NGHIÊN CỨU BÀO CHẾ VÀ ĐÁNH GIÁ SINH KHẢ DỤNG CỦA VIÊN NÉN PYRIDOSTIGMIN BROMID GIẢI PHÓNG KÉO DÀI

Abstract

Objectives: To develop an extended-release pyridostigmine bromide (PB)  tablet  formula  and  evaluate  its  bioavailability  in  experimental  rabbits. Methods: A matrix extended-release formula was developed using the granulation technique using MODDE 8.0 in experiment design and formula optimization. The bioavailability in rabbits was studied, compared to the conventional pharmaceutical PB 30mg tablet (qualified for US Pharmacopoeia (USP) 38)). Results: A combination of control release ingredients of hydroxypropyl methylcellulose (HPMC), carnauba wax, and tricalcium phosphate was used, considered as independent variables. Tablets were prepared using the wet granulation technique, and the percentage of drug released at 1 hour (Y1), 4 hours (Y2), and 8 hours (Y3) were considered as dependent variables. The optimal formula tablet was capable of releasing in vitro active ingredient in the first hour at 36.43 ± 1.15%, after 4 hours at 73.14 ± 2.27%, and after 8 hours at > 85% of the active ingredient content. The bioavailability was 3.35 times higher than the reference tablet. Conclusion: The formula of the extended-release PB tablets was designed and optimized; a study of bioavailability in rabbits showed the bioavailability of the extended-release tablet was three times higher compared to the regular pharmaceutical tablet.