Rapid-acting insulin formulation comprising a substituted anionic compound

Inventors

Soula, Gérard • Alluis, Bertrand

Assignees

Adocia SAS

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 concerns a rapid acting insulin pharmaceutical composition suitable for injection having a pH of 7.4±0.4. The composition comprises insulin in hexameric form in the presence of zinc, with insulin concentration between 100 to 200 IU/mL, and includes a polyanionic compound in a concentration between 9.3 mM and 30 mM, wherein the polyanionic compound is citric acid or the Na+, K+, Ca2+ or Mg2+ salt thereof.

The composition further comprises zinc salts, sodium chloride, and a preservative, and in some embodiments a surfactant. The composition does not include EDTA.

The composition is characterized by circular dichroism signals, wherein for insulin lispro the composition has a circular dichroism signal at 251 nm of ≤−300 deg cm2 dmol−21, and for human insulin the composition has a circular dichroism signal at 275 nm of ≤−250 deg cm2 dmol−21.

Claims Coverage

The document provides independent claims that define rapid acting insulin injectable compositions at pH 7.4±0.4 containing insulin in hexameric form with zinc, a citric-acid-based polyanionic compound at 9.3 to 30 mM, preservative and related excipients, and circular dichroism signal thresholds for insulin lispro and human insulin while excluding EDTA. Across the claims, the inventive features primarily cover composition constraints and circular dichroism-based characterization, with further claim families narrowing specific excipient selections and concentration limits.

Across the independent claims, the shared inventive core is a rapid acting injectable insulin composition at pH 7.4±0.4 with zinc-containing hexameric insulin at 100–200 IU/mL, combined with a citric-acid-based polyanionic compound at 9.3–30 mM, plus zinc salts and a preservative, while excluding EDTA and meeting insulin-specific circular dichroism signal thresholds. The independent claims vary by whether sodium chloride and/or surfactant are included and by whether the insulin type is specified as insulin lispro or human insulin.

Stated Advantages

Documented Applications