Claims for Patent: 12,178,816

Summary for Patent: 12,178,816

Title:	Immediate release pharmaceutical formulation of 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one
Abstract:	The present invention relates to a pharmaceutical formulation comprising the drug 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one in a solid dispersion with a matrix polymer that exhibits low hygroscopicity and high softening temperature, such as copovidone. The invention also relates to a daily pharmaceutical dose of the drug provided by such a formulation. In addition, the invention relates to the use of a matrix polymer that exhibits low hygroscopicity and high softening temperature in solid dispersion with 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one for increasing the bioavailability of the drug.
Inventor(s):	Michael Karl Bechtold, Julie Kay Cahill, Katja Maren Fastnacht, Kieran James Lennon, Bernd Harald Liepold, Claudia Bettina Packhaeuser, Benedikt Steitz
Assignee:	AstraZeneca UK Ltd , Kudos Pharmaceuticals Ltd
Application Number:	US18/785,063
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 12,178,816
Patent Claims:	1. An immediate-release pharmaceutical composition in the form of a tablet comprising: (a) an extrudate comprising: (i) 100 mg to 200 mg of 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluorobenzyl]-2H-phthalazin-1-one (Compound 1); (ii) at least one polymer chosen from copovidone, povidone, hypromellose phthalate, hypromellose acetate succinate, 2-hydroxypropyl-β-cyclodextrin, hypromellose, polymethacrylates, hydroxypropyl cellulose, and cellulose acetate phthalate; and (iii) at least one glidant; and (b) at least one excipient; wherein the weight ratio of Compound 1 to the at least one polymer in the extrudate is in the range of from 1:1 to 1:9; and wherein the total concentration of Compound 1 in the tablet is in the range of from 10% by weight to 35% by weight. 2. The composition of claim 1, wherein the at least one polymer is chosen from copovidone and povidone. 3. The composition of claim 1, wherein the at least one polymer is a combination of copovidone and povidone. 4. The composition of claim 1, wherein the total concentration of Compound 1 in the extrudate is in the range of from 25% by weight to 50% by weight. 5. The composition of claim 4, wherein the at least one polymer is chosen from copovidone and povidone. 6. The composition of claim 4, wherein the at least one polymer is a combination of copovidone and povidone. 7. The composition of claim 1, wherein the total concentration of the at least one polymer in the extrudate is in the range of from 50% by weight to 75% by weight. 8. The composition of claim 7, wherein the at least one polymer is chosen from copovidone and povidone. 9. The composition of claim 7, wherein the at least one polymer is a combination of copovidone and povidone. 10. The composition of claim 1, wherein the total concentration of Compound 1 in the extrudate is in the range of from 25% by weight to 50% by weight; and wherein the total concentration of the at least one polymer in the extrudate is in the range of from 50% by weight to 75% by weight. 11. The composition of claim 10, wherein the at least one polymer is chosen from copovidone and povidone. 12. The composition of claim 10, wherein the at least one polymer is a combination of copovidone and povidone. 13. The composition of claim 1, wherein the at least one glidant is colloidal silicon dioxide. 14. The composition of claim 13, wherein the at least one polymer is chosen from copovidone and povidone. 15. The composition of claim 14, wherein the at least one polymer is a combination of copovidone and povidone. 16. The composition of claim 1, wherein the total concentration of Compound 1 in the extrudate is in the range of from 25% by weight to 50% by weight; wherein the total concentration of the at least one polymer in the extrudate is in the range of from 50% by weight to 75% by weight; and wherein the at least one glidant is colloidal silicon dioxide. 17. The composition of claim 16, wherein the at least one polymer is chosen from copovidone and povidone. 18. The composition of claim 16, wherein the at least one polymer is a combination of copovidone and povidone. 19. The composition of claim 1, wherein the at least one excipient is chosen from at least one soluble filler and at least one lubricant. 20. The composition of claim 19, wherein the at least one polymer is chosen from copovidone and povidone. 21. The composition of claim 19, wherein the at least one polymer is a combination of copovidone and povidone. 22. The composition of claim 1, wherein the total concentration of Compound 1 in the extrudate is in the range of from 25% by weight to 50% by weight; wherein the total concentration of the at least one polymer in the extrudate is in the range of from 50% by weight to 75% by weight; wherein the at least one glidant is colloidal silicon dioxide; and wherein the at least one excipient is chosen from at least one soluble filler and at least one lubricant. 23. The composition of claim 22, wherein the at least one polymer is chosen from copovidone and povidone. 24. The composition of claim 23, wherein the at least one polymer is a combination of copovidone and povidone. 25. The composition of claim 1, wherein the weight ratio of Compound 1 to the at least one polymer in the extrudate is in the range of from 1:1 to 1:4. 26. The composition of claim 25, wherein the at least one polymer is chosen from copovidone and povidone. 27. The composition of claim 26, wherein the at least one polymer is a combination of copovidone and povidone. 28. The composition of claim 1, wherein the weight ratio of Compound 1 to the at least one polymer in the extrudate is in the range of from 1:1 to 1:4; wherein the at least one glidant is colloidal silicon dioxide; and wherein the at least one excipient is chosen from at least one soluble filler and at least one lubricant. 29. The composition of claim 28, wherein the at least one polymer is chosen from copovidone and povidone. 30. The composition of claim 28, wherein the at least one polymer is a combination of copovidone and povidone.