MEDICAL TREATMENT COMPRISING ENTERAL ADMINISTRATION OF EDARAVONE
First Claim
1. A method of treating a disease, comprising:
- (a) dispersing a pharmaceutical composition comprising edaravone (3-methyl-1-phenyl-2-pyrazolin-5-one) into an aqueous liquid to produce a pharmaceutical liquid comprising at least 0.5 grams of the pharmaceutical composition and at least 0.3 g/l of edaravone, followed by(b) enterally administering the pharmaceutical liquid to a human patient in an amount providing a dose of 30-300 mg edaravone, the pharmaceutical composition comprising;
(i) 2-50 wt. % of edaravone; and
(ii) 3-50 wt. % of water soluble alkalizing agent;
wherein the edaravone in the pharmaceutical composition fully dissolves in a solution when the composition is added to demineralized water of 25°
C. in a concentration equivalent to an edaravone concentration of 1.4 g/l, and wherein the pH of the solution at 25°
C. is at least 0.5 pH units higher than the pH of a solution having the same edaravone concentration and consisting exclusively of edaravone and demineralized water.
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Accused Products
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. The solid composition of the present invention offers the advantage that edaravone dissolves very rapidly when the composition is introduced into water and that the enterally administrable liquid so obtained has high oral bioavailability.
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Citations
17 Claims
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1. A method of treating a disease, comprising:
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(a) dispersing a pharmaceutical composition comprising edaravone (3-methyl-1-phenyl-2-pyrazolin-5-one) into an aqueous liquid to produce a pharmaceutical liquid comprising at least 0.5 grams of the pharmaceutical composition and at least 0.3 g/l of edaravone, followed by (b) enterally administering the pharmaceutical liquid to a human patient in an amount providing a dose of 30-300 mg edaravone, the pharmaceutical composition comprising; (i) 2-50 wt. % of edaravone; and (ii) 3-50 wt. % of water soluble alkalizing agent; wherein the edaravone in the pharmaceutical composition fully dissolves in a solution when the composition is added to demineralized water of 25°
C. in a concentration equivalent to an edaravone concentration of 1.4 g/l, and wherein the pH of the solution at 25°
C. is at least 0.5 pH units higher than the pH of a solution having the same edaravone concentration and consisting exclusively of edaravone and demineralized water.- View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17)
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Specification