盐酸地尔硫控释胶囊人体内外相关性

Correlation between dissolution in vitro and absorption in vivo of diltiazem hydrochloride controlled-release capsule

目的:考察盐酸地尔硫控释胶囊(DTZ-CRC)的体外释放度与体内吸收的相关性.方法:测定DTZ- CRC在不同pH释放介质中的释放度;10名男性健康志愿者po 60mg DTZ-CRC,HPLC法测定血药浓度,按照Wagner-Nelson公式计算药物吸收分数.结果:不同释放介质中药物的体外释放度与体内吸收分数的相关系数r分别为0.984 8、0.986 7和0.982 8.结论:DTZ-CRC的体外释放度与体内吸收具有显著的相关性.

AIM: To study the correlation between dissolution in vitro and absorption in vivo of diltiazem hydrochloride controlled-release capsule (DTZ-CRC). METHODS: Dissolution of DTZ-CRC in vitro was tested with ZRS-4 dissolution tester. A single oral dose of 60 mg DTZ-CRC was given to 10 healthy male volunteers. Plasma levels were determined by HPLC and absorption fraction were calculated according to Wagner-Nelson's formula. RE-SULTS: The correlation coefficient (r) between dissolution in vitro in release media of diffe-rent pH and absorption fraction in vivo was 0. 984 8, 0. 986 7 and 0. 982 8 respectively. CON-CLUSION: There is a significant correlation between dissolution in vitro and absorption in vi-vo of DTZ-CRC.