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目的评价单次口服极低剂量甲磺酸伊马替尼在中国男性健康受试者体内的药代动力学特征及安全性。方法 8名中国健康男性受试者给予单次口服甲磺酸伊马替尼胶囊4 mg,用LC-MS/MS法测定给药后不同时间甲磺酸伊马替尼的血药浓度并计算主要药代动力学参数。结果受试者给予单次口服甲磺酸伊马替尼胶囊4 mg后的主要药代动力学参数:Cmax(12.70±6.61)ng·m L-1,tmax(1.94±0.94)h,AUC0-24 h(90.10±37.70)ng·m L-1·h,t1/2(10.40±5.01)h,CL/F(47.20±33.40)L·h-1,V/F(541.00±128.00)L,MRT(7.21±1.30)h。本研究未观察到不良事件和严重不良事件。结论伊马替尼零期微剂量研究药代动力学参数能够在一定程度上反映药物的分布和消除特点,且零期微剂量研究无任何临床和实验室不良事件发生,从保护受试者的角度具有特别的意义。
Objective To evaluate the pharmacokinetics and safety of a single oral low dose of imatinib mesylate in healthy male Chinese subjects. Methods Eight Chinese healthy male volunteers were given 4 mg imatinib mesylate orally. The plasma concentrations of imatinib mesylate at different time points after administration were determined by LC-MS / MS and calculated The main pharmacokinetic parameters. RESULTS: The main pharmacokinetic parameters of 4-mg imatinib mesylate capsules administered to subjects were Cmax (12.70 ± 6.61) ng · m L-1, tmax (1.94 ± 0.94) h, AUC0- 24 h (90.10 ± 37.70) ng · m L-1 · h, t1 / 2 (10.40 ± 5.01) h and CL / F (47.20 ± 33.40) L · h-1, V / F MRT (7.21 ± 1.30) h. No adverse events or serious adverse events were observed in this study. Conclusion The imatinib zero-period micro-dose study pharmacokinetic parameters can reflect the distribution and elimination characteristics of the drug to some extent, and the zero-period micro-dose study without any clinical and laboratory adverse events, from protecting the subjects Angle has special meaning.