RESUMO
The successful conjugation of active theophylline molecules to two new multifunctional high-molecular weight poly(ethylene glycol) derivatives (MultiPEG) and their pharmacokinetic evaluations are reported. The drug loading was increased up to six times in comparison with commercial PEG of the same molecular weight. A clear increase of the time of persistence within the body and a concomitant improvement of the overall pharmacokinetic properties of those prodrugs were also observed. These studies sustain the use of these new PEG-based polymeric supports as a valuable alternative for an effective drug delivery system.
Assuntos
Broncodilatadores/farmacocinética , Polietilenoglicóis/química , Polietilenoglicóis/farmacocinética , Teofilina/análogos & derivados , Teofilina/farmacocinética , Animais , Área Sob a Curva , Biotransformação , Broncodilatadores/química , Broncodilatadores/toxicidade , Fenômenos Químicos , Físico-Química , Cromatografia Líquida de Alta Pressão , Sistemas de Liberação de Medicamentos , Feminino , Espectroscopia de Ressonância Magnética , Masculino , Camundongos , Camundongos Endogâmicos ICR , Peso Molecular , Coelhos , Ratos , Espectrofotometria Ultravioleta , Teofilina/químicaRESUMO
One of the most used and useful polymers, poly(ethylene glycol) (PEG) was used as a carrier for warfarin. The drug-polymer conjugate was freely water soluble at room temperature. The hydrolytic stability of the PEG-warfarin was investigated at physiological pH and confirmed the stability of the conjugate. In vivo release studies demonstrated a good release of parent drug, without the initial high plasma level of warfarin.
