Claims for Patent: 8,236,759

Summary for Patent: 8,236,759

Title:	GLP-1 pharmaceutical compositions
Abstract:	The present invention is directed to peptide analogues of glucagon-like peptide-1, the pharmaceutically-acceptable salts thereof, to methods of using such analogues to treat mammals and to pharmaceutical compositions useful therefore comprising said analogues.
Inventor(s):	Dong; Zheng Xin (Holliston, MA), Cherif-Cheikh; Roland (Barcelona, ES), Alloza Miravete; Resurreccion (Amer, ES), Cordero Rigol; Jose-Antonio (Rubi, ES), Lacombe; Frederic (Sant Cugat del Valles, ES), Tobalina Maestre; Maria Dolores (Barcelona, ES)
Assignee:	Ipsen Pharma SAS (Paris, FR)
Application Number:	11/479,074
Patent Claims:	1. A pharmaceutical composition comprising an analog of glucagon-like peptide-1 according to the formula: [Aib.sup.8,35]hGLP-1(7-36)NH.sub.2; together with zinc and a pharmaceutically acceptable carrier or diluent, wherein said diluent comprises a pharmaceutically acceptable aqueous solution and said pharmaceutical composition is a clear solution when said composition is administered, said analog of glucagon-like peptide-1 is released within said subject for at least approximately two weeks, with the proviso that said composition does not consist of a clear aqueous ZnCl.sub.2 solution having pH 4 in which said [Aib.sup.8,35]hGLP-1(7-36)NH.sub.2 is present at a concentration of 4 mg/ml and said ZnCl.sub.2 is present at a concentration of 0.5 mg/ml. 2. The pharmaceutical composition according to claim 1, wherein said zinc is present in a concentration from 0.0005 mg/mL to 50 mg/mL. 3. The pharmaceutical composition according to claim 2, wherein said zinc is present in a concentration from 0.01 mg/mL to 0.50 mg/mL. 4. The pharmaceutical composition according to claim 1, wherein said diluent comprises sterile water. 5. The pharmaceutical composition according to claim 1, wherein said pharmaceutical composition comprises an aqueous mixture, suspension or solution, and wherein said analog of glucagon-like peptide-1 is present at a concentration of approximately 0.5%-30% (w/w). 6. The pharmaceutical composition according to claim 5, wherein the concentration of said analog of glucagon-like peptide-1 in said aqueous mixture, suspension or solution is approximately 1%, 2%, 3%, 4%, 5%, 6%, 7%, 8%, 9%, 10%, 11%, 12%, 13%, 14%, 15%, 16%, 17%, 18%, 19%, 20%, 21%, 22%, 23%, 24%, 25%, 26%, 27%, 28%, 29%, or 30% (w/w). 7. The pharmaceutical composition according to claim 6, wherein the concentration of said analog of glucagon-like peptide-1 in said aqueous solution is approximately 1%, 2%, 3%, 4%, 5%, 6%, 7%, 8%, 9%, 10%, 11%, 14%, 15%, 16%, 19%, 20%, 21%, 22%, 23%, 24%, 25%, 26%, 29%, or 30% (w/w). 8. The pharmaceutical composition according to claim 7, wherein the concentration of said analog: of glucagon-like peptide-1 in said aqueous solution is approximately 1%, 2%, 3%, 4%, 5%, 6%, 9%, 10%, 11%, 22%, 23%, 24%, 25%, or 26% (w/w). 9. The pharmaceutical composition according to claim 8, wherein the concentration of said analog of glucagon-like peptide-1 in said aqueous solution is approximately 1%, 2%, 3%, 4%, 5%, 6%, 10%, 22%, 23%, 24%, 25%, or 26% (w/w). 10. The pharmaceutical composition according to claim 9, wherein the concentration of said analog of glucagon-like peptide-1 in said aqueous solution is approximately 1%, 2%, 5%, 10%, 23% or 25% (w/w). 11. The pharmaceutical composition according to claim 5, wherein the molar ratio of said analog of glucagon-like peptide-1 to zinc in said pharmaceutical composition ranges from approximately 6:1 to approximately 1:1. 12. The pharmaceutical composition according to claim 11, wherein said ratio ranges from approximately 5.5:1 to approximately 1:1. 13. The pharmaceutical composition according to claim 12, wherein said ratio ranges from approximately 5.4:1 to approximately 1.5:1. 14. The pharmaceutical composition according to claim 13, wherein said ratio is approximately 5.4:1, 4.0:1, or 1.5:1. 15. The pharmaceutical composition according to claim 14, wherein said ratio is approximately 1.5:1. 16. The pharmaceutical composition according to claim 5, wherein said zinc is provided as zinc chloride or zinc acetate. 17. The pharmaceutical composition according to claim 16, wherein said zinc acetate is provided as ZnAc.sub.2.2H.sub.2O. 18. The pharmaceutical composition according to claim 1, wherein when said composition is administered to said subject in need thereof, said analog of glucagon-like peptide-1 is released within said subject for at least approximately three weeks. 19. The pharmaceutical composition according to claim 1, wherein when said composition is administered to said subject in need thereof, the analog of glucagon-like peptide-1 is released within said subject for at least approximately four weeks. 20. The pharmaceutical composition according to claim 11, wherein when said composition is administered to said subject in need thereof, said analog of glucagon-like peptide-1 is released within said subject for at least approximately three weeks. 21. The pharmaceutical composition according to claim 11, wherein when said composition is administered to said subject in need thereof, the analog of glucagon-like peptide-1 is released within said subject for at least approximately four weeks. 22. The pharmaceutical composition according to any one of claims 18-19, wherein said subject is a mammal. 23. The pharmaceutical composition according to any one of claims 20-21, wherein said subject is a mammal. 24. The composition according to claim 15, wherein the concentration of [Aib.sup.8,35]hGLP-1(7-36)NH.sub.2 in said composition is about 1% (weight/volume). 25. The composition according to claim 15, wherein the concentration of [Aib.sup.8,35]hGLP-1(7-36)NH.sub.2 in said composition is about 2% (weight/volume). 26. The composition according to claim 15, wherein the concentration of [Aib.sup.8,35]hGLP-1(7-36)NH.sub.2 in said composition is about 10% (weight/volume). 27. The composition according to claim 15, wherein the concentration of [Aib.sup.8,35]hGLP-1(7-36)NH.sub.2 in said composition is about 25% (weight/volume). 28. The composition according to claim 14, wherein the concentration of [Aib.sup.8,35]hGLP-1(7-36)NH.sub.2 in said composition is about 5% (weight/volume) and said ratio is approximately 5.4:1. 29. The composition according to claim 14, wherein the concentration of [Aib.sup.8,35]hGLP-1(7-36)NH.sub.2 in said composition is about 5% (weight/volume) and said ratio is approximately 4.0:1. 30. The composition according to claim 14, wherein the concentration of [Aib.sup.8,35]hGLP-1(7-36)NH.sub.2 said composition is about 10% (weight/volume) and said ratio is approximately 5.4:1. 31. The composition according to claim 14, wherein the concentration of [Aib.sup.8,35]hGLP-1(7-36)NH.sub.2 in said composition is about 23% (weight/volume) and said ratio is approximately 4.0:1. 32. The composition according to claim 15, wherein the concentration of [Aib.sup.8,35]hGLP-1(7-36)NH.sub.2 in said composition is about 23% (weight/volume). 33. The pharmaceutical composition according to claim 22, wherein said subject is a human. 34. The pharmaceutical composition according to claim 23, wherein said subject is a human. 35. The composition according to claim 15, wherein the concentration of [Aib.sup.8,35]hGLP-1(7-36)NH.sub.2 in said pharmaceutical composition is about 10% (weight/volume) and the molar ratio of [Aib.sup.8,35]hGLP-1(7-36)NH.sub.2 to zinc is about 1.5:1. 36. A method of treating a subject afflicted with Type I diabetes, Type II diabetes or gestational diabetes comprising administering to said subject the pharmaceutical composition according to claim 1. 37. The method according to claim 36, wherein said subject is a human being. 38. The method according to claim 37, wherein said disease is Type I diabetes or Type II diabetes. 39. A method of stimulating beta-cell proliferation or reducing beta-cell deterioration comprising administering to a subject in need thereof the pharmaceutical composition according to claim 1. 40. The method according to claim 39, wherein said subject is a human being. 41. A method of treating a subject afflicted with Type I diabetes, Type II diabetes or gestational diabetes comprising administering to said subject the pharmaceutical composition according to claim 5. 42. The method according to claim 41, wherein said subject is a human being. 43. The method according to claim 42, wherein said disease is Type I diabetes or Type II diabetes. 44. A method of stimulating beta-cell proliferation or reducing beta-cell deterioration comprising administering to a subject in need thereof the pharmaceutical composition according to claim 5. 45. The method according to claim 32, wherein said subject is a human being.

Details for Patent 8,236,759

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Merck Sharp & Dohme Corp.	ZOSTAVAX	zoster vaccine live	For Injection	125123	05/25/2006		2026-06-30