摘要
目的制备紫杉醇羟丙基-β-环糊精(HP--βCD)包合物并对其进行鉴定。方法运用相溶解度法进行增溶实验,采用溶液搅拌法制备紫杉醇HP-β-CD包合物,利用FT-IR、XRD和DSC对包合物进行鉴定。结果紫杉醇与HP-β-CD的相溶解度曲线呈现典型的AP型,包合物鉴定结果显示,物理混合物图谱与包合物图谱有显著性差异。结论HP-β-CD可以显著提高紫杉醇的溶解度及溶出速率,紫杉醇被HP--βCD包合后呈现了新的物相特征,表明包合物已经形成。
OBJECTIVE To investigate and identify the inclusion complexation of paclitaxel with HP-β-CD. METHODS Phase solubility method was used to study the solubility of paelitaxel and solution stirring method was utilized to prepare the inclusion complex. Paclitaxel/HP-β-CD complexes were investigated and confirmed by FT-IR, DSC and X-ray power diffraction method. RESULTS The inclusion complex of with the molar ratio of paelitaxel with HP-β-CD above 1 : 1 was formed in aqueous solution. The phase solubility ctiagram exhibited Ap-type, and the change of enthalpy change (△H°) was found to be positive. High temperature favored the progress of complexing process. Additive was helpful to increase the solubility of paclitaxel. CONCLUSION HP-β-CD could increase the solubility and dissolution rate of paclitaxel. The inclusion complex exhibited some new physical characteristics and the results showed the inclusion complex was formed.
出处
《中国药学杂志》
CAS
CSCD
北大核心
2010年第4期283-286,共4页
Chinese Pharmaceutical Journal
基金
中国博士后科学基金项目(20060390978)资助
关键词
羟丙基-Β-环糊精
紫杉醇
包合物
体外溶出度
物相鉴定
HP-β-CD
paclitaxel
inclusion complex
in vitro dissolution
physiochemical identification