Abstract
These studies were designed to evaluate some of the in vivo characteristics of the insulin derivative, succinyl amido phenyl glucopyranoside insulin (SAPG-insulin). The in vitro bioeffectiveness studies in isolated rat fat cells demonstrated that the monosubstituted SAPG-insulin derivatives retained their full biological activity, while disubstituted SAPG-insulin had a reduced bioactivity. This is in good agreement with previous in vivo biological assay results. The antigenicity of both SAPG-insulin and native bovine insulin was examined in a rabbit model; no antibody formation was observed, indicating that the derivatization of insulin does not result in an immune response. In addition, plasma disappearance and liver uptake studies in dogs demonstrated that SAPG-insulin is handled in the same manner as native insulin in vivo.
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