新型蒽环类衍生物HYY-014大鼠体内药代动力学和组织分布的研究
发布时间：2018-10-05 11:43
【摘要】：目的研究新型蒽环类衍生物HYY-014在大鼠体内的药代动力学和组织分布特征,为临床研究提供实验依据。方法大鼠单次尾静脉注射1.5 mg/kg的HYY-014后,采用LC-MS/MS法测定各时间点血浆和组织中HYY-014及其代谢物HYY-M3的浓度,药代动力学参数经DAS 3.0统计软件计算获得。结果采用统计矩方法处理药物浓度时间数据,HYY-014药代动力学参数Cmax、T1/2、Vd、CL、AUC0-t、MRT0-t分别为(1 628.6±618.6)μg/L、(24.4±3.6)h、(23.4±5.2)L/kg、(0.66±0.08)L/kg/h、(2 219.5±276.9)μg/L·h、(15.1±2.4)h;HYY-M3药代动力学参数Cmax、AUC0-t分别为(2.2±0.6)μg/L、(103.1±13.7)μg/L·h。静脉注射该药后,很快向机体的各组织广泛分布,且具有明显的靶向性,主要分布在脾、肾、肺、心脏、肝等组织,脑组织中浓度极低。结论静脉注射HYY-014组织分布广泛,具有明显的靶向性,肺、肝组织中的药物浓度均较高,不能通过血脑屏障。
[Abstract]:Objective to study the pharmacokinetics and tissue distribution of HYY-014, a novel anthracycline derivative, in order to provide experimental evidence for clinical study. Methods the concentration of HYY-014 and its metabolite HYY-M3 in plasma and tissue were determined by LC-MS/MS method after 1. 5 mg/kg HYY-014 was injected into rat tail vein. The pharmacokinetic parameters were calculated by DAS 3. 0 statistical software. 缁撴灉閲囩敤缁熻鐭╂柟娉曞鐞嗚嵂鐗╂祿搴︽椂闂存暟鎹，
本文编号：2253249
[Abstract]:Objective to study the pharmacokinetics and tissue distribution of HYY-014, a novel anthracycline derivative, in order to provide experimental evidence for clinical study. Methods the concentration of HYY-014 and its metabolite HYY-M3 in plasma and tissue were determined by LC-MS/MS method after 1. 5 mg/kg HYY-014 was injected into rat tail vein. The pharmacokinetic parameters were calculated by DAS 3. 0 statistical software. 缁撴灉閲囩敤缁熻鐭╂柟娉曞鐞嗚嵂鐗╂祿搴︽椂闂存暟鎹，
本文编号：2253249
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