| 引用本文: | 章莹,鲁一,刘静宇,王娟,师俊萍.羟丙基-β-环糊精对西罗莫司的增溶作用研究[J].中国现代应用药学,2012,29(12):1116-1120. |
| ZHANG Ying,LU Yi,LIU Jingyu,WANG Juan,SHI Junping .Solubilization Effect of Hydroxypropyl-β-cyclodextrin on Sirolimus[J].Chin J Mod Appl Pharm(中国现代应用药学),2012,29(12):1116-1120. |
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| 摘要: |
| 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。 |
| 关键词: 西罗莫司 羟丙基-β-环糊精 包合 |
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| Solubilization Effect of Hydroxypropyl-β-cyclodextrin on Sirolimus |
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ZHANG Ying, LU Yi, LIU Jingyu, WANG Juan, SHI Junping
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The First People’s Hospital of Kaifeng, Kaifeng 475000, China
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| Abstract: |
| 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. |
| Key words: sirolimus hydroxypropyl-β-cyclodextrin inclusion |
