Posted by admin on Jun 1, 2011 in |
Cyclocondensation of α-bromo ketones with thiourea afforded 4-substituted 1, 3-thiazole-2-amines. These compounds on further treatment with α-bromo ketones afforded 3, 6-disubstituted imidazo[2, 1-b][1, 3]thiazole (1a-1j). All the synthesized compounds were confirmed for their structure by FTIR, 1H NMR and GSMS spectra and tested in vitro for their anti-microbial activity by cup plate method against Gram-positive bacterial strains (Bacillus subtillis, Staphylococcus aureus) Gram-negative bacterial strains (Pseudomonas aerugenosa, Kleibsella pneumonia) and fungal strains (Aspergillus niger, Candida albicans). The analogues 1b, 1h and 1i showed promising antimicrobial activity against gram-negative Kleibsella pneumonia; where as analogues 1b, 1e, 1g and 1h showed promising antifungal activity against Candida...
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Posted by admin on Jun 1, 2011 in |
Gliclazide is a second-generation hypoglycaemic sulfonylurea that is useful in the treatment of Type 2 diabetes mellitus. It shows low aqueous solubility and dissolution rate and often shows low and irregular bioavailability after oral administration. This paper describes an approach to improve the Solubility of gliclazide by using solid dispersions (SDs) in polyethylene glycol 4000 (PEG 4000). Solid dispersions were prepared by a solvent-melting method and Solubility determinations were performed in triplicate according to the method of Higuchi and Connors. The solubility of gliclazide is 0.86 mg/ml in water but after the addition of different concentration of PEG 4000, the solubility of gliclazide is increased maximum 3.07 mg/ml at 20%w/v of PEG 4000, was observed. The main conclusion of this article is that the solubility of gliclazide can be enhanced in Solid Dispersion with PEG 4000. The solubilization effect of PEG 4000, reduction of particle aggregation of the drug, absence of crystallinity, increased wettability and dispersibility, and alteration of surface properties of the drug particles may be responsible for...
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Posted by admin on Jun 1, 2011 in |
The purpose of this research was to develop fast dissolving tablets of olanzapine and to optimize the processing variables. Tablets containing olanzapine, camphor, crosscarmellose, and directly compressible lactose were prepared by direct compression technique. The tablets were compressed and later exposed to vacuum. Sublimation of camphor from tablets resulted in superior fast dissolving tablets. The tablets were evaluated for percentage friability, wetting time, and disintegration time. In this investigation, a 22 full factorial design was used to investigate the joint influence of 2 formulation variables: amount of camphor and crosscarmellose. A checkpoint batch was also prepared to prove the validity of the evolved mathematical model. The results of multiple linear regression analysis revealed that for obtaining a rapidly disintegrating dosage form, tablets should be prepared using an optimum concentration of camphor and a higher percentage of crosscarmellose. The systematic formulation approach helped in understanding the effect of formulation processing...
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Posted by admin on Jun 1, 2011 in |
In the present study crude methanolic extract of Stephania japonica leaf was investigated for possible antioxidant, analgesic and cytotoxic activity. The extract showed antioxidant activity in DPPH radical scavenging activity, nitric oxide scavenging activity and reducing power assays. In both DPPH radical and NO scavenging assay, the extract exhibited moderate antioxidant activity and the IC50 values in DPPH radical scavenging and NO scavenging assays were found to be 105.55 ± 1.06 μg/ml and 129.12 ± 0.15 μg/ml, respectively while the IC50 values of ascorbic acid were 12.30 ± 0.11 μg/ml and 18.64 ± 0.22 μg/ml, respectively. Reducing power activity of the extract increased in a dose dependent manner. Analgesic activity of the crude extract was evaluated using acetic acid-induced writhing model of pain in mice. The crude extract at 200 mg/kg and 400 mg/kg b.w. doses displayed significant (p < 0.001) reduction in acetic acid induced writhing in mice with a maximum effect of 75.89 % reduction at 400 mg/kg b.w. which is comparable to the standard, diclofenac sodium...
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Posted by admin on Jun 1, 2011 in |
An HPTLC method for estimation of Fluoxetine in its capsule formulation has been developed. It employs aluminium backed silica gel 60 F254 TLC plates, (20 cm × 10 cm, layer thickness 0.2 mm) prewashed with methanol and mobile phase comprising of toluene: 2-propanol: ammonia 2:2:0.4 (v/v/v). The developing solvent was run upto 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 software Version 1.3.0 at λmax 227 nm. The Rf value was found to be 0.74. The recovery of Fluoxetine was found to be 99.90% ± 1.68. The limit of detection and limit of quantitation were found to be 43.55 ng/spot and 131.99 ng/spot. The % RSD of intra-day variation and inter day variation were 0.54 and 0.41...
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