PREPARATION AND EVALUATION OF ACTIVE FILM COATING TABLET OF TENELIGLIPTIN HYDROBROMIDE HYDRATE WITH METFORMIN HYDROCHLORIDE FIXED DOSE COMBINATION

Abstract

The aim of the present study was to formulate fixed-dose combination tablets of metformin hydrochloride and teneligliptin hydrobromide hydrate. The extended-release core tablet consisted of a seal coating over metformin and outer layer coated by teneligliptin for immediate release using perforated film coating equipment. The seal coating is necessary to prevent the contact between metformin and teneligliptin. 23 Full factorial design was planned to determine critical processing parameters like the effect of hydroxypropyl methyl cellulose and ethyl cellulose in seal coating, ratio of drug and polymer in the coating solution, and spray rate as variables with lower and higher level. Optimized (F9) batch prepared from the design space from experimental variable as seal coat ratio of 0.33, drug coat ratio of 2 with rate of spray 3 g mL-1, gave desired release pattern. The optimized formulation was subjected to in vivo kinetic studies using Wistar rats. Metformin 100 mg kg-1 was administered orally and blood was withdrawn at various time intervals to assess the kinetic parameters. The observed AUC and Cmax were found to be 260 ng*h mL-1, and 58.0 ng mL-1, respectively, and the time needed to reach Tmax was 6 h for metformin tablets.