Development and evaluation of floating microspheres ofPioglitazone hydrochloride using ethyl cellulose

[摘要] Various approaches have been used to retain the dosage form in the stomach as a way ofincreasing the gastric residence time (GRT), including floatation systems; high-density systems;mucoadhesive systems; magnetic systems; unfoldable, extendible, or swellable systems; andsuperporous hydrogel systems. The aim of this study was to prepare and evaluate floatingmicrospheres of Pioglitazone hydrochloride for the prolongation of gastric residence time. Themicrospheres were prepared by emulsion solvent diffusion-evaporation method using ethylcellulose and HPMC K100M. A full factorial design was applied to optimize the formulation.Preliminary studies revealed that the concentration of polymer and stirring speed significantlyaffected the characteristics of floating microspheres. The optimum batch of microsphereexhibited smooth surfaces with good flow and packing properties, prolonged sustained drugrelease, remained buoyant for more than 10 hrs, high entrapment efficiency upto 97%w/w.Scanning electron microscopy confirmed the hollow structure with particle size in the order of190 μm. The studies revealed that increase in concentration of hydrophillic polymer (HPMC)increased the drug release from the floating mcirospheres. The results of 32 full factorial designrevealed that the concentration of ethylcellulose 10 cps (X1) and stirring speed (X2) significantlyaffected drug entrapment efficiency, percentage release after 8 h and particle size ofmicrospheres.

[学科分类] 药理学