Bertol C D, Oliveira P R, Kuminek G, Rauber G S, Stulzer H K, Silva M A S
Department of Pharmaceutical Sciences, Health Science Centre, Federal University of Santa Catarina, Trindade, 88040-900 Florianópolis-SC, Brazil.
Ann Trop Med Parasitol. 2011 Oct;105(7):475-84. doi: 10.1179/2047773211Y.0000000003.
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.
伯氨喹（PQ）用于间日疟原虫疟疾的根治，但在某些个体中可能会引起严重的副作用。人们研究了以聚环氧乙烷作为亲水性聚合物的缓释剂型，以提高药物疗效和耐受性。本研究的目的是对一种新的60毫克PQ缓释制剂进行体内评估。将该制剂给予比格犬，并将血浆PQ浓度与常规的60毫克PQ速释制剂进行比较。使用经过验证的高效液相色谱法和固相萃取法进行评估。与速释片相比，比格犬中PQ的总暴露量高2.2倍（曲线下面积分别为12193和5678纳克·小时/毫升），PQ的消除半衰期长19倍（分别为12.95小时和0.68小时）。这些发现表明，PQ缓释制剂在治疗间日疟原虫疟疾和/或化学预防方面值得进一步评估。
