3-正丁基苯酞大鼠在体肠吸收动力学

Absorption Kinetics of 3-n-butylphthalide in Intestines of Rats

摘要:

目的: 研究3-正丁基苯酞(NBP)在大鼠各肠段的吸收动力学特征。 方法: 采用大鼠在体肠段灌流实验,利用紫外分光光度法和HPLC法分别测定酚红和3-正丁基苯酞的量,分别研究药物质量浓度和羟丙基-β-环糊精(HPCD)用量对3-正丁基苯酞吸收的影响。 结果: 在1,10,100 mg·L^-1药物质量浓度对各肠段的表观吸收系数(P_app)无明显影响;灌流液中随HPCD用量的增加对NBP在大鼠肠黏膜的吸收抑制作用增强。 结论: NBP在各肠段的吸收均呈被动扩散机制,NBP在各肠段均有较好的吸收;HPCD的加入对NBP在大鼠肠黏膜的吸收具有较强的抑制作用。

Abstract:

Objective: To investigate the absorption kinetics of 3-n-butylphthalide(NBP) in intestines of rats. Method: The intestine in rat was cannulated for in situ perfusion. UV and HPLC were used to determine the concentration of phenolsulfonphthalein and NBP, respectively. The effect of drug concentration and hydroxypropyl cyclodextrin(HPCD) on the absorption had been studied. Result: When the NBP concentration of perfusion solution was increased, no specific absorption was founded in different segment. The P_app for NBP decreased when HPCD was co-perfused in the intestine. Conclusion: Passive diffusion dominates the absorptive transport behavior of NBP. NBP is well absorbed at all segments of intestine in rats. HPCD can inhibit the absorption of NBP in the intestinal segment.