星点设计-效应面法优化大蒜素-羟丙基-β-环糊精包合物滴鼻液的制备工艺

Optimization of preparation of allicin-hydroxyl-β-cyclodextrin inclusion complex nasal drops by central composite design-response surface method

目的:制备大蒜素-羟丙基(HP)-β-环糊精(CD)包合物滴鼻液并对其工艺进行优化。方法:以HP-β-CD对大蒜素进行包合,以包合物收率、滴鼻液中大蒜素含量为综合评价指标,采用星点设计-效应面法对大蒜素滴鼻液的工艺进行优化,考察HP-β-CD与大蒜素比例、包合温度、包合时间等因素的影响,并对大蒜素包合物进行红外、紫外和显微鉴别。结果:大蒜素滴鼻液的最佳制备工艺为:以水为包合溶媒,HP-β-环糊精和大蒜素的比例为32∶1,搅拌速度200 r·min-1,包合温度35℃,包合时间1.5 h。在此条件下,大蒜素的包合率达到90.25%。红外、紫外和显微鉴别结果均表明,大蒜素以包合物形式存在于滴鼻液中。结论:采用星点设计-效应面法优化所得大蒜素HP-β-CD包合物滴鼻液的制备工艺合理可行,为大蒜素液体制剂的进一步开发奠定了基础。

OBJECTIVE To prepare the inclusion complex nasal drops of allicin oil with hydroxyl-β-cyclodextrin （HP-β-CD）, and optimize the preparation process. METHODS With the overall desirability （OD） values of inclusion ratio and allicin con- tent as indexes, the influence of HP-β-CD-allicin ratio, inclusion temperature and inclusion time on inclusion process was inves- tigated by central composite design-response surface method （CCD-RSM）. The inclusion complex was verified by IR, UV and microscopical identification. RESULTS The inclusion ratio of allicin reached to 90. 25 % with the optimum inclusion technology as follows： inclusion solvent water, HP-β-CD to allicin oil 32：1, stirring rate 200 r-min-1, inclusion temperature 35 ℃, inclu- sion time 1.5 h. The results of IR, UV and microscopical identification showed that allicin existed in nasal drops in the form of inclusion. CONCLUSION The preparation process of inclusion complex of allicin oil with HP-β-CD optimized by CCD-RSM is reasonable and feasible, and can lay the foundation for the further development of allicin liquid preparations.