Novel oral microspheres of insulin with protease inhibitor protecting from enzymatic degradation

Eudragit L100 insulin microspheres (IMS) containing a protease inhibitor were prepared for an oral dosage form of insulin. The efficiencies of insulin incorporation of IMS containing trypsin inhibitor (TI), chymostatin (CS), Bowman-Birk inhibitor (BBI) and aprotinin (AP) amounted to approx. 80% and did not differ among the preparations. In a release study, the more than 90% of insulin remaining after treatment of simulated gastric fluid was...