Abstract: The complexation of Toltrazuril (Tol) with hydroxypropyl-b-cyclodextrin (HP-b-CD) was studied. Solution-stirring method was selected to prepare the Toltrazuil-hydroxypropyl-b-cyclodextrin inclusion complex (Tol-HP-b-CD). The effects of concentration of acetonitrile, temperature, inclusion molar ratio of HP-b-CD to Tol, and pH value on its yield, inclusion ratio and drug loading ratio were studied. The complex was evaluated by thin layer chromatography, phase solubility technique and microscope. The results showed that the complex prepared under the optimized conditions had the average yield, inclusion ratio and drug loading ratio of 86.45%, 60.44% and 7.00%, respectively. Solubility of Tol was increased up to 9.90 mg/mL by complexation with HP-b-CD, compared with the unprocessed Tol. It is evident from the results that complexation with HP-b-CD is a feasible way to prepare a rapidly dissolved Tol oral product.

Key words: Toltrazuril, hydroxypropyl-b-cyclodextyin, inclusion complex, phase solubility

摘要： 采用溶剂搅拌法制备妥曲珠利羟丙基-β-环糊精包合物，考察了乙腈浓度、包合温度、主客分子比、pH值对回收率、包合率和含药率的影响，用显微镜法、薄层法及相溶解度法对包合物进行鉴定，测定包合物的饱和溶解度，并对包合机制进行了探讨. 结果表明，优化工艺所制包合物平均回收率为86.45%，平均包合率为60.44%，平均含药率为7.00%，饱和溶解度达9.90 mg/mL，具有良好的水溶性.

关键词: 妥曲珠利, 羟丙基-β-环糊精, 包合物, 相溶解度