Pharmaceutical compositions comprising a JAK inhibitor
Pharmaceutical compositions comprising filgotinib maleate Form I characterized by an XRPD pattern substantially the same as shown in FIG. 1 and uses thereof are described herein.
1. A pharmaceutical composition comprising . . . filgotinib maleate Form I characterized by an XRPD pattern substantially the same as shown in FIG. 1 .
2. The pharmaceutical composition of claim 1 , further comprising fumaric acid.
3. The pharmaceutical composition of claim 1 or 2 , further comprising magnesium stearate.
4. The pharmaceutical composition of claim 1 or 2 , further comprising magnesium stearate, microcrystalline cellulose, lactose monohydrate, pregelatinized starch, and colloidal silicon dioxide.
5. The pharmaceutical composition of claim 1 or 2 , further comprising magnesium stearate, microcrystalline cellulose, lactose monohydrate, pregelatinized starch, colloidal silicon dioxide, PEG 3350, polyvinyl alcohol, talc, titanium dioxide, and iron oxide red.
6. A pharmaceutical composition according to claim 1 comprising:
about 32 wt % filgotinib maleate Form I;
about 36 wt % microcrystalline cellulose;
about 20 wt % lactose monohydrate;
about 5.0 wt % pregelatinized starch;
about 1.0 wt % colloidal silicon dioxide;
about 1.5 wt % magnesium stearate; and
about 5.0 wt % fumaric acid.
7. A pharmaceutical composition according to claim 1 comprising:
about 29 wt % to about 35 wt % filgotinib maleate Form I;
about 32 wt % to about 40 wt % microcrystalline cellulose;
about 18 wt % to about 22 wt % lactose monohydrate;
about 4.5 wt % to about 5.5 wt % pregelatinized starch;
about 0.9 wt % to about 1.1 wt % colloidal silicon dioxide;
about 1.3 wt % to about 1.8 wt % magnesium stearate; and
about 4.5 wt % to about 5.5 wt % fumaric acid.
8. The pharmaceutical composition of claim 1 or 2 wherein the composition is in the form of a tablet.
9. The pharmaceutical composition of claim 1 or 2 wherein the filgotinib maleate Form I is characterized by a differential scanning calorimetry (DSC) curve substantially the same as shown in FIG. 2 .
10. The pharmaceutical composition of claim 1 or 2 wherein the filgotinib maleate Form I is characterized by thermogravimetric analysis (TGA) comprising a thermogram substantially the same as shown in FIG. 2 .
11. The pharmaceutical composition of claim 1 or 2 wherein the filgotinib maleate Form I is characterized by a proton nuclear magnetic resonance spectrum ( 1 H NMR) substantially the same as shown in FIG. 3 .
12. A method of treating an inflammatory disease or disorder . . . according to claim 1 or 2 to a patient in need thereof, wherein the inflammatory disease or disorder is selected from the group consisting of rheumatoid arthritis, Crohn's disease, ulcerative colitis, alopecia areata, uveitis, acute graft-versus-host disease, cutaneous lupus nephritis, membranous lupus nephritis, atopic dermatitis, psoriasis, ankylosing spondylitis and psoriatic arthritis.