中国中药杂志

2005, (18) 1458-1461

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健康志愿者口服大黄制剂后大黄酸在人体内的药代学研究
The pharmacokinetics of rhein in 12 healthy volunteers after oral administration of rhubarb extract

朱伟,张莉,王学美,王保秀,李晓晔
ZHU Wei~(1), ZHANG Li~(2), WANG Xue-mei~(1), WANG Bao-xiu~(3), LI Xiao-ye~(2) (1. Institute of Integrated Traditional and Western Medicine of Peking University First Hospital, Beijing 100034, China; 2. Department of Chemistry, Fourth Military Medical University of China, Shanxi 710032, China;3. Department of Pharmacology, Zhejiang Pharmacology College, Zhejiang 315010,China)

摘要(Abstract):

目的:研究健康志愿者口服大黄制剂后大黄酸在人体内的药代学过程。方法:12名健康自愿者单次口服大黄制剂(50mg.kg-1),分别在服药0,0.083,0.5,1,1.5,2,3,4,5,7,10h后11个不同时间点取静脉血,血药浓度采用高效液相色谱法(HPLC)测定,药代学参数采用3P97程序计算。结果:人口服大黄制剂后,大黄酸以很快的速度从肠道被吸收入血。其主要药代学参数为最大血药浓度(Cmax)(3.20±1.08)μg.mL-1;最大浓度时间(tmax)(1.03±0.41)h;分布半衰期(t1/2α)(0.21±0.02)h;消除半衰期(t1/2β)(2.68±1.09)h;平均滞留时间(MRT)(5.31±1.78)h;药时曲线下面积(AUC0-∞)(1573.08±366.48)μg.mL-1.min-1。结论:大黄制剂口服后大黄酸能迅速被人体吸收,其药代学符合二室模型。
Objective: To study the pharmacokinetics of rhein in 12 healthy volunteers after oral administration of rhubarb extract. Method: The blood sample were obtained at 0,0.083,0.5,1,1.5,2,3,4,5,7,10 h after a single dose oral administration of rhubarb extract(50 mg·kg~(-1)). The plasma rhein concentration was determined by HPLC. The pharmacokinetics of rhein were analysed by 3P97 program. Result: The absorption of rhein was very fastafter oral administration of rhubarb extract in the healthy volunteers. The main pharmacokinetic parameters of rhein were C_(max) (3.20±1.08) μg·mL~(-1); t_(max) (1.03±0.41) h; t_(1/2α)(0.21±0.02) h; t_(1/2β)(2.68±1.09) h; MRT(5.31±1.78) h; AUC_(0-∞) (1 573.08±366.48) μg·mL~(-1)·min~(-1), respectively. Conclusion: Rhein could be absorbed rapidly and its pharmacokinetics was consistent with two-compartment model.

关键词(KeyWords): 大黄酸;药代学;血浆
rhein; pharmacokinetics; plasma

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作者(Author): 朱伟,张莉,王学美,王保秀,李晓晔
ZHU Wei~(1), ZHANG Li~(2), WANG Xue-mei~(1), WANG Bao-xiu~(3), LI Xiao-ye~(2) (1. Institute of Integrated Traditional and Western Medicine of Peking University First Hospital, Beijing 100034, China; 2. Department of Chemistry, Fourth Military Medical University of China, Shanxi 710032, China;3. Department of Pharmacology, Zhejiang Pharmacology College, Zhejiang 315010,China)

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