尼群地平片剂生物利用度的研究

STUDIES ON THE BIOAVAILABILITY OF NITRENDIPINE TABLET

为提高国产尼群地平片剂的生物利用度,采用球磨混合粉碎法工艺进行处方设计,试制出新处方片剂,与西德Bayer公司片剂进行了体外溶出、体内生物利用度的比较。体内血浆药浓用GC-MS法测定,体内数据按零级溶出、一级吸收口服单室模型,经计算机用Gauss-Newton-Damping法处理求得药动学参数。本文研制的尼群地平新处方片剂生物利用度已超过西德Bayer公司片剂。

The problem of nitrendipine tablets manufactured in China is its low bioavailability. To solve this, a new tablet formulation was developed by using milling method to increase its relative bioavailability. The commercially available conventional tablet A (Nanjing factory) and C (a Hebei factory) and the new tablet formulation D were compared with the reference tablet B (Bayer Company, West Germany)in vitro and in vivo. The determination ofnitrendipine in vivo was carried out by GC-MS. The pharmacokinetic parameters of nitrendipine in vivo were estimated by using the nonlinear least square computer program on the basis of the compartment model (zero order dissolution, first order absorption).The bioavailability of A, C and D relative to B was 31.8%, 72.2% and 138.9% respectively. The new tablet formuiation D is superior to the imported tablet B in both the extent and rate of absorption.