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Degradation of insulin was studied in this work. Casein and protamine could obviously suppress degradation of insulin by intestinal enzymes, and could protect insulin from degradation by the mechanism of competition and combination with proteolysis enzyme. What is more, co-incubated with HP-β-CD-casein or HP-β-CD-protamine, most insulin was protected from degradation by intestinal enzymes. In addition, it was found that the complexation of insulin with HP-β-CD was characterized by UV absorption spectra. These results indicated that HP-β-CD, casein and protamine could offer some positive and useful results, and could protect insulin from degradation during their transit through the intestinal tract.