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的零期临床研究

发布时间：2019-03-01 10:36

【摘要】：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。
[Abstract]:Objective To evaluate the pharmacokinetics and safety of imatinib mesylate in Chinese male healthy subjects. Methods Eight Chinese healthy male subjects were given a single oral dose of imatinib mesylate 4 mg, and the plasma concentrations of imatinib mesylate were measured with LC-MS/ MS method at different times and the main pharmacokinetic parameters were calculated. Results The subject was given the main pharmacokinetic parameters following a single oral administration of imatinib capsules 4 mg: Cmax (12.70-6.61) ng 路 m L-1, tmax (1.94-0.94) h, AUC0-24h (90.10-37.70) ng 路 m-L-1 路 h, t1/2 (10.40-5.01) h, CL/ F (47.20-33.40) L 路 h-1, V/ F (541.00-128.00) L, MORT (7.21-1.30) h. Adverse events and serious adverse events were not observed in this study. Conclusion The pharmacokinetic parameters of the imatinib zero-phase microdose study can reflect the distribution and elimination of the drug to some extent, and there is no clinical and laboratory adverse event in the zero-phase microdose study, which is of particular significance in protecting the subject's angle.
【作者单位】： 首都医科大学附属北京世纪坛医院药物Ⅰ期研究室;
【基金】：北京市科委课题“重大项目科技成果转化落地培育”项目-肿瘤药物临床评价关键技术平台建设基金资助项目(Z111100059411059) 北京市留学人员科技活动择优资助经费(2014ZYZZ1)
【分类号】：R979.1

【共引文献】

中国期刊全文数据库 前10条

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2 吴丽敏;张美玲;娄依依;李e，

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