沙丁胺醇乙基化β环糊精包合物的研制

Preparation of inclusion complex of salbutamol-ethylated β cyclodextrins

目的 制备沙丁胺醇 乙基化 β环糊精包合物 ,考察其有关性质。方法 采用冷冻干燥法和研磨法制备其包合物。结果 经ESI MS和X射线衍射法鉴定 ,表明沙丁胺醇与乙基化 β环糊精 (ECD)确已形成包合物 ,ESI MS和含量测定证明包合物主、客分子比为 1∶1;包合物的相溶解度图为BI 型 ,表明难溶性包合物形成。结论 沙丁胺醇 乙基化 β环糊精包合物可明显降低沙丁胺醇的溶解度和释放度 ,说明ECD可作为一种缓释载体。

OBJECTIVE: To prepare the inclusion complex of salbutamol(SAL)-ethylated β-cyclodextrins(ECD) and investigate its properties. METHODS: The inclusion complex of SAL-ECD was prepared by freeze-drying or milling. RESULTS: The inclusion complex of SAL-ECD was confirmed by powder X-ray diffractometry as a solid or by ESI-MS as a methanol solution. Meanwhile, the ESI-MS and the content analysis of the inclusion complex showed that the molecular ratio of SAL to ECD was 1: 1. The phase solubility diagram showed that it was BI-type, which indicated the formation of insoluble inclusion complex in water. CONCLUSION: The aqueous solubility and release rate of SAL were decreased when the drug was included by ECD. These results indicated ECD may be used as a hydrophobic drug carrier for sustained-release of drugs.