16^#化合物药代动力学研究

The Study of Pharmacokinetics for 16^#

目的16^#化合物的药代动力学性质．方法采用液-液萃取生物样品，反相高效液相色谱-紫外检测定量分析16^#化合物，Extend—C18色谱柱（4．6mm×250mm，5μm），流动相为乙腈-水（37：63）[含2．5％（V／V）的NaH2PO4，0．08％（V／V）的三乙胺]，流速0．8mL／min，检测波长265nm．结果大鼠腹腔注射16^#化合物后，Tmax在3～8min，消除半衰期t1／2β约70min．糖尿病模型大鼠腹腔注射16^#化合物后，体内过程表现为一室模型，血药浓度达峰时间推迟，Tmax约15min；Cmax降低，体内消除加快．结论在5—20mg／kg剂量范围内16^#在大鼠体内过程为线性动力学，符合一级吸收二室模型．

Objective To know the pharmacokinetics character of 16^#. Methods established a method for the analysis of 16^# in rat blood, samples was deal with liquid- liquid extraction, then detect it with HPLC - UV, Using Extend- C18 column （4. 6 mm ×250mm,5μm）. The mobile phase consisting of Acetonitrile- water （35 ： 65） [ containing 2.5% （V/V） NaH2PO4, 0. 08% （V/V） triethylamine ], a flow rate of 0. 8 mL/min and detected at 265 nm. Results After ip 16^# in rat, Tmax is 3 -8 min, t1/2β is about 70 min. When ip 16^# in diabetic rat, it is one- compartment model, Tmax is extended, about 15 min. The speed of metabolism speeds up. It can＇ t be detected when 2 h, but normal rat can be done when 4 h with same dosage. Conclusion it belongs to linearity kinetics at the dosage range from 5 - 20 mg/kg, the pharmacokinetic model is 2 - compartment model.