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目的:研究尼群地平3种晶型在家兔体内药动学和生物利用度。方法:家兔单剂量交叉口服尼莫地平不同晶型胶囊80mg·kg-1,采用高效液相色谱(HPLC)法测定血药浓度,非房室模型计算药动学参数。结果:尼群地平晶型Ⅰ、Ⅱ和Ⅲ的Cmax分别为(351.5±18.7),(392.7±50.8),(822.1±39.7)μg.L-1;tmax为(1.72±0.16),(1.83±0.11),(1.81±0.18)h;t1/2为(13.3±3.5),(8.6±1.2),(8.0±1.2)h;AUC0→t为(3635.1±230.8),(2697.0±209.4)和(6428.6±585.6)h.μg.L-1。尼群地平晶型Ⅱ、Ⅲ相对于晶型Ⅰ的相对生物利用度为62.1%和169.0%。结论:尼群地平3种晶型具有不同的生物利用度。
Objective: To study the pharmacokinetics and bioavailability of nitrendipine in three kinds of rabbits. Methods: Different doses of nimodipine 80 mg · kg-1 were given to the rabbits at single-dose crossover. Plasma concentrations were determined by high performance liquid chromatography (HPLC). Pharmacokinetic parameters were calculated in non-compartmental models. Results: The C max values of (351.5 ± 18.7), (392.7 ± 50.8), (822.1 ± 39.7) μg.L-1 for nitrendipine crystal form Ⅰ, Ⅱ and Ⅲ were respectively 1.72 ± 0.16 and 1.83 ± (13.3 ± 3.5), (8.6 ± 1.2), (8.0 ± 1.2) h respectively; AUC0 → t was (3635.1 ± 230.8), (2697.0 ± 209.4) and ( 6428.6 ± 585.6) h.μg.L-1. The relative bioavailabilities of nitrendipine II and III to Form I were 62.1% and 169.0%, respectively. CONCLUSION: The three crystalline forms of nitrendipine have different bioavailability.