Rapid-acting insulin formulation comprising a substituted anionic compound
Inventors
Soula, Olivier • Soula, Gerard • DAUTY, Emmanuel • Charvet, Richard
Assignees
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Publication Number
US-10583175-B2
Publication Date
2020-03-10
Expiration Date
Abstract
A composition in aqueous solution includes insulin and at least one substituted anionic compound chosen from substituted anionic compounds consisting of a backbone formed from a discrete number u of between 1 and 8 (1≤u≤8) of identical or different saccharide units, linked via identical or different glycoside bonds, the saccharide units being chosen from the group consisting of hexoses, in cyclic form or in open reduced form, said compound comprising partially substituted carboxyl functional groups, the unsubstituted carboxyl functional groups being salifiable. A pharmaceutical formulation including the composition is also set forth.
Core Innovation
The invention relates to an insulin pharmaceutical composition in aqueous solution comprising insulin in hexameric form together with at least one substituted anionic compound and a polyanionic compound. The substituted anionic compound is a substituted anionic saccharide compound having a backbone formed from a discrete number u of 1 to 8 identical or different saccharide units linked via identical or different glycoside bonds, and the saccharide units are hexoses in cyclic form or in open reduced form and are substituted with at least one substituent of general formula I.
The substituent chemistry includes an amino acid residue denoted by −[AA], with the −[AA] being directly linked to the backbone via a function G or linked through a C2 to C15 carbon-based chain that forms an amide function and attaches to the backbone via a function F. The saccharide units are partially salifiable carboxyl functional groups, and the degree of substitution of the saccharide units j is strictly greater than 0 and less than or equal to 6, with the optional substituent −R'1 present with a degree of substitution i satisfying 0≤i≤6−j and i+j≤6.
The polyanionic compound is selected from polycarboxylic acids and Na+, K+, Ca2+ or Mg2+ salts thereof, or from polyphosphoric acids and Na+, K+, Ca2+ or Mg2+ salts thereof, or is a compound consisting of a saccharide backbone formed from a discrete number of saccharide units. The formulation makes it possible, after administration, to accelerate the passage of the insulin into the blood and to reduce the glycemia more rapidly when compared with a formulation free of substituted anionic compound.
Claims Coverage
The independent claims center on three inventive features: hexameric insulin in aqueous solution with a substituted anionic compound and a polyanionic compound, an insulin pharmaceutical formulation with faster blood passage and glycemia reduction, and a substituted anionic saccharide compound defined by backbone length, substituent type, and substitution constraints.
Insulin hexameric composition with substituted anionic saccharide and polyanionic compound
An aqueous composition comprising insulin in hexameric form, at least one substituted anionic compound, and a polyanionic compound, wherein the substituted anionic compound has a saccharide backbone of u between 1 and 8 hexose units linked by glycoside bonds and substituted with at least one substituent of general formula I, and the polyanionic compound is selected from polycarboxylic acids and salts, polyphosphoric acids and salts, or a compound consisting of a saccharide backbone formed from a discrete number of saccharide units.
Insulin formulation that accelerates blood passage and reduces glycemia more rapidly
An insulin pharmaceutical formulation comprising insulin in hexameric form with at least one substituted anionic compound and a polyanionic compound, wherein administration accelerates the passage of insulin into the blood and reduces glycemia more rapidly compared with a formulation free of substituted anionic compound.
Substituted anionic saccharide compound with amino-acid substituents and defined glycoside bonds
A substituted anionic compound consisting of a backbone formed from a discrete number u of 1 to 8 saccharide units linked via identical or different glycoside bonds, wherein the saccharide units are hexoses substituted with at least one substituent of general formula I and optionally with one or more −R'1 substituents, with the substitution degrees j and i constrained as stated in the input.
The claims collectively define hexameric insulin in aqueous solution or in an insulin pharmaceutical formulation with a substituted anionic saccharide compound and a polyanionic compound, together with a structural definition for the substituted anionic saccharide compound itself.
Stated Advantages
After administration, accelerates the passage of insulin into the blood.
Reduces glycemia more rapidly compared with a formulation free of substituted anionic compound.
Preserves hexamer stability while achieving faster glycemia reduction.
Documented Applications
An insulin pharmaceutical formulation for administration, configured to accelerate insulin passage into the blood and to reduce glycemia more rapidly compared with a formulation free of substituted anionic compound.
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