Pharmaceutical preparation of N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acetamide
The invention relates to a pharmaceutical preparation for oral administration comprising N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acetamide or its hydrates and/or solvates, as well as an acid, a method for its production as well as the use of this preparation for the treatment and/or prophylaxis of diseases which are caused by herpes viruses, in particular diseases which are caused by herpes simplex viruses.
1. A pharmaceutical preparation for oral application comprising
N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acetamide or a hydrate thereof,
optionally one or more dry binders,
at least one disintegration auxiliary,
at least one lubricant and
optionally a tenside,
said preparation comprising methanesulfonic acid which is used in a stoichiometric ratio of N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acetamide or said hydrate to acid of 1 to 0.10 to 1.10 whereby said acetamide and said acid form a salt.
2. The preparation of claim 1 , comprising 30 to 1200 mg of N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acetamide or a hydrate based on a single tablet.
3. The preparation of claim 1 , wherein said dry binder is microcrystalline cellulose.
4. The preparation of claim 1 , wherein said disintegration auxiliary is croscarmellose sodium or a mixture of croscarmellose sodium and cross-linked polyvinylpyrrolidone (4:1).
5. The preparation of claim 1 , wherein said lubricant is magnesium stearate.
6. The preparation of claim 1 , wherein said tenside is polysorbate 80.
7. The preparation of claim 1 , comprising:
50 to 70% N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acetamide or hydrates thereof,
15 to 29% croscarmellose sodium and cross-linked polyvinylpyrrolidone (4:1),
0.5 to 1.1% magnesium stearate,
1 to 5% microcrystalline cellulose,
optionally 0.4 to 0.5% polysorbate 80, as well as
methanesulfonic acid with a stoichiometric ratio of acetamide to acid of 1 to 0.90 to 0.98 whereby said acetamide and said acid form a salt.
8. A tablet preparation for oral application comprising a core of said pharmaceutical preparation of claim 1 and a varnish coating.
9. The preparation of claim 1 , comprising N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acetamide.
10. The preparation of claim 8 , comprising N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acetamide.
11. The preparation of claim 1 for the treatment of diseases which are caused by herpes viruses, in particularly diseases which are caused by herpes simplex viruses.
12. The preparation of claim 8 for the treatment of diseases which are caused by herpes viruses, in particularly diseases which are caused by herpes simplex viruses.
13. A method for the production of the pharmaceutical preparation for oral application of claim 1 , wherein N-[5-(Aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acetamide or a hydrate thereof, optionally one or more dry binders and an acid are subjected to an aqueous granulation to form granules, said granules are subsequently mixed with at least one disintegration auxiliary and at least one lubricant and optionally a wetting agent and optionally tabletted and varnished.
14. A method for the production of the pharmaceutical preparation for oral application of claim 8 , wherein N-[5-(Aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acetamide or a hydrate thereof, optionally one or more dry binders and an acid are subjected to an aqueous granulation to form granules, said granules are subsequently mixed with at least one disintegration auxiliary and at least one lubricant and optionally a wetting agent and optionally tabletted and varnished.
15. A compound selected from the group consisting of:
N-[5-(Aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acetamide mesylate, and its hydrates.
16. The preparation of claim 1 , wherein, when treated with 0.1 N HCl at 37° C., the preparation releases said acetamide faster than a preparation lacking methanesulfonic acid releases said acetamide.
17. The preparation of claim 1 , wherein at least 80% of said acetamide is released from the preparation within 30 minutes in 0.1 N HCl at 37° C.