青木香及冠心苏合丸中马兜铃酸-I和 -II 在大鼠血清的药代动力学研究

青木香及冠心苏合丸中马兜铃酸-I和 -II 在大鼠血清的药代动力学研究

白玛卓玛, 杨东辉^*, 俞捷, 王璇, 蔡少青

北京大学药学院天然药物学系, 北京 100191

收稿日期:2008-11-12 修回日期:2009-02-10 出版日期:2009-03-15 发布日期:2009-03-15
通讯作者: 杨东辉*

Pharmacokinetics studies of aristolochic acid-I and -II in rats after intragastrical administration of Radix Aristolochiae and Muskone

Pema Dolma, Dong-Hui Yang^*, Jie Yu, Xuan Wang, Shao-Qing Cai

Department of Natural Medicines, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China

Received:2008-11-12 Revised:2009-02-10 Online:2009-03-15 Published:2009-03-15
Contact: Dong-Hui Yang*

摘要/Abstract

摘要：

比较了大鼠分别灌胃给予青木香生药混悬液和含有等量青木香的冠心苏合丸生药混悬液后马兜铃酸-I (AA-I) 和 -II (AA-II) 在大鼠血清的药代动力学参数。AA-I和 AA-II在大鼠血清中的浓度变化情况符合血管外给药二室模型。灌胃给药冠心苏合丸和青木香后AA-I 的消除半衰期分别为1573.2 min和475.8 min; AA-I的消除半衰期分别为2344.8 min 和427.8 min。AA-I 的曲线下面积分别为13.07 μg/h/mL和3.86 μg/h/mL; AA-II的曲线下面积分别为67.67 μg/h/mL和23.93 μg/h/mL。研究结果表明, 与单独灌胃给药青木香相比, 灌胃冠心苏合丸后大鼠血清中AA-I 和 AA-II的消除半衰期明显延长, 药时曲线下面积明显增加。

Abstract: The pharmacokinetic parameters of aristolochic acid-I (AA-I) and -II (AA-II) in rat serum after intragastrical administration of the crude drug powders of Radix Aristolochiae (RA) and Muskone containing equal amounts of RA were compared. The pharmacokinetic profiles of AA-I and AA-II could be fitted with a two-compartment model. The elimination half time (T1/2β) of AA-I in Muskone was 1573.2 min and that of AA-I in RA was 475.8 min; T1/2β of AA-II in Muskone was 2344.8 min and that of AA-II in RA was 427.8 min. The area under the concentration-time curve (AUC) of AA-I in Muskone was 13.07 μg/h/mL and that of AA-I in RA was 3.86 μg/h/mL; AUC of AA-II in Muskone was 67.67 μg/h/mL and that of AA-II in RA was 23.93 μg/h/mL. The bioavailabilities of AA-I and AA-II in Muskone were markedly increased compared with that in RA based on the elimination half-time and AUC values.

Key words: Aristolochiae Radix, Aristolochiae Radix, Muskone, Muskone, Aristolochic acid-I, Aristolochic acid-I, Aristolochic acid-II, Aristolochic acid-II, Pharmacokinetics, Pharmacokinetics

中图分类号:

R969.1

Supporting: Foundation items: The 10^th Five Years Programs for Science and Technology Development of China (Grant No. 2004BA721A10), National Natural Science Foundation of China (Grant No.30371748).
^*Corresponding author. Tel./fax: 86-10-82802534

白玛卓玛, 杨东辉^*, 俞捷, 王璇, 蔡少青

青木香及冠心苏合丸中马兜铃酸-I和 -II 在大鼠血清的药代动力学研究

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Pema Dolma, Dong-Hui Yang^*, Jie Yu, Xuan Wang, Shao-Qing Cai

Pharmacokinetics studies of aristolochic acid-I and -II in rats after intragastrical administration of Radix Aristolochiae and Muskone

[J]. .