International Journal of Pharmaceutical Sciences and Drug Research

384-394

Authors: Dinesh Kaushik*, Pankaj Kumar, Satish Sardana

The objective of this study is to prepare a formulation of Azithromycin which increase the oral bioavailability as well as increased solubility and dissolution rate. In the present study nine formulations were formulated by using the three different polymers and varying the concentration of PEG and also varying the rotation speed of the stirrer. Results of preformulation studies like melting point 117°C, UV spectroscopy and FTIR studies showed that the drug was pure. The spherical and rough surface of F9 viewed through SEM. In-vitro dissolution study had shown satisfactory results. On the basis of release data and graphical analysis formulation F8 and F9 showed a good controlled zero order release profile.

401-406

Authors: Abdul Malik P.H*, S Satyanandam, Sunil Murala

In the present work, an attempt has been made to formulate pH-induced in-situ gel as an ophthalmic drug delivery system. In situ gels are made from polymers that exhibit phase transition due to physicochemical change in the environment. They can be conveniently dropped as a solution into the conjuctival sac in the eye. Upon contact with the lacrimal fluid, the polymer changes its conformation to form a gel. This delivery system has the ease of administration similar to an opthalmic solution and has a long retention time because of the gel formation. Different polymers for preparing pH induced in-situ gels have been evaluated. The topical application of ophthalmically active drugs to the eye is the most prescribed route of administration for the treatment of various ocular diseases. It is generally agreed that the intraocular bioavailability of topically applied drugs is extremely poor. Upon instillation of an ophthalmic solution; most of the instilled volume is eliminated from the pre-corneal area. This loss is mainly due to drainage of the excess fluid by the nasolacrimal duct or elimination of the solution by tear turnover, which will results in poor ocular bioavailability. Lomefloxacin is member of the fluoroquinolone class of antimicrobial drugs. It is active against a wide range of gram positive and gram negative organisms.

412-416

Authors: Somara Sasikala1*, Siddamsetty Lakshminarasaiah1, Malepati Dhananjaya Naidu2

This study was conducted to evaluate the therapeutic effect of methanol extract Centella asiatica leaves by assaying the activities of diagnostic markers (aminotransferases) in the streptozotocin induced diabetic rats. The rats were divided into five groups with 6 rats in each group. The methanol extract of Centella asiatica leaves was orally administered at a dose of 300 mg/kg body weight (b.w), and glibenclamide was administered at a dose of 5 mg/kg b.w. The effect of methanol extract of Centella asiatica leaves on total protein and the activities of diagnostic marker enzymes aspartate aminotransferase (AST), alanine aminotransferase (ALT) were examined in the liver and kidney of control and experimental rats. The result showed a significant (p < 0.001) decrease in total protein concentration and increase in AST and ALT activities in the liver of diabetic rats whereas the levels were unaltered in the kidney of diabetic rats. The daily oral treatment of methanol extract of Centella asiatica leaves to diabetic rats for 30 days reversed the above changes in a significant (p < 0.001) manner. From our observations, we conclude that methanol extract of Centella asiatica leaves was able to restore the altered activities of aminotransferases. The obtained results were compared with glibenclamide, a standard antidiabetic drug. These results indicate that oral treatment with methanol extract of Centella asiatica leaves may be used to alleviate the liver functions impairment associated with diabetic condition.

421-424

Authors: Saurabh Kumar Sinha*

Some new Schiff bases of 4-aminopyridine were synthesized and evaluated for antiamnesic and cognition enhancing activity. In the current study to further understand the mechanism of action of these derivatives we have evaluated in-vitro acetycholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activity. Enzyme kinetics and docking studies were performed for all compounds to observe their nature of inhibition. The IC50 value of synthesized compounds showed maximum activity of compound 4APg compared to standard drug donepezil and rivastigmine whereas its kinetic analysis of enzyme inhibition demonstrated non-competitive inhibition for both enzymes AChE and BChE. The docking study confirmed their consensual interaction with AChE and BChE active sites justifying the experimental outcome.