Some poly(ethyleneglycol) derivatives of propranolol were prepared, in which the drug molecule was linked to the oligomeric carrier via urethane bonds in order to study the suitability of this bond as a linkage between the carrier and the drug moiety in oligomeric prodrugs. For comparison purposes also ethanol- and butanol-based prodrugs of propranolol were prepared, with the same linkage between drug and promoiety. The urethane compounds were obtained by condensation via N,N'-carbonyldiimidazole. None of these compounds gave rise to appreciable blood concentrations of propranolol after oral administration, thus suggesting in this particular case, a relative in vivo resistance of urethane bonds towards cleavage.

ON THE SUITABILITY OF URETHANE BONDS BETWEEN THE CARRIER AND THE DRUG MOIETY IN POLY(ETHYLENEGLYCOL)-BASED OLIGOMERIC PRODRUGS / E. RANUCCI, Spagnoli, G., Latini, R., Bernasconi, R., Ferruti, P.. - In: JOURNAL OF BIOMATERIALS SCIENCE POLYMER EDITION. - ISSN 0920-5063. - 6:2(1994), pp. 133-139.

ON THE SUITABILITY OF URETHANE BONDS BETWEEN THE CARRIER AND THE DRUG MOIETY IN POLY(ETHYLENEGLYCOL)-BASED OLIGOMERIC PRODRUGS

E. RANUCCI
Primo
;
1994

Abstract

Some poly(ethyleneglycol) derivatives of propranolol were prepared, in which the drug molecule was linked to the oligomeric carrier via urethane bonds in order to study the suitability of this bond as a linkage between the carrier and the drug moiety in oligomeric prodrugs. For comparison purposes also ethanol- and butanol-based prodrugs of propranolol were prepared, with the same linkage between drug and promoiety. The urethane compounds were obtained by condensation via N,N'-carbonyldiimidazole. None of these compounds gave rise to appreciable blood concentrations of propranolol after oral administration, thus suggesting in this particular case, a relative in vivo resistance of urethane bonds towards cleavage.
Settore CHIM/04 - Chimica Industriale
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/2434/188457
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