發(fā)布時間：2019-03-01 10:36

【摘要】：目的評價單次口服極低劑量甲磺酸伊馬替尼在中國男性健康受試者體內(nèi)的藥代動力學(xué)特征及安全性。方法 8名中國健康男性受試者給予單次口服甲磺酸伊馬替尼膠囊4 mg,用LC-MS/MS法測定給藥后不同時間甲磺酸伊馬替尼的血藥濃度并計算主要藥代動力學(xué)參數(shù)。結(jié)果受試者給予單次口服甲磺酸伊馬替尼膠囊4 mg后的主要藥代動力學(xué)參數(shù):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。本研究未觀察到不良事件和嚴重不良事件。結(jié)論伊馬替尼零期微劑量研究藥代動力學(xué)參數(shù)能夠在一定程度上反映藥物的分布和消除特點,且零期微劑量研究無任何臨床和實驗室不良事件發(fā)生,從保護受試者的角度具有特別的意義。
[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.
【作者單位】： 首都醫(yī)科大學(xué)附屬北京世紀(jì)壇醫(yī)院藥物Ⅰ期研究室;
【基金】：北京市科委課題“重大項目科技成果轉(zhuǎn)化落地培育”項目-腫瘤藥物臨床評價關(guān)鍵技術(shù)平臺建設(shè)基金資助項目(Z111100059411059) 北京市留學(xué)人員科技活動擇優(yōu)資助經(jīng)費(2014ZYZZ1)
【分類號】：R979.1

【共引文獻】

中國期刊全文數(shù)據(jù)庫 前10條

1 陳毅挺;蘇碧玲;黃露;林棋;;泛昔洛韋解離常數(shù)和結(jié)合常數(shù)的測定[J];分析測試技術(shù)與儀器;2011年01期

2 吳麗敏;張美玲;婁依依;李e，

本文編號：2432348