Impact of Insulin Tregopil and its Permeation Enhancer on Pharmacokinetics of Metformin in Healthy Volunteers: Randomized, Open‐label, Placebo Controlled, Crossover Study

Abstract

Oral insulin tregopil (IN‐105; new drug under development) may be co‐administered with oral anti‐diabetic drugs such as metformin in type 2 diabetes mellitus patients for optimal glycemic control. IN‐105 has sodium caprate excipient, a permeation enhancer, for enhancing absorption in stomach and increasing bioavailability via oral route. Sodium caprate may increase bioavailability of metformin by a similar mechanism. Therefore, it was necessary to study effect of IN‐105 on pharmacokinetics of metformin. In this randomized, open‐label, cross‐over study, metformin was administered to healthy volunteers receiving IN‐105/placebo under fed/fasting conditions. 90% CI of GMR of AUC_0‐inf (fasting and fed) and C_max (fed) of metformin were within 0.80–1.25. Under fasting conditions, upper bound margin of C_max was just beyond this range (i.e. 1.27) and was concluded as functionally not relevant. There was no clinically significant effect of sodium caprate/IN‐105 on pharmacokinetics of metformin under fasting/fed conditions and it was safe.

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