离体外翻肠囊法研究安石榴苷的大鼠肠吸收特性

Rat Intestine Absorption Characteristics of Punicalagins with Isolated Everted Intestine Model

摘要:

目的: 考察安石榴苷的肠吸收特性. 方法: 采用离体外翻肠囊法考察石榴皮多酚中安石榴苷在不同肠段(十二指肠、空肠、回肠、结肠)、不同质量浓度(153.34,301.70 mg·L^-1)下、不同时间点(0,30,60,90,120 min)的肠吸收特性,采用 HPLC法[YMC-Triart C₁₈色谱柱(4.6 mm×250 mm,5 μm);流动相 甲醇-0.1%磷酸]测定样品浓度. 结果: 随着药液中安石榴苷浓度的上升,肠吸收速率常数(Ka)也随之增加;安石榴苷在各个肠段的吸收无显著性差异,低浓度时,吸收速率常数回肠>结肠>空肠>十二指肠,高浓度时,空肠>结肠>回肠>十二指肠;各肠段累积吸收量均随药物质量浓度的增加而增加,在高浓度时,安石榴苷在二十指肠、空肠、回肠结肠的累积吸收量分别为(0.60±0.10),(0.64±0.59),(0.71±0.13),(0.73±0.11) μg·cm^-2. 结论: 安石榴苷在大鼠肠道内不存在特殊的“吸收窗”, 其吸收符合零级动力学方程.

Abstract:

Objective: To study the intestine absorption of punicalagins. Method: The isolated everted intestine model was used to study the absorption of different drug concentration(153.34,301.70 mg·L^-1)in different regions of rat intestine(duodenum,jejunum,ileum and colon), and different time(0,30,60,90,120 min).The sample was determined with HPLC on an YMC-Triart C₁₈ column(4.6 mm×250 mm,5 μm)with methanol-0.1%phosphoric acid. Result: The intestine absorption rate constant increased along with the increase in concentration of punicalagins.Absorption of index components for punicalagins in different intestinal segments had no significant difference,at low concentration, the absorption rate constant is ileum>colon>jejunum>duodenum, at high concentration, jejunum>colon>ileum>duodenum;every intestine segments cunmlative absorption increased along with concentration of punicalagins,at high concentration,every intestine segments cunmlative absorption of punicalagins is (0.60±0.10),(0.64±0.59),(0.71±0.13),(0.73±0.11) μg·cm^-2. Conclusion: Absorption of punicalagins didn't be a special ‘absorption window’, punicalagins intestinal absorption followed the Zero-order kinetic equation.