吴茱萸对黄连生物碱在大鼠肠道吸收中的影响研究

Effect of Compatibility on Intestinal Absorption of Alkaloids in Fructus Evodiae and Rhizoma Coptidis in Rats

目的:研究吴茱萸对黄连中小檗碱和巴马汀在大鼠肠道吸收中的影响及其机制。方法:采用大鼠单向肠灌流模型,考察维拉帕米和吴茱萸提取物对小檗碱和巴马汀在各肠段吸收的影响,利用HPLC分别测定小檗碱和巴马汀的量,计算两种生物碱的肠吸收速率常数(Ka)和表观吸收系数(Papp)。结果:黄连提取物和吴茱萸提取物配比为6∶12时小檗碱和巴马汀的Ka和Papp显著增加。黄连生物碱单体化合物小檗碱、巴马汀与吴茱萸提取物6∶12配伍时,能明显促进小檗碱和巴马汀的吸收;6∶1配伍时,减弱小檗碱的吸收,促进巴马汀的吸收。P-糖蛋白(P-gp)抑制剂维拉帕米的存在均能促进小檗碱和巴马汀的吸收。结论:黄连配伍吴茱萸可促进黄连中小檗碱和巴马汀的肠吸收,其机制可能与抑制P-gp的活性有关。

Objective：To study the effect of compatibility with Fructus Evodiae on intestinal absorption of alkaloids in Rhizoma Coptidis and its mechanism in rats.Method： In situ single-pass perfused rat intestinal model was used and the concentrations of berberine and palmatine were determined by HPLC.The drug absorption rate constant（Ka） and apparent absorption coefficient（Papp） were tested to evaluate the effect of compatibility with verapamil or Fructus Evodiae on their absorption.Result： Rhizoma Coptidis extractive and Fructus Evodiae extractive（6∶12） can significantly enhance Ka and Papp of berberine and palmatine.Two alkaloids in Rhizoma Coptidis and Fructus Evodiae extractive（6∶12） promoted their intestine absorption.When the compatible proportion was 6∶1,the absorption of berberine decreased,and the absorption of palmatine increased.Verapamil had a promoting effect on the absorption of berberine and palmatine.Conclusion： Fructus Evodiae extractive can promote the intestine absorption of berberine and palmatine,and the mechanism may be related to its inhibition of P-glycoprotein activity.