Volume 79, Issue 4
  • ISSN: 0002-9637
  • E-ISSN: 1476-1645


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 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 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.


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  • Received : 07 Mar 2008
  • Accepted : 08 Jul 2008

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