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Effects of Ginkgo biloba Extract Ingestion on the Pharmacokinetics of Talinolol in Healthy Chinese Volunteers

Assistant Professor, Pharmacogenetics Research Institute, Institute of Clinical Pharmacology, Central South University, Changsha, Hunan, China

Gong-You Tao, MD

Pharmacology student, Assistant Professor, Pharmacogenetics Research Institute, Institute of Clinical Pharmacology, Central South University

Guo Wang, PhD

Postdoctoral student, Assistant Professor, Pharmacogenetics Research Institute, Institute of Clinical Pharmacology, Central South University

Yao Chen, PhD

Assistant Professor, Pharmacogenetics Research Institute, Institute of Clinical Pharmacology, Central South University

Wei Zhang, PhD

Vice Professor, Pharmacogenetics Research Institute, Institute of Clinical Pharmacology, Central South University

Yi-Jing He, PhD

Assistant Professor, Pharmacogenetics Research Institute, Institute of Clinical Pharmacology, Central South University

Qing Li, PhD

Assistant Professor, Pharmacogenetics Research Institute, Institute of Clinical Pharmacology, Central South University

He-Ping Lei, PhD

Pharmacology student, Pharmacogenetics Research Institute, Institute of Clinical Pharmacology, Central South University

Feng Jiang, PhD

Assistant Professor, Pharmacogenetics Research Institute, Institute of Clinical Pharmacology, Central South University

Dong-Li Hu, MD

Pharmacology student, Pharmacogenetics Research Institute, Institute of Clinical Pharmacology, Central South University

Yuan-Fei Huang, MD

Pharmacology student, Pharmacogenetics Research Institute, Institute of Clinical Pharmacology, Central South University

Hong-Hao Zhou, MD

Professor, Director, Pharmacogenetics Research Institute, Institute of Clinical Pharmacology, Central South University

Reprints: Dr. Hong-Hao Zhou, Pharmacogenetics Research Institute, Central South University, 110 Xiang Ya Rd., Changsha, Hunan 410078, China, fax 86 731 2354476, hhzhou2003{at}163.com

BACKGROUND: 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.

OBJECTIVE: To investigate the effects of single and repeated GBE ingestion on the oral pharmacokinetics of talinolol, a substrate drug for P-glycoprotein in humans.

METHODS: 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).

RESULTS: 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- by 22% (90% CI 8 to 37; p = 0.014), respectively, without significant changes in elimination half-life and the time to C_max.

CONCLUSIONS: 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.

Key Words: Gingko biloba extract, herb-drug interaction, P-glycoprotein inhibition, pharmacokinetics, talinolol

Published Online, April 28, 2009. www.theannals.com, DOI 10.1345/aph.1L656