Repaglinide Fast Dissolving Tablet: In vitro & In vivo studies.

      Аннотация: Repaglinide according to the biopharmaceutics classification system is considered as class II drug, which suffers from low aqueous solubility and hence, low bioavailability. The current study concerned with improvement of the aqueous solubility and dissolution rate of repaglinide by using solid dispersion techniques with different polymers. Moreover, fast-dissolving tablets of repaglinide solid dispersion with superdisintegrant were formulated to enhance the repaglinide bioavailability. In the present study, solid dispersion formulae of repaglinide were prepared by utilizing different polymers as PEG 6000 ,mannitol and urea in various drug: polymer ratio by using melting and solvent evaporation methods. The solubility of repaglinide in different carriers was estimated, and solid dispersions were prepared and characterized. The drug release profile was carried out. Furthermore; pharmacokinetic studies with the selected fast dissolving tablet of repaglinide in solid dispersion were conducted on human volunteers. The fast dissolving tablet is a promising formulation for repaglinide that results in higher solubility, a rapid onset of action, and enhanced systemic bioavailability.

Ключевые слова: fusion, in vitro drug release, Pharmacokinetics, Repaglinide, phase solubility, solid dispersion.