【摘要】 目的:制备硝苯地平缓释小丸胶囊,考察其在beagle犬体内的药动学及相对生物利用度。方法:采用喷雾流化包衣法将硝苯地平与聚乙烯吡咯烷酮(PVP)制成固体分散体,再包以缓释膜制得硝苯地平24h缓释小丸;采用高效液相色谱法对犬体内血药浓度进行分析;利用3P97软件计算药动学参数。结果:在选定的色谱条件下,硝苯地平质量浓度在2～200μg·L-1内线性关系良好(r=0.9997),自制缓释微丸与参比制剂的主要药动学参数分别为:tmax(4.0±1.4),(0.75±0.3)h;Cmax(41.56±5.9),(116.34±8.1)μg·L-1;AUC0-t(257.3±75.3),(228.7±64.8)μg·h·L-1;相对生物利用度为(112.5±13.1)%。结论:自制硝苯地平骨架缓释小丸胶囊具有明显的缓释效果。更多还原

【Abstract】 OBJECTIVE To prepare nifedipine capsules containing sustained-release pellets and to evaluate its pharmacokinetics in beagle dog. METHODS Nifedipine solid dispersion was made with PVP by using the fluid bed,and then coated with membrane to prepare sustained-release pellets. HPLC method was developed to quantify the drug plasma concentration of beagle dogs,the pharmacokinetics parameters of nifedipine were analyzed by the 3P97. RESULTS The concentration of nifedipine in beagl dog plasmas was determined by HPLC with UV detection. The assay in beagle dog plasmas was linear from 2 to 200 g·L-1 (r=0.999 7).The main pharmacokinetics parameters of the self-made capsules and reference formulation were as follows: tmax (4.0±1.4)and(0.75±0.3)h;Cmax(41.56±5.9) and (116.34±8.1)g·L-1;AUC0-t(257.3±75.3) and (228.7±64.8)μg·h·L-1,Relative bioavailability was (112.5±13.1)%. CONCLUSION Self-made nifedipine capsules show the significant sustained-release behavior.更多还原