脱氢卡维丁的肠道转运特性研究

Intestinal transport characteristics of dehydrocavidine

目的研究岩黄连生物碱中主要活性成分脱氢卡维丁的肠道转运特性。方法采用外翻肠囊模型,以单位面积渗透量及表观渗透系数为指标,研究不同质量浓度岩黄连生物碱中脱氢卡维丁在大鼠不同肠段的转运特性;采用Ca-co-2细胞单层模型研究脱氢卡维丁的双向跨膜转运行为及盐酸维拉帕米对其转运的影响。结果脱氢卡维丁在大鼠不同肠段部位的离体肠囊上均有转运,试验质量浓度下同一部位肠段的表观渗透系数无显著性差异;脱氢卡维丁在Ca-co-2细胞单层的双向转运存在显著性差异,加入盐酸维拉帕米后,吸收渗透系数显著增大。结论脱氢卡维丁的肠黏膜转运存在转运蛋白的外排机制,但在较高浓度范围内呈现被动转运特征。

AIM To study the intestinal transport mechanism of dehydrocavidine which was the active constituent of alkaloids of Corydalis saxicola Bunting. METHODS Based on the cumulative permeation quantity per unit area and apparent permeability coefficient （Papp） as index, everted intestinal sac method was used to study the transport characteristics of different concentrations of dehydrocavidine at different intestine segments in rats. Caco-2 monolayer was applied to the bi-directional transport of dehydrocavidine as compared with P-gp inhibitor verapamil hydrochloride. RESULTS Transport of dehydrocavidine was carried out in vitro at different intestine segments, and there was no significant difference on Papp among different concentrations tested. The bi-directional transport of dehydrocavidine in Caco-2 monolayer model showed significant difference, and the PAn increased remarkably when verapamil hydrochloride was added. CONCLUSION The intestinal transport of dehydrocavidine may be related to efflux mechanism of transporters and characteristic of passive transport in the higher concentration range.