Sustained release of buserelin acetate, a luteinizing hormone-releasing hormone agonist, from an injectable oily preparation utilizing ethylated beta-cyclodextrin.
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.
Uekama
K
K
Faculty of Pharmaceutical Sciences, Kumamoto University, Japan.
Arima
H
H
Irie
T
T
Matsubara
K
K
Kuriki
T
T
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
D003505:Cyclodextrins; D003692:Delayed-Action Preparations; D005079:Excipients; D013535:Suspensions; D047392:beta-Cyclodextrins; C031215:betadex; D002064:Buserelin