茶树油羟丙基-β-环糊精包合工艺研究及其包合物评价

Study on the inclusion technic of hydroxypropyl-β-cyclodextrin in tea tree oil and evaluation of its included compounds

目的以羟丙基-β-环糊精(hydroxypropyl-β-cyclodextrin,HP-β-CD)为包合材料,优化茶树油包合物制备工艺,并对其药剂学性能进行考察。方法以茶树油HP-β-CD包合物的产率、包封率为评价指标,采用正交试验法优化茶树油HP-β-CD的制备工艺,利用差示扫描量热法、红外光谱法对包合物进行物相鉴别,考察茶树油HP-β-CD的稳定性。结果茶树油HP-β-CD制备的最佳工艺为:茶树油∶HP-β-CD=1∶10(ml∶g),包合温度为40℃,包合时间1 h。茶树油载药量为(9.25±3.25)%。红外光谱和差示扫描量热法检测结果显示,制成包合物后茶树油特征峰消失,表明茶树油和HP-β-CD确已形成包合物。包合物80℃水浴8 h后,茶树油保留率为40%,为未包合茶树油保留率的4.32倍,表明茶树油HP-β-CD稳定性良好。结论以HP-β-CD为骨架材料,制备的茶树油包合物包合率高、稳定性良好,在药品及化妆品制剂中具有一定的推广价值和应用前景。

Objective This study takes hydroxypropyl-β-cyclodextrin(HP-β-CD)as the inclusion materials to optimize the preparation technic of tea tree oil(TTO)and evaluate its pharmaceutical performance.Methods Take the production rate of HP-β-CD tea tree oil inclusion and entrapment rate as the evaluation index,taking the orthogonal test method to optimize the production technic of tea tree oil(HP-β-CD)inclusion and using infrared(IR),differential thermal scanning(DSC)method to characterize the inclusion compound to analyze the stability of TTO-HP-β-CD.Results The best technic to produce HP-β-CD tea tree oil is as follow:the ratio of TTO and HP-β-CD should be equal to 1/10,at 40℃,within 1 h.The average drug loading shoud be 9.25%±3.25%.The IR,DSC characterization results showed that the characteristic peak of tea tree oil disappeared after the microspheres,which indicated the HP-β-CD encapsulated the tea tree oil with good compatibility.In 80℃water bath,the TTO-HP-β-CD was stable with the retention rate 40%after 8 h,the retention rate was 4.32 times than that of the unwrapped tea tree oil.Conclusions The HP-β-CD tea tree oil obviously has higher rate of inclusion and stability.Therefore,it’s worth to promoting and being used in the pharmacy preparations and cosmetics field.