Method for producing stable acetylsalicylic acid solutions
OwnerWalter Burghart, Kurt Burghartinventors
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Abstract
In a method for producing stable acetylsalicylic acid solutions with pharmaceutically acceptable non-aqueous organic solvents such as, e.g., dimethylisosorbide, propylene glycol or diethylene glycol monoethyl ether, 0.005-2% by weight of a cyclic acid imide and/or 0.005-2% by weight of a sulfaminic acid as well as, preferably, 1-40% by weight, based on the weight of the solution, of a compound of the general formula are added to the solution. In the general formula, R1 represents H, CH3 or C2H5, n=0 or 1, and R2 represents H or one or more lower alkyl, lower alkyloxy or lower alkenyl residues having 1 to 5 carbon atoms.
Claims15
A method for producing a stable acetylsalicylic acid solution comprising dissolving acetylsalicylic acid in a pharmaceutically acceptable non-aqueous organic solvent selected from the group consisting of dimethylisosorbide, propylene glycol and diethylene glycol monethyl ether, together with 0.05-2% by weight of a cyclic acid imide, or 0.05-2% by weight of a sulfaminic acid or both a cyclic acid imide and a sulfaminic acid and 1-40% by weight, based on the weight of the solution, of a compound of the formula:
- wherein R1 represents H, CH3 or C2H5, n=0 or 1, and R2 represents H or a lower alkyl, lower alkyloxy or lower alkenyl group each having 1 to 5 carbon atoms.
A stable solution of acetylsalicylic acid consisting essentially of:
- 5-15% by weight acetylsalicylic acid,
- 10-40% by weight propylene glycol,
- 0-40% by weight dimethylisosorbide,
- 0-70% by weight diethylene glycol monoethyl ether and,
- 0.05-2% by weight saccharin and/or cyclamic acid, and/or
- 1-40% by weight anethole and/or benzyl alcohol.
A stable solution consisting essentially of:
- 12.5% by weight acetylsalicylic acid,
- 30% by weight each of propylene glycol and dimethylisosorbide, or both the propylene glycol and dimethyl isosorbide are replaced totally or partially with benzyl alcohol or anethole or a mixture thereof,
- the balance being diethylene glycol monoethyl ether and 0.1-0.5% by weight, based on the weight of the solution, of saccharin and/or cyclamic acid.
A stable solution consisting essentially of:
- 10-24% by weight acetylsalicylic acid,
- 0.05-2% by weight saccharin and/or cyclamic acid,
- 20-80% by weight methoxy propanol, and
- optionally:
- 1-30% by weight benzyl alcohol and/or anethole, propylene glycol, diethylene glycol monoethyl ether, oleic acid, tocopherol or mixtures thereof.
A method of administering acetylsalicylic acid to a patient comprising dermally or sublingually administering to said patient a stable solution of acetylsalicylic acid consisting essentially of 5-15% by weight acetylsalicylic acid,
- 10-40% by weight propylene glycol, 0-40% by weight dimethylisosorbide,
- 0-70% by weight diethylene glycol monoethyl ether and,
- 0.05-2% by weight saccharin and/or cyclamic acid, and/or
- 1-40% by weight anethole and/or benzyl alcohol.
A method of administering acetylsalicylic acid to a patient comprising dermally or sublingually administering to said patient a stable solution of 12.5% by weight acetylsalicylic acid,
- 30% by weight each of propylene glycol and dimethylisosorbide, or both the propylene glycol and dimethyl isosorbide are replaced totally or partially with benzyl alcohol or anethole or a mixture thereof,
- the balance being diethylene glycol monoethyl ether and 0.1-0.5% by weight, based on the weight of the solution, of saccharin and/or cyclamic acid.
In a method for producing a stable acetylsalicylic acid solution with pharmaceutically acceptable non-aqueous organic solvents selected from dimethylisosorbide, propylene glycol or diethylene glycol monoethyl ether,
- the improvement comprising adding to the solution 0.05-2% by weight of a cyclic acid imide or 0.05-2% by weight of a sulfaminic acid or both a cyclic acid and a sulfaminic acid and 1-40% by weight, based on the weight of the solution, of a compound of the formula
- wherein R1 represents H, CH3 or C2H5, n=0 or 1, and R2 represents H or one or a lower alkyl, lower alkyloxy or lower alkenyl group each having 1 to 5 carbon atoms.
Dependencies are inferred from the claim text.