FIELD: pharmaceuticals.
SUBSTANCE: group of inventions concerns an edaravone suspension for oral administration and its use, as well as a kit for its preparation. The proposed edaravone suspension contains edaravone particles, a dispersant and water, wherein the dispersant is one or more selected from polyvinyl alcohol, methylcellulose, hypromellose, sucrose fatty acid ester and polysorbate. Also the following is proposed: the use of the above edaravone suspension for oral administration to a human, wherein when a suspension containing 90–120 mg of edaravone is orally administered to a human, edaravone in plasma exhibits an average Cmax of 500–2,500 ng/ml and an average AUC0-∞ 1,000–2,500 h*ng/ml; a therapeutic agent for the treatment of amyotrophic lateral sclerosis (ALS) for single oral administration, containing the above edaravone suspension, in which the drug dose per oral administration is 1–20 ml, and the dose contains 50–210 mg of edaravone; kit for the preparation of edaravone suspension for oral administration to humans, containing: (A) a solid composition containing edaravone particles; and (B) a dispersant solution, wherein the dispersant is one or more selected from polyvinyl alcohol, methylcellulose, hypromellose, sucrose fatty acid ester, and polysorbate. The use of the above dispersing agents ensures uniform dispersion in water, and even if edaravone particles precipitate during storage, such particles can be quickly redispersed by gentle shaking.
EFFECT: suspension exhibits high bioavailability when administered orally to humans and may provide an anti-ALS therapeutic effect equivalent to that of injection and may consequently reduce the burden on ALS patients and caregivers.
17 cl, 11 tbl, 42 ex, 1 dwg
