目的 研究黄芩苷和黄芩素的肠吸收特性。方法 采用大鼠在体肠吸收模型,以高效液相色谱法测定循环液中药物的浓度。结果 不结扎胆管时,黄芩苷和黄芩素的吸收速率常数分别为(-0.0047±0.0134)h^-1和(0.4960±0.0512)h^-1;结扎胆管时,黄芩苷和黄芩素的吸收速率常数分别为(0.0239±0.0262)h^-1和(0.2106±0.0735)h^-1;结扎胆管,在单独以黄芩苷或黄芩素进行在体肠循环时,循环液中分别出现了随时间增加的黄芩素和黄芩苷;结扎胆管尾静脉注射黄芩素时,循环液中出现了黄芩苷。结论 黄芩素比黄芩苷更适于口服给药;胆汁不但可以分泌黄芩苷,而且可以促进黄芩素的吸收;黄芩苷在肠内经过菌群代谢为黄芩素而被吸收,被吸收的或静脉注射的黄芩素可在体内还原为黄芩苷,并再被小肠分泌排出。
OBJECTIVE To study the absorption characteristics of baicalin and baicalein. METHODS The model of in situ intestinal perfusion was used. A HPLC method was established to determine the drug concentration in the perfusate. RESULTS When the bile duct was not ligated, the absorption rate constant of baicalin and baicalein were ( - 0.004 7 ±0.013 4)h^-1 and(0.496 0±0.051 2)h^-1, respectively; When the bile duct was ligated, the absorption rate constant of baicalin and baicalein were (0. 023 9 ± 0.026 2) h^- 1 and (0.210 6±0- 073 5 ) h^-1, respectively. When baicalin or baicalein was perfused alone after the ligation of the bile duct, the concentrations of baicalein or baicalin were increased in the pedhsate respectively. When baicalein was intravenous administered to rats after the ligation of the bile duct, baicalin were obtained in the perfusate. CONCLUSION Baicalin is more suitable to be administered orally than baicalin. Bile can not only excrete baicalin, but also evidently promote the absorption of baicalein. Baiealin is absorbed as baiealein formed by the intestinal bacteria, and then restored as its original form in the body. The part of the baicalin formed from the absorbed or intravenous administered baicalein can be excreted back into the gut.