RIBOCICLIB TABLET

• US 20180071292A1
• Filed: 04/14/2016
• Published: 03/15/2018
• Est. Priority Date: 04/16/2015
• Status: Active Grant

• Current Assignee: Novartis Pharmaceuticals Corporation (Novartis Ag)
• Original Assignee: Bindhumadhavan Gururajan
• Inventors: Gururajan, Bindhumadhavan, Grandeury, Arnaud, Costa, Rui
• Granted Patent: US 10,799,506 B2
• Time in Patent Office: Days
• CPC Class Codes: A61K 31/496 Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
• CPC Class Codes: A61K 31/519 ortho- or peri-condensed with heterocyclic rings
• CPC Class Codes: A61K 9/2027 obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
• CPC Class Codes: A61K 9/2054 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61K 9/2077 Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
• CPC Class Codes: A61K 9/284 obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone
• CPC Class Codes: A61P 35/00 Antineoplastic agents
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Abstract

The present disclosure is directed to oral tablet of ribociclib including its salt(s). One embodiment of the present disclosure is directed to tablet of ribociclib with high drug load with an immediate release profile. One embodiment of the present disclosure is directed to coated tablet of ribociclib. Another embodiment of the present disclosure is directed to coated tablet of ribociclib where the coating is an advanced moisture barrier coating (e.g., Opadry® amb II coating where the coating is PVA based).

Claims

1. A pharmaceutical oral tablet comprising ribociclib or its pharmaceutically acceptable salt.

2. The tablet of claim 1 comprising ribociclib succinate.

3. The tablet of claim 1 comprising ribociclib or its salt wherein the tablet releases at least 75% of the ribociclib or its salt after 45 minutes when tested with the rotating basket at 100 rpm with 900 ml of dissolution media pH 2 or pH4.5, at 37°

C., according to USP <

711>

.

4. The tablet of claim 1 comprising ribociclib or its salt in a tablet core wherein the tablet core comprises at least 32% (w/w) of ribociclib measured in terms of ribociclib free base.

5. The tablet of claim 4 wherein the % of ribociclib (w/w) is at least 40% of the tablet core.

6. The tablet of claim 5 wherein the % of ribociclib (w/w) is at least 44% of the tablet core.

7. The tablet of claim 6, wherein the % of ribociclib (w/w) is at about 44% to 52% of the tablet core.

8. The tablet of claim 4 wherein the % of ribociclib (w/w) is at about 47% of the tablet core.

9. A pharmaceutical oral tablet comprising ribociclib succinate, wherein the % of ribociclib succinate (w/w) is at least 40% of the tablet core.

10. The tablet of claim 9 wherein the % of ribociclib succinate (w/w) is at least 50% of the tablet core.

11. The tablet of claim 10 wherein the % of ribociclib succinate (w/w) is at least 55% of the tablet core.

12. The tablet of claim 11, wherein the % of ribociclib succinate (w/w) is at about 55% to 65% of the tablet core.

13. The tablet of claim 9 wherein the % of ribociclib (w/w) is at about 60% of the tablet core.

14. A coated pharmaceutical oral tablet comprising ribociclib or its pharmaceutically acceptable salt wherein the coating comprises polyvinyl alcohol (PVA).

15. A coated pharmaceutical oral tablet comprising ribociclib succinate wherein the coating comprises PVA.

16. A coated pharmaceutical oral tablet comprising ribociclib or its salt wherein the tablet releases at least 75% of the ribociclib or its salt after 45 minutes when tested with the rotating basket at 100 rpm with 900 ml of dissolution media pH 2 or pH4.5, at 37°

C., according to USP <

711> and

wherein the coating comprises PVA.

17. A coated pharmaceutical oral tablet comprising ribociclib or its salt wherein, measured in terms of ribociclib free base, the % of ribociclib (w/w) is at least 32% of the tablet core, and wherein the coating comprises PVA.

18. The tablet of claim 17 wherein the % of ribociclib (w/w) is at least 40% of the tablet core.

19. The tablet of claim 18 wherein the % of ribociclib (w/w) is at least 44% of the tablet core.

20. The tablet of claim 19, wherein the % of ribociclib (w/w) is at about 44% to 52% of the tablet core.

21. The tablet of claim 17 wherein the % of ribociclib (w/w) is at about 47% of the tablet core.

22. A coated pharmaceutical oral tablet comprising ribociclib succinate, wherein the % of ribociclib succinate (w/w) is at least 40% of the tablet core.

23. The tablet of claim 22 wherein the % of ribociclib succinate (w/w) is at least 50% of the tablet core.

24. The tablet of claim 23 wherein the % of ribociclib succinate (w/w) is at least 55% of the tablet core.

25. The tablet of claim 24, wherein the % of ribociclib succinate (w/w) is at about 55% to 65% of the tablet core.

26. The tablet of claim 22 wherein the % of ribociclib (w/w) is at about 60% of the tablet core.