Claims for Patent: 8,846,618

Summary for Patent: 8,846,618

Title:	Stable formulation of modified GLP-1
Abstract:	Pharmaceutical formulations of GLP-1 compounds and methods for preparation thereof.
Inventor(s):	Flink; James M. (Klanpenborg, DK), Larsen; Silke Moller (Charlottenlund, DK), Jensen; Simon Bjerregaard (Frederiksberg, DK), Engelund; Dorthe Kot (Holte, DK)
Assignee:	Novo Nordisk A/S (Bagsvaerd, DK)
Application Number:	12/785,861
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,846,618
Patent Claims:	1. A pharmaceutical formulation comprising: a GLP-1 compound, wherein said GLP-1 compound is: Arg.sup.34, Lys.sup.26(N-.epsilon.-(.gamma.-Glu(N-.alpha.-hexadecanoyl)))-GLP-1 (7-37), and wherein said GLP-1 compound binds to a GLP-1 receptor with an affinity constant (K.sub.D) below about 1 .mu.M or a potency EC.sub.50 below about 1 .mu.M, and wherein said GLP-1 compound is present in a concentration from 0.1 mg/ml to 100 mg/ml; an isotonic agent; a buffer; and a preservative; wherein said pharmaceutical formulation has a pH from 7.5 to 9.4. 2. The formulation according to claim 1, further comprising water. 3. The formulation according to claim 1, wherein the concentration of said GLP-1 compound is from 0.1 mg/ml to 10 mg/ml. 4. The formulation according to claim 1, wherein the concentration of said GLP-1 compound is 1-5 mg/ml. 5. The formulation according to claim 1, wherein said preservative is present in a concentration from 0.1 mg/ml to 20 mg/ml. 6. The formulation according to claim 1, wherein said isotonic agent is present in a concentration from 1 mg/ml to 50 mg/ml. 7. The formulation according to claim 1, further comprising a chelating agent. 8. The formulation according to claim 7, wherein said chelating agent is present in a concentration from 0.1 mg/ml to 5 mg/ml. 9. The formulation according to claim 1, further comprising a stabiliser. 10. The formulation according to claim 9, wherein said stabiliser is selected from the group consisting of L-histidine, imidazole and arginine. 11. The formulation according to claim 9, 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. 12. The formulation according to claim 1, further comprising a surfactant. 13. A method of preparing a physically stable pharmaceutical formulation of a GLP-1 compound wherein said GLP-1 compound is Arg.sup.34, Lys.sup.26(N-.epsilon.-(.gamma.-Glu(N-.alpha.-hexadecanoyl)))-GLP-1(7-37)- , and wherein said GLP-1 compound binds to a GLP-1 receptor with an affinity constant (K.sub.D) below about 1 .mu.M or a potency EC.sub.50 below about 1 .mu.M, said method comprising preparing a formulation containing the GLP-1 compound, an isotonic agent, a preservative, 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 7.5 to 9.4. 14. A pharmaceutical formulation comprising: a GLP-1 compound, wherein said GLP-1 compound is Arg.sup.34, Lys.sup.26(N-.epsilon.-(.gamma.-Glu(N-.alpha.-hexadecanoyl)))-GLP-1 (7-37), and wherein said GLP-1 compound binds to a GLP-1 receptor with an affinity constant (K.sub.D) below about 1 .mu.M or a potency EC.sub.50 below about 1 .mu.M; an isotonic agent; a buffer; and a preservative; wherein said pharmaceutical formulation has a pH from 7.5 to 9.4.