E. Ziv et al., ORAL-ADMINISTRATION OF INSULIN IN SOLID FORM TO NONDIABETIC AND DIABETIC DOGS, Journal of pharmaceutical sciences, 83(6), 1994, pp. 792-794
It was previously demonstrated that a biologically active insulin coul
d cross the mucosal membrane in the gut by using surface active substa
nces. In this report we describe studies in which insulin administered
orally, in a solid formulation, was effectively absorbed in the canin
e model. The insulin was mixed with cholate and soybean trypsin inhibi
tor. It was delivered orally, as enterocoated microtablets, to nondiab
etic and diabetic (pancreatectomized) dogs in a fasting state. The tim
e 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 fo
r more than 90 min following administration of the drug. In this model
a pronounced increment in plasma insulin levels was shown prior to th
e drop of plasma glucose concentrations. It is concluded that with thi
s novel oral insulin formulation a beneficial biological effect can be
achieved in the treatment of diabetes.