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为全面了解多索茶碱在大鼠体内代谢情况,用高效薄层色谱法和光密度扫描法,给大鼠ig多索茶碱后,测定在不同时间各组织和体液中多索茶碱的含量。结果表明,多索茶碱在大鼠体内药代动力学为一室模型并能在体内迅速转化为其它代谢产物。T1/2(Ke)为117~375h,达峰时间T(peak)为072~146h,Cmax,AUC及CL/F呈剂量依赖关系。给药1h,以胃壁浓度最高,8h除胃肠组织浓度降低较慢外,其它组织中药物浓度明显降低。尿、粪及胆汁中原形药总排出量占给药量的52%。血浆蛋白结合率约25%。提示多索茶碱在体内可能转化为其它代谢产物。
To fully understand the metabolism of doxofylline in rats, the content of doxofylline in various tissues and body fluids at different times was determined by high performance thin layer chromatography and optical densitometry, . The results show that the pharmacokinetics of doxofylline in rats as a one-compartment model and can be rapidly transformed into other metabolites in the body. T1 / 2 (Ke) was 117 ~ 375h, peak time was 072 ~ 146h, and Cmax, AUC and CL / F were dosedependent. Administration of 1h, the highest gastric wall concentration, 8h except gastrointestinal tissue concentration decreased slower, the concentration of other tissues significantly decreased. Urine, manure and bile in the total amount of prototype drugs accounted for 5 2% of the dose. Plasma protein binding rate of about 25%. Tip Doxofylline may be converted to other metabolites in the body.