Search

Aim: Zolmitriptan is a 5-HT receptor agonist (1B/1D). It is used in the acute treatment of migraine having low bioavailability about 40% orally due to hepatic fi rst pass metabolism. The purpose of the present research was to formulate fast acting sublingual tablets of zolmitriptan. Materials and Methods: Sublingual tablets were prepared using ispaghula husk powder, gellan gum, sodium alginate as super disintegrating polymers and citric acid, tartaric acid and camphor as permeation enhancers by direct compressible technique and evaluated for weight variation, thickness, friability, content uniformity, hardness, disintegration time, wetting time, in-vitro drug release, in-vitro and ex-vivo permeation study. Stability study of optimized formulation was performed as per ICH (International Conference on Harmonisation) guideline. Results: The in-vitro disintegration time of the optimized formulation (D5) was 9 ± 2 s and all formulations showed 100% of dissolution within 6 ± 2 min. Formulation containing 4% of gellan gum (D5) showed highest disintegration and 2% of citric acid formulation (P3) showed highest permeation 88% within 30 min and ex-vivo permeation was 52% within 30 min. Optimized formulation was stable for 1 month during stability study as per ICH guideline. Conclusion: The sublingual tablet formulation gives better results using natural super disintegrant for fast onset of action. [ABSTRACT FROM AUTHOR]

Aim: To develop a simple, accurate, sensitive, rapid and precise method for the determination of galantamine hydrobromide in bulk drug and pharmaceutical dosage form. Material and Methods: The method employs wavelength detection and determination of galantamine hydrobromide at excitation wavelength 282 nm and emission wavelength 607 nm in a solution of simple distilled water. Result and Conclusion: The method was found to be linear in the range of 2-14 μg/ml having r2 = 0.9999. The mean accuracy was found to be 98.12% to 99.67%. The intraday and interday precision was found to be 0.18-0.35% and 0.13-0.46%, respectively. The limit of detection was found to be 0.29 μg/ml. The limit of quantification was found to be 0.89 μg/ml. The method was successfully applied for the determination of galantamine hydrobromide in bulk drug as well as pharmaceutical dosage form. [ABSTRACT FROM AUTHOR]

Introduction: A practical synthesis of pyrimidinone would be very helpful for chemists because pyrimidinone is found in many bioactive natural products and exhibits a wide range of biological properties. The biological significance of pyrimidine derivatives has led us to the synthesis of substituted pyrimidine. Materials and Methods: With the aim of developing potential antimicrobials, new series of 5-cyano-6-oxo-1,6-dihydro-pyrimidine derivatives namely 2-(5-cyano-6-oxo-4-substituted (aryl)-1,6-dihydropyrimidin-2-ylthio)-N-substituted (phenyl) acetamide (C1-C41) were synthesized and characterized by Fourier transform infrared spectroscopy (FTIR), mass analysis, and proton nuclear magnetic resonance (1H NMR). All the compounds were screened for their antifungal activity against Candida albicans (MTCC, 227). Results and Discussion: Quantitative structure activity relationship (QSAR) studies of a series of 1,6-dihydro-pyrimidine were carried out to study various structural requirements for fungal inhibition. Various lipophilic, electronic, geometric, and spatial descriptors were correlated with antifungal activity using genetic function approximation. Developed models were found predictive as indicated by their square of predictive regression values (r2 pred) and their internal and external cross-validation. Study reveals that CHI_3_C, Molecular_SurfaceArea, and Jurs_DPSA_1 contributed significantly to the activity along with some electronic, geometric, and quantum mechanical descriptors. Conclusion: A careful analysis of the antifungal activity data of synthesized compounds revealed that electron withdrawing substitution on N-phenyl acetamide ring of 1,6-dihydropyrimidine moiety possess good activity. [ABSTRACT FROM AUTHOR]

The purpose of this research was to prepare a floating matrix tablet containing domperidone as a model drug. Polyethylene oxide (PEO) and hydroxypropyl methylcellulose (HPMC) were evaluated for matrix-forming properties. A simplex lattice design was applied to systemically optimize the drug release profile. The amounts of PEO WSR 303, HPMC K15M and sodium bicarbonate were selected as independent variables and floating lag time, time required to release 50% of drug (t50) and 80% of drug (t80), diffusion coefficient (n) and release rate (k) as dependent variables. The amount of PEO and HPMC both had significant influence on the dependent variables. It was found that the content of PEO had dominating role as drug release controlling factor, but using suitable concentration of sodium bicarbonate, one can tailor the desired drug release from hydrophilic matrixes. The linear regression analysis and model fitting showed that all these formulations followed Korsmeyer and Peppas model, which had a higher value of correlation coefficient (r). The tablets of promising formulation were found to be stable for 3 months under accelerated (40°C / 75% RH) stability testing. [ABSTRACT FROM AUTHOR]

Objective: A simple, precise and accurate isocratic reversed phase (RP) column high-performance liquid chromatographic (HPLC) method has been developed for simultaneous analysis of eprosartan (EPR) and hydrochlorothiazide (HCT) in tablet formulations. Materials and Methods: Isocratic RP-HPLC separation was achieved on phenomenex C18 column (250 x 4.6 mm i.d., 5 µm particle size) using mobile phase composed of 0.5% formic acid-methanol-acetonitrile [(80 : 25 : 20 v/v/v) pH, 2.80 ± 0.04] at a low rate of 1.0 ml/min. The retention time for EPR and HCT was 7.69 ± 0.10 and 4.24 ± 0.09 minutes, respectively. The detection was performed at 272 nm. Results: The method was linear in the concentration range of 60-600 µg/ml for EPR and 2.5-25 µg/ml for HCT with a correlation coefficient of 0.9992 and 0.9997, respectively. The repeatability for six samples was 0.53 and 0.61 % RSD for EPR and HCT, respectively. The accuracy (recovery) was found to be in the range of 99.46 to 100.61% for EPR and 99.06 to 100.93% for HCT, respectively. Conclusions: The method was validated and successfully used for determination of the drugs in tablets. [ABSTRACT FROM AUTHOR]

The purpose of this research was to prepare a floating matrix tablet containing domperidone as a model drug. Polyethylene oxide (PEO) and hydroxypropyl methylcellulose (HPMC) were evaluated for matrix-forming properties. A simplex lattice design was applied to systemically optimize the drug release profile. The amounts of PEO WSR 303, HPMC K15M and sodium bicarbonate were selected as independent variables and floating lag time, time required to release 50% of drug (t50) and 80% of drug (t80), diffusion coefficient (n) and release rate (k) as dependent variables. The amount of PEO and HPMC both had significant influence on the dependent variables. It was found that the content of PEO had dominating role as drug release controlling factor, but using suitable concentration of sodium bicarbonate, one can tailor the desired drug release from hydrophilic matrixes. The linear regression analysis and model fitting showed that all these formulations followed Korsmeyer and Peppas model, which had a higher value of correlation coefficient (r). The tablets of promising formulation were found to be stable for 3 months under accelerated (40°C / 75% RH) stability testing.

Background & Objectives: The aim of the present study is to investigate the physicochemical equivalence of seven brands of tablets containing chloroquine phosphate, an antimalarial purchased from different retail pharmacy outlets., Methods: The quality and physicochemical equivalence of seven different brands of chloroquine phosphate tablets were assessed. The assessment included the evaluation of uniformity of weight, friability, crushing strength, disintegration and dissolution tests as well as chemical assay of the tablets., Results: All the seven brands of the tablets passed the British Pharmacopoeia (BP) standards for uniformity of weight, disintegration and crushing strength. One of seven brands failed the friability test. One of the brands did not comply with the standard assay of content of active ingredients. Dissolution test passes the pharmacopoeial standards for chloroquine phosphate tablets. There were no significant differences in the amounts of chloroquine phosphate released from the different brands., Interpretation & Conclusion: Out of the seven brands of anti-malarial chloroquine phosphate tablets only one brand fails to meet BP quality specifications which shows constant market monitoring of new products to ascertain their equivalency to pharmacopoeial standards.