Herb-Drug Pharmacokinetic Interactions: Transport and Metabolism of Indinavir in the Presence of Selected Herbal Products

Molecules

Carlemi Calitz²  Chrisna Gouws²  Joe Viljoen²  Jan Steenekamp²  Lubbe Wiesner¹  Efrem Abay¹  Josias Hamman² 

[1] Department of Medicine, University of Cape Town, Observatory 7925, South Africa;Centre of Excellence for Pharmaceutical Sciences, North-West University, Private Bag X6001, Potchefstroom 2520, South Africa;

关键词: herb-drug interactions;    efflux;    P-glycoprotein;    cytochrome P450;    Caco-2;    LS180;    metabolism;   

DOI  :  10.3390/molecules201219838

来源: mdpi

【 摘 要 】

Patients receiving anti-retroviral drug treatment are sometimes simultaneously taking herbal remedies, which may result in pharmacokinetic herb-drug interactions. This study aimed to determine if pharmacokinetic interactions exist between selected commercially available herbal products (i.e., Linctagon Forte^®, Viral Choice^® and Canova^®) and indinavir in terms of in vitro transport and metabolism. Bi-directional transport of indinavir was evaluated across Caco-2 cell monolayers in the presence and absence of the selected herbal products and verapamil (positive control). Metabolism of indinavir was determined in LS180 cells in the presence and absence of the selected herbal products as well as ketoconazole (positive control). The secretory transport of indinavir increased in a concentration dependent way in the presence of Linctagon Forte^® and Viral Choice^® when compared to that of indinavir alone. Canova^® only slightly affected the efflux of indinavir compared to that of the control group. There was a pronounced inhibition of the metabolism of indinavir in LS180 cells over the entire concentration range for all the herbal products investigated in this study. These in vitro pharmacokinetic interactions indicate the selected herbal products may affect indinavir’s bioavailability, but the clinical significance needs to be confirmed with in vivo studies before final conclusions can be made.

【 授权许可】

CC BY   
© 2015 by the authors; licensee MDPI, Basel, Switzerland.