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喜树碱前体的药物动力学研究
引用本文:胡成久,周晓燕,张清民,顾学裘,夏东亚. 喜树碱前体的药物动力学研究[J]. 沈阳药科大学学报, 1990, 0(1)
作者姓名:胡成久  周晓燕  张清民  顾学裘  夏东亚
作者单位:北京:中国医学科学院药物研究所(胡成久),沈阳药学院药剂研究所(周晓燕,张清民,顾学裘),中国人民解放军沈阳军区总医院(夏东亚)
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。

关 键 词:喜树碱前体  药物动力学  血药浓度  组织分布

STUDIES ON THE PHARMACOKINETICS OF PRO-CAMPTOTHECIN
Hu Chengjiu,Zhou Xiaoyan,Zhang Qingmin,Gu Xueqiu. STUDIES ON THE PHARMACOKINETICS OF PRO-CAMPTOTHECIN[J]. Journal of Shenyang Pharmaceutical University, 1990, 0(1)
Authors:Hu Chengjiu  Zhou Xiaoyan  Zhang Qingmin  Gu Xueqiu
Affiliation:Hu Chengjiu,Zhou Xiaoyan,Zhang Qingmin,Gu Xueqiu,Institute of pharmaceuticsXia Dongya,General Hospital of Shenyang Command,PLA
Abstract:The pharmacokinetics of pro-camptothecin (A-CPT) in mice was studied withprecipitation-fluorescence method. The results showed that the plasma concentrationtime course of A-CPT in mice fitted in with a three-compartment open model. Thet1/2a, 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 were6.07×10~(-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 thatthe areas under the curve of tissue concentration time course within 24hs followingiv 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 (withcontents), lung, spleen, plasma and heart. The concentration time curve of mosttissues except stomach and intestine tended downwards monotoneously.
Keywords:Pro-camptothecin  Pharmacokinetics  Plasma concentration  Tissue distribution  
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