Posted by admin on Jul 31, 2015 in |
6-(2-Amino-3,5-substituted phenyl)-1,2,4-triazines were prepared by refluxing semicarbazones or thiosemicarbazones in presence of sodium hydroxide solution. 6-(3,5-Substituted-2-bromophenyl)-1,2,4-triazine derivatives and 6-(3,5-substituted-2-hydroxyphenyl)-1,2,4-triazine derivatives were prepared from 6-(2-amino-3,5-substituted phenyl)-1,2,4-triazine derivatives by sodium nitrite, hydrobromic acid, copper (I) bromide and sodium nitrite, sulfuric acid, respectively. The structures of the synthesized compounds were confirmed on the basis of their elemental analysis and spectral data (FT-IR and H1-NMR). Amongst synthesized compounds, some displayed significantly active profile against the electrically induced seizures at a dose of 30 mg/kg after 0.5 h. At the same dose level, one compound also showed activity after 4.0 h. Two compounds exhibited protection at dose level of 100 mg/kg after 0.5 h. At 4.0 h, two compounds persisted to reveal anti-MES protection at same dose, whereas two other compounds indicated to prevent seizure spread at a higher dose of 300 mg/kg after 4h. One compound displayed protection at 300 mg/kg after 0.5 h. The neurotoxicity screening data revealed that two compounds were exhibited neurotoxicity at a dose level of 300 mg/kg after...
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Posted by admin on Jul 31, 2015 in |
The number of patients with Diabetes mellitus is increasing rapidly both in developed and developing countries around the world. The existing medications especially synthetic drugs often fail to bring back normal glycemic control without complications. Numerous herbal medicines are widely explored as alternative medicine in diabetes. The objective of this work was to evaluate one such herbal extract of Benincasa hispida fruit for its anti-diabetic activity in experimentally induced diabetic rats. The extract at a dose of 200mg/kg/day and 400mg/kg/day was administered to streptozotocin induced diabetic animals for 15 consecutive days. Blood glucose levels, lipid profiles and body weight were measured for the evaluation of its anti-diabetic effect. The results of the study at both low and high dose of extract showed significant (p<0.01) decrease in blood glucose levels in diabetic rats. In addition, both the dose of extract also showed significant (p<0.05) decrease in serum triglyceride, VLDL levels, and an increase in HDL levels, though not significant. Only high dose of extract and glibenclamide treated group showed significant...
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Posted by admin on Jul 31, 2015 in |
Novel 1- Phenyl 1-H-Pyrazolo[3,4-d]Pyrimidine Derivatives were synthesized from the key intermediate chloro derivative (1).The conversion of chloro derivative(1) into 1,2,4 triazoles, 1,3,4 thiadiazoles and thiazoles was accomplished with the intermediacy of the ester(2) and hydrazide (3). Moreover triazole ring was annelated to the pyrazolopyrmidine core in two step reaction involving reaction with acid hydrazides followed by intramolecular cyclization in boiling glacial acetic acid Majority of the synthesized compounds showed variable antimicrobial activity on the hand tricyclic compounds(9a-b) were deprived from any antimicrobial activity against the tested micro-organisms. The hydrazine carbothioamide derivative (4) and 1,3,4 thiadiazole derivative (6) showed antimicrobial activity against Streptococcus pneumoniae and Bacillis subtilis comparable to ampicillin and a moderate antifungal activity against Asp. Fumigates and C....
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Posted by admin on Jul 31, 2015 in |
Present research work aims to develop venlafaxine hydrochloride gastro retentive tablets for prolonged release and increased gastric retention time. Venlafaxine is an antidepressant of the serotonin nor- epinephrine reuptake inhibitor (SNRI) class. Bioavailability is 45% following oral administration and half life is 5 hours. To study the effect of formulation variables on drug release and buoyancy properties of the sustained release venlafaxine hydrochloride gastro retentive floating drug delivery system, the floating matrix tablets of venlafaxine hydrochloride were prepared by bilayer tablet technology with sustained and floating layers. The different hydrophilic polymers for sustained release layer studied, were HPMC K 4M, HPMC K 15M, xanthan gum studied in order to obtain the desired sustained release up to 12 hrs and the effervescent component of floating layer was sodium bicarbonate along with HPMC K 100M. Drug compatibility with excipients was checked by FTIR studies. The formulation optimization batches were studied for physical parameters and floating behavior, dissolution studies and kinetics of drug release. Hardness of tablets was kept 6 kg/cm2. The effect...
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Posted by admin on Jul 31, 2015 in |
In the recent days targeted drug delivery has gained more prominence for various advantages like site specific delivery and controlled release from the formulations. Amongst the plethora of avenues explored for targeted drug delivery, bioadhesive nanoparticles backed foremost attention offering local drug delivery and controlled drug release solving problems like tissue damage and drug wastage. Formulating nanoparticles with mucoadhesive polymers may provide a significant increase in the gastrointestinal residence time. Neostigmine bromide is a cholinesterase inhibitor used for the treatment of Myasthenia Gravis and is given by conventional routes like oral and intra venous. Bioadhesive nanoparticles of Neostigmine Bromide using synthetic and semi synthetic polymers like Carbopol, HPMC and ethyl cellulose were prepared by emulsification solvent evaporation method. The nanoparticles were characterized for their preformulation and post formulation parameters like compatibility, particle size, zeta potential, encapsulation efficiency, surface morphology, in vitro mucoadhesion, in vivo bioavailability, drug release and stability studies. Out of six, formulations F1 and F4 showed the best results for different evaluated parameters of nanoparticles. Entrapment efficiency...
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