摘要
目的 研究关木通及其复方制剂龙胆泻肝丸 (水丸 )中马兜铃酸A在大鼠体内的药动学特征 ,观察马兜铃酸A在大鼠体内吸收、分布、消除的规律 ,为探索马兜铃酸A的毒副作用提供参考。方法 将 12只SD大鼠随机分为两组 ,每组 6只 ,即刻用乙醚轻度麻醉 ,行颈动脉插管术 ,按 6mg·kg 1 马兜铃酸A的剂量灌胃给予含相同量马兜铃酸A的关木通提取液和龙胆泻肝丸 (水丸 )提取液 ,分别于 0 ,10 ,15 ,2 0 ,3 0 ,45 ,60 ,90 ,12 0 ,15 0min经颈动脉导管取血 0 5mL ,采用反相高效液相色谱 (RP HPLC)法测定血浆中马兜铃酸A的含量 ,比较两组大鼠血浆中马兜铃酸A的含量。结果 大鼠灌胃后 ,关木通和龙胆泻肝丸 (水丸 )中的马兜铃酸A的代谢符合一室模型 ,龙胆泻肝丸 (水丸 )中马兜铃酸A的血药浓度曲线下面积 (AUC)和最大血药浓度 (Cmax)与关木通中马兜铃酸A比较明显降低。结论 龙胆泻肝丸 (水丸 )中共存组分对马兜铃酸A的吸收可能有抑制作用。
Objective To study in the rat the pharmacokinetics of aristolochic acid A (AAA) in Caulis Aristolochiae Manshuriensis and longdanxiegan pills, that is to survey the general pattern of absorption, distribution and elimination of AAA so as to provide references for the rational use of AAA in the clinical practice and revelation of its toxic side effects. Methods 12 SD rats were randomly divided into 2 groups, with 6 animals in each group. Carotid cannulation was performed under low-grade ether anesthesia. Rats of the 2 groups were given each by gastrogavage 6 mg·kg -1 of AAA which was separately contained in extracts of Caulis Aristolochiae Manshuriensis and longdanxiegan pills.0.5 mL of blood per rat was taken from the carotid cannula 0, 10, 15, 20, 30, 45, 60, 90, 120, 150 min, respectively, after the beginning of the experiment. Blood plasma was separated and plasma concentrations of AAA were determined with RP-HPLC. Contents of AAA in blood plasma samples from animals of the 2 groups were compared. Results The AAA metabolism in Caulis Aristolochiae Manshuriensis and longdanxiegan pills after gastrogavage in rats accorded with the one compartment model. The area under the concentration-temperature curve(AUC) and maximum concentration(C max) of AAA in longdanxiegan pills were significantly smaller and lower, respectively, than those of AAA in Caulis Aristolochiae Manshuriensis. Conclusion The co-existing component in longdanxiegan pills may have an inhibitory effect on the absorption of AAA.
出处
《医药导报》
CAS
2005年第2期116-118,共3页
Herald of Medicine
