Peracylated beta-cyclodextrins as novel sustained-release carriers for a water-soluble drug, molsidomine.
J Pharm Pharmacol
; 46(9): 714-7, 1994 Sep.
Article
em En
| MEDLINE
| ID: mdl-7837039
ABSTRACT
Peracylated beta-cyclodextrins with different alkyl chains (acetyl-octanoyl) were prepared by acylating all hydroxyl groups of beta-cyclodextrin (beta-CyD), and their physical properties were evaluated. These hydrophobic beta-CyDs decreased the release rate of molsidomine, a peripheral vasodilator, in proportion to the lengthening of alkyl chain and suppressed a peak plasma level of molsidomine following oral administration of peracylated beta-CyD complexes to dogs. Among the peracylated beta-CyDs tested, perbutanoyl-beta-CyD maintained sufficient plasma drug levels for a long period of time, while other peracylated beta-CyDs having shorter or longer chains were inappropriate to control the in-vivo release behaviour of molsidomine. The prominent retarding effect of perbutanoyl-beta-CyD was ascribable to the appropriate mucoadhesive property and hydrophobicity, compared with other peracylated beta-CyDs. The present results suggest that perbutanoyl-beta-CyD is particularly useful in modifying the release rate of water-soluble drugs as a novel slow-release carrier.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Molsidomina
/
Ciclodextrinas
/
Beta-Ciclodextrinas
Limite:
Animals
Idioma:
En
Revista:
J Pharm Pharmacol
Ano de publicação:
1994
Tipo de documento:
Article