IN-VIVO STUDY OF CLOZAPINE ORAL DISINTEGARTING TABLETS FOR THE TREATMENT OF SCHIZOPHRENIA

*Ramesh Babu Kota, Saravanan Kaliyaperumal

ABSTRACT

In this study, clozapine was formulated as orally disintegrating tablets (ODTs) employing a direct compression method, incorporating superporous hydrogels as super disintegrants. The disintegration time, hardness, friability, and stability of these ODT formulations were systematically evaluated, along with detailed dissolution profiles. According to the USP monograph, Q point for oral disintegrating tablet is not less than 85% at the end of 15 minutes. Formulation containing superporous hydrogel as super disintegrants has showed rapid drug release in comparison to the commercial grades of superdisintegrants available in the market. Formulation (CF9-O) was considered as the optimized formulation, as the formulation showed rapid drug release (85.29%) at the end of 15 minutes. An in vivo study was conducted in new zealand rabbits to determine the pharmacokinetic parameters for the optimized formulation. Time vs. plasma concentration plots of the convention tablet (without superdisintegrant) and Optimized formulation (CF9-O) was observed. Plotted Area under the curve indicates the extent of drug absorption inside the body. Pharmacokinetic analysis of Optimized formulation (CF9-O) drug plasma concentration–time data provided the following pharmacokinetic parameters like Cmax value (23.21 ± 1.15 μg/mL), Tmax value (1.5 Hours), AUC value (229.37 ± 5.04 h.μg/mL), Half Life (6.5 Hours) and other pharmacokinetic parameters are depicted. Study demonstrates the variability in pharmacokinetic parameters like Tmax, Cmax, T1/2 (Hours), AUC & Ke.

Keywords: Clozapine, Superdisintegrant, Pharmacokinetic, In-Vivo, Superporous, ODT.