羟丙基-β-环糊精对西罗莫司的增溶作用研究

Solubilization Effect of Hydroxypropyl-β-cyclodextrin on Sirolimus

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 investigate the enhancement of dissolution of sirolimus by its complexation with hydroxy- propyl-β-cyclodextrin. METHODS The inclusion complexes of sirolimus were prepared by ultrasonic method. The solubilizing power of hydroxypropyl-β-cyclodextrin were determined by phase solubility technique. X-ray diffraction（XRD）, Fourier transform infrared spectroscopy（FT-IR） and differential scanning calorimetry（DSC） were used to verify the formation of inclusion complexes. RESULTS Sirolimus and hydroxypropyl-β-cyclodextrin formed inclusion complexes. At 25 ℃, with hydroxypropyl-β-cyclodextrin concentration increased, the solubility of sirolimus rised from 1.18 mg.L^-1 up to 118.15 mg·L^-1, increased 100 times approximately. CONCLUSION Hydroxypropyl-β-cyclodextrin inclusion technology can rise the solubility of sirolimus significantly.