二聚细辛醚药代动力学研究

二聚细辛醚是具有降脂作用的新成分,小鼠和大鼠ig、iv后,血中放射性—时间曲线符合开放二室模型。ig和iv后的平均t 1/2β:小鼠分别为107.1±7h、107.5±5h;大鼠101±7.9h、102.9±6.4h。Vd:小鼠为11.9±2.3L/kg、7.9±3.7L/kg;大鼠5.0±0.21/kg、6.0±3.4L/kg。该药吸收快,分布迅速、广泛,体内消除较缓慢。21d内从尿和粪中排泄分别为96.7％和1.02％。血浆蛋白结合率为48％。尿液提取物经TLC放射自显影和液体闪烁仪测定结果主要以原形药物排出,并有代谢产物。

A STUDY ON PHARMACOKINETICS AND MATABOLISM OP (~3H) BISASARICIN

Bisasaricin is a new antihyperlipidemic constituent. After ig and iv use in mice and rats, the decline of radioactivity in the plasma showed a biphasic curve. Mean half-life ( T1/2 β) was 107.1 ± 7h(ig) and 107.5±5h ( iv ) for mice, 101.0±7.9h ( ig ) and 102.9±6.4h (iv) for rats, respectively. The mean Volume of distribution (Vd ) was 11.9±2.3L/kg (ig) and 7.9±3.7 L/kg (iv) for mice, 5.0±0.2L/kg ( ig ) and 6.0±3.4 L/kg (iv) for rats, respectively. [3H]bisasaricin given intragastrically was readily absorbed from the gut of mice and rats, and rapidly taken up by various organs. The radioactivity in organs was eliminated slowly. In 21 d, cumulative excretion of radioactivity in urine was 96.7% of the total dose, while that in feces was 1.2%. The rate of binding with plasma protein was 48%. Upon measurement by TLC autoradiography and liquid scintillation counting was found to consist mainly of the drug in its original form with some of its metabolites.