US2018125944A1PendingUtilityA1

Stabilized pharmaceutical formulations of insulin aspart

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Assignee: SANOFI SAPriority: Jan 9, 2014Filed: Oct 6, 2017Published: May 10, 2018
Est. expiryJan 9, 2034(~7.5 yrs left)· nominal 20-yr term from priority
Inventors:Oliver BleyPetra LoosBernd BidlingmaierWalter KammHarald Berchtold
A61K 38/28A61K 47/02A61K 9/08A61K 38/1825A61K 2300/00A61K 47/10A61K 33/30A61K 9/0019A61K 38/26A61P 3/10A61K 45/06A61K 47/42
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Claims

Abstract

Stabilized pharmaceutical formulations of insulin aspart are disclosed.

Claims

exact text as granted — not AI-modified
1 . A pharmaceutical formulation comprising
 (a). insulin aspart;   (b). Zn(II); and   (c). optionally protamine,   wherein the pharmaceutical formulation contains less than 0.17 mg/mL sodium chloride.   
     
     
         2 . The pharmaceutical formulation according to  claim 1 , wherein the pharmaceutical formulation is an aqueous pharmaceutical formulation. 
     
     
         3 . The pharmaceutical formulation according to  claim 1 , wherein the pharmaceutical formulation has a pH value in the range from 6.0 to 9.0. 
     
     
         4 . The pharmaceutical formulation according to  claim 3 , wherein the pharmaceutical formulation has a pH value in the range from 7.0 to 7.8. 
     
     
         5 . The pharmaceutical formulation according to  claim 1 , wherein insulin aspart is present in a concentration from 10 U/mL to 1000 U/mL. 
     
     
         6 . The pharmaceutical formulation according to  claim 1 , wherein Zn(II) is present in a concentration from 0.0100 to 0.0600 mg/100 U of insulin aspart. 
     
     
         7 . The pharmaceutical formulation according to  claim 1 , wherein the pharmaceutical formulation is essentially free of sodium chloride. 
     
     
         8 . The pharmaceutical formulation according to  claim 1 , wherein protamine is present in a concentration from 0.1 to 0.5 mg/mL. 
     
     
         9 . The pharmaceutical formulation according to  claim 1 , wherein the pharmaceutical formulation further contains a buffering agent. 
     
     
         10 . The pharmaceutical formulation according to  claim 1 , wherein the pharmaceutical formulation comprises one or more further active pharmaceutical ingredients. 
     
     
         11 . The pharmaceutical formulation according to  claim 8 , wherein the further active pharmaceutical ingredient is an antidiabetic agent. 
     
     
         12 . The pharmaceutical formulation according to  claim 8 , wherein the further active pharmaceutical ingredient is an antidiabetic agent selected from the group consisting of:
 (a). a GLP-1 receptor agonist;   (b). a dual GLP-1 receptor/glucagon receptor agonist;   (c). human FGF-21;   (d). a FGF-21 analogue;   (e). a FGF-21 derivative;   (f). insulin;   (g). human insulin;   (h). an analogue of insulin; and   (i). a derivative of insulin.   
     
     
         13 . The pharmaceutical formulation according to  claim 1 , wherein the pharmaceutical formulation further comprises a fast acting analogue and/or derivative of insulin or a long acting analogue and/or derivative of insulin. 
     
     
         14 . The pharmaceutical formulation according to  claim 13 , wherein the fast acting insulin is one or more insulin selected from the group consisting of insulin lispro and insulin glulisine and wherein the long acting insulin is one or more insulin selected from the group consisting of insulin detemir, insulin glargin and insulin degludec. 
     
     
         15 - 16 . (canceled) 
     
     
         17 . A method for preparing the pharmaceutical formulation according to  claim 1 , wherein the components are mixed together in the form of a solution or suspension, the pH is adjusted to reach a desired pH, and water is added to reach a final volume. 
     
     
         18 . A kit comprising one or more separate packages of
 (a). the pharmaceutical formulation according to  claim 1 ; and   (b). a medical device.   
     
     
         19 . A kit comprising one or more separate packages of
 (a). the pharmaceutical formulation according to  claim 1 ;   (b). at least one further active pharmaceutical ingredient; and   (c). optionally a medical device.   
     
     
         20 . The kit according to  claim 19 , wherein the further active pharmaceutical ingredient is an antidiabetic agent. 
     
     
         21 . The kit according to  claim 19 , wherein the further active pharmaceutical ingredient is an antidiabetic agent selected from the group consisting of:
 (a). a GLP-1 receptor agonist;   (b). a dual GLP-1 receptor/glucagon receptor agonist;   (c). human FGF-21;   (d). a FGF-21 analogue;   (e). a FGF-21 derivative;   (f). insulin;   (g). human insulin;   (h). an analogue of insulin; and   (i). a derivative of insulin.   
     
     
         22 . The kit according to  claim 19 , wherein the further active pharmaceutical ingredient is an analogue or derivative of insulin selected from the group consisting of fast acting insulin and long acting insulin. 
     
     
         23 . The kit according to  claim 22 , wherein the fast acting insulin is selected from the group consisting of insulin aspart, insulin lispro and insulin glulisine and wherein the long acting insulin is selected from the group consisting of insulin glargin, insulin detemir and insulin degludec. 
     
     
         24 . A method of treating diabetes mellitus in a subject in need thereof comprising using the kit of  claim 18  to administer to the subject the pharmaceutical formulation of the kit employing the medical device of the kit. 
     
     
         25 . A method of treating hyperglycemia in a subject in need thereof comprising using the kit of  claim 18  to administer to the subject the pharmaceutical formulation of the kit employing the medical device of the kit. 
     
     
         26 . A method of lowering blood glucose level in a subject in need thereof comprising using the kit of  claim 18  to administer to the subject the pharmaceutical formulation of the kit employing the medical device of the kit. 
     
     
         27 . A method of treating diabetes mellitus in a subject in need thereof comprising administering to the subject a therapeutically effective amount of the pharmaceutical formulation of  claim 1 . 
     
     
         28 . A method of treating hyperglycemia in a subject in need thereof comprising administering to the subject a therapeutically effective amount of the pharmaceutical formulation of  claim 1 . 
     
     
         29 . A method of lowering blood glucose levels in a subject in need thereof comprising administering to the subject a therapeutically effective amount of the pharmaceutical formulation of  claim 1 . 
     
     
         30 . A medical device comprising the pharmaceutical formulation as claimed in  claim 1 , for administering the pharmaceutical formulation to an animal and/or human.

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