US2012122774A1PendingUtilityA1

Long-acting formulations of insulins

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Assignee: BECKER REINHARDPriority: May 19, 2010Filed: Dec 2, 2011Published: May 17, 2012
Est. expiryMay 19, 2030(~3.9 yrs left)· nominal 20-yr term from priority
A61P 3/08A61P 3/10A61P 5/50A61P 5/48A61K 47/02A61K 47/10A61K 9/08A61K 38/28A61K 38/2278A61K 9/0019A61K 38/26A61K 47/30A61K 47/26
55
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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 300 U/mL of insulin glargine [equimolar to 300 IU human insulin]. 
     
     
         2 . The aqueous pharmaceutical formulation of  claim 1  comprising an analogue of exendin-4. 
     
     
         3 . The aqueous pharmaceutical formulation of  claim 2 , wherein the analogue of exedin-4 is selected from a group comprising lixisentatide, exenatide and liraglutide. 
     
     
         4 . The aqueous pharmaceutical formulation of  claim 3  comprising 0.1 μg to 10 μg lixisenatide per U insulin glargine. 
     
     
         5 . The aqueous pharmaceutical formulation of  claim 4  comprising 0.2 to 1 μg lixisenatide per U insulin glargine. 
     
     
         6 . The aqueous pharmaceutical formulation of  claim 5  comprising 0.25 μg to 0.7 μg lixisenatide per U insulin glargine. 
     
     
         7 . The aqueous pharmaceutical formulation of  claim 1  comprising at least one excipient selected from the group comprising zinc, m-cresol, glycerol, polysorbate 20 and sodium. 
     
     
         8 . The aqueous pharmaceutical formulation of  claim 7  comprising 90 μg/mL zinc, 2.7 mg/mL m-cresol and 20 mg/ml glycerol 85%. 
     
     
         9 . The aqueous pharmaceutical formulation of  claim 7  comprising 90 μg/mL zinc, 2.7 mg/mL m-cresol, 20 μg/mL polysorbate 20 and 20 mg/mL glycerol 85%. 
     
     
         10 . The aqueous pharmaceutical formulation of  claim 1 , wherein the pH is between 3.4 and 4.6. 
     
     
         11 . The aqueous pharmaceutical formulation of  claim 10 , wherein the pH is 4. 
     
     
         12 . The aqueous pharmaceutical formulation of  claim 10 , wherein the pH is 4.5. 
     
     
         13 . A method of treating Type I and Type II Diabetes Mellitus in a patient comprising administering to said patient an aqueous pharmaceutical formulation comprising 300 U/mL of insulin glargine [equimolar to 300 IU human insulin]. 
     
     
         14 . The method of  claim 13  wherein said aqueous pharmaceutical formulation further comprises an analogue of exendin-4. 
     
     
         15 . The method of  claim 14  wherein the analogue of exendin-4 is selected from a group comprising lixisentatide, exenatide and liraglutide. 
     
     
         16 . The method of  claim 15  comprising 0.1 μg to 10 μg lixisenatide per U insulin glargine. 
     
     
         17 . The method of  claim 16  comprising 0.2 to 1 μg lixisenatide per U insulin glargine. 
     
     
         18 . The method of  claim 17  comprising 0.25 μg to 0.7 μg lixisenatide per U insulin glargine. 
     
     
         19 . The method of  claim 13  further comprising at least one excipient selected from the group comprising zinc, m-cresol, glycerol, polysorbate 20 and sodium. 
     
     
         20 . The method of  claim 19  comprising 90 μg/mL zinc, 2.7 mg/mL m-cresol and 20 mg/mL glycerol 85%. 
     
     
         21 . The method of  claim 19  comprising 90 μg/mL zinc, 2.7 mg/mL m-cresol, 20 μg/mL polysorbate 20 and 20 mg/mL glycerol 85%. 
     
     
         22 . The method of  claim 13  wherein the pH is between 3.4 and 4.6. 
     
     
         23 . The method of  claim 22  wherein the pH is 4. 
     
     
         24 . The method of  claim 22  wherein the pH is 4.5. 
     
     
         25 . An aqueous pharmaceutical formulation comprising 300 U/mL of insulin glargine [equimolar to 300 IU human insulin], 90 μg zinc, 2.7 mg m-cresol, 20 mg glycerol 85%, HCL and NaOH ad and having a pH of 4.0.

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