Posted by admin on Dec 1, 2014 in |
This work involves synthesis of pyrazolyl thiazine derivatives from different chalcones [1(a-b)] synthesized from substituted acetophenones and different aromatic aldehydes in basic medium by Claisen-Schmidt reaction. These chalcones [1(a-b)] on condensation with different hydrazides [2(a-b)] and isothiocyanates [3(a-b)] when irradiated with microwaves (20%, 140watts) in scientific microwave oven, give different 2-phenyl-2,5-dihydro-pyrazole-1-carbothioic acid phenyl amide derivatives [4(a-g)] which on further MW assisted condensation with substituted acetophenones and different aromatic aldehydes, furnish pyrazolyl thiazine derivatives [7(a-j)]. Library of such pyrazolyl thiazine derivatives has been generated and the structures were subjected to PASS for their probabilities of being active biologically. QSAR study of the library was done to find out most active...
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Posted by admin on Dec 1, 2014 in |
The objective of present research work is to provide green technique for synthesis of 4-(4-Hydroxyphenyl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylic acid ethyl ester. Pyrimidine derivatives are well known in the pharmaceutical industry and exhibit to possess a broad spectrum of biological activities which makes their wider application as a key building block for pharmaceutical agents. Highly efficient and simple methods complying with principle of Green chemistry have been described in this manuscript for the synthesis with competent yields. As part of current studies, we here in report economical practical techniques like- microwave synthesis, mortal-pastel method (mechanochemistry) and by application of green solvents for the synthesis. On completion of reaction the products were characterized by Infra Red Spectroscopy, Nuclear Magnetic Resonance Spectroscopy and Mass Spectra. The specified methods for synthesis are more convenient and reactions can be carried out in higher yield (80-96%), shorter reaction time (3-30 min) and milder conditions, without generation of pollution and safer to...
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Posted by admin on Dec 1, 2014 in |
The aim of present research work to develop and optimize orodispersible film of baclofen to improve bioavailability and patient compliance. Orodispersible films of baclofen were prepared by solvent casting method using HPMC E5 LV as a film forming polymer and propylene glycol as a plasticizer, crospovidone as a superdisintegrant and sucralose was added as a sweetener. The physical mixture of drug and polymer characterized by FT-IR showed no incompatibility. A 32 central composite design was applied using two independent variables such as X1 (Polymer) and X2 (Propylene glycol) and folding endurance (Y1), T90% (Y2), In-vitro Disintegration time (Y3).The prepared films were evaluated for weight, thickness, folding endurance, disintegration time, in vitro drug release, drug content and their mechanical properties such as tensile strength and % elongation. From the result obtained optimized formulation was prepared with 2.58% w/v HPMC E5 LV and 2.02 % w/v of propylene glycol showed folding endurance of 68.59, disintegration time 53.4 seconds,T90% of 9.12 minutes. A stability study result reveals that there was no significant...
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Posted by admin on Dec 1, 2014 in |
ABSTRACT: The present work describes high sensitive and reproducible method of Carbidopa and Levodopa assay in Carbidopa, Entacapone and Levodopa film coated tablet. It was developed by usingkromosil C18, 125mm × 4.0mm × 5µm column, mobile phase (A) phosphate buffer pH 3.8 and, mobile phase (B) methanol and water with gradient method. Retention time of carbidopa and levodopa is 3.83 and 1.80 minutes respectively. It was evaluated for identification and quantification by using high performance liquid chromatography their separation being dependent on the pH of mobile phase. Critical resolutions between carbidopa and 3-Methoxy DL-Tyrosine (Levodopa impurity) and Levodopa impurity and Levodopa in assay method, it has been validated according to ICH Guidelines. Precision study was obtained results average of 12 sample % RSD Carbidopa 0.88 and Levodopa 0.71. And linearity was found to be (Carbidopa R2 = 0.9991 and Levodopa 0.9990). Recovery was found to be (97% to 103%). Robustness, solution stability and degradation impurities are determined by this method. Based on validation results, it is a stability indicating...
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Posted by admin on Dec 1, 2014 in |
This study was aimed to design and develop iontophoretic drug delivery of L-Tyrosine in the treatment of phenylketonuria. The In-house iontophoretic drug delivery device was designed and validation was performed respect to Current intensity, Voltage, and Power Resistance. The study was also focused various parameters such as effect of different drug concentrations (2.5mg/5ml, 5mg/5ml, 10mg/5ml, 15mg/5ml) and effect of different current intensities (0.1mA/cm2, 0.25mA/cm2, 0.5mA/cm2, 0.75mA/cm2). The results concluded there is a significant increase in Percentage of drug release in iontophoretic drug delivery of L-Tyrosine from 1-47 folds when compare to passive diffusion. The drug release increased up to certain concentration range after that if concentration increased means there is a decrease of drug release due to skin boundary saturation. Among the four drug concentrations 2.5mg/5ml,5mg/5ml showed good reliable release. 10mg/5ml, 15mg/5ml showed very less release due to saturation. Among the different current intensities the drug release increased with increase of current...
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