Abstract

Seven methoxy deoxy vasicinone [CDRI compound No. 73/602] (I), is an antiallergic agent presently undergoing phase II clinical trials. The observations in clinical trials suggested a dosing schedule of the drug to be 50 mg t.i.d. or b.i.d. Therefore development of a sustained release formulations of the drug was undertaken for better patient compliance. The formulations were prepared by using process of direct compression and wet granulation. Tamarind seed polyose (TSP), hydroxypropylmethyl cellulose (HPMC) and hydroxyethyl cellulose (HEC) were used as hydrophilic polymers and binders like starch and methyl cellulose (MC) were used in wet granulation method. In vitro evaluation of matrices was done on the Sartorius dissolution simulator using different combinations of drug polymer. The formulations,TSP-B and HPMC-B, which gave the best results in the in vitro system, were subjected to in vivo studies in rabbits by using cross over design. Pharmacokinetic parameters like AUC, Tmax and Cmax were calculated.