PHARMACEUTICAL COMPOSITIONS COMPRISING A JAK INHIBITOR
Pharmaceutical compositions comprising filgotinib maleate Form I and uses thereof are described herein.
1 - 17 . (canceled)
17 . A method of treating uveitis comprising administering a pharmaceutical composition comprising a therapeutically effective amount of filgotinib maleate Form I to a patient in need thereof.
18 . The method of claim 17 , wherein the pharmaceutical composition further comprises fumaric acid.
19 . The method of claim 17 , wherein the pharmaceutical composition further comprises magnesium stearate.
20 . The method of claim 17 , wherein the pharmaceutical composition further comprises magnesium stearate, microcrystalline cellulose, lactose monohydrate, pregelatinized starch, and colloidal silicon dioxide.
21 . The method of claim 17 , wherein the pharmaceutical composition further comprises magnesium stearate, microcrystalline cellulose, lactose monohydrate, pregelatinized starch, colloidal silicon dioxide, PEG 3350, polyvinyl alcohol, talc, titanium dioxide, and iron oxide red.
22 . The method of claim 17 wherein the pharmaceutical composition comprises:
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.
23 . The method of claim 17 wherein the pharmaceutical composition comprises:
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.
24 . The method of claim 17 , wherein the pharmaceutical composition is in the form of a tablet.
25 . The method of claim 17 , wherein the pharmaceutical composition comprises filgotinib maleate Form I characterized by an XRPD pattern comprising peaks at 8.2, 11.9, 16.4, and 18.9° 2θ±0.2° 2θ as determined on a diffractometer using Cu-Kα radiation.
26 . The method of claim 17 , wherein the pharmaceutical composition comprises filgotinib maleate Form I characterized by an XRPD pattern substantially the same as shown in FIG. 1 .
27 . The method of claim 17 , wherein the pharmaceutical composition comprises filgotinib maleate Form I characterized by a differential scanning calorimetry (DSC) curve substantially the same as shown in FIG. 2 .
28 . The method of claim 17 , wherein the pharmaceutical composition comprises filgotinib maleate Form I characterized by thermogravimetric analysis (TGA) comprising a thermogram substantially the same as shown in FIG. 2 .
29 . The method of claim 17 , wherein the pharmaceutical composition comprises filgotinib maleate Form I characterized by a proton nuclear magnetic resonance spectrum ( 1 H NMR) substantially the same as shown in FIG. 3 .
30 . The method of claim 17 , wherein the pharmaceutical composition comprises filgotinib maleate Form I characterized by an XRPD pattern comprising peaks at 28.9, 16.4, 8.2, 18.9, 20.0, 11.9, 14.9, 18.1, 20.5, and 22.6° 2θ±0.2° 2θ as determined on a diffractometer using Cu-Kα radiation.