羟丙基-β-环糊精对吴茱萸次碱的增溶作用研究

摘要

Objective To improve the water solubility and bioavailability of rutaecarpine by using inclusion compound of hydroxypropyl-β-cyclodextrins and widening the application of rutaecarpine.Methods The inclusion compound of rutaecarpine-hydroxypropyl-β-cyclodextrins was prepared by using ultrasonic method.Then,powder X-ray diffraction,differential scanning calorime-try and infrared spectroscopy were used to identify and characterize the compound.High performance liquid chromatography (HPLC) was used to detect the solubility of the inclusion compound.Results Rutaecarpine and hydroxypropyl-β-cyclodextrins formed the inclu-sion compound,and the solubility of the inclusion compound was 90.40 mg/L,following formation of the compound.Conclusion Hydroxypropyl-β-cyclodextrins seemed to have good effect on the water solubility of rutaecarpine.The solubility of rutaecarpine was greatly increased through the formation of the inclusion compound.Consequently,it provided good evidence for further basic theoretic research in the development and application of rutaecarpine.%目的：为提高吴茱萸次碱的水溶性和生物利用度，用羟丙基-β-环糊精对其进行包合，拓宽吴茱萸次碱的药用途径。方法利用超声法制备吴茱萸次碱-羟丙基-β-环糊精包合物，通过粉末 X 射线衍射分析、差示扫描量热分析和红外光谱分析等方法对制备的吴茱萸次碱羟丙基-β-环糊精包合物进行鉴定和表征；应用高效液相色谱法对包合物的溶解度进行了测定。结果吴茱萸次碱与羟丙基-β-环糊精形成了包合物，包合后吴茱萸次碱的溶解度为90．40 mg／L。结论羟丙基-β-环糊精对吴茱萸次碱具有良好的增溶作用，通过包合物的生成大大提高了吴茱萸次碱的溶解度，为吴茱萸次碱的进一步开发利用提供了基础研究数据。