›› 2018, Vol. 36 ›› Issue (03): 398-404.

• • 上一篇    

妥曲珠利复合纳米胶束的制备

任丹丹,周建瑜,符华林,申芸,刘畅,凡国庆   

  1. 四川农业大学
  • 收稿日期:2017-08-14 修回日期:2018-04-28 出版日期:2018-06-28 发布日期:2018-11-29
  • 通讯作者: 符华林 E-mail:fuhl2005@sohu.com
  • 基金资助:
    四川省科技厅科技创新创业苗子工程项目

Preparation of toltrazuril composited nano-micelles

  • Received:2017-08-14 Revised:2018-04-28 Online:2018-06-28 Published:2018-11-29

摘要: 摘要:【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,选出NaDC(A)、Tx100(B)、Brij58(C)、水体积(D)和投药量(E)等5个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】妥曲珠利复合纳米胶束的最优处方为:NaDC:149.00mg,Tx100:198.50mg,Brij58:249.00mg,水化体积:5.58 mL),投药量:14.95mg。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3921.70±0.01μg/mL,是原药的8170.21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。

关键词: 妥曲珠利, 纳米胶束, 制备

Abstract: Abstract:[Objective] Construction of toltrazuril composited nano-micelles, improve the solubility of toltrazuril. [Methods] Through the single factor screening test of influence of formulation factors for preparing composited nano-micelles solution,results showed that the amount of NaDC (A), Tx100 (B), Brij58 (C), water volume (D) and dosage (E) possessed relatively higher effect on the formation of this drug delivery system, which were optimized by response surface method. [Results] The optimum prescription and process were as follows: the amount of NaDC, Tx100, Brij 58, water volume and dosage were 149.00mg, 198.50mg, 249.00mg, 5.58 mL and 14.95mg, respectively. The drug loading and encapsulation efficiency of the prepared nano-micelles were 20.3% and 89.8%.The saturated solubility of toltrazuril in the compositednano-micelles freeze-drying formulation in water at 37℃ was 3921.70± 0.01 mg/mL, 8170.21 times compared with the original drug.[Conclusion] Composite nano-micelles effectively increases the solubility of toltrazuril, can be further used in clinical.

Key words: Toltrazuril, Nano-micelles, Preparation