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过程工程学报 ›› 2022, Vol. 22 ›› Issue (4): 533-541.DOI: 10.12034/j.issn.1009-606X.221127

• 研究论文 • 上一篇    下一篇

响应曲面法优化植物甾醇固体自微乳的工艺条件

黄硕， 胡雨欣， 沙露平， 刘剑桥， 郭永学*
  

  1. 沈阳药科大学制药工程学院，辽宁 本溪 117004
  • 收稿日期:2021-04-17 修回日期:2021-06-09 出版日期:2022-04-28 发布日期:2022-04-24
  • 通讯作者: 郭永学 yongxueguo@163.com
  • 作者简介:黄硕(1995-)，女，辽宁省本溪市人，硕士研究生，生物化工专业，E-mail: hs998hs@163.com；郭永学，通讯联系人，E-mail: yongxueguo@163.com.

Optimization of the technological conditions of phytosterol solid self?microemulsion using response surface methodology

Shuo HUANG,  Yuxin HU,  Luping SHA,  Jianqiao LIU,  Yongxue GUO*   

  1. School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Benxi, Liaoning 117004, China
  • Received:2021-04-17 Revised:2021-06-09 Online:2022-04-28 Published:2022-04-24
  • Contact: GUO Yong-Xue yongxueguo@163.com

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摘要： 为了提高植物甾醇在体内的生物利用度，促进其在医药中的广泛应用，在制备的植物甾醇液体自微乳基础上，进一步利用喷雾干燥制备固体自微乳，以提高其长期储存稳定性。首先筛选了载体材料的种类和用量，然后以集粉率为考察指标，在单因素实验的基础上进行响应面优化，确定喷雾干燥的最优工艺参数。结果表明，最优载体为胶体二氧化硅，在载体与自微乳的质量比为1:1、喷雾干燥的进风温度为120℃、进料速度10 mL/min、进风流量540 L/h，此时得到的集粉率为49.36%，与理论预测值基本一致。制得的S-SMEDDS为白色粉末，平均载药量为1.00%，重新分散在水中能形成淡蓝色澄清透明的乳液，再分散粒径为27.20±1.15 nm，多分散系数为0.137±0.010。药物以无定形的状态被吸附在胶体二氧化硅的孔径中，在不同的pH条件下，释放度有所不同，但与原料药相比，释放效果有了很大改善。

关键词: 植物甾醇, 自微乳, 胶体二氧化硅, 喷雾干燥, 响应面

Abstract: To improve the bioavailability of phytosterols in the body and promote the wide application of phytosterols in medicine, based on the preparation of phytosterol liquid self-microemulsions, the solid self-microemulsion is further prepared by spray drying to improve its transportation and long-term storage stability. First, the type and dosage of the optimal carrier material were selected by analyzing the adsorption capacity, desorption rate, and drug load capacity. Then, with the powder collection rate as an inspection indicator, based on a single factor, the experiment carried out response surface optimization, determined the optimal process parameters of spray drying, and carried out in vitro evaluation. The results showed that the optimal carrier was colloidal SiO2, the ratio of carrier to self-microemulsion was 1:1, the inlet air temperature of spray drying was 120℃, the feeding speed was 10 mL/min, and the inlet air flow was 540 L/h. At this time, the obtained powder collection rate was the largest, the value obtained by the fitting was 49.36%, which wa basically consistent with the theoretical prediction value.There was no significant difference between the predicted value and the actual value, indicating a good fit. The prepared S-SMEDDS was the white powder with an average drug loading of 1.00%. It can be re-dispersed in water to form a light blue clear and transparent emulsion. The re-dispersed particle size was 27.20±1.15 nm and the polydispersity coefficient was 0.137±0.010. According to DSC and SEM, the drug was adsorbed in the pore size of colloidal silica in an amorphous state. Under different pH conditions, the release degree was different, but compared with the bulk drug, the release effect had been greatly improved. It showed that the self-emulsifying drug delivery system can indeed increase the solubility of the drug in water and the permeability in the intestinal tract. In addition, the solid self-microemulsion obtained by spray drying and solidification was uniform in content, easy to store and transport and the application should be considered.

Key words: Phytosterol, self-microemulsion, colloidal silicon dioxide, spray dried, response