Long-Acting Formulations of Insulin
The application relates to an aqueous pharmaceutical formulation comprising 200-1000 U/mL [equimolar to 200-1000 IU human insulin] of insulin glargine.
1 . An aqueous pharmaceutical formulation comprising 200-1000 U/mL of insulin glargine [equimolar to 200-1000 IU human insulin].
2 . An aqueous pharmaceutical formulation comprising 270-330 U/mL of insulin glargine [equimolar to 270-330 IU human insulin].
3 . The aqueous pharmaceutical formulation of claim 2 further comprising at least one excipient selected from the group consisting of zinc, m-cresol, glycerol, and polysorbate 20.
4 . The aqueous pharmaceutical formulation of claim 3 further comprising 90 μg/mL zinc, 2.7 mg/mL m-cresol, and 20 mg/mL glycerol 85%.
5 . The aqueous pharmaceutical formulation of claim 4 , wherein the zinc is present in the form of zinc chloride.
6 . The aqueous pharmaceutical formulation of claim 2 , wherein the pH of the aqueous pharmaceutical formulation is between 3.4 and 4.6.
7 . The aqueous pharmaceutical formulation of claim 6 , wherein the pH of the aqueous pharmaceutical formulation is 4.0.
8 . An aqueous pharmaceutical formulation comprising 270-330 U/mL of insulin glargine [equimolar to 270-330 IU human insulin] wherein the pH of the aqueous pharmaceutical formulation is between 3.4 and 4.6.
9 . The aqueous pharmaceutical formulation of claim 8 , wherein the pH of the aqueous pharmaceutical formulation is 4.0.
10 . The aqueous pharmaceutical formulation of claim 8 further comprising at least one excipient selected from the group consisting of zinc, m-cresol, glycerol, and polysorbate 20.
11 . The aqueous pharmaceutical formulation of claim 10 further comprising 90 μg/mL zinc, 2.7 mg/mL m-cresol, and 20 mg/mL glycerol 85%.
12 . The aqueous pharmaceutical formulation of claim 11 , wherein the zinc is present in the form of zinc chloride.
13 . An aqueous pharmaceutical formulation comprising 270-330 U/mL of insulin glargine [equimolar to 270-330 IU human insulin], 90 μg/mL zinc chloride, 2.7 mg/mL m-cresol, and 20 mg/mL glycerol 85%, wherein the pH of the aqueous pharmaceutical formulation is 4.0.
14 . The aqueous pharmaceutical formulation of claim 2 , wherein the pharmacokinetic profile and the pharmacodynamic profile of the aqueous pharmaceutical formulation following administration to a patient are flatter than the pharmacokinetic profile and the pharmacodynamic profile of an aqueous pharmaceutical formulation comprising 100 U/mL of insulin glargine, and wherein the pH of the aqueous pharmaceutical formulation is between 3.4 and 4.6.
15 . The aqueous pharmaceutical formulation of claim 14 , wherein the pH of the aqueous pharmaceutical formulation is 4.0.
16 . The aqueous pharmaceutical formulation of claim 14 further comprising at least one excipient selected from the group consisting of zinc, m-cresol, glycerol, and polysorbate 20.
17 . The aqueous pharmaceutical formulation of claim 16 further comprising 90 μg/mL zinc, 2.7 mg/mL m-cresol, and 20 mg/mL glycerol 85%.
18 . The aqueous pharmaceutical formulation of claim 17 , wherein the zinc is present in the form of zinc chloride.
19 . The aqueous pharmaceutical formulation of claim 2 , wherein the aqueous pharmaceutical formulation provides a peakless long acting basal insulin, and wherein the pH of the aqueous pharmaceutical formulation is between 3.4 and 4.6.
20 . The aqueous pharmaceutical formulation of claim 2 , wherein the aqueous pharmaceutical formulation exhibits an extended duration of exposure of insulin glargine than an aqueous pharmaceutical formulation comprising 100 U/mL insulin glargine, and wherein the pH of the aqueous formulation is between 3.4 and 4.6.