文章摘要
苏卫,贺双艳.辅酶Q10过饱和自微乳的制备及特性研究[J].中国药事,2022,36(9):1049-1060
辅酶Q10过饱和自微乳的制备及特性研究
On Preparation and Characteristics of Coenzyme Q10 Supersaturated Selfmicroemulsion
  
DOI:10.16153/j.1002-7777.2022.09.011
中文关键词: 辅酶Q10  促过饱和物质  过饱和自微乳化释药系统  粒径  Box-Behnken响应面法  溶解度  稳定性
英文关键词: coenzyme Q10  supersaturated promoting substances  supersaturated self-emulsifying drug delivery system  particle size  box-behnken response surface methodology  solubility  stability
基金项目:
作者单位
苏卫 湖南省肿瘤医院,长沙 410013 
贺双艳 湖南省肿瘤医院,长沙 410013 
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中文摘要:
      目的: 制备辅酶Q10过饱和自微乳化释药系统(S-SMEDDS),并对其体外特性进行研究。 方法:以粒径和自乳化时间为指标,通过Box-Behnken响应面法优化得出最佳SMEDDS处方比例; 再通过考察混合油相中辅酶Q10的饱和溶解度来确定辅酶Q10 SMEDDS处方载药量;最后考察促饱和物质与辅酶Q10 SMEDDS的相容性及乳化后的稳定性,得出加入促饱和物质的种类和用量;并对辅酶Q10 S-SMEDDS的理化特性进行测定。结果:辅酶Q10 S-SMEDDS的最优处方为中链甘油三酯(MCT)-聚氧乙烯醚氢化蓖麻油(Cremophor EL)-辛酸癸酸聚乙二醇甘油酯(Labrasol)配比为30.92∶58.94∶40,辅酶Q10的载药量为8.3%,羟丙甲基纤维素K100(HPMC K100)的加入量为 2%,形成的微乳粒径平均值为28.90 nm,乳化时间平均值为29.49 s,电位平均值为-31.15 mV,溶出度在20 min时达到90.11%。结论:所制备的辅酶Q10 S-SMEDDS可明显提高其溶解度,且乳化后稳定性更好,比普通SMEDDS更具有优势。
英文摘要:
      Objective: To prepare Coenzyme Q10 supersaturated self-microemulsion drug delivery system (Coenzyme Q10 S-SMEDDS) and study its in vitro properties. Methods: Taking particle size and selfemulsification time as indicators, the optimal proportion of SMEDDS prescription was obtained through optimizing Box-Behnken response surface methodology; the drug loading of Coenzyme Q10 SMEDDS was determined by investigating the saturated solubility of Coenzyme Q10 in mixed oil phase; Finally, the type and dosage of saturation promoting substances were gotten by investigating the compatibility of saturation promoting substances with Coenzyme Q10 SMEDDS and the stability after emulsification; the physical and chemical properties of Coenzyme Q10 S-SMEDDS were determined. Results: The optimal prescription of Coenzyme Q10 S-SMEDDS is MCT-Cremophor EL-Labrasol (30.92∶58.94∶40). The drug loading of Coenzyme Q10 in SMEDDS is 8.3%, the addition amount of Hydroxypropyl methyl cellulose K100 (HPMC K100) is 2%, the formed microemulsion has an average particle size of 28.90 nm, an average emulsification time of 29.49 s and an average potential of -31.15 mV, and the dissolution rate reaches 90.11% at 20 min. Conclusion: The prepared Coenzyme Q10 S-SMEDDS could significantly improve its solubility, and the stability is better after emulsification. S-SMEDDS has more advantages than ordinary SMEDDS.
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