[目的]构建妥曲珠利复合纳米胶束,改善妥曲珠利溶解性能.[方法]通过单因素试验筛选影响制备复合纳米胶束溶液的处方因素,进行响应面法优化设计,并对妥曲珠利复合纳米胶束的相关性质进行测定.[结果]选出NaDC(A)、Tx100(B)、Brij58(C)、水体积(D)和投药量(E)等5个因素,通过优化设计得到妥曲珠利复合纳米胶束的最优处方为:NaDC:149.00 mg,Tx100:198.50 mg,Brij58:249.00 mg,水化体积:5.58 mL,投药量:14.95 mg.该条件制得纳米胶束形态良好,妥曲珠利包封率为98.63％,载药量为3.38％,37℃饱和溶解度为(3 921.70±0.01)μg/mL,是原药的8 170.21倍.[结论]复合纳米胶束有效地增加了妥曲珠利溶解度,可以进一步用于临床.%[Objective]The aim of this study was to improve the solubility of toltrazuril by building toltrazuril composited nano-micelles.[Method]The factors that affect the preparation of composited nano-micelles solution were determined and optimized by response surface method in a single-factor experiment.Then the related properties of totrichol compound nano-micelle were measured.[Result]Five factors [NaDC(A),Tx100(B),Brij58(C),water volume(D)and dosage(E)] possessed relatively higher effect on the forma-tion of this drug delivery system were screened out.The optimum prescription and process were as follows:the amount of NaDC,Tx100,Brij 58,water volume and dosage were 149.00 mg,198.50 mg,249.00 mg,5.58 mL and 14.95 mg,respectively.The drug loading and encapsulation efficiency of the prepared nano-micelles were 20.3％and 89.8％,respectively.The saturated solubility of toltrazuril in the com-posited nano-micelles freeze-drying formulation in water at 37 ℃ was(3 921.70±0.01)mg/mL,which was 8 170.21 times as much as the solubility of the original drug.[Conclusion]Composite nano-micelles effectively increases the solubility of toltrazuril,providing important reference to further clinical applications.
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