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甲氨碟呤多相脂质体药物动力学和药物分布的研究
引用本文:万建胜,陶钧,马竹卿,顾学裘.甲氨碟呤多相脂质体药物动力学和药物分布的研究[J].沈阳药科大学学报,1989(2).
作者姓名:万建胜  陶钧  马竹卿  顾学裘
作者单位:沈阳药学院药剂研究室 (万建胜,陶钧),上海市长宁区中心医院 (马竹卿),沈阳药学院药剂研究室(顾学裘)
摘    要:采用荧光法测定血和织组中MTX含量,用阻尼非线性最小二乘法及矩量法处理和比较MTX多相脂质体(PL—MTX)及MTX水溶液(F-MTX),尾静脉一次给药18mg/kg后,9hr内小鼠体内的药物动力学和药物分布。得到PL-MTX的药-时曲线为:C(μg)=30.5e~(-3.771)+3.27e~(0.381),具有开放二房室模型特征,清除率Cl:为927ml/h,血药平均滞留时间MRT为100min;F-MTX的药-时曲线为:C(μg)=39.7e~(-13.2t)+15.1e~(-2.77t)+0.633e~(-0.216t),具有开放三房室模型特征,Cl_s为1579ml/h,MRT为57min。两者结果存在显著差异。另外,PLMTX较F-MTX在脾、肺、肝、骨髓的药量分布有显著提高。表明多相脂质体剂型可能增加化疗药物在上述器官为病灶的癌细胞的药物浓度。

关 键 词:甲氨喋呤  药物动力学  体内分布  房室模型

A STUDY ON PHARMACOKINETICS AND DRUG DISTRIBUTION OF MTX POLYPHASE LIPOSOME
Wan Jiansheng,Tao Jun,Ma Zhuqing,Gu Xueqiu Shenyang College of Pharmacy,Pharmaceutical Research Lab Shanghai Changning District Centrall Hospital.A STUDY ON PHARMACOKINETICS AND DRUG DISTRIBUTION OF MTX POLYPHASE LIPOSOME[J].Journal of Shenyang Pharmaceutical University,1989(2).
Authors:Wan Jiansheng  Tao Jun  Ma Zhuqing  Gu Xueqiu Shenyang College of Pharmacy  Pharmaceutical Research Lab Shanghai Changning District Centrall Hospital
Abstract:In this paper, a comparison of Pharmacokinetics and drug distribution afterintravenous injection of both PL-MTX and F-MTX into L615 mice is reported.The results show PL-MTX and F-MTX plasma drug concentration-time curvesreflected two and three compartmental characterristics, respectively. PL-MTX canmaintain plasma drug concentration at higher level and for a longer time thanF-MTX. The amount of MTX in spleen, lung, bone marrow was found signifi-cantly higher after injection of PL-MTX than F-MTX.This implies that PL-MTXprobably has some advantages over F-MTX in the treatment of leukemias.
Keywords:Methotrexate  Polyphase liposome  Pharmacokinetics  Compartment model  Body distribution
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