摘要
用沉淀荧光法研究了喜树碱前体(A-CPT)在小鼠体内的药物动力学,结果表明,A-CPT在小鼠体内的血药浓度经时过程符合三隔室开放模型。其α、β及γ相的半衰期分别为1.8,64.5及852min;Vc及Vd分别为4.63×1O^(-3)及O.741,Cl及AUC分别为6.07×10^(-4)l/min及2082μg·min/ml;MRT为999min。组织分布研究表明,静脉注射给药后24h内的组织浓度时间曲线下面积按照肠(含内容物),骨(含髓),肾,脑,肝(含胆),胃(含内容物)肺,脾,血及心的顺序依次递减。除胃、肠的组织浓度时间曲线有浓度峰以外,其它组织的浓度时间曲线呈单调下降的趋势。
The pharmacokinetics of pro-camptothecin (A-CPT) in mice was studied with
precipitation-fluorescence method. The results showed that the plasma concentration
time course of A-CPT in mice fitted in with a three-compartment open model. The
t1/2a, t1/2b, and t1/2r of A-CPT were 1.8min, 64 5rain and 852min respectively.
The Vc and Vd were 4.63×10^(-3)1 and 0 7461 respectively The CL and AUC were
6.07×10^(-4)1/min and 2082/μg. min/ml respectively. The MRT was 999min.
The result of our study on the tissue distribution of A-CPT demonstrated that
the areas under the curve of tissue concentration time course within 24hs following
iv A-CPT 20mg/kg (AUC_0^(24)) decreased in the following order, intestine (with con-
ten), bone (with marrow), Kidney, brain, liver (with gallbladder), stomach (with
contents), lung, spleen, plasma and heart. The concentration time curve of most
tissues except stomach and intestine tended downwards monotoneously.
