Posted by admin on Jun 1, 2010 in |
Reaction of 1- (1- benzyl- 1H- benzo [d] imidazol- 2- yl) hydrazine (1) with 3-aryl-1-phenyl-1H-pyrazole-4-carbaldehydes (2a-f) in ethanol yielded the corresponding Schiff bases (3a-f). Further, cyclization of compounds 3a- f with thioglycollic acid in benzene in presence of anhydrous ZnCl2 furnished desired novel compounds 3- (1 – Benzyl – 1h – Benzo [D] Imidazol – 2 – L Amino) – 2 – (3 – Aryl – 1- Phenyl – 1h – Pyrazol – 4 – Yl) Thiazolidin – 4- Ones (4a- f) in 41-65% yield. All the synthesized compounds were screened for antibacterial and antifungal activities. Among the synthesized compounds 3b, 3d, 4a and 4f have shown good activity against bacteria P. aeruginosa, S. aureus and P. vulgaris, where as other compounds have shown moderate to poor activity against all the organisms. The compounds 3a and 3c exhibited good activity against fungal strains A. niger and A. flavus. All remaining synthesized compounds exhibited moderate to poor activity against all the organisms. The structures of synthesized compounds have been established...
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Posted by admin on Jun 1, 2010 in |
Celecoxib, a selective cyclo- oxygenase – 2 inhibitor has been recommended orally for the treatment of arthritis and osteoarthritis. Long term oral administration of celecoxib produces serious gastrointestinal side effects. Therefore the aim of the present investigation was to assess the potential of nanosized emulsion formulations for transdermal delivery of celecoxib (CXB), to reduce the side effects produced by oral administration of the drug, to increase the stability and to produce a novel controlled delivery system with better pharmaceutical and therapeutic properties. Optimized oil in water nanosized emulsion of celecoxib was prepared by ultra sonication method. The prepared nano- sized emulsion was subjected to physical characterization, Drug content analysis and stability tests. Skin permeation mechanism of celecoxib from nanosized emulsion was evaluated by In-vitro skin permeation studies, activation energy measurement and histopathological examination. The anti-inflammatory effects of formulations were compared with marketed formulation by carrageenan-induced paw edema in rats. The nanosized emulsions showed acceptable physical properties and exhibited slow drug release. Photomicrograph of skin sample supports the in-vitro skin...
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Posted by admin on May 1, 2010 in |
A simple, sensitive and selective high performance liquid chromatography (HPLC) method with ultraviolet detection (220 nm) was developed and validated for the quantification of Ibuprofen and in human plasma. Following rapid sample preparation, the analytes and internal standard (Diclofenac sodium) were separated using an isocratic mobile phase on a reverse phase C8 column. The lower limit of quantification was 1µg/mL for Ibuprofen. A linear dynamic range of 1µg/mL to 100µg/mL for Ibuprofen was established. This HPLC method was validated with between and within-batch precision of 1.2- 4.7% and 1.8- 4.8 %, respectively. The between and within batch accuracy was 99.4- 104.2% and 99.7- 104.1%, respectively. Frequently co-administered drugs did not interfere with the described methodology. Stability of Ibuprofen in plasma was >90%, with no evidence of degradation during sample processing (autosampler) and 60 days storage in a freezer. This validated method is sensitive and simple with between-batch precision of < 5 % and was used in pharmacokinetic...
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Posted by admin on May 1, 2010 in |
The different extracts of the roots of Bruguiera gymnorhiza (Family- Rhizophoraceae) were tested for anti-diabetic activity, by glucose tolerance test in normal rats and alloxan induced diabetic rats. Aqueous ethanol and butanol extracts had shown significant protection and lowered the blood glucose levels to normal in glucose tolerance test. In alloxan induced diabetic rats the maximum reduction in blood glucose was observed after 3h at a dose level of 250 mg/kg of body weight. The percentage protections by aqueous ethanol and butanol extracts were 30 and 48% respectively. In long term treatment of alloxan induced diabetic rats, the degree of protection was determined by measuring blood glucose, triglycerides, cholesterol and urea levels on 0,3,5,7 and 10th day. Both the extracts showed a significant anti- diabetic activity comparable with that of glibenclamide. The histopathological studies during the long-term treatment have shown to ameliorate the biochemical damages caused by alloxan. These results indicate that the B. gymnorhiza root possess significant anti -diabetic...
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Posted by admin on May 1, 2010 in |
Inflammation is a biological reaction attributed with several acute and chronic pathological conditions. The study revealed the pharmacological effect of Tecomella undulate: bark against carrageenan induced paw edema and cotton pellet induced granuloma in rat. Wistar albino rats of either sex (180-240 g) were employed into the study. Acute inflammation was induced by injecting carrageenan (1%) in rat paw and estimated using plethysmograph. Chronic inflammation was induced by cotton pellet induced granuloma method. Serum nitrate/nitrate estimation was also done as an index of inflammatory reactions. Acute toxicity study was also done using Swiss albino mice. Butanolic and water fractions of Tecomella undulate (200 & 400 mg/kg) and indomethacin (10 mg/kg) were used as test drugs. Carrageennan caused a marked increase in rat paw volume due to edema formation. T. undulate: butanolic fraction significantly inhibited paw volume in successive hours similar to indomethacin. Interscapular implanted cotton caused significant increase in granuloma wt. and serum nitrate/nitrite level in control group. However, the test drugs lowered the effects of cotton pellet induced...
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