盐酸普鲁卡因胺膜控片的研究

STUDIES ON A SUSTAINED RELEASE PROCAINAMIDE HYDROCHLORIDE PREPARATION—A MEMBRANE CONTROLLED RELEASE TABLET

本文研究了盐酸普鲁卡因胺(PA·HCl)膜控片(B)的处方组成,制备工艺,体外溶出速率;利用HPLC法测定了体内PA及其活性代谢物N-乙酰普鲁卡因胺(NAPA)的血药浓度经时曲线;体内PA实验数据按双室模型用电子计算机进行处理得各药动学参数;B片剂体内外测定数据具有相关性。

This paper deals with the formulation, preparation of a membrane-controlled release tablet of procainamidc hydrochloride(B). The in vitro dissolution and in vivo pharmacokinetics of the tablet were also determined and compared. Experiments utilized a permeable cellulose acetate to coat the core tablet. The determination of PA and its active metabolite N-acetylprocainamide in serum or saliva by HPLC method were established. The pharmacokinetic parameters were fitted by using a two-compartment model. The studies showed that tablet Breleased drug with a zero-order kinetics, and a significant correlation was found to be between in vitro dissolution and in absorption.