IP Library Patent Application 16154038
Patent Application
App. No. 16/154,038

High Dosage Strength Tablets of Rucaparib

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Quick Facts
Patent No.
US None
App. No.
16/154,038
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 (37)

1 - 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.

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 26, 2023
From: CLOVIS ONCOLOGY, INC.
To: PHARMA& SCHWEIZ GMBH
Reel/Frame 063773/0353 →
SECURITY INTEREST Recorded May 6, 2019
From: CLOVIS ONCOLOGY, INC.
To: TOP IV SPV GP, LLC
Reel/Frame 049088/0950 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 8, 2018
From: ETTER, JEFFREY
To: CLOVIS ONCOLOGY, INC.
Reel/Frame 047092/0903 →