Abstract |
Primaquine (PQ) is used for the radical cure of Plasmodium vivax malaria and can cause serious side effects in some individuals. The development of an extended-release dosage with poly( ethylene oxide) as a hydrophilic polymer has been investigated to improve drug efficacy and tolerability. The aim of this study was to evaluate in vivo a new extended-release formulation of PQ (60 mg). The formulation was administered to beagle dogs and plasma PQ concentrations were compared to a conventional immediate-release formulation of PQ (60 mg). The evaluation was carried out using a validated high-performance liquid chromatography method using solid-phase extraction. Total PQ exposure in beagle dogs was 2.2 times higher (area under curve of 12 193 versus 5678 ng h/ml) and the elimination half-life of PQ was a 19-fold greater (12.95 hours versus 0.68 hours) with the extended-release tablets compared with the immediate-release tablets. These findings suggest that the extended-release formulation of PQ merits further evaluation for the treatment of P. vivax malaria and/or chemoprophylaxis.
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Authors | C D Bertol, P R Oliveira, G Kuminek, G S Rauber, H K Stulzer, M A S Silva |
Journal | Annals of tropical medicine and parasitology
(Ann Trop Med Parasitol)
Vol. 105
Issue 7
Pg. 475-84
(Oct 2011)
ISSN: 1364-8594 [Electronic] England |
PMID | 22185941
(Publication Type: Journal Article)
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Chemical References |
- Antimalarials
- Delayed-Action Preparations
- Drug Carriers
- Tablets
- Polyethylene Glycols
- Primaquine
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Topics |
- Animals
- Antimalarials
(pharmacology)
- Biological Availability
- Delayed-Action Preparations
(pharmacology)
- Dogs
- Drug Carriers
- Female
- Malaria
(blood, drug therapy)
- Plasmodium vivax
(drug effects)
- Polyethylene Glycols
(pharmacology)
- Primaquine
(pharmacology)
- Tablets
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