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目的:研究盐酸西布曲明滴丸在健康人体的药动学和相对生物利用度并求证其生物等效性。方法:男性健康志愿者20名,随机交叉单剂量口服受试制剂盐酸西布曲明滴丸和参比制剂盐酸西布曲明胶囊各15mg,采用高效液相色谱-质谱联用法测定血浆中西布曲明的活性代谢产物之一双去甲基西布曲明的浓度。计算药动学参数和相对生物利用度,评价其生物等效性。结果:口服受试和参比制剂后的主要药动学参数经统计矩参数计算:试验制剂t1/2为(20.8±6.0)h和(21.2±6.2)h;tmax为(4.2±1.0)h和(4.8±1.2)h;Cmax为(7.3±2.1)μg.L-1和(7.6±2.0)μg.L-1;AUC0-96h为(159.5±56.4)μg.h.L-1和(168.4±57.3)μg.h.L-1。受试制剂与参比制剂比较的相对生物利用度F为(96.4±18.2)%。结论:两制剂具有生物等效性。
OBJECTIVE: To study the pharmacokinetics and relative bioavailability of sibutramine hydrochloride droppill in healthy human and to verify its bioequivalence. Methods: Twenty healthy male volunteers were randomized to receive a single oral dose of sibutramine hydrochloride (15 mg / kg) and reference drug sibutramine hydrochloride (15 mg) respectively. Plasma sibutramine was determined by high performance liquid chromatography-mass spectrometry The concentration of one of the active metabolites of demycinated sibutramine. Pharmacokinetic parameters and relative bioavailability were calculated and their bioequivalence was evaluated. Results: The main pharmacokinetic parameters after oral administration and reference formulation were calculated by the statistical moment parameters: t1 / 2 was (20.8 ± 6.0) h and (21.2 ± 6.2) h, tmax was (4.2 ± 1.0) h And (4.8 ± 1.2) h respectively; Cmax was (7.3 ± 2.1) μg.L-1 and (7.6 ± 2.0) μg.L-1; AUC0-96h was (159.5 ± 56.4) μg.hL- 57.3) μg.hL-1. The relative bioavailability, F, of the test formulation versus the reference formulation was (96.4 ± 18.2)%. Conclusion: The two preparations are bioequivalent.