论文部分内容阅读
目的研究千金子甾醇在Caco-2细胞单层模型中的吸收和转运。方法用Caco-2细胞模型研究千金子甾醇在Caco-2细胞模型中的双向转运,考察时间、药物浓度和P-糖蛋白抑制剂对千金子甾醇跨膜转运的影响。采用UPLC-MS/MS法测定药物浓度,计算表观渗透系数(Papp)以及表观渗透率(PDR)。结果在Caco-2细胞中的转运过程中,不同浓度千金子甾醇的Papp值介于1×10-6~1×10-5,其累积转运量随时间和浓度的增加而增加,具有浓度依赖性。10、30、50μmol/L千金子甾醇的PDR分别为1.35、0.83、0.65。盐酸维拉帕米可以促进千金子甾醇由AP侧→BL侧的转运。结论千金子甾醇在肠道中的吸收中等,以被动转运为主,可能存在肠道转运蛋白的外排机制。
OBJECTIVE: To study the absorption and transport of semitoerythritol in a monolayer model of Caco-2 cells. Methods The Caco-2 cell model was used to study the bidirectional transport of sesto sterol in Caco-2 cell model. The effects of time, drug concentration and P-glycoprotein inhibitors on the transmembrane transport of sesquiterpene sterol were investigated. The drug concentration was determined by UPLC-MS / MS, and the apparent permeability coefficient (Papp) and apparent permeability (PDR) were calculated. Results During the translocation of Caco-2 cells, the Papp values of different concentrations of cadmium sterol ranged from 1 × 10-6 to 1 × 10-5, and their cumulative transport volume increased with time and concentration, with a concentration-dependent Sex. The PDR of 10, 30 and 50μmol / L cadmium sterol were 1.35, 0.83 and 0.65 respectively. Verapamil Hydrochloride can promote the transfer of the trichostatin from the AP side to the BL side. Conclusions Chrysogenum is moderately absorbed in the intestine and mainly undergoes passive transport. The efflux mechanism of intestinal transporter may exist.