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OwnerAlain Constancis, David Duracher +2inventors
InventorsAlain Constancis, David Duracher, Olivier Soula, Nathan Bryson
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The invention relates to injectable long-acting insulin formulations for the treatment of type I and II diabetes in humans and animals. The main objective of the invention is to provide a long-acting insulin formulation in the form of a colloidal suspension: which allows easy filling of a syringe through a small diameter needle (for example with the gauge 29 G, 30 G or 31 G) and/or which can be easily injected through a small diameter needle (for example with the gauge 29 G, 30 G or 31 G), without damaging the therapeutic efficacy of the insulin. To achieve this objective, the subject of the invention is an aqueous and stable colloidal formulation of nanoparticles of at least one poly(Leu-block-Glu), loaded with insulin, in which the pH is such that: 6.0≦pH≦7.0 which comprises at least one magnesium salt in a quantity such that: the osmolarity Osm (in mOsmol) is such that: 270≦Osm≦600, the viscosity v (in mPa·s), measured according to a procedure Mv, is such that: v≦15; the poly(Leu-block-Glu) concentration (in mg/ml) is between 30 and 70, preferably between 38 and 65.
An injectable long-acting insulin formulation comprising an aqueous and stable colloidal suspension of nanoparticles based on at least one poly(Leu-block-Glu) and loaded with insulin, the pH of this suspension being such that:
The formulation as claimed in claim 1 or 2, wherein the counter-anion of Mg2+ is chosen in the group comprising Cl−, SO4−− and mixtures thereof.
The formulation as claimed in any one of the preceding claims, wherein the insulin/poly(Leu-block-Glu) ratio by mass, expressed in %, is such that:
The formulation as claimed in any one of the preceding claims, wherein the maximum loading rate Ta of the nanoparticles with insulin, expressed in % by mass of insulin combined relative to the mass of poly(Leu-block-Glu) and measured according to a procedure Ma, is such that:
The formulation as claimed in any one of the preceding claims, wherein the insulin is an unmodified human insulin.
The formulation as claimed in any one of the preceding claims, which comprises at least one preservative, preferably selected from the group comprising:
A method for preparing an injectable formulation of protein(s), which mainly consists:
Dependencies are inferred from the claim text.