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

Authors
RANUCCI E SPAGNOLI G LATINI R BERNASCONI R FERRUTI P
Citation
E. Ranucci et al., ON THE SUITABILITY OF URETHANE BONDS BETWEEN THE CARRIER AND THE DRUGMOIETY IN POLY(ETHYLENEGLYCOL)-BASED OLIGOMERIC PRODRUGS, Journal of biomaterials science. Polymer ed., 6(2), 1994, pp. 133-139
Citations number
13
Categorie Soggetti
Engineering, Biomedical","Polymer Sciences","Materials Science, Biomaterials
Journal title
Journal of biomaterials science. Polymer ed. → ACNP
ISSN journal
09205063
Volume
6
Issue
2
Year of publication
1994
Pages
133 - 139
Database
ISI
SICI code
0920-5063(1994)6:2<133:OTSOUB>2.0.ZU;2-R
Abstract
Some poly(ethyleneglycol) derivatives of propranolol were prepared, in which the drug molecule was linked to the oligomeric carrier via uret hane bonds in order to study the suitability of this bond as a linkage between the carrier and the drug moiety in oligomeric prodrugs. For c omparison purposes also ethanol- and butanol-based prodrugs of propran olol were prepared, with the same linkage between drug and promoiety. The urethane compounds were obtained by condensation via N,N'-carbonyl diimidazole. None of these compounds gave rise to appreciable blood co ncentrations of propranolol after oral administration, thus suggesting in this particular case, a relative in vivo resistance of urethane bo nds towards cleavage.