Back to results
US 2020/0368166 A1Published application
Oral Formulations And Uses Thereof
AssigneeEustralis Pharmaceuticals Limited (Trading As Pressura Neuro)
InventorsPierre Vankan, Andreea Sasarman, Grasiela Bourscheit Willmbrink
Life of this patent
Estimating the term…
Abstract
Disclosed are therapeutic oral formulations comprising particular substituted pyridine based compounds, their manufacture, and methods and uses of the formulations in treating substance P mediated pathways in the brain such as elevated intracranial pressure or the modification of expression of (hyper)-phosphorylated tau protein (τ) in the brain for indications such as, but not limited to concussion, post-concussive (or post-concussion) syndrome (PCS), chronic traumatic encephalopathy (CTE), traumatic brain injury (TBI) and stroke.
Claims20
A pharmaceutical composition in the form of a tablet comprising:
- (i) a compound of Formula (I) or a pharmaceutically acceptable salt, solvate or prodrug thereof:
- wherein R1 is H or C1-4 alkyl;
- and
- wherein the compound of Formula (I) or the pharmaceutically acceptable salt, solvate or prodrug thereof within the composition has a D(0.5) particle size distribution of less than about 60 μm;
- (ii) at least one diluent selected from the group consisting of lactose, sorbitol, dibasic calcium phosphate dihydrate, calcium sulphate dihydrate, calcium carbonate, croscarmellose sodium, calcium phosphate, calcium hydrogen phosphate dihydrate, crospovidone, ferric oxide, magnesium carbonate, magnesium oxide, sucrose, or sodium chloride, wherein the at least one diluent is present in the composition in an amount from about 35% to about 70% wt/wt based on the total weight of the composition;
- (iii) at least one lubricant selected from the group consisting of magnesium stearate, stearic acid, calcium stearate, paraffin, sodium lauryl sulphate, sodium benzoate, castor oil hydrogenated, glyceryl monostearate, glyceryl behenate, sodium stearyl fumarate, mineral oil, polaxamer, PEG 400, PEG 600, or PEG 8000, wherein the at least one lubricant is present in the composition in an amount from about 0.1% to about 2% wt/wt based on the total weight of the composition;
- (iv) at least one disintegrant selected from the group consisting of microcrystalline cellulose, alginic acid, citric acid, croscamellose sodium, carboxy methyl cellulose calcium, cysteine HCl, methyl cellulose, polyoxy stearate, sodium starch glycolate, sodium alginate, or carboxy methyl cellulose sodium, wherein the at least one disintegrant is present in the composition in an amount from about 20% to about 30% wt/wt based on the total weight of the composition;
- (v) at least one binder selected from the group consisting of starch, gelatin, glucose, polyvinyl pyrrolidone (Povidone), carboxymethylcellulose, acacia, candelilla wax, carnuba wax, cornstarch, glyceryl behenate, hypromellose, or polyethylene oxide, wherein the at least one binder is present in the composition in an amount from about 5% to about 15% wt/wt based on the total weight of the composition;
- and
- (vi) at least one anti-caking agent selected from the group consisting of fumed silica, silicon dioxide, or talc, wherein the at least one anti-caking agent is present in the composition in an amount from about 0.2% to about 2% wt/wt based on the total weight of the composition.
7 more elements
(canceled)
A method for treating over-expression of hyper-phosphorylated tau protein (τ) in the brain, post-concussion syndrome (PCS), chronic traumatic encephalopathy (CTE) or elevated intracranial pressure in a subject in need thereof, the method comprising administering to the subject a pharmaceutical composition in the form of a tablet comprising:
- (i) a compound of Formula (I) or a pharmaceutically acceptable salt, solvate or prodrug thereof:
- wherein R1 is H or C1-4 alkyl;
- and
- wherein the compound of Formula (I) or the pharmaceutically acceptable salt, solvate or prodrug thereof within the composition has a D(0.5) particle size distribution of less than about 60 μm;
- (ii) at least one diluent selected from the group consisting of lactose, sorbitol, dibasic calcium phosphate dihydrate, calcium sulphate dihydrate, calcium carbonate, croscarmellose sodium, calcium phosphate, calcium hydrogen phosphate dihydrate, crospovidone, ferric oxide, magnesium carbonate, magnesium oxide, sucrose, or sodium chloride, wherein the at least one diluent is present in the composition in an amount from about 35% to about 70% wt/wt based on the total weight of the composition;
- (iii) at least one lubricant selected from the group consisting of magnesium stearate, stearic acid, calcium stearate, paraffin, sodium lauryl sulphate, sodium benzoate, castor oil hydrogenated, glyceryl monostearate, glyceryl behenate, sodium stearyl fumarate, mineral oil, polaxamer, PEG 400, PEG 600, or PEG 8000, wherein the at least one lubricant is present in the composition in an amount from about 0.1% to about 2% wt/wt based on the total weight of the composition;
- (iv) at least one disintegrant selected from the group consisting of microcrystalline cellulose, alginic acid, citric acid, croscamellose sodium, carboxy methyl cellulose calcium, cysteine HCl, methyl cellulose, polyoxy stearate, sodium starch glycolate, sodium alginate, or carboxy methyl cellulose sodium, wherein the at least one disintegrant is present in the composition in an amount from about 20% to about 30% wt/wt based on the total weight of the composition;
- (v) at least one binder selected from the group consisting of starch, gelatin, glucose, polyvinyl pyrrolidone (Povidone), carboxymethylcellulose, acacia, candelilla wax, carnuba wax, cornstarch, glyceryl behenate, hypromellose, or polyethylene oxide, wherein the at least one binder is present in the composition in an amount from about 5% to about 15% wt/wt based on the total weight of the composition;
- and
- (vi) at least one anti-caking agent selected from the group consisting of fumed silica, silicon dioxide, or talc, wherein the at least one anti-caking agent is present in the composition in an amount from about 0.2% to about 2% wt/wt based on the total weight of the composition.
7 more elements
(canceled)
Dependencies are inferred from the claim text.