the pulmonary TB cases admitted to Quefia Chest Hospital Benghazi, Libya, from 1/1/2009 till 1/6/2010 showed that 4 cases out of 430 TB patients were positive for sensitivity culture and didn\'t respond to the first line anti-TB therapy and therefore were diagnosed as Multidrug Resistant Tuberculosis (MDR-TB). One of these patients was Libyan while others were aliens. The 2nd line anti-TB drugs were given in the form of Amikacin injection, cycloserine, moxifloxacin and pyrazinamide for the first 6 months followed by 18 months therapy with moxifloxacin, cycloserine and pyrazinamide. Follow-up with the patients exhibited clinical-radiological and microbiological improvement.
Pharmacokinetics study of ethyl acetate extract of cylicodiscus gabunensis (mimosaceae) after oral administration and its effect on the eradication of shigella dysenteriae infection on rats
Laure Brigitte Mabeku Kouitcheu , Joseph Lebel Tamesse and Oyono Essame Jean Louis
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Cylicodiscus gabunensis (CG) is a tropical plant traditionally known for its medicinal use. The plant has also been investigated for a number of pharmacological activities. However kinetic studies are lacking for this. Hence to better elucidate the effects of the body on this plant preparation, this study was planned. Sixty Wistar albino rats were giving orally a single dose of 500 mg/kg of plant extract. Blood samples were then collected in EDTA coated tubes prior to plant extract administration and at 10, 20, 40, 80, 160, 320, 640, 960 and 1280 minutes after. Plasma obtained was analyzed to measure concentration of plant extract using its anti-shigellosis properties. Various kinetic parameters were then calculated from the plasma concentrations. For the in vivo anti-shigellosis activity of the plant extract, a suspension of Shigella dysenteriae type I (sd1) was orally administered to thirty rats. The diarrheic rats were then divided into the control group and four others received 125, 250, 500 mg/kg of the plant extract and ciprofloxacin (20 mg/kg) respectively for 7 days. The frequency and weight of normal and diarrheic faeces emitted was recorded. The presence of stools containing mucus or blood and the number of sd1 in faeces were also recorded. The peak plasma levels (81.937 mg/ml) of CG were reached at 10.66 h. The concentration declined with a mean elimination half life of 6.61 ± 0.97 h. The AUC0-∞ was 1367.7 mg h/ml. CG reduces the frequency faeces released and sd1 density from 100% (diarrheic rats) to 50.79 and 45.33% (500 mg/kg) respectively. We concluded that CG extract is effectively absorbed though the intestinal wall. The elimination half life suggests that the drug needs to be given orally at the interval of seven hours. These parameters provide a baseline for the further exploration of what the body does to the drug and justify the pharmacodynamic correlation.
Stability indicating HPLC method for the determination of Dacarbazine in pharmaceutical dosage form
M.L. Lal Prasanth, Sridhar Siddiraju
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A simple, rapid, and precise stability indicating HPLC method is developed for the quantitative determination of dacarbazine in pharmaceutical dosage form. The chromatographic separation of dacarbazine was achieved with an agilent eclipse XDB C18, 150 x 4.6 mm, 5m particle size analytical column using buffer and acetonitrile taken in 96:4%v/v and the response was detected at 323nm by using PDA detector. The retention time was found to be 4.333. Dacarbazine drug substance was exposed to thermal, photolytic, hydrolytic, and oxidative stress conditions, and the stressed samples were analyzed by the proposed method. Peak homogeneity data of dacarbazine is obtained by photodiode array detector in the stressed sample chromatograms, demonstrating the specificity of the method for its estimation in presence of degradation product. The described method shows excellent linearity over a range of 25–150 μg/mL. The correlation coefficient for dacarbazine was found to be 0.9999. The relative standard deviation for six measurements in two sets of dacarbazine in injection is always less than 2%. The proposed method was found to be suitable and accurate for quantitative determination and stability study of dacarbazine in pharmaceutical preparations.
Innovative training program for pharmacists in the Second Xiangya Hospital of Central South University
Hoan Linh Banh, Ping Xu, Da Xiong Xiang, Andrew Cave
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Pharmacists are one of the most accessible health care providers in many parts of the world, including China. To better prepare pharmacists to provide pharmaceutical care and comprehensive care, often they are sent to train in a developed countries such as Canada. Because the health care systems are completely different between the countries, most of the pharmacists have difficulties applying their newly acquired skills and knowledge to their own health care. As a result, the Second Xiangya Hospital of Central South University agreed to second a Faculty Member/pharmacist for 8 months. The Faculty member will be at the Second Xiangya Hospital of Central South University to implement a pharmacy clinical program and a structured training program for pharmacists.