Claims for Patent: 11,478,450

Summary for Patent: 11,478,450

Title:	Edaravone suspension for oral administration
Abstract:	An edaravone suspension for human oral administration includes edaravone particles, a dispersant, and water.
Inventor(s):	Tetsuo Hayama, Tomohiro Takahashi, Tomoyuki Omura, Kouji Hayashi, Munetomo Matsuda, Tadashi Miyazawa
Assignee:	Mitsubishi Tanabe Pharma Corp
Application Number:	US17/560,493
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 11,478,450
Patent Claims:	1. A method for treating amyotrophic lateral sclerosis, comprising: orally administering, to a patient in need thereof, an oral formulation comprising edaravone such that an amount of the edaravone in oral administration is in a range of 60 to 400 mg/day, wherein the oral formulation is an edaravone suspension comprising water, the edaravone comprising edaravone particles dispersed in the water, and a dispersant dispersing the edaravone particles in the water such that the dispersant maintains the edaravone particles in a solid particle state in the water, the oral administration comprises administering the oral formulation to the patient in need thereof such that the oral administration of the edaravone is in a range of 50 to 210 mg/dose and that a dose of the oral formulation is in an amount in a range of 1 to 20 mL, the oral administration comprises a number of administrations in a range of once to 3 times per day and includes administering the oral formulation to the patient in need thereof daily or intermittently, and the oral formulation is formulated such that when the oral formulation comprising the edaravone in a range of 90 to 120 mg is orally administered to the patient, edaravone in the plasma of the patient exhibits a mean Cmax in a range of 500 to 2500 ng/mL and a mean AUC0-∞ in a range of 1000 to 2500 h*ng/mL. 2. The method of claim 1, wherein the oral formulation is administered to the patient in need thereof daily. 3. The method of claim 1, wherein the oral formulation is administered to the patient in need thereof intermittently. 4. The method of claim 3, wherein the oral formulation is administered to the patient in need thereof intermittently such that an intermittent administration period has an administration period of 14 days or 10 days out of 14 days, and a drug holiday period of 14 days. 5. The method of claim 1, wherein the oral administration comprises administering the oral formulation to the patient in need thereof such that the number of administrations is once per day. 6. The method of claim 1, wherein the oral administration comprises administering the oral formulation to the patient in need thereof such that the oral administration of the edaravone is 105 mg/day. 7. The method of claim 1, wherein a blending amount of the edaravone particles is in a range of 0.5% (w/v) to 36% (w/v), and the dispersant is at least one dispersant selected from the group consisting of polyvinyl alcohol, methylcellulose, hypromellose, sucrose fatty acid ester and polysorbate. 8. The method of claim 1, wherein the edaravone suspension has a density of in a range of 1 g/mL to 1.5 g/mL. 9. The method of claim 1, wherein the edaravone suspension has an edaravone dissolution rate of 80% or more 30 minutes after starting a dissolution test according to Japanese Pharmacopeia. 10. The method of claim 1, wherein the edaravone particles in the edaravone suspension have a D50 particle size in a range of 10 μm to 100 μm and a D90 particle size of in a range of 50 μm to 300 μm. 11. The method of claim 1, wherein when the edaravone in the oral formulation is in a range of 90 to 120 mg, and a crossover study is performed such that the oral formulation is orally administered to a human and that an edaravone injection is used as a control drug product, a lower limit of a 90% confidence interval of a ratio of a Cmax geometric mean value with respect to the control drug product and a lower limit of a 90% confidence interval of a ratio of an AUC0-∞ geometric mean value with respect to the control drug product both exceed 0.8. 12. The method of claim 1, wherein when the edaravone in the oral formulation is in a range of 90 to 120 mg, and a crossover study is performed such that the oral formulation is orally administered to a human and that an edaravone injection is used as a control drug product, a ratio of a Cmax geometric mean value with respect to the control drug product and a ratio of an AUC0-∞ geometric mean value with respect to the control drug product are both in a range of 0.8 to 1.25. 13. The method of claim 1, wherein a blending amount of the edaravone particles is in a range of 0.5% (w/v) to 36% (w/v). 14. The method of claim 1, wherein a blending amount of the dispersant is in a range of 0.001% (w/v) to 1.0% (w/v). 15. The method of claim 13, wherein the oral formulation is administered to the patient in need thereof daily. 16. The method of claim 13, wherein the oral formulation is administered to the patient in need thereof intermittently. 17. The method of claim 16, wherein the oral formulation is administered to the patient in need thereof intermittently such that an intermittent administration period has an administration period of 14 days or 10 days out of 14 days and a drug holiday period of 14 days. 18. The method of claim 14, wherein the oral formulation is administered to the patient in need thereof daily. 19. The method of claim 14, wherein the oral formulation is administered to the patient in need thereof intermittently. 20. The method of claim 19, wherein the oral formulation is administered to the patient in need thereof intermittently such that an intermittent administration period has an administration period of 14 days or 10 days out of 14 days and a drug holiday period of 14 days.