Solid dosage forms of palbociclib
The present invention relates to solid dosage forms of palbociclib comprising a water-soluble acid. The dosage forms described herein have desirable pharmacokinetic characteristics.
1. A tablet consisting of about 20 wt % of palbociclib, about 10 wt % of succinic acid, about 50 wt % to about 75 wt % of microcrystalline cellulose, about 5 wt % to about 10 wt % of crospovidone, about 0.5 wt % to about 6 wt % of magnesium stearate, and about 0.5 wt % to about 2 wt % of silicon dioxide.
2. The tablet of claim 1 , wherein the tablet is film coated.
3. The tablet of claim 1 , wherein the amount of palbociclib in the tablet is 25 mg, 75 mg, 100 mg or 125 mg.
4. The tablet of claim 3 , wherein the amount of palbociclib in the tablet is 125 mg.
5. A tablet consisting of: (i) as intragranular components, about 20 wt % of palbociclib, about 39.2 wt % of microcrystalline cellulose, about 1 wt % of silicon dioxide, about 3 wt % of crospovidone, and about 0.3 wt % of magnesium stearate; and (ii) as extragranular components, about 10 wt % of succinic acid, about 21.5 wt % of microcrystalline cellulose, about 3 wt % of crospovidone, and about 2 wt % of magnesium stearate.
6. The tablet of claim 5 , comprising 25.0 mg, 75.0 mg, 100.0 mg or 125.0 mg of palbociclib.
7. The tablet of claim 6 , wherein the tablet is film coated to a weight gain of about 2% to about 4%.
8. A tablet consisting of:
(i) intragranular components:
palbociclib
125.000
mg
microcrystalline cellulose (Avicel PH102)
244.812
mg
colloidal silicon dioxide (Aerosil 200 Pharma)
6.250
mg
crospovidone (Kollidon CL)
18.750
mg
magnesium stearate
2.063
mg
and
(ii) extragranular components:
succinic acid (100 to 350 micron)
62.500
mg
microcrystalline Cellulose (Avicel PH200)
134.375
mg
crospovidone (Kollidon CL-SF)
18.750
mg
magnesium stearate (fine grade)
12.500
mg.
9. The tablet of claim 8 , wherein the tablet is film coated to a weight gain of 4% with a film coating.