US2016228516A1PendingUtilityA1

Long-Acting Formulations of Insulin

58
Assignee: SANOFI SAPriority: May 19, 2010Filed: Apr 20, 2016Published: Aug 11, 2016
Est. expiryMay 19, 2030(~3.8 yrs left)· nominal 20-yr term from priority
Inventors:Reinhard BeckerAnnke HahnPeter BoderkeChristiane FuerstWerner MuellerUlrich Werner
A61P 5/50A61P 3/10A61P 5/48A61P 3/08A61K 38/26A61K 38/28A61K 47/26A61K 9/08A61K 38/2278A61K 47/02A61K 9/0019A61K 47/10A61K 47/30
58
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Claims

Abstract

The application relates to an aqueous pharmaceutical formulation comprising 200-1000 U/mL [equimolar to 200-1000 IU human insulin] of insulin glargine.

Claims

exact text as granted — not AI-modified
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 μg/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 2  further comprising 90 μg/mL zinc, 2.7 mg/mL m-cresol, 20 μg/mL polysorbate 20, and 20 mg/mL glycerol 85%. 
     
     
         6 . The aqueous pharmaceutical formulation of  claim 5 , wherein the zinc is present in the form of zinc chloride. 
     
     
         7 . The aqueous pharmaceutical formulation of  claim 1 , 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 . 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. 
     
     
         10 . The aqueous pharmaceutical formulation of  claim 9 , wherein the pH of the aqueous pharmaceutical formulation is 4.0. 
     
     
         11 . The aqueous pharmaceutical formulation of  claim 9  further comprising at least one excipient selected from the group consisting of zinc, m-cresol, glycerol, and polysorbate 20. 
     
     
         12 . The aqueous pharmaceutical formulation of  claim 11  further comprising 90 μg/mL zinc, 2.7 mg/mL m-cresol, and 20 mg/mL glycerol 85%. 
     
     
         13 . The aqueous pharmaceutical formulation of  claim 12 , wherein the zinc is present in the form of zinc chloride. 
     
     
         14 . The aqueous pharmaceutical formulation of  claim 11  further comprising 90 μg/mL zinc, 2.7 mg/mL m-cresol, 20 μg/mL polysorbate 20, and 20 mg/mL glycerol 85%. 
     
     
         15 . The aqueous pharmaceutical formulation of  claim 14 , wherein the zinc is present in the form of zinc chloride. 
     
     
         16 . 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. 
     
     
         17 . 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, 20 μg/mL polysorbate 20, and 20 mg/mL glycerol 85%, wherein the pH of the aqueous pharmaceutical formulation is 4.0. 
     
     
         18 . An aqueous pharmaceutical formulation comprising 270-330 U/mL of insulin glargine [equimolar to 270-330 IU human insulin], wherein the pharmacokinetic profile and the pharmacodynamic profile of the 270-330 U/mL aqueous pharmaceutical formulation 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 270-330 U/mL aqueous pharmaceutical formulation is between 3.4 and 4.6. 
     
     
         19 . The aqueous pharmaceutical formulation of  claim 18 , wherein the pH of the aqueous pharmaceutical formulation is 4.0. 
     
     
         20 . The aqueous pharmaceutical formulation of  claim 18  further comprising at least one excipient selected from the group consisting of zinc, m-cresol, glycerol, and polysorbate 20. 
     
     
         21 . The aqueous pharmaceutical formulation of  claim 20  further comprising 90 μg/mL zinc, 2.7 mg/mL m-cresol, and 20 mg/mL glycerol 85%. 
     
     
         22 . The aqueous pharmaceutical formulation of  claim 21 , wherein the zinc is present in the form of zinc chloride. 
     
     
         23 . The aqueous pharmaceutical formulation of  claim 20  further comprising 90 μg/mL zinc, 2.7 mg/mL m-cresol, 20 μg/mL polysorbate 20, and 20 mg/mL glycerol 85%. 
     
     
         24 . The aqueous pharmaceutical formulation of  claim 23 , wherein the zinc is present in the form of zinc chloride. 
     
     
         25 . An aqueous pharmaceutical formulation comprising 270-330 U/mL of insulin glargine [equimolar to 270-330 IU human insulin] providing a peakless long acting basal insulin, wherein the pH of the aqueous pharmaceutical formulation is between 3.4 and 4.6. 
     
     
         26 . An aqueous pharmaceutical formulation comprising 270-330 U/mL of insulin glargine [equimolar to 270-330 IU human insulin] exhibiting an extended duration of exposure of insulin glargine than an aqueous pharmaceutical formulation comprising 100 U/mL insulin glargine, wherein the pH of the 270-330 U/mL aqueous formulation is between 3.4 and 4.6. 
     
     
         27 . The aqueous pharmaceutical formulation of  claim 1  further comprising an analogue of exendin-4. 
     
     
         28 . The aqueous pharmaceutical formulation of  claim 27 , wherein the analogue of exendin-4 is selected from the group consisting of lixisenatide, exenatide, and liraglutide. 
     
     
         29 . The aqueous pharmaceutical formulation of  claim 28  comprising 0.1 μg to 10 μg lixisenatide per Unit insulin glargine. 
     
     
         30 . The aqueous pharmaceutical formulation of  claim 29  comprising 0.2 to 1 μg lixisenatide per Unit insulin glargine 
     
     
         31 . The aqueous pharmaceutical formulation of  claim 30  comprising 0.25 μm to 0.7 g lixisenatide per Unit insulin glargine. 
     
     
         32 . A method of treating Type I or Type II Diabetes Mellitus in a patient in need thereof comprising subcutaneously administering to the patient an aqueous pharmaceutical formulation comprising 270-330 U/mL of insulin glargine [equimolar to 270-330 IU human insulin]. 
     
     
         33 . The method of  claim 32 , wherein the aqueous pharmaceutical formulation further comprises at least one excipient selected from the group consisting of zinc, m-cresol, glycerol, and polysorbate 20. 
     
     
         34 . A method of extending the duration of exposure of a long acting insulin in the treatment of Type I or Type II Diabetes Mellitus in a patient in need thereof comprising subcutaneously administering to the patient an aqueous pharmaceutical formulation comprising 270-330 U/mL insulin glargine [equimolar to 270-330 IU human insulin]. 
     
     
         35 . The method of  claim 34 , wherein the aqueous pharmaceutical formulation further comprises at least one excipient selected from the group consisting of zinc, m-cresol, glycerol, and polysorbate 20. 
     
     
         36 . A method of reducing the incidence of hypoglycaemia in the treatment of Type I or Type II Diabetes Mellitus in a patient in need thereof comprising subcutaneously administering to the patient an aqueous pharmaceutical formulation comprising 270-330 U/mL insulin glargine [equimolar to 270-330 IU human insulin]. 
     
     
         37 . The method of  claim 36 , wherein the aqueous pharmaceutical formulation further comprises at least one excipient selected from the group consisting of zinc, m-cresol, glycerol, and polysorbate 20. 
     
     
         38 . A method of providing a peakless long acting basal insulin in the treatment of Type I or Type II Diabetes Mellitus in a patient in need thereof comprising subcutaneously administering to the patient an aqueous pharmaceutical formulation comprising 270-330 U/mL insulin glargine [equimolar to 270-330 IU human insulin]. 
     
     
         39 . The method of  claim 38 , wherein the aqueous pharmaceutical formulation further comprises at least one excipient selected from the group consisting of zinc, m-cresol, glycerol, and polysorbate 20. 
     
     
         40 . The method of any one of  claims 32 ,  34 ,  36 , or  38 , wherein the aqueous pharmaceutical formulation is administered once daily. 
     
     
         41 . The method of any one of  claims 33 ,  35 ,  37 , or  39 , wherein the aqueous pharmaceutical formulation further comprises 90 μg/mL zinc, 2.7 mg/mL m-cresol, and 20 mg/mL glycerol 85%. 
     
     
         42 . The method of any one of  claims 33 ,  35 ,  37 , or  39 , wherein the aqueous pharmaceutical formulation further comprises 90 μg/mL zinc, 2.7 mg/mL m-cresol, 20 μg/mL polysorbate 20, and 20 mg/mL glycerol 85%. 
     
     
         43 . The method of any one of  claims 33 ,  35 ,  37 , or  39 , wherein the zinc in the aqueous pharmaceutical formulation is present in the form of zinc chloride. 
     
     
         44 . The method of any one of  claims 32 ,  34 ,  36 , or  38 , wherein the pH of aqueous pharmaceutical formulation is between 3.4 and 4.6. 
     
     
         45 . The method of  claim 44 , wherein the pH of the aqueous pharmaceutical formulation is 4.0. 
     
     
         46 . The method of any one of  claims 33 ,  35 ,  37 , or  39 , wherein the aqueous pharmaceutical formulation further comprises 90 μg/mL zinc chloride, 2.7 mg/mL m-cresol, and 20 mg/mL glycerol 85%, and wherein the pH of the aqueous pharmaceutical formulation is 4.0. 
     
     
         47 . The method of any one of  claims 32 ,  34 ,  36 , or  38 , wherein the pharmacokinetic profile and pharmacodynamic profile of the 270-330 U/mL aqueous pharmaceutical formulation are flatter than the pharmacokinetic profile and pharmacodynamic profile of an aqueous pharmaceutical formulation comprising 100 U/mL of insulin glargine, and wherein the pH of the 270-330 U/mL aqueous pharmaceutical formulation is between 3.4 and 4.6. 
     
     
         48 . A method of treating Type I or Type II Diabetes Mellitus in a patient in need thereof comprising subcutaneously administering to the patient 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. 
     
     
         49 . The method of  claim 48 , wherein the pH of the aqueous pharmaceutical formulation is 4.0. 
     
     
         50 . The method of  claim 48 , wherein the aqueous pharmaceutical formulation further comprises at least one excipient selected from the group consisting of zinc, m-cresol, glycerol, and polysorbate 20. 
     
     
         51 . The method of  claim 50 , wherein the aqueous pharmaceutical formulation further comprises 90 μg/mL zinc, 2.7 mg/mL m-cresol, and 20 mg/mL glycerol 85%. 
     
     
         52 . The method of  claim 51 , wherein the zinc is present in the form of zinc chloride. 
     
     
         53 . The method of  claim 50 , wherein the aqueous pharmaceutical formulation further comprises 90 μg/mL zinc, 2.7 mg/mL m-cresol, 20 μg/mL polysorbate 20, and 20 mg/mL glycerol 85%. 
     
     
         54 . The method of  claim 53 , wherein the zinc is present in the form of zinc chloride. 
     
     
         55 . The method of any one of  claims 32 ,  34 ,  36 ,  38 , or  48 , wherein the aqueous pharmaceutical formulation further comprises an analogue of exendin-4. 
     
     
         56 . The method of  claim 55 , wherein the analogue of exendin-4 is selected from the group consisting of lixisenatide, exenatide and liraglutide. 
     
     
         57 . The method of  claim 56 , wherein the aqueous formulation comprises 0.1 μg to 10 μg lixisenatide per Unit insulin glargine. 
     
     
         58 . The method of  claim 57 , wherein the aqueous formulation comprises 0.2 to 1 μg lixisenatide per Unit insulin glargine. 
     
     
         59 . The method of  claim 58 , wherein the aqueous formulation comprises 0.25 μg to 0.7 μg lixisenatide per Unit insulin glargine.

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