Research Journal of Pharmaceutical Dosage Form and Technology

V. Saikishore ¹, G. Srikanth ¹, Ch. Pooja ¹, Y. Mrudula ¹, R. Pavani ¹, Ch. Jyosthna ¹, C. Mayuren ¹

Affiliations
1 Dept. of Pharmaceutics, Bapatla College of Pharmacy, Bapatla-522101, Andhra Pradesh, IN

Abstract

Glibenclamide is a second generation antidiabetic drug used for the treatment of Type -II Diabetes. Glibenclamide is practically insoluble in water and so possesses poor solubility, GI absorption and bioavailability. In order to improve the dissolution rate and thereby the absorption, fast dissolving tablets of Glibenclamide were prepared using superdisintegrants by direct compression. To study the influence of concentration of the sodium starch glycolate on the performance of Glibenclamide, a set of four formulations (F1, F2, F3, F4) were prepared using four different concentrations of sodium starch glycolate (2%, 3%, 4%&amp;5%w/w) respectively. The formulation prepared with 5%w/w of sodium starch glycolate was offered relatively rapid release of Glibenclamide when compared with other concentrations employed in this investigation. To study the influence of superdisintegrants on the performance of Glibenclamide, a set of three formulations (F4, F5 and F6) were prepared using three different superdisintegrants viz, Sodium starchglycolate(5%),Ac-Di-Sol(5%), Crospovidone (5%) respectively. Based on the dissolution rate, superdisintegrants can be rated as Sodium starchglycolate < Ac-Di-Sol < Crospovidone. Nature and concentration of the superdisintegrant showed influence on the rate of dissolution. The formulated tablets were subjected to various quality control tests and the results were complied with the pharmacopoeial standards. The drug release profiles followed first-order kinetics. The rate of drug release was found to be increased by increasing the concentration of the superdisintegrant and found to be highest for tablets formulated with 5%w/w of crospovidone. Blood glucose concentrations for developed formulation at times 1 and 2 hr were significantly lower than those for pure drug and marketed formulation. There is a correlation between in vivo and in vitro parameters. These correlations indicate that drug hypoglycemic effects are highly controlled by the drug dissolution. The higher the dissolution the higher is the corresponding in vivo parameter.

Keywords

Glibenclamide, Sodium Starchglycolate, AC-DI-SOL, Crospovidone, Hypoglycemic Effects.

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