International Journal of Pharmaceutical Sciences and Drug Research

01-07

Authors: P S Yadav*, Devprakash, Senthilkumar G P

Substituted 1, 3-benzothiazole derivatives are an important class of heterocyclic compounds. In recent years heterocyclic compounds analogues and derivatives have attracted strong interest due to their biological and pharmacological properties. The benzothiazole nucleus containing compounds involved in research aimed at evaluating new products that possess biological activities, such as antimicrobial, anticancer, antifungal, anthelmintic, anti-diabetic, amyloid imagining agents and anticancer agents. The present review focus on the different methods of synthesis of substituted benzothiazoles with potential activities that are now in developing phase.

13-18

Authors: Bijay Kumar Sahoo1*, Amiya Kumar Mishra1, Tapan Kumar Pal2

The objective of the present study was, 1) to systematically device a model of factors that would yield an optimized sustained release dosage form of model drug (Ranitidine HCl), 2) to validate the models using R2 values, 3) to optimize the formulation by response surface methodology (RSM). A three - factor, three - level Box-Behnken design was used for the optimization procedure, with the amounts of HPMC K100M (X1), MCC (X2) and Compression Force (X3) as independent variables. Three dependent variables were considered: percentage of drug release at 1 h, 12 h and T50%. The regression equation obtained from experiment i. e Y2 = 92.41 + 3.18X1+ 2.05 X2 + 2.14X3 + 2.41X1X2 + 0.24 X1X3 + 0.11 X2X3 -3.82X12 - 2.59X22 -0.46X32 , explained the main and interaction effects of factors that influenced the drug release. Optimization was performed by maximizing the drug release in 12 hrs and placing constraints on Y1, Y2 and Y3. Validation of optimization by carrying out by performing 8 experimental runs showed high degree of prognostic ability of response surface methodology. The results showed that the optimized formulation provided a dissolution pattern similar to the predicted curve, which indicated that the optimal formulation could be obtained using RSM. A simple high performance liquid chromatography method was developed and the dissolution samples were analysed by this procedure.

23-28

Authors: Izhar Ahmed Syeda*, Lakshmi Narsu Mangamoorib, Yamsani Madhusudan Raoc

In the present study matrix and triple layer matrix tablets of metoprolol tartrate were formulated by using xanthan gum as the matrix forming agent and Sodium Carboxy Methyl Cellulose (Na CMC) as barrier layers. The prepared tablets were analysed for their hardness, friability, drug content and in-vitro drug release studies. Marked differences in dissolution characteristics of (M3) and (M3L3) were observed and showed a significant difference statistically. Mean dissolution time (MDT) for M3 and M3L3 were found to be 4.02h and 12.75h, while dissolution efficiency (DE8%) decreased, indicating that the release of metoprolol tartrate is slower from triple layer matrix tablets. The finding of the study indicated that the matrix tablets prolonged the release, but predominantly in a first order kinetics. Layering with Na CMC granules on the matrix core, provided linear drug release with zero order kinetics. The triple layer matrix tablets (M3L3) shows precise controlled release of the drug than that of plain matrix tablets. FT-IR and DSC studies confirmed that there was no chemical interaction between drug and excipients used in the formulation.

32-34

Authors: S. B. Dahikar1, 2*, S. A. Bhutada2, D. H. Tambekar2, S. K. Vibhute1, S. B. Kasture1

Phytochemical screening of the plant leaves reveals the presence of carbohydrates, alkaloids, flavonoids, steroids, and tannins. Petroleum ether extract, chloroform extract, ethyl acetate extract and methanol extracts of leaves of Bauhinia racemosa Linn. were prepared and antibacterial activity were studied by disc diffusion method against certain enteric bacterial pathogens such as Escherichia coli, Staphylococcus aureus, Klebsiella pneumonia, Enterobacter aerogenes, Pseudomonas aeruginosa, Salmonella typhimurium, Salmonella typhi, Staphylococcus epidermidis and Proteus vulgaris. The Methanol extracts had wide range of antibacterial activity against enteric bacterial pathogens than the petroleum ether extract, where as ethyl acetate extract were slightly higher antibacterial activity than chloroform extract. Antibacterial activity of various extract of leaves of Bauhinia racemosa was carried in attempt to develop a new pharmaceutical drug from natural origin for prevention of enteric infection.

38-41

Authors: CH Ravikanth1, A Anil Kumar1*, V Uday Kiran1, S Prashanth2, B Madhu1, Y Narsimha Reddy1

A sensitive, accurate and rapid high-performance liquid chromatography with UV-visible detection (HPLC-UV) method for the determination of Pioglitazone in rat serum has been developed. Rosiglitazone was used as internal standard. Pioglitazone and Rosiglitazone are extracted from serum using a liquid–liquid extraction procedure using ethyl acetate. Isocratic separation of Pioglitazone and Rosiglitazone is carried out using a reversed-phase phenomenex C18 (250 mm × 4.6 mm, 5µm) column with mobile phase consisting of methanol and 30 mM ammonium acetate buffer (pH adjusted to 5 with ortho-phosphoric acid) in the ratio 60:40 (v/v) and quantified by UV detection at 269 nm. Analytical run time was less than 10 min. Mean recovery was 97.12% for 0.1-10µg/ml concentrations. The assay exhibited good linear relationship. Quantification limit was at 50ng/ml of Pioglitazone and accuracy and precision were over the concentration range of 0.1-10µg/ml. This method can be used for routine clinical monitoring of Pioglitazone.

45-47

Authors: Reecha Madaan1*, Anupam Sharma2

Actaea spicata Linn. (Ranunculaceae) has been traditionally used for the treatment of various ailments such as rheumatism, inflammation, nerve diseases, lumbago, scrofula and chorea. Despite a long tradition of use, no systematic phytochemical and pharmacological work has been carried out on this potential plant. Thus, A. spicata was subjected to preliminary anti-anxiety screening studies, with a view to ascertain the verity of its traditional use as an anxiolytic. In the present investigation, roots of the plant were extracted using solvents in order of increasing polarity viz., petroleum ether (60-80C), chloroform, methanol and distilled water. All the crude extracts were evaluated for anti-anxiety activity in mice using elevated plus maze apparatus. Among all these extracts, only methanol extract exhibited significant anti-anxiety activity at a dose of 100 mg/kg in mice with respect to control as well as standard (diazepam, 2 mg/kg). Phytochemical screening showed presence of alkaloids and polyphenols in methanol extract of A. spicata. Thus, Specific methods were adopted to extract total alkaloidal and polyphenol fractions from the plant material and methanol extract of plant, respectively. Polyphenol fraction exhibited significant anxiolytic activity at the dose of 50 mg/kg, while alkaloidal fraction was found to be devoid of any activity.

52-55

Authors: Rubesh kumar S1*, P Gayathri3, Duganath N1, Kiran CH1, Sridhar C2, Jayaveera K N1

Present work is to carry out an analytical method development and validation of Fluoxetine HCl (FLU) and Olanzapine (OLZ) in bulk drug and pharmaceutical dosage form. The developed method is based upon simultaneous equations (Vierodt’s) method by using UV/Visible spectroscopy. Both drugs come in the categories of anti- depressant and anti-psychotic agent. The developed method can be used for the simultaneous estimation of FLU and OLZ in pharmaceutical dosage form without separating from each other or from the excipients. Primarily the λ max of Fluoxetine HCl (FLU) and Olanzapine (OLZ) was determined as 226 and 258 nm respectively. The suggested method is validated by using ICH validation parameters like accuracy, precession, linearity and LOD and LOQ respectively. Accuracy study showed percentage recovery in the range of 97-102% w/w respectively. Precision studies were carried out for 6 successive absorbance and studied for their percentage relative standard deviation (%RSD) was < 2%, LOD and LOQ was studied and the limit of detection and limit of quantification were found to be was 1-100 µg/ml for Olanzapine and Fluoxetine HCl, the slope of interception Y=0.23x6+0.054 (R2 0.993) and Y=0.222x6-0.014 (R 2 0.995) respectively. Relative standard deviation for Fluoxetine hydrochloride and Olanzapine were 0.4904 and 0.53969, the co-relation coefficient were 0.997 and 0.825 respectively. This procedure was applied successfully for the analysis of FLU and OLZ in bulk drug and Pharmaceutical preparations.

62-66

Authors: S. T. Kumbhar*, G. K. Chougule, V. S. Tegeli, G. B. Gajeli, Y. S. Thorat, U. S. Shivsharan

A HPTLC method for the estimation of Nebivolol (NBV) and Hydrochlorothiazide (HCTZ) has been developed. It employs aluminum backed silica gel 60 F254 TLC plates, (20 cm × 10 cm, layer thickness 0.2 mm) pre-washed with methanol and mobile phase comprising of 1,4-dioxane: toluene: triethylamine (5:3:0.1 v/v). The developing solvent was run up to 80 mm in Camag chamber previously saturated with 10.0 ml of solvent mixture for 30 min. Densitometric scanning was then performed with Camag TLC Scanner-3 equipped with winCATS (version 1.3.0) at λ max 281 nm. The Rf values were found to be 0.75 and 0.43 for Nebivolol and Hydrochlorothiazide respectively. The limit of detection and limit of quantitation were found to be 43ng/spot & 130ng/spot for Nebivolol and 25ng/spot & 76ng/spot for Hydrochlorothiazide respectively. The % RSD of intra-day variation and inter day variation were 0.54 and 0.41 respectively for NBV and 0.46 and 0.39 for HCTZ respectively. The proposed method can also be used for routine quality control to accurately determine Nebivolol and Hydrochlorothiazide in bulk and tablet dosage form.