Uekama K, Arima H, Irie T, Matsubara K, Kuriki T
Faculty of Pharmaceutical Sciences, Kumamoto University, Japan.
J Pharm Pharmacol. 1989 Dec;41(12):874-6. doi: 10.1111/j.2042-7158.1989.tb06393.x.
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.
已对七（2,6 - 二 - O - 乙基）-β-环糊精（DE-β-CyD）作为醋酸布舍瑞林（一种促黄体生成激素释放激素超级激动剂）的肠胃外缓释载体的潜在用途进行了研究。与DE-β-CyD络合显著延缓了布舍瑞林从油性混悬液中的体外释放，这主要是由于络合物的水溶性较差。向大鼠单次皮下注射含布舍瑞林 - DE-β-CyD络合物的混悬液，可使布舍瑞林在血浆中有效持续至少一个月，表明其对内分泌依赖性疾病的治疗具有潜在疗效。这些结果表明，DE-β-CyD可作为一种适用于醋酸布舍瑞林长期治疗的可注射缓释药物载体。
