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目的为提高吴茱萸次碱的水溶性和生物利用度,用β-环糊精对其进行包合,拓宽吴茱萸次碱的药用途径。方法利用溶液搅拌法制备吴茱萸次碱-β-环糊精包合物,通过粉末X射线衍射分析、红外光谱分析和差示扫描量热分析等方法对制备的吴茱萸次碱β-环糊精包合物进行鉴定和表征;应用HPLC法对包合物的溶解度进行了测定。结果吴茱萸次碱与β-环糊精形成了包合物,吴茱萸次碱不溶于水,包合后吴茱萸次碱的溶解度为10.67μg·ml-1。结论β-环糊精对吴茱萸次碱具有良好的增溶作用,吴茱萸次碱环糊精包合物的制备方法简捷实用,达到了增加药物溶解度的目的,有助于吴茱萸次碱的进一步开发利用。
OBJECTIVE To improve the water solubility and bioavailability of rutaecarpine, β-cyclodextrin inclusion and broadening of the pharmacological pathway of rutaecarpine were investigated. Methods The contents of rutaecarpine-β-cyclodextrin inclusion complex were prepared by solution stirring method. The contents of rutaecarpine-Ⅱ-cyclodextrin inclusion complex were determined by powder X-ray diffraction analysis, infrared spectroscopy and differential scanning calorimetry The compounds were identified and characterized. The solubility of inclusion compound was determined by HPLC. Results The residues of rutaecarpine and β-cyclodextrin formed inclusion complexes. The rutaecarpine was insoluble in water, and the solubility of rutaecarpine was 10.67μg · ml-1 after inclusion. Conclusion β-cyclodextrin has good solubilization on rutaecarpine. The preparation method of rutaecarpine-based cyclodextrin inclusion complex is simple and practical, and has the purpose of increasing the solubility of the drug and contributing to the further development and utilization of rutaecarpine .