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目的研究羟丙基-β-环糊精包合对难溶于水的西罗莫司溶解度的增强作用。方法采取超声法制备西罗莫司-羟丙基-β-环糊精包合物,用相溶解度法考察羟丙基-β-环糊精的增溶能力,以X射线衍射法、傅立叶红外光谱法、差示扫描量热法验证包合物的形成。结果西罗莫司与羟丙基-β-环糊精形成了包合物,在25℃条件下,随着羟丙基-β-环糊精浓度的增加,西罗莫司的溶解度由1.18 mg·L-1上升到118.15 mg·L-1,提高了约100倍。结论羟丙基-β-环糊精的包合技术能显著提高西罗莫司的溶解度。
Objective To study the effect of hydroxypropyl-β-cyclodextrin inclusion on the solubility of sirolimus insoluble in water. Methods The inclusion compound of sirolimus-hydroxypropyl-β-cyclodextrin was prepared by ultrasonic method. The solubility of hydroxypropyl-β-cyclodextrin was investigated by phase solubility method. The X-ray diffraction, Fourier transform infrared Spectroscopy and Differential Scanning Calorimetry were used to verify the formation of inclusion complexes. Results Sirolimus and hydroxypropyl-β-cyclodextrin form an inclusion complex. The solubility of sirolimus increases with the increase of hydroxypropyl-β-cyclodextrin concentration at 25 ℃ from 1.18 mg · L-1 increased to 118.15 mg · L-1, increased about 100 times. Conclusion The inclusion of hydroxypropyl-β-cyclodextrin can significantly improve the solubility of sirolimus.