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Arzneimittelforschung ; 35(5): 808-13, 1985.
Artigo em Inglês | MEDLINE | ID: mdl-4026904

RESUMO

2,6-Dimethyl-3,5-dimethoxycarbonyl-4-(o-difluoromethoxyphenyl)-1, 4-dihydropyridine (ryodipine, PP-1466) at oral administration in the form of a suspension with Tween (polysorbate) 80 addition is comparatively rapidly absorbed in the gastro-intestinal tract and circulates in blood for a long period of time. PP-1466 practically does not bind to plasma proteins. The drug is mainly excreted via the kidneys and with faeces by 49 and 46% of the dose administered after 96 h, respectively. PP-1466 metabolites are present in rat urine-2,6-dimethyl-4-arylpyridine-3,5-dicarbonic acid derivatives: oxidation product of PP-1466 dihydropyridine cycle into pyridine one, products of partial or complete hydrolysis of ester groups of PP-1466 oxidized form, lactones. There have been performed the synthesis of labelled 14C-PP-1466 as well as counter-synthesis of PP-1466 metabolites. Unchanged PP-1466 is not detected in urine.


Assuntos
Anti-Hipertensivos/metabolismo , Nifedipino/análogos & derivados , Animais , Bile/metabolismo , Biotransformação , Fenômenos Químicos , Química , Cromatografia Líquida de Alta Pressão , Cromatografia em Camada Fina , Absorção Intestinal , Cinética , Masculino , Espectrometria de Massas , Nifedipino/metabolismo , Ratos , Distribuição Tecidual
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