Fast-acting insulin composition comprising a substituted anionic compound and a polyanionic compound
Inventors
Soula, Olivier • Charvet, Richard • Alluis, Bertrand
Assignees
Interested in licensing this patent?
MTEC can help explore whether this patent might be available for licensing for your application.
Publication Number
US-9795678-B2
Publication Date
2017-10-24
Expiration Date
Abstract
A composition, in the form of an aqueous solution, including insulin in hexameric form, at least one substituted anionic compound of non-saccharide structure and at least one polyanionic compound other than the substituted anionic compound.
Core Innovation
The invention relates to aqueous insulin compositions that comprise insulin in hexameric form and at least one substituted anionic compound of non-saccharide structure. The substituted anionic compound corresponds to formula I and is defined by hydrocarbon-based radical R, an aromatic amino acid radical AA bearing at least one free acid function, and a divalent radical E.
The formula includes functions F, F', and F'' selected from amide, carbamate and urea functions, with p being an integer between 1 and 3, m and n being integers between 0 and 6, and m+n being an integer between 1 and 6. The compositions additionally comprise at least one polyanionic compound other than the substituted anionic compound.
The compound comprises at least two carboxylic acid functions in the form of a salt of an alkali metal chosen from Na+ and K+, and the documented formulations specify aqueous solution clarity or turbidity criteria and a pH range of 6-38, with optional inclusion of zinc, buffers, tonicity agents and preservatives, while maintaining hexameric insulin.
Claims Coverage
The claim coverage centers on one independent composition claim, with the core invention defined by an aqueous insulin hexameric solution containing a substituted anionic non-saccharide compound of formula I plus at least one additional polyanionic compound other than the substituted anionic compound. The independent claim specifies the insulin hexameric composition, the formula I substituted anionic compound with defined radicals and linkage functions, constrained indices, and salt-form carboxylates.
Hexameric insulin aqueous composition with substituted anionic non-saccharide compound plus other polyanion
An aqueous solution comprising insulin in hexameric form, at least one substituted anionic compound of non-saccharide structure corresponding to formula I, and at least one polyanionic compound other than said substituted anionic compound.
Formula I substituted anionic compound defined by R, aromatic amino acid radical AA, divalent radical E and functions F/F'/F''
The substituted anionic compound corresponds to formula I wherein R is a saturated or unsaturated, linear, branched or cyclic hydrocarbon-based radical optionally comprising at least one function chosen from ether, alcohol and carboxylic acid functions; AA is a radical resulting from an aromatic amino acid comprising a phenyl group or an indole group, substituted or not substituted, bearing at least one free acid function; E is an at least divalent radical comprising from 2 to 6 carbon atoms; and F, F' and F'' independently are functions chosen from amide, carbamate and urea functions.
Salt-form carboxylic acid functions with carboxylate-defined parameters
The compound comprises at least two carboxylic acid functions in the form of a salt of an alkali metal chosen from Na+ and K+, with p being an integer between 1 and 3, m being an integer between 0 and 6, n being an integer between 0 and 6, and m+n being an integer between 1 and 6.
Overall, the claim set centers on an aqueous insulin hexameric composition that includes a substituted anionic non-saccharide compound defined by formula I plus an additional polyanionic compound other than that substituted anionic compound, with the substituted anionic compound further restricted by integer parameters and by at least two carboxylic acid functions as Na+ or K+ salts.
Stated Advantages
A reduced delay-of-action compared with reference products at matched concentrations.
Avoids compromising hexamer stability while accelerating action.
Notably improved delay-of-action versus regular human insulin and rapid analog references at matched concentrations.
Documented Applications
Use as a fast-acting insulin formulation with delay-of-action improvement described against regular human insulin and rapid analog references.
Interested in licensing this patent?