Rapid-acting insulin formulation comprising a substituted anionic compound
Inventors
Soula, Olivier • Soula, Gérard • DAUTY, Emmanuel • Charvet, Richard
Assignees
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Publication Number
US-9700599-B2
Publication Date
2017-07-11
Expiration Date
Abstract
The invention relates to a composition in aqueous solution, including 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, said 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. The invention also relates to a pharmaceutical formulation comprising a composition as claimed in any one of the preceding claims.
Core Innovation
The invention relates to an aqueous composition comprising insulin in hexameric form, human insulin or an insulin analog, at least one substituted anionic compound, and a polyanionic compound. The composition is configured so that the insulin remains in hexameric form while the substituted anionic compound and the polyanionic compound act together in the formulation.
The substituted anionic compound is defined by a backbone formed from a discrete number u of between 1 and 8 saccharide units, the saccharide units being hexoses in cyclic form or in open reduced form. The units are linked by glycoside bonds of (1,1), (1,2), (1,3), (1,4) or (1,6) type with alpha or beta geometry, and are substituted with at least one substituent of general formula I comprising an amino acid residue and salifiable carboxyl functionality.
The formulation additionally includes a polyanionic compound chosen from citric acid and Na+, K+, Ca2+, or Mg2+ salts thereof. The document states that the insulin pharmaceutical formulation accelerates the passage of insulin into the blood and reduces the glycemia more rapidly when compared with a formulation free of substituted anionic compound.
Claims Coverage
The independent claims center on an aqueous insulin composition and an insulin pharmaceutical formulation, both combining hexameric insulin with defined substituted anionic compounds and a polyanionic compound. The claims specify the saccharide backbone, glycoside bond types, alpha or beta geometry, amino acid residue-containing substitution, and citric acid or specified metal salts as the polyanionic compound.
Hexameric insulin aqueous composition with substituted anionic compound and polyanionic compound
A composition in an aqueous solution comprising insulin in hexameric form, human insulin or an insulin analog, at least one substituted anionic compound defined by a saccharide backbone with discrete number u between 1 and 8, hexose cyclic or open reduced units, specified glycoside bond types (1,1; 1,2; 1,3; 1,4; 1,6) with alpha or beta geometry, and at least one substituent of general formula I including an amino acid residue and salifiable carboxyl functional groups, together with a polyanionic compound chosen from citric acid and Na+, K+, Ca2+ or Mg2+ salts thereof.
Insulin formulation accelerating blood passage and glycemia reduction using substituted anionic and polyanionic components
An insulin pharmaceutical formulation comprising insulin and at least one substituted anionic compound having a saccharide backbone formed from a discrete number u between 1 and 8 of identical or different saccharide units linked via identical or different glycoside bonds, with hexoses in cyclic form or open reduced form and partially substituted carboxyl functional groups, together with a polyanionic compound chosen from citric acid and Na+, K+, Ca2+, or Mg2+ salts thereof, wherein after administration it accelerates passage of the insulin into the blood and reduces glycemia more rapidly compared with a formulation free of substituted anionic compound.
Across the independent claims, the subject matter centers on insulin in hexameric form or in an insulin pharmaceutical formulation combined with a substituted anionic saccharide backbone and a specific polyanionic component. The second independent claim also states the functional outcome of accelerated insulin passage into the blood and more rapid glycemia reduction.
Stated Advantages
Accelerates the passage of insulin into the blood.
Reduces glycemia more rapidly when compared with a formulation free of substituted anionic compound.
Documented Applications
Insulin pharmaceutical formulation for administration to accelerate insulin passage into the blood and to reduce glycemia more rapidly versus a formulation free of substituted anionic compound.
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