溶剂法制备降血糖肽固体分散体及稳定性研究

以降血糖肽为模型，Eudragit L-100和HPMC为载体，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开展了研究。本文以降血糖肽固体分散体2 h的累计释放率和DPP-IV抑制率为评价指标，通过对肠溶载体和释放调节剂的比例进行优化，利用扫描电镜、傅里叶红外光谱仪和透射电镜对固体分散体进行表征，并考察了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，降血糖肽固体分散体的最佳比例为降血糖肽:Eudragit L-100:HPMC=1:2:0.2，此比例下制备的固体分散体2 h的累计释放率能达到93.54%，且DPP-IV抑制率仍具有较高水平。扫描电镜和透射电镜图像表明，活性肽分散在固体分散体中，红外光谱表明，活性肽二级结构的构象发生了变化。制成固体分散体后，降血糖肽的稳定性显著增强，常温储存10 d后累计释放率仍高达90.32%，在高温环境下也表现出较强的稳定性。综上所述，利用固体分散技术能在保持降血糖肽生理活性的基础上显著提高稳定性和累计溶出率，该方法对活性肽的综合利用，特别是基于活性肽的功能性食品的研发有较大的参考价值。

Preparation of hypoglycemic peptide solid dispersions by solvent method and its stability

Taking hypoglycemic peptides as models, Eudragit L-100 and HPMC as the carriers, the solid dispersions of hypoglycemic peptides were prepared by Solvent method, and their stability and in vitro release were studied. In this paper, the cumulative release rate and DPP-IV inhibition rate of the glycemic peptide solid dispersion at 2 h were evaluated, and the solid dispersion was characterized by scanning electron microscopy, Fourier infrared spectroscopy and transmission electron microscope by optimizing the ratio of enteric-coated carrier and release regulator, and the stability of the solid dispersion under different storage times and storage temperatures was investigated. The results showed that the optimal proportion of glycemic peptide solid dispersions was hypoglycemic peptides: Eudragit L-100: HPMC=1:2:0.2, and the cumulative release of the solid dispersions prepared under this ratio for 2 h could reach 93.54%, and the DPP-IV inhibition rate still had a high level. Scanning electron microscopy and transmission electron microscopy images show that the active peptide is dispersed in a solid dispersion, and infrared spectroscopy indicates that the conformation of the secondary structure of the active peptide has changed. After making a solid dispersion, the stability of hypoglycemic peptides was significantly enhanced, and the cumulative release rate after 10 days of storage at room temperature was still as high as 90.32%, which also showed strong stability in high temperature environment. In summary, the use of solid dispersion technology can significantly improve the stability and cumulative dissolution rate on the basis of maintaining the physiological activity of hypoglycemic peptides, and this method has great reference value for the comprehensive utilization of active peptides, especially the research and development of functional foods based on active peptides.