Patent
Stable formulation of modified GLP-1
| العنوان: | Stable formulation of modified GLP-1 |
|---|---|
| Patent Number: | 8,846,618 |
| تاريخ النشر: | September 30, 2014 |
| Appl. No: | 12/785861 |
| Application Filed: | May 24, 2010 |
| مستخلص: | Pharmaceutical formulations of GLP-1 compounds and methods for preparation thereof. |
| Inventors: | Flink, James M. (Klanpenborg, DK); Larsen, Silke Møller (Charlottenlund, DK); Jensen, Simon Bjerregaard (Frederiksberg, DK); Engelund, Dorthe Kot (Holte, DK) |
| Assignees: | Novo Nordisk A/S (Bagsvaerd, DK) |
| Claim: | 1. A pharmaceutical formulation comprising: a GLP-1 compound, wherein said GLP-1 compound is: Arg 34 , Lys 26 (N-ε-(γ-Glu(N-α-hexadecanoyl)))-GLP-1 (7-37), and wherein said GLP-1 compound binds to a GLP-1 receptor with an affinity constant (K D) below about 1 μM or a potency EC 50 below about 1 μM, 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. |
| Claim: | 2. The formulation according to claim 1 , further comprising water. |
| Claim: | 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. |
| Claim: | 4. The formulation according to claim 1 , wherein the concentration of said GLP-1 compound is 1-5 mg/ml. |
| Claim: | 5. The formulation according to claim 1 , wherein said preservative is present in a concentration from 0.1 mg/ml to 20 mg/ml. |
| Claim: | 6. The formulation according to claim 1 , wherein said isotonic agent is present in a concentration from 1 mg/ml to 50 mg/ml. |
| Claim: | 7. The formulation according to claim 1 , further comprising a chelating agent. |
| Claim: | 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. |
| Claim: | 9. The formulation according to claim 1 , further comprising a stabiliser. |
| Claim: | 10. The formulation according to claim 9 , wherein said stabiliser is selected from the group consisting of L-histidine, imidazole and arginine. |
| Claim: | 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. |
| Claim: | 12. The formulation according to claim 1 , further comprising a surfactant. |
| Claim: | 13. A method of preparing a physically stable pharmaceutical formulation of a GLP-1 compound wherein said GLP-1 compound is Arg 34 , Lys 26 (N-ε-(γ-Glu(N-α-hexadecanoyl)))-GLP-1(7-37), and wherein said GLP-1 compound binds to a GLP-1 receptor with an affinity constant (K D) below about 1 μM or a potency EC 50 below about 1 μM, 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. |
| Claim: | 14. A pharmaceutical formulation comprising: a GLP-1 compound, wherein said GLP-1 compound is Arg 34 , Lys 26 (N-ε-(γ-Glu(N-α-hexadecanoyl)))-GLP-1 (7-37), and wherein said GLP-1 compound binds to a GLP-1 receptor with an affinity constant (K D) below about 1 μM or a potency EC 50 below about 1 μM; an isotonic agent; a buffer; and a preservative; wherein said pharmaceutical formulation has a pH from 7.5 to 9.4. |
| Current U.S. Class: | 514/117 |
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| Primary Examiner: | Cordero Garcia, Marcela M |
| Attorney, Agent or Firm: | Wilk-Orescan, Rosemarie R. |
| رقم الانضمام: | edspgr.08846618 |
| قاعدة البيانات: | USPTO Patent Grants |
| الوصف غير متاح. |