Claims for Patent: 11,633,396

Summary for Patent: 11,633,396

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:	Kudos Pharmaceuticals Ltd
Application Number:	US17/821,833
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 11,633,396
Patent Claims:	1. An immediate-release pharmaceutical composition comprising: a core composition comprising a solid dispersion comprising (i) 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one (Compound 1); and (ii) at least one matrix polymer, wherein one of said at least one matrix polymers is copovidone; and wherein the total concentration of Compound 1 in the core composition is in the range of from 10% by weight to 40% by weight; wherein the weight ratio of Compound 1 to copovidone in the core composition is in the range of from 1:1 to 1:4. 2. The composition of claim 1, wherein Compound 1 is in an amorphous form. 3. The composition of claim 1, wherein at least 90% of Compound 1 is in an amorphous form. 4. The composition of claim 1, wherein the core composition is made by solvent evaporation or melt extrusion. 5. The composition of claim 4, wherein the core composition is made by melt extrusion. 6. The composition of claim 1, wherein the total concentration of Compound 1 in the core composition is in the range of from 15% by weight to 30% by weight. 7. The composition of claim 1, wherein the total amount of Compound 1 in the core composition is in the range of from 25 mg to 400 mg. 8. The composition of claim 7, wherein the core composition comprises 100 mg of Compound 1. 9. The composition of claim 7, wherein the core composition comprises 150 mg of Compound 1. 10. The composition of claim 1, wherein the pharmaceutical composition further comprises at least one glidant. 11. The composition of claim 10, wherein the at least one glidant is colloidal silicon dioxide. 12. The composition of claim 10, wherein the solid dispersion further comprises at least one glidant. 13. The composition of claim 1, wherein the solid dispersion further comprises at least one matrix polymer chosen from povidone, hypromellose phthalate, hypromellose acetate succinate, 2-hydroxypropyl-β-cyclodextrin, hypromellose, polymethacrylates, hydroxypropyl cellulose, and cellulose acetate phthalate. 14. The composition of claim 1, wherein the pharmaceutical composition further comprises at least one filler. 15. The composition of claim 14, wherein at least one filler is mannitol. 16. The composition of claim 1, wherein the pharmaceutical composition further comprises at least one lubricant. 17. The composition of claim 16, wherein at least one lubricant is sodium stearyl fumarate. 18. The composition of claim 1, wherein the pharmaceutical composition further comprises colloidal silicon dioxide, mannitol, and sodium stearyl fumarate. 19. An immediate-release pharmaceutical composition comprising: a core composition comprising a solid dispersion comprising (i) at least one active agent chosen from 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one (Compound 1), pharmaceutically acceptable salts thereof, and solvates thereof; and (ii) at least one matrix polymer, wherein one of said at least one matrix polymers is copovidone; and wherein the total concentration of Compound 1 in the core composition is in the range of from 10% by weight to 40% by weight; wherein the weight ratio of Compound 1 to copovidone in the core composition is in the range of from 1:1 to 1:9. 20. The composition of claim 19, wherein the weight ratio of Compound 1 to copovidone in the core composition is in the range of from 1:1 to 1:4. 21. The composition of claim 19, wherein the total concentration of Compound 1 in the core composition is in the range of from 15% by weight to 30% by weight. 22. The composition of claim 19, wherein the core composition comprises 100 mg of Compound 1. 23. The composition of claim 19, wherein the core composition comprises 150 mg of Compound 1. 24. An immediate-release pharmaceutical composition comprising: a core composition comprising a solid dispersion comprising 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one (Compound 1) and copovidone; wherein the total concentration of Compound 1 in the core composition is 25% by weight; and wherein the weight ratio of Compound 1 to copovidone in the core composition is 1:2.3. 25. The composition of claim 24, wherein the pharmaceutical composition further comprises at least one glidant, at least one filler, and at least one lubricant. 26. The composition of claim 24, wherein the pharmaceutical composition further comprises colloidal silicon dioxide, mannitol, and sodium stearyl fumarate. 27. The composition of claim 24, wherein the pharmaceutical composition further comprises 1.8% by weight colloidal silicon dioxide, 14.7% by weight mannitol, and 1% by weight sodium stearyl fumarate. 28. The composition of claim 24, wherein the core composition comprises 100 mg of Compound 1. 29. The composition of claim 24, wherein the core composition comprises 150 mg of Compound 1. 30. The composition of claim 24, wherein at least 90% of Compound 1 is in an amorphous form.