摘要
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。
Doxophylline, a new antibronchospastic drug, being more active and less toxic than aminophyline, was detected by high performance thin layer chromatography. The pharmacokinetics of doxophylline have been characterized in rats, whose serum concentration were monitored after 100, 200, 400 mg·kg -1 oral dose. The drug was found to conform to a one compartment model and can be bio transformed quickly in rats. The C max, AUC and CL /F appeared to be dose dependent. T 1/2 (Ke) was 1 17±0 13 h after the 100 mg·kg -1 dose, 2 54±0 60 h after the 200 mg·kg -1 dose and 3 75±0 92 h after the 400 mg·kg -1 dose. The doxophylline concentration in tissues decreased rapidly. Total excretion of the drug in urine, bile and faeces was 5 2 per cent of the dose. Plasma protein binding was about 25 percent.
出处
《药学学报》
CAS
CSCD
北大核心
1997年第2期81-84,共4页
Acta Pharmaceutica Sinica
关键词
多索茶碱
药代动力学
高效薄层色谱法
解痉药
Doxophylline
Pharmacokinetics
High performance thin layer chromatography
