Pharmacokinetics of the antimalarial drug piperaquine in healthy Vietnamese subjects
| Autor: | Michael D. Edstein, Thomas Travers, Nguyen Xuan Thanh, Bui Dai, Nguyen Ngoc Quang, Nguyen Trong Chinh |
|---|---|
| Rok vydání: | 2008 |
| Předmět: |
Drug
Adult Male Meal business.industry media_common.quotation_subject Cmax Biological Availability Pharmacology Bioavailability Single oral dose Antimalarials Infectious Diseases Pharmacokinetics Virology Piperaquine Area Under Curve Quinolines Medicine Humans Parasitology Geometric mean business media_common |
| Zdroj: | The American journal of tropical medicine and hygiene. 79(4) |
| ISSN: | 1476-1645 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|