Pharmaceutical composition of a pyrazole compound dispersed in a polymer matrix
A pharmaceutical composition of pyrazole compound dispersed in a polymer matrix and a method of using the same to treat atopic dermatitis.
1 . A solid pharmaceutical composition comprising
a) a pharmaceutically effective amount of a compound of Formula (I)
dispersed in a hydroxypropyl methylcellulose acetate succinate (HPMCAS) polymer matrix; and
b) a pharmaceutically acceptable carrier;
wherein the compound of Formula (I) is present in substantially an amorphous form; and wherein the pharmaceutical composition is a tablet and wherein at least 80% of the compound of Formula (I) is in amorphous form and the ratio of the polymer to the compound of Formula (I) in the dispersion is between about 10:1 and about 5:1.
2 . The pharmaceutical composition of claim 1 , wherein the hydroxypropyl methylcellulose acetate succinate polymer is L grade (HPMCAS-L).
3 . The pharmaceutical composition of claim 1 , wherein the amount of the compound of Formula (I) in the pharmaceutical composition is between about 0.5 and about 10% or is between about 1.0 and about 5.0% or is about 2% (w/w).
4 . The pharmaceutical composition of claim 1 , wherein the amount of HPMCAS polymer in the pharmaceutical composition is between about 10 and about 30% or is between about 15 and about 25% or is about 20% (w/w).
5 . The pharmaceutical composition of claim 1 , wherein the pharmaceutically acceptable carrier comprises one or more excipients selected from a filler, a lubricant, a binder, an anti-nucleating agent and a disintegrant.
6 . The pharmaceutical composition of claim 5 , wherein the filler is a microcrystalline cellulose, a lactose or mixtures thereof.
7 . The pharmaceutical composition of claim 5 , wherein the lubricant is magnesium stearate.
8 . The pharmaceutical composition of claim 5 , wherein the disintegrant is sodium starch glycolate.
9 . The pharmaceutical composition of claim 5 , wherein the binder is hydroxypropyl cellulose.
10 . The pharmaceutical composition of claim 5 , wherein the anti-nucleating agent is methyl cellulose A4C or hydroxypropyl methylcellulose E50.
11 . A solid pharmaceutical composition comprising a compound of Formula (I)
dispersed in a hydroxypropyl methylcellulose acetate succinate (HPMCAS) polymer matrix wherein in the solid pharmaceutical composition comprises
a) about 0.5 to about 10% w/w of the compound of Formula (1);
b) about 10 to about 30% w/w of HPMCAS;
c) about 0.25 to about 1.5% w/w of magnesium stearate;
d) about 0 to about 75% w/w of microcrystalline cellulose;
e) about 0 to about 75% w/w of lactose monohydrate; and
f) optionally about 0 to 5% w/w of hydroxypropyl cellulose;
wherein the combined w/w percentages of microcrystalline cellulose and lactose monohydrate must be at least 40%.