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利用人源结肠腺癌细胞系Caco-2细胞单层模型,研究了脉君安片中主要降压活性成分葛根素、钩藤碱与氢氯噻嗪配伍使用前后对氢氯噻嗪体外吸收与转运的影响,探讨了氢氯噻嗪与葛根素、钩藤碱配伍使用时在吸收阶段的药物相互作用。结果表明,氢氯噻嗪在Caco-2单层细胞模型中的吸收可能存在由载体介导的主动转运,葛根素能减少P-糖蛋白(P-gp),对氢氯噻嗪的外排,钩藤碱对氢氯噻嗪的吸收转运无显著影响,葛根素、钩藤碱与氢氯噻嗪合用能增强氢氯噻嗪的吸收。同时,实验还发现氢氯噻嗪可能是P-gp的作用底物,且pH值对氢氯噻嗪的转运有重要影响,在弱酸性条件下,氢氯噻嗪的吸收比在中性条件下好。
The human colon adenocarcinoma cell line Caco-2 cell monolayer model was used to study the effects of puerarin on the in vitro absorption and transport of hydrochlorothiazide before and after the combination of puerarin, rhynchophylline and hydrochlorothiazide. Hydrochlorothiazide and puerarin, rhynchophylline compatibility when used in the absorption phase of drug interactions. Hydrochlorothiazide in the Caco-2 monolayer cell model may exist by the carrier-mediated active transport, puerarin can reduce P-glycoprotein (P-gp), the hydrochlorothiazide efflux of rhynchophylline on hydrochlorothiazide Absorption and transport had no significant effect, puerarin, rhynchophylline and hydrochlorothiazide can enhance the absorption of hydrochlorothiazide. Hydrochlorothiazide was also found to be the substrate of P-gp, and the pH value had an important influence on the transshiurenicity of hydrochlorothiazide. Hydrochlorothiazide showed a better absorption under neutral conditions than that under neutral conditions.