Song Bei, Zhu Jingjing, Wang Weihao, Hu Guang, Song Xiaomei, Wang Zhimin
Shaanxi University of Chinese Medicine, Xi'an 712046, China.
Zhongguo Zhong Yao Za Zhi. 2012 Apr;37(7):969-73.
To establish a method for quickly investigating the absorption ingredients which could be used as the index of quality control of Gentianae Radix et Rhizoma.
The absorption ingredients of Gentianae Radix et Rhizoma were investigated by using the model of in vitro everted intestinal sac (VEIS). The intestinal sac liquors of jejunum and ileum were collected at 6 intervals (15, 30, 45, 60, 90, 120 min) and gentiopicroside, loganin acid, swertiamarin and sweroside were detected by HPLC as the representative marker. The accumulative absorption quantity of gentiopicroside, loganin acid, swertiamarin and sweroside were calculated, respectively.
Six components could be detected in intestinal sac. In different concentrations of Gentianae Radix et Rhizoma, gentiopicroside and swertiamarin in various intestinal sections were the linear absorption (R2 > 0.9), conformed to zero order absorption rate. In jejunum the constant of absorption rate (Ka) of gentiopicroside and swertiamarin increased with the raised dosage of Gentianae Radix et Rhizoma (P < 0.05), which indicated a passive absorption manner, and the value of Ka of high and middle dosage of those in ileum were higher than that of low dosage, and the difference of Ka between high and middle dosage were not significant, which indicated a positive absorption manner. The Ka of high and middle dosage of sweroside in ileum and jejunum were higher than that of low dosage (P < 0.05), and the difference of Ka between high and middle dosage were not significant, which indicated a positive absorption manner. The Ka of loganin acid in jejunum and ileum increased along with the raised dosage of Gentianae Radix et Rhizoma (P < 0.05), which indicated a passive absorption manner.
SEMAC could be used as a tool to investigate the absorption ingredients of Gentianae Radix et Rhizoma. Drug in intestine sac was selective, and the absorption part of intestine was also different.
建立一种快速考察龙胆吸收成分的方法，为龙胆质量控制提供指标。
采用体外翻肠囊（VEIS）模型考察龙胆的吸收成分。在6个时间点（15、30、45、60、90、120分钟）收集空肠和回肠的肠囊液，以HPLC检测龙胆苦苷、马钱子酸、獐牙菜苦苷和獐牙菜苷作为代表性指标成分。分别计算龙胆苦苷、马钱子酸、獐牙菜苦苷和獐牙菜苷的累积吸收量。
肠囊中可检测到6种成分。在不同浓度的龙胆中，各肠段的龙胆苦苷和獐牙菜苦苷呈线性吸收（R2>0.9），符合零级吸收速率。空肠中龙胆苦苷和獐牙菜苦苷的吸收速率常数（Ka）随龙胆剂量增加而增大（P<0.05），呈被动吸收方式；回肠中高、中剂量的龙胆苦苷和獐牙菜苦苷的Ka值高于低剂量，高、中剂量之间Ka差异不显著，呈主动吸收方式。回肠和空肠中高、中剂量的獐牙菜苷的Ka值高于低剂量（P<0.05），高、中剂量之间Ka差异不显著，呈主动吸收方式。空肠和回肠中马钱子酸的Ka值随龙胆剂量增加而增大（P<0.05），呈被动吸收方式。
体外翻肠囊模型可用于考察龙胆的吸收成分。肠囊对药物有选择性，肠道吸收部位也不同。
