Xu Shunjun, Yu Jiejing, Yang Liu, Zhu Yaling, Sun Shuai, Xu Zhengdi
ImVin Pharmaceutical Co., Ltd., 2 Fangcaodian Road, Guangzhou 510663, China.
Guangdong Provincial Hospital of Chinese Medicine, 111 Dade Road, Guangzhou 510120, China.
J Anal Methods Chem. 2016;2016:5093537. doi: 10.1155/2016/5093537. Epub 2016 Aug 11.
Chuan-Ke-Zhi (CKZ), a purified Herba Epimedii extract, is a potent Chinese medicine preparation whose main bioactive components are a class of flavonoid glycosides such as epimedins A, B, and C and icariin. And epimedin C is far more abundant than other flavones in this extract. This study aims to investigate the pharmacokinetic and bioavailability of epimedin C and what effects, if any, other ingredients in CKZ have on its pharmacokinetics. Epimedin C, CKZ, and a combination of epimedins A, B, and C and icariin were, respectively, administrated to rats, and then the pharmacokinetic parameters of epimedin C in the three groups were calculated and compared. The result indicated that CLZ, MRT0-∞, and AUC0-∞ of epimedin C were significantly different among the three groups (P < 0.05), and compared with the epimedin C group, the absorption of epimedin C significantly increased in the CKZ group. Furthermore, in this study the absolute bioavailability of epimedin C was also investigated by comparing intramuscular and intravenous administration of epimedin C. As a result, epimedin C could be quickly absorbed with extremely high absolute bioavailability after intramuscular administration.
川梀子(CKZ)是一种纯化的淫羊藿提取物,是一种有效的中药制剂,其主要生物活性成分是一类黄酮苷,如淫羊藿苷A、B和C以及淫羊藿苷。并且在该提取物中,淫羊藿苷C的含量远高于其他黄酮类化合物。本研究旨在研究淫羊藿苷C的药代动力学和生物利用度,以及CKZ中的其他成分对其药代动力学有何影响(如果有影响的话)。分别给大鼠灌胃淫羊藿苷C、CKZ以及淫羊藿苷A、B、C和淫羊藿苷的组合,然后计算并比较三组中淫羊藿苷C的药代动力学参数。结果表明,三组中淫羊藿苷C的清除率(CLZ)、平均滞留时间(MRT0-∞)和药时曲线下面积(AUC0-∞)有显著差异(P < 0.05),与淫羊藿苷C组相比,CKZ组中淫羊藿苷C的吸收显著增加。此外,在本研究中,还通过比较淫羊藿苷C的肌肉注射和静脉注射来研究其绝对生物利用度。结果显示,淫羊藿苷C肌肉注射后可快速吸收,绝对生物利用度极高。