Uekama K, Otagiri M, Sakai A, Irie T, Matsuo N, Matsuoka Y
J Pharm Pharmacol. 1985 Aug;37(8):532-5. doi: 10.1111/j.2042-7158.1985.tb03061.x.
Inclusion complex formation of beclomethasone dipropionate (BMDP) with gamma-cyclodextrin (gamma-CyD) in water and in solid state was assessed by solubility analysis and X-ray diffractometry. The solid complex of BMDP with gamma-CyD in a molar ratio of 1:2 was prepared and its in-vitro release behaviour was investigated using an ointment release simulator. The release of BMDP from hydrophilic ointment was significantly improved by the gamma-CyD complexation. Permeation and uptake studies indicated that the enhanced release of BMDP from the ointment may be due to the faster dissolution and the lower binding affinity of the complex in the ointment base. The vasoconstrictor activity of BMDP in man was found to be increased by gamma-CyD complexation, suggesting an improvement in the percutaneous absorption of BMDP.
通过溶解度分析和X射线衍射法评估了丙酸倍氯米松(BMDP)与γ-环糊精(γ-CyD)在水相和固态下包合物的形成。制备了摩尔比为1:2的BMDP与γ-CyD的固体复合物,并使用软膏释放模拟器研究了其体外释放行为。γ-CyD包合作用显著改善了BMDP从亲水性软膏中的释放。渗透和摄取研究表明,软膏中BMDP释放增强可能是由于复合物在软膏基质中溶解更快且结合亲和力更低。发现γ-CyD包合作用可增强BMDP在人体中的血管收缩活性,表明BMDP的经皮吸收得到改善。