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Am. J. Trop. Med. Hyg., 79(4), 2008, pp. 620-623
Copyright © 2008 by The American Society of Tropical Medicine and Hygiene

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SHORT REPORT


Pharmacokinetics of the Antimalarial Drug Piperaquine in Healthy Vietnamese Subjects

Nguyen Trong Chinh, Nguyen Ngoc Quang, Nguyen Xuan Thanh, Bui Dai, Thomas Travers, AND Michael D. Edstein*
Department of Infectious Diseases, Central Military Hospital 108, Hanoi, Vietnam; Department of Malaria, Military Institute of Hygiene and Epidemiology, Hanoi, Vietnam; Australian Army Malaria Institute, Brisbane, Queensland Australia

 

ABSTRACT

We compared plasma maximum concentration (Cmax) and area under the concentration-time curve (AUC) of the antimalarial drug piperaquine in 26 healthy Vietnamese subjects after treatment with either a single oral dose of 500 mg (n = 6) or 1,000 mg (n = 6) of piperaquine phosphate and a three-day course of 500 mg of piperaquine/ day in the fasting state (n = 7) or with food (approximately 17 g fat) (n = 7). The geometric mean plasma Cmax and AUC(0–28) was 2.8-fold (200 ng/mL versus 70 ng/mL) and 1.9-fold (5,736 ng · h/mL versus 2,999 ng · h/mL), respectively, and higher in subjects receiving the 1,000-mg dose than in those receiving the 500-mg dose. The geometric mean Cmax and AUC(0–28) was 1.7-fold (198 ng/mL versus 119 ng/mL) and 1.4-fold (11,187 ng · h/mL versus 7,954 ng · h/mL) higher in the fed state than in the fasting state. Piperaquine AUC was proportional to the two doses tested and a moderate-fat meal enhanced the bioavailability of piperaquine by 41%, which should improve the therapeutic efficacy of this drug.

Received March 7, 2008. Accepted for publication July 8, 2008.

Acknowledgments: This study was carried out under the auspices of the Vietnam Australia Defence Malaria Project, a defence cooperation between the Vietnam People’s Army and the Australian Defence Force. We thank the Vietnam People’s Army Department of Military Medicine for supporting the study and the financial sponsor, the Australian Defence Force International Policy Division. We also thank Professor G. Dennis Shanks and Dr. Bob Cooper for comments on the manuscript.

Disclaimer: The opinions expressed are those of the authors and do not necessarily reflect those of the Defence Health Service or any extant Australian Defence Force policy.

* Address correspondence to Michael D. Edstein, Australian Army Malaria Institute, Enoggera, Brisbane, Queensland 4051, Australia. E-mail: mike.edstein{at}defence.gov.au

Authors’ addresses: Nguyen Trong Chinh and Nguyen Ngoc Quang, Department of Infectious Diseases, Central Military Hospital 108, Hanoi, Vietnam. Nguyen Xuan Thanh and Bui Dai, Department of Malaria, Military Institute of Hygiene and Epidemiology, Hanoi, Vietnam. Thomas Travers and Michael D. Edstein, Australian Army Malaria Institute, Brisbane, Queensland, Australia.




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