Page 102 - 《精细化工》2022年第5期

第 39 卷第 5 期 精 细 化 工 Vol.39, No.5
2022 年 5 月 FINE CHEMICALS May 2022

医药与日化原料
溶剂法制备降血糖肽固体分散体及其稳定性

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陈百科 ，李 慧 ，金素莱曼 ，包海蓉 1,2,3*
〔1. 上海海洋大学 食品学院，上海 201306；2. 上海水产品加工及贮藏工程技术研究中心，上海 201306；
3. 农业部水产品贮藏保鲜质量安全风险评估实验室（上海），上海 201306〕

摘要：以降血糖肽为模型，尤特奇 L-100（EL-100）为载体，羟丙基甲基纤维素（HPMC）为释放调节剂，采用
溶剂法制备了降血糖肽固体分散体，并对其稳定性和体外释放进行了研究。以降血糖肽固体分散体 2 h 的累积
释放率和二肽基肽酶-Ⅳ（DPP-Ⅳ）抑制率为评价指标，对肠溶载体和释放调节剂配比进行了优化，利用 SEM、
FTIR 和 TEM 对降血糖肽固体分散体进行了表征，并考察了降血糖肽固体分散体不同储存时间和储存温度下的
稳定性。结果表明，在 m(降血糖肽)∶m(EL-100)∶m(HPMC)=1∶2∶0.2 条件下制备的降血糖肽固体分散体 2 h
的累积释放率达到 93.54%，且 DPP-Ⅳ抑制率具有较高水平。SEM 和 TEM 分析表明，降血糖肽分散在固体分散
体中；FTIR 表明，降血糖肽二级结构的构象发生了变化。降血糖肽固体分散体能显著增强降血糖肽的稳定性，
常温（25 ℃）储存 10 d 后累积释放率仍高达 90.32%，在高温环境下也表现出较强的稳定性。
关键词：降血糖肽；固体分散技术；累积释放率；稳定性；DPP-Ⅳ抑制率；医药原料
中图分类号：TS218 文献标识码：A 文章编号：1003-5214 (2022) 05-0956-07

Preparation and stability of hypoglycemic peptide
solid dispersion by solvent method

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CHEN Baike , LI Hui , JIN Sulaiman , BAO Hairong 1,2,3*
[1. College of Food Science and Technology, Shanghai Ocean University, Shanghai 201306, China; 2. Shanghai
Engineering Research Center of Aquatic-Processing and Preservation, Shanghai 201306, China; 3. Laboratory of
Quality and Safety Risk Assessment for Aquatic Products on Storage and Preservation (Shanghai), Ministry of
Agriculture, Shanghai 201306, China]
Abstract: Hypoglycemic peptide solid dispersion was prepared by solvent method using hypoglycemic
peptide as model, Eudragit L-100 (EL-100) as carrier, hydroxypropyl methylcellulose (HPMC) as release
regulator. The stability and in-vitro release of hypoglycemic peptide solid dispersion were studied. The 2 h
cumulative release rate of solid dispersion and the inhibition rate of dipeptidyl peptidase Ⅳ (DPP-Ⅳ) were
used as evaluation indexes. The ratio of enteric carrier to release regulator was optimized. The solid
dispersion was characterized by SEM, FTIR and TEM, and its stability at different storage times and
temperatures was investigated. The results showed that m(hypoglycemic peptide)∶m(EL-100)∶m(HPMC) =
1∶2∶0.2 was the optimum mass ratio of hypoglycemic peptide solid dispersion. The 2 h cumulative
release rate of the solid dispersion prepared under this condition reached 93.54%, and the inhibition rate of
DPP-Ⅳ reached high level. SEM and TEM results indicated that the bioactive peptide was dispersed in the
solid dispersion. FTIR spectrum showed that the conformation of the secondary structure of the bioactive
peptide changed. The solid dispersion could significantly enhance the stability of hypoglycemic peptide,
and the cumulative release rate wass still as high as 90.32% after 10 d of storage at room temperature, it
also exhibited strong stability in high temperature environment.
Key words: hypoglycemic peptide; solid dispersion technology; cumulative release rate; stability; DPP-Ⅳ
inhibition rate; drug materials

收稿日期：2021-12-28; 定用日期：2022-02-08; DOI: 10.13550/j.jxhg.20211327
基金项目：国家重点研发计划项目（2019YFD0902000）
作者简介：陈百科（1996—），男，硕士生，E-mail：15869106150@163.com。联系人：包海蓉（1969—）,女，副教授，E-mail：
hrbao@shou.edu.cn。