枸橼酸他莫昔芬-羟丙基-β-环糊精包合物的制备与表征

Preparation and characterization of Tamoxifen hydroxypropyl-β-cyclodextrin inclusion complex

目的制备和鉴定枸橼酸他莫昔芬包合物,并考察包合物的有关性质。方法通过影响因素考察选择适当的pH和包合材料,摩尔连续递变法确定最佳主客分子的摩尔比,采用研磨法、水溶液搅拌-冷冻干燥法和超声-冷冻干燥法制备枸橼酸他莫昔芬包合物;采用热重分析法、红外和紫外色谱法鉴定包合物,并考察包合物的包合率、光照稳定性、溶解度和体外溶出度等性质。结果采用HP-β-CD为包合材料,确定HP-β-CD与枸橼酸他莫昔芬包合的最佳摩尔比为4∶1,所得产品经鉴别已形成包合物。枸橼酸他莫昔芬-HP-β-CD包合物能明显增大药物的溶解度,提高药物的溶出度和光照稳定性。结论研究结果可为研发枸橼酸他莫昔芬的新剂型提供实验依据。

OBJECTIVE To prepare and identify Tamoxifen hydroxypropyl - β - cyclodextrin （ Tam - HP - β - CD） inclusion complex, and to investigate its characteristics. METHODS The appropriate pH,inclusion material and the best molar ratio of host and guest were determined by influencing factor experiment and mole gradient and continuing alternation method ,respectively. The inclusion complex was prepared by grinding, aqueous mixing - freeze drying and ultrasonic - freeze drying and then identified by thermogravimetric analysis, infrared chromatography（ FT - IR） and UV. At last, the properties of the inclusion complex, including the inclusion rate, light stability, dissolvability and in vitro dissolution rate were investigated. RESULTS The 4 ： 1 ratio of HP - β - CD and Tam was determined to prepare inclusion complex, which was also identified by the above three methods and techniques. CONCLUSION The results provide the experiment basis for the further study of Tam new dosage forms.