Separation Engineering of Chinese Traditional Medicine Compound, Nanjing University of Chinese Medicine, Nanjing 210028, China.
Thermo Fisher Scientific, Shanghai, China.
Evid Based Complement Alternat Med. 2013;2013:349531. doi: 10.1155/2013/349531. Epub 2013 Dec 3.
Huang-Lian-Jie-Du-Tang (HLJDT), a classical Chinese prescription, has been clinically employed to treat cerebral ischemia for thousands of years. Geniposide is the major active ingredient in HLJDT. The aim is to investigate the comparative evaluations on pharmacokinetics of geniposide in MCAO rats in pure geniposide, geniposide : berberine, and geniposide : berberine : baicalin. Obviously, the proportions of geniposide : berberine, geniposide : baicalin, and geniposide : berberine : baicalin were determined according to HLJDT. In our study, the cerebral ischemia model was reproduced by suture method in rats. The MCAO rats were randomly assigned to four therapy groups and orally administered with different prescription proportions of pure geniposide, geniposide : berberine, geniposide : baicalin, and geniposide : berberine : baicalin, respectively. The concentrations of geniposide in rat serum were determined using HPLC, and main pharmacokinetic parameters were investigated. The results indicated that the pharmacokinetics of geniposide in rat serum was nonlinear and there were significant differences between different groups. Berberine might hardly affect the absorption of geniposide, and baicalin could increase the absorption ability of geniposide. Meanwhile, berberine could decrease the absorption increase of baicalin on geniposide.
黄连解毒汤（HLJDT）是一种经典的中药方剂，临床上已经有数千年用于治疗脑缺血。栀子苷是 HLJDT 的主要活性成分。本研究旨在比较纯栀子苷、栀子苷-小檗碱和栀子苷-小檗碱-黄芩苷三种处方比例在 MCAO 大鼠体内栀子苷的药代动力学。显然，栀子苷-小檗碱、栀子苷-黄芩苷和栀子苷-小檗碱-黄芩苷的比例是根据 HLJDT 确定的。在本研究中，通过缝线法在大鼠中复制脑缺血模型。将 MCAO 大鼠随机分为四组治疗组，分别灌胃给予不同处方比例的纯栀子苷、栀子苷-小檗碱、栀子苷-黄芩苷和栀子苷-小檗碱-黄芩苷。采用 HPLC 法测定大鼠血清中栀子苷的浓度，考察主要药代动力学参数。结果表明，大鼠血清中栀子苷的药代动力学是非线性的，不同组之间存在显著差异。小檗碱可能几乎不影响栀子苷的吸收，黄芩苷可以提高栀子苷的吸收能力。同时，小檗碱可以降低黄芩苷对栀子苷吸收增加的作用。
