Oral Administration of Insulin in Solid Form to Nondiabetic and Diabetic Dogs

• Published in: Journal of pharmaceutical sciences 1994-06, Vol.83 (6), p.792-794
• Main Authors: Ziv, Ehud, Kidron, Miriam, Raz, Itamar, Bar‐On, Hanoch, Krausz, Michael, Blatt, Yoav, Rotman, Avner
• Format: Article
• Language: English
• Subjects: Administration, Oral; Animals; Biological and medical sciences; Diabetes Mellitus, Experimental - drug therapy; Diabetes Mellitus, Experimental - metabolism; Dogs; General and cellular metabolism. Vitamins; Insulin - administration & dosage; Insulin - pharmacokinetics; Medical sciences; Pharmacology. Drug treatments
• ISSN: 0022-3549; 1520-6017
• DOI: 10.1002/jps.2600830606

It was previously demonstrated that a biologically active insulin could cross the mucosal membrane in the gut by using surface active substances. In this report we describe studies in which insulin administered orally, in a solid formulation, was effectively absorbed in the canine model. The insulin was mixed with cholate and soybean trypsin inhibitor. It was delivered orally, as enterocoated microtablets, to nondiabetic and diabetic (pancreatectomized) dogs in a fasting state. The time interval between the administration of the drug and the beginning of a decrease in the plasma glucose levels was 60–140 min. This decrease reached a minimum level of 20–40 % of the initial values and lasted for more than 90 min following administration of the drug. In this model a pronounced increment in plasma insulin levels was shown prior to the drop of plasma glucose concentrations. It is concluded that with this novel oral insulin formulation a beneficial biological effect can be achieved in the treatment of diabetes.