US 12,285,409 B2
Edaravone suspension for oral administration
Tetsuo Hayama, Osaka (JP); Tomohiro Takahashi, Osaka (JP); Tomoyuki Omura, Osaka (JP); Kouji Hayashi, Osaka (JP); Munetomo Matsuda, Osaka (JP); and Tadashi Miyazawa, Osaka (JP)
Assigned to MITSUBISHI TANABE PHARMA CORPORATION, Osaka (JP)
Filed by MITSUBISHI TANABE PHARMA CORPORATION, Osaka (JP)
Filed on Sep. 29, 2023, as Appl. No. 18/477,752.
Application 18/477,752 is a continuation of application No. 17/308,399, filed on May 5, 2021, granted, now 11,826,352.
Application 17/308,399 is a continuation in part of application No. 17/213,501, filed on Mar. 26, 2021, granted, now 11,241,416, issued on Feb. 8, 2022.
Application 17/213,501 is a continuation of application No. 16/872,741, filed on May 12, 2020, granted, now 10,987,341, issued on Apr. 27, 2021.
Application 16/872,741 is a continuation of application No. PCT/JP2019/043013, filed on Nov. 1, 2019.
Claims priority of application No. 2018-207646 (JP), filed on Nov. 2, 2018.
Prior Publication US 2024/0033248 A1, Feb. 1, 2024
This patent is subject to a terminal disclaimer.
Int. Cl. A61K 31/4152 (2006.01); A61K 9/00 (2006.01); A61K 9/16 (2006.01); A61K 47/32 (2006.01); A61K 47/36 (2006.01); A61P 21/00 (2006.01)
CPC A61K 31/4152 (2013.01) [A61K 9/0053 (2013.01); A61K 9/16 (2013.01); A61K 47/32 (2013.01); A61K 47/36 (2013.01); A61P 21/00 (2018.01)] 20 Claims
OG exemplary drawing
 
1. An edaravone suspension for human oral administration, comprising:
water;
edaravone particles comprising edaravone and 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,
wherein the edaravone particles in the 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, a blending amount of the edaravone particles is in a range of 0.2% (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 AUC0-∞ in a range of 1000 to 2500 h*ng/mL when the edaravone suspension is orally administered to a human.