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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。
The contents of MTX in blood and tissue were determined by fluorescence method. The MTX multi-phase liposomes (PL-MTX) and MTX solution (F-MTX) Pharmacokinetics and drug distribution in mice after 18 mg / kg, 9 hr. The drug-time curve of PL-MTX was: C (μg) = 30.5e ~ (-3.771) + 3.27e ~ (0.381), with an open two compartment model, clearance rate Cl: 927ml / The retention time of MRT was 100 min. The drug-time curve of F-MTX was: C (μg) = 39.7e ~ (-13.2t) + 15.1e ~ (-2.77t) + 0.633e ~ (-0.216t) Three-chamber model features, Cl_s 1579ml / h, MRT 57min. There are significant differences between the two results. In addition, PLMTX significantly increased the dose distribution of F-MTX in spleen, lung, liver and bone marrow. Indicating that heterogeneous liposomal dosage forms may increase the drug concentration of chemotherapeutic drugs in cancer cells of the lesion as above.