Claims for Patent: 10,293,030

Summary for Patent: 10,293,030

Title:	Lyophilised pharmaceutical formulation and its use
Abstract:	A pharmaceutical formulation in a lyophilised form, which comprises pharmacologically effective amount of interferon beta-1a as an active ingredient, disaccharides as a bulking agent and a non-ionic surfactant. After reconstitution, the composition can be administered intravenously.
Inventor(s):	Jalkanen; Markku (Piispanristi, FI), Maksimow; Mikael (Turku, FI), Piippo; Ilse (Parainen, FI)
Assignee:	Faron Pharmaceuticals Oy (Turku, FI)
Application Number:	15/355,691
Patent Claims:	1. A pharmaceutical formulation in a lyophilised form, comprising unpegylated interferon beta-1a as an active ingredient in an amount of 2.0-15 .mu.g in a single dosage form, a disaccharide as a bulking agent in an amount of 30-50 mg, and a non-ionic surfactant selected from the group consisting of polysorbate and polyethylene glycol, wherein the disaccharide is trehalose dihydrate or a mixture of trehalose dihydrate and sucrose, and wherein the interferon beta-1a is recombinantly produced interferon beta-1a with a biological activity higher than 150 Million International Units (MIU)/mg. 2. The formulation according to claim 1, wherein said formulation further comprises a buffering agent for maintaining a pH of about 5.5 to 7.5 after reconstitution of the lyophilized formulation. 3. The formulation according to claim 1, wherein said disaccharide is trehalose dihydrate. 4. The formulation according to claim 1, wherein said non-ionic surfactant is polysorbate and said disaccharide is trehalose dihydrate. 5. The formulation according to claim 2, wherein said formulation comprises disodium phosphate dihydrate, sodium dihydrogen phosphate dihydrate, trisodium citrate dihydrate or combination thereof as the buffering agent. 6. The formulation according to claim 2, wherein said formulation further comprises an antioxidant. 7. The formulation according to claim 6, wherein said antioxidant is methionine. 8. The formulation according to claim 1, wherein the recombinantly produced interferon beta-1a is recombinant human interferon beta-1a. 9. The formulation according to claim 1, wherein the content of residual moisture of said lyophilisated formulation is not more than 5% by weight. 10. The formulation according to claim 9, wherein the content of residual moisture of said lyophilisated formulation is between 1-5%. 11. The formulation according to claim 1, wherein the formulation is prepared from an aqueous solution having a pH of 5.5-7.5 and comprising (i) recombinant human interferon beta-1a as an active ingredient, (ii) trehalose dihydrate or a mixture of trehalose dihydrate and sucrose as a bulking agent, (iii) polysorbate or polyethylene glycol as a surfactant, (iv) a combination of disodium phosphate dihydrate, sodium dihydrogen phosphate dihydrate and trisodium citrate dihydrate as a buffering agent, and (v) methionine as an antioxidant. 12. The formulation according to claim 11, wherein the aqueous solution comprises 0.05-0.15% (w/v) polysorbate or polyethylene glycol and 2-6% (w/v) trehalose dihydrate or a mixture of trehalose dihydrate and sucrose. 13. The formulation according to claim 12, wherein said aqueous solution comprises polysorbate. 14. An aqueous pharmaceutical composition obtained by reconstituting a lyophilised formulation of claim 1. 15. The aqueous pharmaceutical composition of claim 14 for intravenous administration. 16. A delivery device comprising the aqueous pharmaceutical composition of claim 14. 17. The delivery device of claim 16, wherein an inner surface of the delivery device is siliconized. 18. A pre-filled syringe comprising the aqueous pharmaceutical composition of claim 14. 19. The pre-filled syringe of claim 18, wherein an inner surface of the pre-filled syringe is siliconized. 20. A method for the treatment of a disease or a disorder which comprises administering a therapeutically effective amount of the lyophilised formulation of claim 1 to a patient in need thereof, wherein the disease or disorder is selected from vascular leakage in acute respiratory distress syndrome (ARDS), or systemic inflammatory response syndrome (SIRS), ischemia-reperfusion injury in vascular or cardiac surgery and organ transplantation, ischemic pre-conditioning prior to major vascular or cardiac surgery and organ transplantation, and multi-organ failure (MOF). 21. The method of claim 20, wherein the administration is intravenous administration. 22. A method for the treatment of a disease or a disorder which comprises administering a therapeutically effective amount of the aqueous pharmaceutical composition of claim 14 to a patient in need thereof, wherein the disease or disorder is selected from vascular leakage in acute respiratory distress syndrome (ARDS), or systemic inflammatory response syndrome (SIRS), ischemia-reperfusion injury in vascular or cardiac surgery and organ transplantation, ischemic pre-conditioning prior to major vascular or cardiac surgery and organ transplantation, and multi-organ failure (MOF). 23. The method of claim 22, wherein the administration is intravenous administration.

Details for Patent 10,293,030

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Biogen Inc.	AVONEX	interferon beta-1a	For Injection	103628	05/17/1996		2036-02-29
Biogen Inc.	AVONEX	interferon beta-1a	Injection	103628	05/28/2003		2036-02-29
Biogen Inc.	AVONEX	interferon beta-1a	Injection	103628	02/27/2012		2036-02-29
Emd Serono, Inc.	REBIF	interferon beta-1a	Injection	103780	03/07/2002		2036-02-29
Emd Serono, Inc.	REBIF	interferon beta-1a	Injection	103780	12/17/2004		2036-02-29
Emd Serono, Inc.	REBIF	interferon beta-1a	Injection	103780	12/21/2012		2036-02-29