Development of Capecitabine Floating Tablet Dosage Forms for Treating Stomach Cancer

Abstract

Objective: In the present research work, oral gastro retentive dosage forms (GRDFs) of capecitabine (CPC) were formulated using floating concept.
 Methods: GRDFs were formulated using hydroxypropyl methyl cellulose (HPMC K4M and K15M) as drug release retardant, sodium bicarbonate (NaHCO3) and calcium carbonate (CaCO3) as gas generating agents, and micro crystalline cellulose (MCC), dicalcium phosphate (DCP), spray dried lactose (SDL), and pre gelatinized starch (PGS) as fillers. The tablets were prepared by direct compression method and evaluated for various parameters. The GRDFs were also characterized by Fourier-transform infrared spectroscopy (FTIR), and differential scanning calorimetry (DSC).
 Results and Discussion: All the formulations were subjected for pre and post compression parameters, shows all the data within the limits. The lag times of GRDFs has decreased significantly for formulations containing calcium carbonate when compared to sodium bicarbonate as gas generating agent. In vitro drug release studies indicate that higher polymer concentration delayed the CPC release, and the sustaining effect was in the order K4M > K15M > LVCR 100. Addition of MCC, DCP, SDL, and PGS as fillers further affected the lag time and in turn the CPC release rates.
 Conclusion: The formulation (F9) containing 10%w/w HPMC K4M as the release retardant, microcrystalline cellulose as filler and 20%w/w CaCO3 as gas generating agent fulfilled regulatory requirements in terms of percent drug release at the end of 24h.
 Keywords: Capecitabine, Gastro retentive floating tablets, floating drug delivery systems, FTIR, DSC.