發(fā)布時(shí)間：2019-03-01 10:36

【摘要】：目的評價(jià)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(dòng)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(shí)間甲磺酸伊馬替尼的血藥濃度并計(jì)算主要藥代動(dòng)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(dòng)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(yán)重不良事件。結(jié)論伊馬替尼零期微劑量研究藥代動(dòng)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(diǎn),且零期微劑量研究無任何臨床和實(shí)驗(yàn)室不良事件發(fā)生,從保護(hù)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(xiàng)目科技成果轉(zhuǎn)化落地培育”項(xiàng)目-腫瘤藥物臨床評價(jià)關(guān)鍵技術(shù)平臺(tái)建設(shè)基金資助項(xiàng)目(Z111100059411059) 北京市留學(xué)人員科技活動(dòng)擇優(yōu)資助經(jīng)費(fèi)(2014ZYZZ1)
【分類號】：R979.1

【共引文獻(xiàn)】

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