Development and in Vitro Evaluation Colon Targeted Drug Delivery System Using Natural Gums
Author: P.S. Salve
Abstract
The present study deals with formulation of sustained release tablet of ibuprofen for colon targeting. Tablets were prepared using combination of guar and xanthan gum. The drug excipient interaction studies were carried out by FTIR and DSC. The prepared matrixes (GG :XG, 4:6) form enzyme controlled delivery systems with nearly 50 to 60% w/w of the tablet content being constituted by polysaccharides degradable by colonic microflora. Biodegradability studies of guar and xanthan gum was carried out in presence of 4% w/v RCC and galactomannase enzyme (0.1 mg/ml.) by viscosity measurement using Brookfield viscometer and significant decrease in viscosity was found with 4% RCC after 24 h incubation. In vitro drug release studies shows that guar and xanthan gum in 4:6 has optimum release in a controlled manner for 24 h.
Synthesis of Novel Thiazole Derivatives as Analgesic Agents
Authors: G. Saravanan, C.R. Prakash, P. Dinesh Kumar, T. Panneer Selvam, V. Alagarsamy
Abstract
Thiazoles have a long history of having number of pharmacological activities such as anti-microbial, analgesic and anti-inflammatory activities. Pyrazoles shows promising anti-microbial, analgesic and anti-inflammatory activities. In the present study, novel thiazoles (8a – 8j) were synthesized by incorporation of pyrazole moiety at 2nd position of 2- hydrazinyl-N-(4-phenylthiazol-2-yl) acetamide (5) by treating with chalcones (7a-7j). The chemical structures of the synthesized compounds were confirmed by means of IR, 1H-NMR, Mass spectral and Elemental analysis. All the spectral data were consistent with the assigned structure. The synthesized compounds were investigated for analgesic activity by tail immersion method in mice. All the synthesized compounds exhibited mild to good analgesic activities. Among the synthesized compounds, 2-(5-(4-dimethylaminophenyl)-3-phenyl-4,5-dihydropyrazol-1-yl)-N-(4- phenylthiazol-2-yl)acetamide (8c) and 2-(5-(4-methylphenyl)-3-phenyl-4,5-dihydropyrazol-1-yl)-N-(4-phenylthiazol- 2-yl)acetamide (8e) exhibited highest analgesic activity.
Hepatoprotective and Anti Pyretic Activities of Methanolic Extract of Butea Monosperma Lam Stem Bark In Wister Rats
Authors: R. Sathish, P. Sravan Kumar, K. Natarajan, N. Sridhar
Abstract
The methanolic extract of stem bark of Butea monosperma Lam (MEBM) was studied for the hepatoprotective and antipyretic activities. Carbontetrachloride (1ml/kg, i.p) induced hepatotoxicity and Brewer’s yeast (10ml/kg, s.c) induced pyrexia rat models were used. The 10 days treatment of MEBM (200 mg/kg and 400 mg/kg, p.o) showed significant (P<0.01) hepatoprotective effect by dose dependent manner. The MEBM significantly (P<0.01) lowered the elevated levels of serum biochemical parameters such as SGOT, SGPT, ALP, total bilirubin and also significantly (P<0.01) increased total protein levels when compared to toxic control rats. The MEBM at both dose levels (200 mg/kg and 400mg/kg, p.o) produced significant (P<0.01) antipyretic activity throughout the observation period up to 6 h. The phytochemical analysis showed the presence of biologically active constituents such as flavonoids, glycosides and sterols. The flavonoids in the MEBM may be responsible for the significant hepatoprotective and antipyretic activities.