Claims for Patent: 12,144,810
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Summary for Patent: 12,144,810
| 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: | US18/785,092 |
| Patent Claims: |
1. An immediate-release pharmaceutical composition in the form of a tablet comprising: a solid dispersion comprising: (i) 100 mg to 200 mg of 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluorobenzyl]-2H-phthalazin-1-one (Compound 1); and (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; wherein the weight ratio of Compound 1 to the at least one polymer in the solid dispersion is in the range of from 1:1 to 1:9; wherein the total concentration of Compound 1 in the tablet is in the range of from 10% by weight to 50% by weight; and wherein the hardness of the tablet is greater than or equal to 25 N. 2. The composition of claim 1, wherein the total concentration of Compound 1 in the tablet is in the range of from 10% by weight to 35% by weight. 3. The composition of claim 2, wherein the hardness of the tablet is in the range of from 80 N to 100 N. 4. The composition of claim 1, wherein the weight ratio of Compound 1 to the at least one polymer in the solid dispersion is in the range of from 1:1 to 1:4. 5. The composition of claim 4, wherein the hardness of the tablet is in the range of from 80 N to 100 N. 6. The composition of claim 4, wherein the weight ratio of Compound 1 to the at least one polymer in the solid dispersion is in the range of from 1:2 to 1:4. 7. The composition of claim 1, wherein the total concentration of Compound 1 in the tablet is in the range of from 10% by weight to 35% by weight; and wherein the weight ratio of Compound 1 to the at least one polymer in the solid dispersion is in the range of from 1:1 to 1:4. 8. The composition of claim 7, wherein the hardness of the tablet is in the range of from 80 N to 100 N. 9. The composition of claim 1, wherein the at least one polymer is chosen from povidone and copovidone. 10. The composition of claim 9, wherein the hardness of the tablet is in the range of from 80 N to 100 N. 11. The composition of claim 9, wherein the at least one polymer is copovidone. 12. The composition of claim 1, wherein the total concentration of Compound 1 in the tablet is in the range of from 10% by weight to 35% by weight; wherein the weight ratio of Compound 1 to the at least one polymer in the solid dispersion is in the range of from 1:1 to 1:4; and wherein the at least one polymer is chosen from povidone and copovidone. 13. The composition of claim 12, wherein the hardness of the tablet is in the range of from 80 N to 100 N. 14. The composition of claim 1, wherein the total concentration of the at least one polymer in the solid dispersion is in the range of from 50% by weight to 75% by weight. 15. The composition of claim 14, wherein the hardness of the tablet is in the range of from 80 N to 100 N. 16. The composition of claim 1, wherein the total concentration of Compound 1 in the solid dispersion is in the range of from 25% by weight to 50% by weight. 17. The composition of claim 16, wherein the hardness of the tablet is in the range of from 80 N to 100 N. 18. The composition of claim 16, wherein the total concentration of Compound 1 in the solid dispersion is 25% by weight. 19. The composition of claim 1, wherein the composition further comprises at least one glidant. 20. The composition of claim 19, wherein the hardness of the tablet is in the range of from 80 N to 100 N. 21. The composition of claim 19, wherein the at least one glidant is colloidal silicon dioxide. 22. The composition of claim 1, wherein the composition further comprises at least one soluble filler. 23. The composition of claim 22, wherein the hardness of the tablet is in the range of from 80 N to 100 N. 24. The composition of claim 22, wherein the at least one soluble filler is mannitol. 25. The composition of claim 1, wherein the composition further comprises at least one lubricant. 26. The composition of claim 25, wherein the hardness of the tablet is in the range of from 80 N to 100 N. 27. The composition of claim 25, wherein the at least one lubricant is sodium stearyl fumarate. 28. The composition of claim 1, wherein the total concentration of Compound 1 in the tablet is in the range of from 10% by weight to 35% by weight; wherein the weight ratio of Compound 1 to the at least one polymer in the solid dispersion is in the range of from 1:1 to 1:4; wherein the at least one polymer is chosen from povidone and copovidone; and wherein the composition further comprises at least one glidant, at least one soluble filler, and/or at least one lubricant. 29. The composition of claim 28, wherein the hardness of the tablet is in the range of from 80 N to 100 N. 30. The composition of claim 28, wherein the at least one glidant if present is colloidal silicon dioxide, the at least one soluble filler if present is mannitol, and the at least one lubricant if present is sodium stearyl fumarate. |
