Formulation, development and optimization of gastroretentive floating pellets of febuxostat

Upasana J Patel, Hitesh kumar A Patel, Bhumika J Limbachiya, Mehzabeen Jhankhwala

Nootan Pharmacy College, Sankalchand Patel University, Visnagar, Gujarat, India

ABSTRACT

The aim of the study was to develop gastro retentive floating pellets of febuxostat used to treat gout condition which having low solubility and high bioavailability. The gastro retentive floating pellets of febuxostat were formulated using Gelucire 43/01 and ethyl cellulose as a sustain release polymer and microcrystalline cellulose as spheronizing agent by extrusion- spheronization technique. A 32 full factorial design was applied to investigate the effect of the two-independent variable, that is, ratio of Drug: Gelucire (X1) and ratio of Drug: ethyl cellulose (X2), on the dependent variables, Floating lag time (Y1) and cumulative % drug release at 24th hour(Y2). The optimized formulation (B11) exhibits a floating lag time 110.2±0.02 sec. and cumulative % drug release at 24th hour 98.8±0.02. The in vitro release of B1- B12 batches were found in between 98.8% and 68.9% at 24 h. Floating lag time of B1- B12 batches was found to be 62.0±0.01 s – 200.2±0.01 s. Gelucire 43/01 and ethyl cellulose had a significant effect on floating lag time and in vitro drug release. Scanning electron microscopy photomicrograph of pellets revealed that the surface was rough and the pellets were spherical shaped in nature. The in vitro release kinetics revealed zero order models are followed.

Keywords:

Gelucire, Gastro retentive floating pellets, Febuxostat, Ethyl cellulose.