[关键词]
[摘要]
目的 探讨环糊精包合物对紫杉醇的溶解作用及环糊精与药物之间的相互作用规律。方法 考察β-环糊精和羟丙基-β-环糊精为包合材料对紫杉醇增溶作用的影响;1H-NMR探讨包合物形成时主客分子之间化学位移的相互作用。结果 包合物材料对包合物形成起主导作用,羟丙基-β-环糊精对紫杉醇增溶作用明显优于β-环糊精,且增溶作用随其比例的增加而增大;1H-NMR分析显示羟丙基-β-环糊精与紫杉醇分子中芳香环的作用最显著。结论 羟丙基-β-环糊精能够有效地提高难溶性药物紫杉醇的溶解度。
[Key word]
[Abstract]
Objective To investigate the solubilitization effect of macromolecular paclitaxel with cyclodextrin and mechanism between inclusion complex and drugs. Methods The influence effects on paclitaxel solubility were studied with β-cyclodextrin (β-CD) and hydroxypropyl-β-cyclodextrin (HP-β-CD) as inclusion carriers. The chemical shifts of hydrogen atom in host and guest molecules were also investigated with 1H-NMR. Results The form of inclusion complex was responsible by host molecules and the enhancement solubility of paclitaxel in HP-β-CD was larger than that in β-CD and increased with the ratio increasing. The benzene ring in the molecular of HP-β-CD and paclitaxel showed the most significant effect. Conclusion The solubility of diossolved paclitaxel is improved by hydroxypropyl-β-cyclodextrin.
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[基金项目]
江苏省科技厅社会发展资助项目(BS200522);江苏省高新技术产业发展资助项目(JHB05-46);苏州大学医学发展基金资助项目(EE132503)