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Eur J Pharm Sci ; 16(4-5): 273-80, 2002 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-12208457

RESUMO

Achievement of controlled drug delivery and stability of drugs during storage is a problem also in transdermal drug delivery. The objective of this study was to determine, whether an easily oxidized drug, levodopa, could be stabilized during storage using pH-adjustment and ion-exchange fibers. Controlled transdermal delivery of the zwitterionic levodopa was attempted by iontophoresis and ion-exchange fiber. Ion-exchange kinetics and transdermal permeation of a cationic (presumably more stable) model drug, metaraminol, were compared to the corresponding data of levodopa. Levodopa was rapidly oxidized in the presence of water, especially at basic pH-values. At acidic pH-values the stability was improved significantly. Ion-exchange group and the pH had a clear effect on the release of both the levodopa and metaraminol from the ion-exchange fiber. The adsorption/release kinetics of metaraminol were more easily controllable than the corresponding rate and extent of levodopa adsorption/release. Iontophoretic enhancement of drug permeation across the skin was clearly more significant with the positively charged metaraminol than with the zwitterionic levodopa. Ion-exchange fibers provide a promising alternative to control drug delivery and to store drugs that are degraded easily.


Assuntos
Composição de Medicamentos , Resinas de Troca Iônica , Iontoforese , Levodopa/química , Metaraminol/química , Preparações de Ação Retardada , Estabilidade de Medicamentos , Armazenamento de Medicamentos , Humanos , Concentração de Íons de Hidrogênio , Técnicas In Vitro , Levodopa/administração & dosagem , Levodopa/farmacocinética , Metaraminol/administração & dosagem , Metaraminol/farmacocinética , Oxirredução , Absorção Cutânea
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