摘要
目的:制备多烯紫杉醇磺丁基醚-β环糊精(SEB-β-CD)包合物,提高药物的溶解度。方法:采用冷冻干燥法制备包合物,考察磺丁基醚-β-环糊精与药物在不同主客分子比例、不同制备时间、不同制备温度时多烯紫杉醇的增溶作用,并利用差示扫描量热法(DSC)、红外光谱法(IR)、X-射线衍射法和1H-NMR核磁共振法对所制备的包合物进行结构验证,选择最佳制备工艺。结果:当药物与SEB7-β-CD摩尔比均为1∶70,制备时间2h,制备温度25℃时,多烯紫杉醇增溶效果最好,溶解度为442.21mg.L-1。经结构验证,说明形成包合物。结论:利用制备多烯紫杉醇环糊精包合物的方式,可显著提高药物的溶解度。
OBJECTIVE To investigate the inclusion complexes of docetaxel （DTX） with sulfobutyl-etherl-β-cyclodextrin （SEB-β-CD）. METHODS The solid inclusion complexes of DTX/SEBT-β-CD were prepared in different mole ratios, reaction time and temperature by freezed drying method. The characteristics of which were studied preliminarily by in vitro dissolution test, differential scanning calorimetry（DSC）, X ray diffraction, infra red spectroscopy,^1H NMR. RESULTS Total drug solubility was evidently increased to 442.21 mg·L^-1 under mole ratios 1：70, 2 h reaction time at 25 ℃. The solid inclusion complexes were formed according to structure verification test. CONCLUSION The e solubility of DTX was improved by SEB7-β-CD complexation obviously.
出处
《中国医院药学杂志》
CAS
CSCD
北大核心
2010年第18期1541-1545,共5页
Chinese Journal of Hospital Pharmacy
关键词
多烯紫杉醇
磺丁基醚-Β-环糊精
包合物
溶解度
制备
docetaxel
sulfobutyl-etherl-β-cyclodextrin
inclusion complexes
dissolution
preparation
