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植物药AM - 1、尼普立散和尼法丁对大鼠体内氯喹药代动力学的影响。

Effect of phytomedicines, AM-1, niprisan and nifadin on the pharmacokinetics of chloroquine in rats.

作者信息

Mustapha K B, Bakare-Odunola M T, Garba M, Obodozie O O, Enemali I S, Inyan U S

机构信息

National Institute for Pharmaceutical Research and Development, Idu, Abuja, Nigeria.

出版信息

Eur J Drug Metab Pharmacokinet. 2009 Jul-Sep;34(3-4):151-5. doi: 10.1007/BF03191166.

Abstract

The single oral dose pharmacokinetics of chloroquine was studied alone and after coadministration with phytomedicines NIPRID\92\001\1-1 (AM-1), Niprisan, and Nifadin in rats. Plasma chloroquine concentrations were measured using High performance liquid chromatography (HPLC) method developed earlier in our laboratory. The data were fitted into a WinNonlin standard non-compartmental programme. The co-administration of the herbal medicines with chloroquine produced decrease in the serum concentration of chloroquine at each sampling time. The highest decrease of 85% occurring at the time of peak concentration (1 h) was recorded with Nifadin, followed by 75% with Niprisan the least was 50% with AM-1. Significant reduction was also observed in some other parameters, such as area under the serum concentration- time curve (AUC(0-24)) and maximum serum concentration (Cmax) while the apparent volume of distribution (Vd) and elimination half-life (t 1/2beta) increased significantly (P< 0.05). It was concluded that the gastric presence of the herbal medicines significantly impaired the absorption of chloroquine in rats.

摘要

在大鼠中,单独研究了氯喹的单次口服药代动力学,并在与植物药NIPRID\92\001\1-1(AM-1)、Niprisan和Nifadin共同给药后进行了研究。使用我们实验室先前开发的高效液相色谱(HPLC)方法测量血浆氯喹浓度。数据被拟合到WinNonlin标准非房室程序中。草药与氯喹共同给药导致每个采样时间氯喹血清浓度降低。Nifadin在峰浓度(1小时)时出现的最大降幅为85%,其次是Niprisan的75%,AM-1的降幅最小,为50%。在其他一些参数中也观察到显著降低,如血清浓度-时间曲线下面积(AUC(0-24))和最大血清浓度(Cmax),而表观分布容积(Vd)和消除半衰期(t 1/2β)显著增加(P<0.05)。得出的结论是,草药在胃中的存在显著损害了大鼠体内氯喹的吸收。

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