title: Increased bioavailability of primaquine using poly(ethylene oxide) matrix extended-release tablets administered to beagle dogs.
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.
authors.affiliation: Department of Pharmaceutical Sciences, Health Science Centre, Federal University of Santa Catarina, Trindade, 88040-900 Florianópolis-SC, Brazil. charibertol@yahoo.com.br
authors.forename: C D
authors.initials: CD
authors.lastname: Bertol
authors.forename: P R
authors.initials: PR
authors.lastname: Oliveira
authors.forename: G
authors.initials: G
authors.lastname: Kuminek
authors.forename: G S
authors.initials: GS
authors.lastname: Rauber
authors.forename: H K
authors.initials: HK
authors.lastname: Stulzer
authors.forename: M A S
authors.initials: MA
authors.lastname: Silva
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000494:pharmacology*; D001682:Biological Availability; D003692:Delayed-Action Preparations / Q000494:pharmacology; D004285:Dogs; D004337:Drug Carriers; D005260:Female; D008288:Malaria / Q000097:blood / Q000188:drug therapy*; D010966:Plasmodium vivax / Q000187:drug effects*; D011092:Polyethylene Glycols / Q000494:pharmacology*; D011319:Primaquine / Q000494:pharmacology*; D013607:Tablets
chemical_list: D000962:Antimalarials; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D013607:Tablets; D011092:Polyethylene Glycols; D011319:Primaquine