Pharmacokinetics of the antimalarial drug piperaquine in healthy Vietnamese subjects.
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 x h/mL versus 2,999 ng x 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 x h/mL versus 7,954 ng x 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.
Nguyen
Trong Chinh
TC
Department of Infectious Diseases, Central Military Hospital 108, Hanoi, Vietnam.
Nguyen
Ngoc Quang
NQ
Nguyen
Xuan Thanh
XT
Bui
Dai
D
Travers
Thomas
T
Edstein
Michael D
MD
D000328:Adult; D000962:Antimalarials / Q000493:pharmacokinetics*; D019540:Area Under Curve; D001682:Biological Availability; D006801:Humans; D008297:Male; D011804:Quinolines / Q000493:pharmacokinetics*; D010879:Piperazines
D000962:Antimalarials; D011804:Quinolines; C034759:piperaquine; D010879:Piperazines