title: Sustained release of buserelin acetate, a luteinizing hormone-releasing hormone agonist, from an injectable oily preparation utilizing ethylated beta-cyclodextrin.
abstract: The possible use of heptakis (2,6-di-O-ethyl)-beta-cyclodextrin (DE-beta-CyD) as a parenteral sustained-release carrier for buserelin acetate, a luteinizing hormone-releasing hormone superagonist, has been examined. The in-vitro release of buserelin from the oily suspension was significantly retarded by the complexation with DE-beta-CyD, mainly due to the poor water solubility of the complex. A single subcutaneous injection of the suspension containing the buserelin-DE-beta-CyD complex to rats provided an effective continuous plasma level of buserelin lasting for at least one month, indicating a potential therapeutic efficacy for the treatment of the endocrine-dependent diseases. These results suggest that DE-beta-CyD serves as an injectable sustained-release drug carrier suitable for chronic treatment with buserelin acetate.
authors.affiliation: Faculty of Pharmaceutical Sciences, Kumamoto University, Japan.
authors.forename: K
authors.initials: K
authors.lastname: Uekama
authors.forename: H
authors.initials: H
authors.lastname: Arima
authors.forename: T
authors.initials: T
authors.lastname: Irie
authors.forename: K
authors.initials: K
authors.lastname: Matsubara
authors.forename: T
authors.initials: T
authors.lastname: Kuriki
mesh_terms: D000818:Animals; D002064:Buserelin / Q000008:administration & dosage / Q000493:pharmacokinetics*; D003505:Cyclodextrins; D003692:Delayed-Action Preparations; D005079:Excipients; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D013535:Suspensions; D047392:beta-Cyclodextrins
chemical_list: D003505:Cyclodextrins; D003692:Delayed-Action Preparations; D005079:Excipients; D013535:Suspensions; D047392:beta-Cyclodextrins; C031215:betadex; D002064:Buserelin