US2019099430A1PendingUtilityA1
High Dosage Strength Tablets of Rucaparib
Est. expiryAug 22, 2034(~8.1 yrs left)· nominal 20-yr term from priority
Inventors:Jeffrey B. Etter
A61P 35/00A61K 9/2009A61K 9/2059A61K 31/185A61K 9/2054A61K 31/55A61K 9/2013
55
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Claims
Abstract
A tablet including high dosage of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one camsylate salt has been disclosed.
Claims
exact text as granted — not AI-modified1 - 14 . (canceled)
15 . A tablet comprising the active pharmaceutical ingredient compound 8-fluoro-2-{4-[(methylamino) methyl] phenyl}-1, 3, 4, 5-tetrahydro-6H-azepino [5,4,3-cd] indol-6-one camsylate, wherein said compound is present in an amount that the tablet contains at least about 200 mg of 8-fluoro-2-{4-[(methylamino) methyl] phenyl}-1, 3, 4, 5-tetrahydro-6H-azepino [5,4,3-cd] indol-6-one, wherein at least 95% w/w of the active pharmaceutical ingredient is released within 60 min, when tested in 0.01N HCl according to USP II Paddles and at 75 rpm.
16 . The tablet according to claim 15 , wherein at least 95% w/w of the active pharmaceutical ingredient is released within 30 min, when tested in 0.01N HCl according to USP II Paddles and at 75 rpm.
17 . The tablet according to claim 15 , wherein at least 95% w/w of the active pharmaceutical ingredient is released within 15 min, when tested in 0.01N HCl according to USP II Paddles and at 75 rpm.
18 . The tablet according to claim 15 , wherein at least 95% w/w of the active pharmaceutical ingredient is released within 10 min, when tested in 0.01N HCl according to USP II Paddles and at 75 rpm.
19 . The tablet of claim 15 , wherein the tablet comprises at least about 250 mg of 8-fluoro-2-{4-[(methylamino) methyl] phenyl}-1, 3, 4, 5-tetrahydro-6H-azepino [5,4,3-cd] indol-6-one.
20 . The tablet of claim 15 , wherein the tablet comprises at least about 300 mg of 8-fluoro-2-{4-[(methylamino) methyl] phenyl}-1, 3, 4, 5-tetrahydro-6H-azepino [5,4,3-cd] indol-6-one.
21 . The tablet of claim 15 , wherein the tablet comprises at least about 350 mg of 8-fluoro-2-{4-[(methylamino) methyl] phenyl}-1, 3, 4, 5-tetrahydro-6H-azepino [5,4,3-cd] indol-6-one.
22 . The tablet of claim 15 further comprising a filler.
23 . The tablet of claim 22 , wherein the tablet comprises 5-50% w/w of the filler.
24 . The tablet of claim 22 , wherein the filler is microcrystalline cellulose.
25 . The tablet of claim 15 further comprising a disintegrant.
26 . The tablet of claim 25 , wherein the tablet comprises 1-20% w/w of the disintegrant.
27 . The tablet of claim 25 , wherein the disintegrant is sodium starch glycolate.
28 . The tablet of claim 15 , further comprising a lubricant.
29 . The tablet of claim 28 , wherein the tablet comprises 0.20-2.5% w/w of the lubricant.
30 . The tablet of claim 28 , wherein the lubricant is magnesium stearate.
31 . The tablet of claim 15 further comprising a glidant.
32 . The tablet of claim 31 , wherein the tablet comprises up to 1% w/w of the glidant.
33 . The tablet of claim 31 , wherein the glidant is colloidal silicon dioxide.
34 . A tablet comprising the active pharmaceutical ingredient 8-fluoro-2-{4-[(methylamino) methyl] phenyl}-1, 3, 4, 5-tetrahydro-6H-azepino [5,4,3-cd] indol-6-one camsylate, wherein said compound is present in an amount that the tablet contains at least about 200 mg of 8-fluoro-2-{4-[(methylamino) methyl] phenyl}-1, 3, 4, 5-tetrahydro-6H-azepino [5,4,3-cd] indol-6-one, wherein the tablet can be compressed to a tensile strength of at least 2 MPa at a compression stress less than 250 MPa.
35 . The tablet of claim 34 , wherein the tablet can be compressed to a tensile strength of at least 2 MPa at a compression stress less than 150 MPa.
36 . The tablet of claim 34 , wherein the tablet comprises at least about 250 mg of 8-fluoro-2-{4-[(methylamino) methyl] phenyl}-1, 3, 4, 5-tetrahydro-6H-azepino [5,4,3-cd] indol-6-one.
37 . The tablet of claim 34 , wherein the tablet comprises at least about 300 mg of 8-fluoro-2-{4-[(methylamino) methyl] phenyl}-1, 3, 4, 5-tetrahydro-6H-azepino [5,4,3-cd] indol-6-one.
38 . The tablet of claim 34 , wherein the tablet comprises at least about 350 mg of 8-fluoro-2-{4-[(methylamino) methyl] phenyl}-1, 3, 4, 5-tetrahydro-6H-azepino [5,4,3-cd] indol-6-one.
39 . The tablet of claim 34 further comprising a filler.
40 . The tablet of claim 39 , wherein the tablet comprises 5-50% w/w of the filler.
41 . The tablet of claim 39 , wherein the filler is microcrystalline cellulose.
42 . The tablet of claim 34 further comprising a disintegrant.
43 . The tablet of claim 42 , wherein the tablet comprises 1-20% w/w of the disintegrant.
44 . The tablet of claim 42 , wherein the disintegrant is sodium starch glycolate.
45 . The tablet of claim 34 , further comprising a lubricant.
46 . The tablet of claim 45 , wherein the tablet comprises 0.20-2.5% w/w of the lubricant.
47 . The tablet of claim 45 , wherein the lubricant is magnesium stearate.
48 . The tablet of claim 34 further comprising a glidant.
49 . The tablet of claim 48 , wherein the tablet comprises up to 1% w/w of the glidant.
50 . The tablet of claim 48 , wherein the glidant is colloidal silicon dioxide.Cited by (0)
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