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目的:研究国产尼索地平片的相对生物利用度、药动学特征及生物等效性。方法:采用随机、开放、2×2拉丁方设计试验,24名男性健康志愿者分别单剂量口服含尼索地平10mg的受试制剂及参比制剂。采用液-质联用法测定给药后不同时间的血药浓度,计算两者的药动学参数及评价其生物等效性。结果:24名健康志愿者口服尼索地平片受试制剂与参比制剂后的主要药动学参数:Cmax分别为(2.94±2.78)、(3.22±2.16)ng·mL-1,tmax分别为(1.70±1.00)、(1.40±1.00)h,t1/2分别为(6.81±4.11)、(5.55±2.35)h,AUC0～24分别为(10.60±7.70)、(9.90±6.76)ng.h.mL-1,AUC0～∞分别为(11.30±7.90)、(10.20±7.00)ng.h.mL-1。尼索地平片的相对生物利用度为(110.3±30.8)%。结论:经统计学分析,国产尼索地平片受试制剂与参比制剂具有生物等效性。
Objective: To study the relative bioavailability, pharmacokinetics and bioequivalence of domestic nisoldipine tablets. METHODS: Twenty-four male healthy volunteers were given a single oral dose of 10 mg nisoldipine test formulation and reference formulation, respectively, using a randomized, open, 2 × 2 Latin square design. The plasma concentration of different time after administration was determined by liquid chromatography-mass spectrometry. The pharmacokinetic parameters and the bioequivalence of the two drugs were calculated. Results: The main pharmacokinetic parameters of 24 healthy volunteers after oral administration of nisoldipine tablets were (2.94 ± 2.78) and (3.22 ± 2.16) ng · mL-1, respectively, with tmax (1.70 ± 1.00), (1.40 ± 1.00) h and t1 / 2 were (6.81 ± 4.11) and (5.55 ± 2.35) h respectively, and the AUC0-24 were (10.60 ± 7.70) and (9.90 ± 6.76) ng.h .mL-1, AUC0 ~ ∞ were (11.30 ± 7.90), (10.20 ± 7.00) ng.h.mL-1. The relative bioavailability of nisoldipine was (110.3 ± 30.8)%. Conclusion: The statistical analysis shows that the domestic nisoldipine tablets are bioequivalent to the reference preparations.