US2008167226A1PendingUtilityA1

Stable formulation of modified GLP-1

57
Assignee: NOVO NORDISK ASPriority: Jun 28, 2001Filed: Apr 11, 2007Published: Jul 10, 2008
Est. expiryJun 28, 2021(expired)· nominal 20-yr term from priority
Inventors:James M. FlinkSilke Moller LarsenSimon Bjerregaard JensenDorthe Kot Engelund
A61P 7/12A61P 3/04A61P 3/00A61P 3/10C07K 14/605A61K 38/26A61P 1/04A61K 47/26A61K 9/0043A61K 9/0019A61K 9/0073A61K 47/183A61K 47/10A61K 47/02A61K 9/08
57
PatentIndex Score
0
Cited by
0
References
0
Claims

Abstract

Pharmaceutical formulations of GLP-1 compounds and methods for preparation thereof.

Claims

exact text as granted — not AI-modified
1 . A pharmaceutical formulation comprising a GLP-1 compound and a buffer, wherein:
 (i) said GLP-1 compound is (a) GLP-1 (7-37) or (b) an analogue thereof wherein an amino acid residue of the parent peptide has a lipophilic substituent attached optionally via a spacer;   (ii) said GLP-1 compound is present in a concentration from 0.1 mg/ml to 100 mg/ml; and   (iii) aid formulation has a pH from 7.0 to 10;   provided that if an isotonic agent is present and the pH of the formulation is 7.4, then mannitol or NaCl is not the isotonic agent.   
     
     
         2 . The formulation according to  claim 1 , wherein the concentration of said GLP-1 compound is from 1 mg/ml to 100 mg/ml. 
     
     
         3 . The formulation according to  claim 1 , further comprising water. 
     
     
         4 . The formulation according to  claim 1 , wherein said pH is from 7.5 to 10. 
     
     
         5 . The formulation according to  claim 1 , wherein the concentration of said GLP-1 compound is from 0.1 mg/ml to 10 mg/ml. 
     
     
         6 . The formulation according to  claim 2 , wherein the concentration of said GLP-1 compound is 1-5 mg/ml. 
     
     
         7 . The formulation according to  claim 1 , further comprising a preservative. 
     
     
         8 . The formulation according to  claim 7 , wherein said preservative is present in a concentration from 0.1 mg/ml to 20 mg/ml. 
     
     
         9 . The formulation according to  claim 1 , further comprising an isotonic agent. 
     
     
         10 . The formulation according to  claim 9 , wherein said isotonic agent is present in a concentration from 1 mg/ml to 50 mg/ml. 
     
     
         11 . The formulation according to  claim 1 , further comprising a chelating agent. 
     
     
         12 . The formulation according to  claim 11 , wherein said chelating agent is present in a concentration from 0.1 mg/ml to 5 mg/ml. 
     
     
         13 . The formulation according to  claim 1 , further comprising a stabiliser. 
     
     
         14 . The formulation according to  claim 13 , wherein said stabiliser is selected from the group consisting of L-histidine, imidazole and arginine. 
     
     
         15 . The formulation according to  claim 13 , wherein said stabiliser is a high molecular weight polymer and/or a low molecular weight compound and is present in a concentration from 0.1 mg/ml to 50 mg/ml. 
     
     
         16 . The formulation according to  claim 1 , further comprising a surfactant. 
     
     
         17 . The formulation according to  claim 1 , wherein said GLP-1 compound is selected from the group consisting of: GLP-1 (7-36), GLP-1 (7-37), and a GLP-1 (7-38) analogue having a lysine residue and optionally a lipophilic substituent attached with or without a spacer to the epsilon amino group of said lysine. 
     
     
         18 . The formulation according to  claim 17 , wherein said GLP-1 (7-36), GLP-1 (7-37), or GLP-1 (7-38) analogue is selected from the group consisting of: Arg34GLP-1 (7-37); Arg26,34,Lys36GLP-1(7-36); Arg26GLP-1 (7-37); and Gly8,Arg26,34,Glu37,Lys38GLP-1 (7-38). 
     
     
         19 . The formulation according to  claim 17 , wherein said lipophilic substituent has from 8 to 40 carbon atoms. 
     
     
         20 . The formulation according to  claim 17 , wherein said spacer is an amino acid. 
     
     
         21 . The formulation according to  claims 1 , wherein said GLP-1 compound is Arg 34 , Lys 26 (N-ε-(γ-Glu(N-α-hexadecanoyl)))-GLP-1 (7-37). 
     
     
         22 . A method of preparing a physically stable pharmaceutical formulation of a GLP-1 compound wherein said GLP-1 compound is GLP-1 (7-37) or an analogue thereof wherein an amino acid residue of the parent peptide has a lipophilic substituent attached optionally via a spacer, said method comprising preparing a formulation containing the GLP-1 compound, and a buffer, wherein said GLP-1 compound is present in a concentration from 0.1 mg/ml to 100 mg/ml, and wherein said formulation has a pH from 7.0 to 10. 
     
     
         23 . The method according to  claim 22 , wherein said GLP-1 compound is present in a concentration from 1 mg/ml to 100 mg/ml. 
     
     
         24 . A method of preparing a physically stable pharmaceutical formulation of a GLP-1 compound wherein said GLP-1 compound is GLP-1 (7-37) or an analogue thereof, wherein an amino acid residue of the parent peptide has a lipophilic substituent attached optionally via a spacer, said method comprising preparing a formulation containing the GLP-1 compound, water, and a buffer, wherein said GLP-1 compound is present in a concentration from 0.1 mg/ml to 100 mg/ml, and wherein said formulation has a pH from 7.0 to 10. 
     
     
         25 . The method according to  claim 24 , wherein said GLP-1 compound is present in a concentration from 1 mg/ml to 100 mg/ml.

Cited by (0)

No later patents cite this yet.

References (0)

No backward citations on record.