New Oral Formulation
OwnerKarel De Bruijn, Günter Engel +4inventors
InventorsKarel De Bruijn, Günter Engel, Hans-Jürgen Pfannkuche, Michael Thewissen, Christian Vitzling, Othmar Züger
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Abstract
The present invention relates to a pharmaceutical composition, in particular to a composition for administering active agents which are poorly soluble in aqueous media, and/or which are acid sensitive.
Claims19
1-26. (canceled)
A solid oral pharmaceutical composition comprising 3-(5-methoxy-1H-indol-3-yl-methylene)-N-pentylcarbazimidamide or a pharmaceutically acceptable salt thereof and a disintegrant which is present in an amount of at least 15% by weight based on the total weight of the composition, wherein the disintegrant is a member selected from the group consisting of crospovidone, sodium starch glycolate, carboxymethylcellulose sodium, sodium alginate, and a mixture thereof.
A solid oral pharmaceutical composition according to claim 34 wherein the disintegrant is crospovidone.
A solid oral pharmaceutical composition according to claim 36 wherein the lubricant comprises a glyceryl mono fatty acid.
A solid oral pharmaceutical composition according to claim 36 wherein the lubricant comprises a mixture of glyceryl monostearate and polyethylene glycol.
A solid oral pharmaceutical composition according to claim 38 further comprising a surfactant.
A solid oral pharmaceutical composition according to claim 39 wherein the surfactant is a member selected from the group consisting of a polyoxytheylene-sorbitan-fatty acid ester, a polyoxyethylene fatty acid ester, a polyoxyethylene-polyoxypropylene block co-polymer, a reaction product of a natural or hydrogenated castor oil and ethylene oxide, dioctylsuccinate, di-[2-ethylhexyl]-succinate, a propylene glycol mono-fatty acid, and a propylene glycol di-fatty acid.
A solid oral pharmaceutical composition according to claim 40 wherein the surfactant comprises a polyoxyethylene-polyoxypropylene block co-polymer.
A solid oral pharmaceutical composition according to claim 41 further comprising lactose and hydroxypropylmethylcellulose.
A solid oral pharmaceutical composition comprising 3-(5-methoxy-1H-indol-3-yl-methylene)-N-pentylcarbazimidamide or a pharmaceutically acceptable salt_thereof and a disintegrant which is present in an amount between 20% and 60% by weight based on the total weight of the composition, wherein the disintegrant is carboxymethylcellulose calcium.
A solid oral pharmaceutical composition according to claim 44 wherein the pharmaceutically acceptable salt is the maleate salt of 3-(5-methoxy-1H-indol-3-yl-methylene)-N-pentylcarbazimidamide.
A solid oral pharmaceutical composition comprising 3-(5-methoxy-1H-indol-3-yl-methylene)-N-pentylcarbazimidamide or a pharmaceutically acceptable salt thereof and a disintegrant which is present in an amount between 30% and 50% by weight based on the total weight of the composition, wherein the disintegrant is pregelatinized starch.
A solid oral pharmaceutical composition according to claim 46 wherein the pharmaceutically acceptable salt is the maleate salt of 3-(5-methoxy-1H-indol-3-yl-methylene)-N-pentylcarbazimidamide.
A solid oral pharmaceutical composition according to claim 45 wherein said composition is a tablet.
A solid oral pharmaceutical composition according to claim 47 wherein said composition is a tablet.
Dependencies are inferred from the claim text.