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 270-330 U/mL of insulin glargine [equimolar to 270-330 IU human insulin].
2 : The aqueous pharmaceutical formulation of claim 1 further comprising at least one excipient selected from the group consisting of zinc, m-cresol, glycerol, and polysorbate 20.
3 : The aqueous pharmaceutical formulation of claim 2 further comprising 90 g/mL zinc, 2.7 mg/mL m-cresol, and 20 mg/mL glycerol 85%.
4 : The aqueous pharmaceutical formulation of claim 3 , wherein the zinc is present in the form of zinc chloride.
5 : The aqueous pharmaceutical formulation of claim 1 , wherein the pH of the aqueous pharmaceutical formulation is between 3.4 and 4.6.
6 : The aqueous pharmaceutical formulation of claim 5 , wherein the pH of the aqueous pharmaceutical formulation is 4.0.
7 : 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.
8 : The aqueous pharmaceutical formulation of claim 7 , wherein the pH of the aqueous pharmaceutical formulation is 4.0.
9 : The aqueous pharmaceutical formulation of claim 7 further comprising at least one excipient selected from the group consisting of zinc, m-cresol, glycerol, and polysorbate 20.
10 : The aqueous pharmaceutical formulation of claim 9 further comprising 90 μg/mL zinc, 2.7 mg/mL m-cresol, and 20 mg/mL glycerol 85%.
11 : The aqueous pharmaceutical formulation of claim 10 , wherein the zinc is present in the form of zinc chloride.
12 : 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.
13 : The aqueous pharmaceutical formulation of claim 1 , 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.
14 : The aqueous pharmaceutical formulation of claim 13 , wherein the pH of the aqueous pharmaceutical formulation is 4.0.
15 : The aqueous pharmaceutical formulation of claim 13 further comprising at least one excipient selected from the group consisting of zinc, m-cresol, glycerol, and polysorbate 20.
16 : The aqueous pharmaceutical formulation of claim 15 further comprising 90 μg/mL zinc, 2.7 mg/mL m-cresol, and 20 mg/mL glycerol 85%.
17 : The aqueous pharmaceutical formulation of claim 16 , wherein the zinc is present in the form of zinc chloride.
18 : The aqueous pharmaceutical formulation of claim 1 , 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.
19 : The aqueous pharmaceutical formulation of claim 1 , 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.