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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。
Objective: To prepare nifedipine sustained-release pellets and study its pharmacokinetics and relative bioavailability in beagle dogs. Methods: Nifedipine and polyvinylpyrrolidone (PVP) were made into solid dispersions by spray fluidized coating method, and then coated with sustained-release film to prepare nifedipine 24h sustained-release pellets. High-performance liquid chromatography In vivo plasma concentrations were analyzed; pharmacokinetic parameters were calculated using 3P97 software. Results: Under the selected chromatographic conditions, the linearity of nifedipine in the range of 2 ~ 200μg · L-1 was good (r = 0.9997). The main pharmacokinetic parameters of self-made sustained-release pellets and reference preparation were : 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; relative bioavailability was (112.5 ± 13.1)%. Conclusion: The self-made nifedipine sustained-release pellets have a sustained-release effect.