Abstract: The invention relates to a salt of 3-methyl-1-phenyl-2-pyrazolin-5-one (edaravone), wherein the salt is 3-methyl-1-phenyl-2-pyrazolin-5-one napadisylate or 3-methyl-1-phenyl-2-pyrazolin-5-one hemi-napadisylate. These napadisylate salts of edaravone are easy to manufacture and dissolve more rapidly in water than the free edaravone base. In addition, the edaravone salts of the present invention are very stable and easy to handle. The invention also relates to a pharmaceutical composition comprising the aforementioned edaravone salt and to a method of preparing such edaravone salt.
Type:
Grant
Filed:
April 10, 2020
Date of Patent:
September 14, 2021
Assignee:
TREEWAY TW001 B.V.
Inventors:
Ana Fernandez Casares, Ronald Van Der Geest, Sytske Hyke Moolenaar
Abstract: A solid water-dispersible pharmaceutical composition for use in the treatment of a disease is disclosed. The treatment comprises dispersing the pharmaceutical composition into an aqueous liquid to produce an enterally administrable liquid containing at least 0.5 grams of the pharmaceutical composition and at least 0.3 g/l of edaravone, followed by enterally administering the enterally administrable liquid to a human patient in an amount providing a dose of 30-300 mg edaravone. The pharmaceutical composition comprises 2-50 wt. % of 3-methyl-1-phenyl-2-pyrazolin-5-one (edaravone) and 3-50 wt. % of a water soluble alkalizing agent. This solid edaravone containing composition can easily be dispersed in aqueous liquid to prepare an aqueous edaravone solution that can be ingested by a patient.
Abstract: The invention relates to a salt of 3-methyl-1-phenyl-2-pyrazolin-5-one (edaravone), wherein the salt is 3-methyl-1-phenyl-2-pyrazolin-5-one napadisylate or 3-methyl-1-phenyl-2-pyrazolin-5-one hemi-napadisylate. These napadisylate salts of edaravone are easy to manufacture and dissolve more rapidly in water than the free edaravone base. In addition, the edaravone salts of the present invention are very stable and easy to handle. The invention also relates to a pharmaceutical composition comprising the aforementioned edaravone salt and to a method of preparing such edaravone salt.
Type:
Application
Filed:
April 10, 2020
Publication date:
October 1, 2020
Applicant:
Treeway TW001 B.V.
Inventors:
Ana Fernandez Casares, Ronald Van Der Geest, Sytske Hyke Moolenaar