Fan Lan, Tao Gong-You, Wang Guo, Chen Yao, Zhang Wei, He Yi-Jing, Li Qing, Lei He-Ping, Jiang Feng, Hu Dong-Li, Huang Yuan-Fei, Zhou Hong-Hao
Pharmacogenetics Research Institute, Institute of Clinical Pharmacology, Central South University, Changsha, Hunan, China.
Ann Pharmacother. 2009 May;43(5):944-9. doi: 10.1345/aph.1L656. Epub 2009 Apr 28.
Ginkgo biloba extract (GBE), the best selling herbal medicine in the world, has been reported to inhibit P-glycoprotein in vitro. However, the effects of GBE on P-glycoprotein activity in humans have not been clarified.
To investigate the effects of single and repeated GBE ingestion on the oral pharmacokinetics of talinolol, a substrate drug for P-glycoprotein in humans.
Ten unrelated healthy male volunteers were selected to participate in a 3-stage sequential study. Plasma concentrations of talinolol from 0 to 24 hours were measured by high-performance liquid chromatography after talinolol 100 mg was administrated alone, with a single oral dose of GBE (120 mg), and after 14 days of repeated GBE ingestion (360 mg/day).
A single oral dose of GBE did not affect the pharmacokinetics of talinolol. Repeated ingestion of GBE increased the talinolol maximum plasma concentration (C(max)) by 36% (90% CI 10 to 68; p = 0.025), the area under the concentration-time curve (AUC)(0-24) by 26% (90% CI 11 to 43; p = 0.008) and AUC(0-infinity) by 22% (90% CI 8 to 37; p = 0.014), respectively, without significant changes in elimination half-life and the time to C(max).
Our results suggest that long-term use of GBE significantly influenced talinolol disposition in humans, likely by affecting the activity of P-glycoprotein and/or other drug transporters.
银杏叶提取物（GBE）是全球最畅销的草药，据报道其在体外可抑制P-糖蛋白。然而，GBE对人体P-糖蛋白活性的影响尚未明确。
研究单次和重复摄入GBE对他林洛尔（一种人体P-糖蛋白底物药物）口服药代动力学的影响。
选择10名无亲缘关系的健康男性志愿者参与一项3阶段的序贯研究。在单独给予100 mg他林洛尔、单次口服GBE（120 mg）以及重复摄入GBE 14天（360 mg/天）后，采用高效液相色谱法测定0至24小时他林洛尔的血浆浓度。
单次口服GBE不影响他林洛尔的药代动力学。重复摄入GBE使他林洛尔的最大血浆浓度（C(max)）增加36%（90%CI 10至68；p = 0.025），浓度-时间曲线下面积（AUC）(0-24)增加26%（90%CI 11至43；p = 0.008），AUC(0-∞)增加22%（90%CI 8至37；p = 0.014），消除半衰期和达峰时间无显著变化。
我们的结果表明，长期使用GBE对人体他林洛尔的处置有显著影响，可能是通过影响P-糖蛋白和/或其他药物转运体的活性。
