Claims for Patent: 11,241,416

Summary for Patent: 11,241,416

Title:	Edaravone suspension for oral administration
Abstract:	An edaravone suspension for human oral administration includes edaravone particles, a dispersant, and water.
Inventor(s):	Hayama; Tetsuo (Osaka, JP), Takahashi; Tomohiro (Osaka, JP), Omura; Tomoyuki (Osaka, JP), Hayashi; Kouji (Osaka, JP), Matsuda; Munetomo (Osaka, JP), Miyazawa; Tadashi (Osaka, JP)
Assignee:	MITSUBISHI TANABE PHARMA CORPORATION (Osaka, JP)
Application Number:	17/213,501
Patent Claims:	1. An edaravone suspension for human oral administration, comprising: water; edaravone particles comprising edaravone and dispersed in the water; and a dispersant exhibiting a transmission scattering light intensity of 1% or more and dispersing the edaravone particles in the water such that the dispersant maintains the edaravone particles in a solid particle state in the water, wherein a blending amount of the dispersant is in a range of 0.001% (w/v) to 1.0% (w/v), a blending amount of the edaravone particles is in a range of 0.5% (w/v) to 36% (w/v), and when edaravone in the edaravone suspension is in a range of 90 to 120 mg, edaravone in a plasma exhibits a mean Cmax in a range of 500 to 2500 ng/mL and a mean AUC.sub.0-.infin. in a range of 1000 to 2500 h*ng/mL when the edaravone suspension is orally administered to a human. 2. The edaravone suspension according to claim 1, wherein the dispersant is a dispersant exhibiting a contact angle of 80 degrees or less. 3. The edaravone suspension according to claim 1, further comprising a thickening agent. 4. The edaravone suspension according to claim 3, wherein the thickening agent is one or two thickening agents selected from the group consisting of xanthan gum and tragacanth powder. 5. The edaravone suspension according to claim 3, wherein the thickening agent is xanthan gum. 6. The edaravone suspension according to claim 3, wherein a blending amount of the thickening agent is in a range of 0.1% (w/v) to 1.2% (w/v). 7. The edaravone suspension according to claim 1, wherein the edaravone particles in the suspension have a D50 particle size in a range of 10 .mu.m to 100 .mu.m and a D90 particle size of in a range of 50 .mu.m to 300 .mu.m. 8. The edaravone suspension according to claim 1, wherein a blending amount of the edaravone particles is in a range of 1% (w/v) to 36% (w/v). 9. The edaravone suspension according to claim 1, further comprising at least one additive selected from the group consisting of a sweetener, a stabilizer and a pH regulator. 10. The edaravone suspension according to claim 1 having a density of in a range of 1 g/mL to 1.5 g/mL. 11. The edaravone suspension according to claim 1, wherein the suspension has an edaravone dissolution rate of 80% or more 30 minutes after starting a dissolution test according to Japanese Pharmacopeia. 12. The edaravone suspension according to claim 1, wherein when edaravone in the edaravone suspension is in a range of 90 to 120 mg, and a crossover study is performed such that the edaravone suspension 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 AUC.sub.0-.infin. geometric mean value with respect to the control drug product both exceed 0.8. 13. The edaravone suspension according to claim 1, wherein when edaravone in the edaravone suspension is in a range of 90 to 120 mg, and a crossover study is performed such that the edaravone suspension 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 AUC.sub.0-.infin. geometric mean value with respect to the control drug product are both in a range of 0.8 to 1.25. 14. An edaravone suspension for human oral administration, comprising: water; edaravone particles comprising edaravone and dispersed in the water; and a dispersant exhibiting a contact angle of 80 degrees or less and dispersing the edaravone particles in the water such that the dispersant maintains the edaravone particles in a solid particle state in the water, wherein a blending amount of the dispersant is in a range of 0.001% (w/v) to 1.0% (w/v), a blending amount of the edaravone particles is in a range of 0.5% (w/v) to 36% (w/v), and when edaravone in the edaravone suspension is in a range of 90 to 120 mg, edaravone in a plasma exhibits a mean Cmax in a range of 500 to 2500 ng/mL and a mean AUC.sub.0-.infin. in a range of 1000 to 2500 h*ng/mL when the edaravone suspension is orally administered to a human. 15. The edaravone suspension according to claim 14, further comprising a thickening agent in a blending amount in a range of 0.1% (w/v) to 1.2% (w/v). 16. The edaravone suspension according to claim 14, wherein the thickening agent is one or two thickening agents selected from the group consisting of xanthan gum and tragacanth powder. 17. The edaravone suspension according to claim 14, wherein the edaravone particles in the suspension have a D50 particle size in a range of 10 .mu.m to 100 .mu.m and a D90 particle size of in a range of 50 .mu.m to 300 .mu.m. 18. The edaravone suspension according to claim 14, wherein a blending amount of the edaravone particles is in a range of 1% (w/v) to 36% (w/v). 19. The edaravone suspension according to claim 14, wherein when edaravone in the edaravone suspension is in a range of 90 to 120 mg, and a crossover study is performed such that the edaravone suspension 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 AUC.sub.0-.infin. geometric mean value with respect to the control drug product both exceed 0.8. 20. The edaravone suspension according to claim 14, wherein when edaravone in the edaravone suspension is in a range of 90 to 120 mg, and a crossover study is performed such that the edaravone suspension 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 AUC.sub.0-.infin. geometric mean value with respect to the control drug product are both in a range of 0.8 to 1.25.