SciELO - Scientific Electronic Library Online

vol.45 número4Standardization of method for determining glycosylated hemoglobin (Hb A1c) by cation exchange high performance liquid chromatographyDevelopment of granules from Phyllanthus niruri spray-dried extract índice de autoresíndice de assuntospesquisa de artigos
Home Pagelista alfabética de periódicos  

Serviços Personalizados




Links relacionados


Brazilian Journal of Pharmaceutical Sciences

versão On-line ISSN 2175-9790


CARDOSO, Carmem Dickow  e  BONATO, Pierina Sueli. Enantioselective metabolism of hydroxychloroquine employing rats and mice hepatic microsomes. Braz. J. Pharm. Sci. [online]. 2009, vol.45, n.4, pp.658-667. ISSN 2175-9790.

Hydroxychloroquine (HCQ) is an important chiral drug used, mainly, in the treatment of rheumatoid arthritis, systemic lupus erythematosus and malaria, and whose pharmacokinetic and pharmacodynamic properties look to be stereoselective. Respecting the pharmacokinetic properties, some previous studies indicate that the stereoselectivity could express itself in the processes of metabolism, distribution and excretion and that the stereoselective metabolism looks to be a function of the studied species. So, the in vitro metabolism of HCQ was investigated using hepatic microsomes of rats and mice. The microsomal fraction of livers of Wistar rats and Balb-C mice was separated by ultracentrifugation and 500 μL were incubated for 180 minutes with 10 μL of racemic HCQ 1000 μg mL-1. Two stereospecific analytical methods, high performance liquid chromatography (HPLC) and capillary electrophoresis (CE), were used to separate and quantify the formed metabolites. It was verified that the main formed metabolite is the (-)-(R)-desethyl hydroxychloroquine for both animal species.

Palavras-chave : Hydroxychloroquine; Stereoselective metabolism [in vitro study]; High performance liquid chromatography; Capillary electrophoresis.

        · resumo em Português     · texto em Inglês     · Inglês ( pdf )


Creative Commons License Todo o conteúdo deste periódico, exceto onde está identificado, está licenciado sob uma Licença Creative Commons