硝苯地平双层渗透泵片的制备及家兔体内药动学研究

目的:以硝苯地平为模型药物制备渗透泵制剂,并进行家兔体内药动学研究.方法:与Adalat@GITS硝苯地平控释片比较,采用相似因子法对处方进行考察优化;将制备的硝苯地平渗透泵片和自制的普通片,分别对家兔单剂量口服给药,采用HPLC法对给药后家兔血浆中药物浓度进行测定.结果:通过处方优化,制备了难溶性药物硝苯地平24 h的控释制剂;渗透泵控释片和普通片的达峰时间分别为(12.05±0.28)h和(5.98±0.47)h,峰浓度分别为(0.299±0.035)mg·L<'-1>和(0.452±0.038)mg·L<'-1>,相对生物利用度为119.5%±7.2%.结论:通过制备双层渗透泵片,能够实现硝苯地平体外溶出实验下24 h零级释药,能显著延长硝苯地平家兔体内达峰时间,降低峰浓度,并且提高了药物的生物利用度.

Preparation and Pharmacokinetics of Nifedipine Osmotic Pump Tablets in rabbits

Objective: To investigate the formulations and pharmacokinetics of nifedipine double-layer osmotic pump tablets.Methods: In present study,nifedipine was as the model drug to prepare the bi-layer osmotic pump tablets.The effects of many factors including formulation of drug layer,push layer and membrane,release media on the in-vitro release behavior of nifedipine tablets were investigated.The plasma nifedipine concentration of osmotic pump tablets and self-prepared ordinary tablets after single oral administ...