EP4048230A1 — Oral gliptin compositions and method for preparation thereof

USPTO Abstract

Described is an aqueous liquid oral gliptin composition comprising a gliptin or a pharmaceutically acceptable salt or ester thereof, and an artificial non-sugar alcohol sweetening agent, the solution having a sugar alcohol content of less than 25 w/v%. The composition has an improved taste and stability as compared to known compositions. Also described is a method comprising the steps of heating 80 – 95 v/v% of the water to 40 - 65°C, admixing the antioxidant, and, if present, the chelating agent and buffering agent, optionally, cooling down to 25 - 35°C, admixing sweetener, and, if present, preservative agent, and optionally pH adjusting agent or a portion of the pH adjusting agent, admixing the gliptin, if necessary, adjust the pH to the envisaged value by addition of a pH adjusting agent, admix the thickening agent, optionally in the form of a solution of the thickening agent in a co-solvent, homogenising the obtained mixture, admixing, if present, the wetting agent, if necessary, adjust the final volume by adding from the rest of the water, optionally filter through a 10 µm sieve, and filling in an appropriate container.