Patent application EP17151475A (EP), filed 2012-03-09
Publication number: EP3225235A1
Title: STABLE PEPTIDE FORMULATIONS FOR PARENTERAL INJECTION
Abstract: Stable formulations for parenteral injection of peptide drugs and methods of using such stable formulations are provided. In particular, the present invention provides stable formulations for parenteral injection of glucagon and methods of using such glucagon formulations to treat hypoglycemia, especially severe hypoglycemia in emergency situations.
IPC codes: A61K   9/    08            A I
A61K   9/    19            A I
A61K  38/    02            A I
A61K  38/    09            A I
A61K  38/    16            A I
A61K  38/    17            A I
A61K  38/    18            A I
A61K  38/    22            A I
A61K  38/    25            A I
A61K  38/    26            A I
A61K  38/    28            A I
A61K  38/    29            A I
A61K  38/    30            A I
A61K  38/    48            A I
A61K  47/    10            A I
A61K  47/    20            A I
A61K  47/    22            A I
A61K   9/    00            A I
A61K  47/    12            A I
A61K  47/    14            A I
A61K  47/    18            A I
Claims: number: 1
text: A stable formulation for parenteral injection, comprising:
number: 2
text: The formulation in accordance with claim 1, wherein the peptide or salt thereof is selected from the group consisting of glucagon, pramlintide, insulin, leuprolide, an LHRH agonist, parathyroid hormone (PTH), amylin, botulinum toxin, hematide, an amyloid peptide, cholecystikinin, a conotoxin, a gastric inhibitory peptide, an insulin-like growth factor, a growth hormone releasing factor, an anti-microbial factor, glatiramer, glucagon-like peptide-1 (GLP-1), a GLP-1 agonist, exenatide, analogs thereof, and mixtures thereof.
number: 3
text: The formulation in accordance with claim 2, wherein the peptide is exenatide.
number: 4
text: The formulation in accordance with any of the preceding claims, wherein the non-volatile buffer is selected from a glycine buffer, a citrate buffer, a phosphate buffer, and mixtures thereof, in particular glycine buffer or a mixture of citrate buffer and phosphate buffer.
number: 5
text: The formulation in accordance with any of the preceding claims, wherein the aprotic polar solvent is selected from dimethylsulfoxide (DMSO), n-methyl pyrrolidone (NMP), ethyl acetate, and mixtures thereof.
number: 6
text: The formulation in accordance with claim 5, wherein the aprotic polar solvent is DMSO.
number: 7
text: The formulation in accordance with claim5, wherein the aprotic polar solvent is a mixture of DMSO and NMP.
number: 8
text: The formulation in accordance with claim 5, wherein the aprotic polar solvent is a mixture of DMSO and ethyl acetate.
number: 9
text: The formulation in accordance with any of the preceding claims, further comprising a co-solvent that depresses the freezing point of the formulation, wherein the co-solvent is selected from ethanol, propylene glycol, glycerol, and mixtures thereof.
number: 10
text: The formulation in accordance with claim 9 or claim 10, wherein the co-solvent is ethanol or propylene glycol.
number: 11
text: The formulation in accordance with claim 9, wherein the co-solvent is present in the formulation in an amount ranging from about 10% (w/v) to about 50% (w/v).
number: 12
text: The formulation in accordance with any of the preceding claims, further comprising a stabilizing excipient.
number: 13
text: The formulation in accordance with claim 12, wherein the stabilizing excipient is selected from sugars, starches, and mixtures thereof.
number: 14
text: The formulation in accordance with claim 13, wherein the stabilizing excipient is a sugar, in particular trehalose.
number: 15
text: The formulation in accordance with claim 13, wherein the stabilizing excipient is a starch, in particular hydroxyethyl starch (HES).
Office action: search_report, dated 2017-10-04
Rejection reasons: novelty_epc_54
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Final disposition: pending (2017-10-04)