盐酸雷尼替丁胃内滞留漂浮型缓释片的制备及药物动力学研究

Development and Pharmacokinetic Study of Ranitidine Hydrochloride Sustained Release Floating Tablet for Oral Use

本文研制了盐酸雷尼替丁胃内滞留漂浮型缓释片剂(RSRT)。本品的体外溶出符合一级动力学过程:RSRT在胃内滞留时间5-6h,明显比普通对照片(2h内)长;RSRT体内以单室模型描述较适宜,RSRT体内为一级释药。药动学参数为:Ka=0.2550h^(-1),K=0.2765h^(-1),Vd=84.38L,t_(max)=3.77h,C_(max)=627.7ng/ml。本品的体内外数据具有显著相关性。

A novel ranitidine sustained release floating tablet for oral use was developed. It was found that in vitro release characteristics showed basically first-order kineties; the γ-Scintiphotographic study after oral ingestion showed that ranitidine sustanined release tablet was retained in human stomach for longer time (5—6 h) than the conventional ranitidine tablet (2 h). The plasma concentration-time course of ranitidine sustained release tablet was demonstrated to fit a one—compartment model with apparant first order absorption and first order elimination. The pharmacokinetic parameters were calculated using a nonlinear regression computer program with the values of K_a, K, V_b, T_(max), C_(max), being 0.2550 h^(-1), 0.2765 h^(-1), 101.4 h^(-1), 3.8 h, 627.7 ng/ml, respectively. The fraction absorbed from ranitidine release tablet in vivo well correlated with dissolution rate in vitro.