Claims for Patent: 12,016,927

Summary for Patent: 12,016,927

Title:	Injectable preparation
Abstract:	An object of the present invention is to provide a storage-stable injectable preparation comprising a composition comprising a poorly soluble drug as an active ingredient and a dispersion medium. Another object of the present invention is to provide a compact, lightweight prefilled syringe by filling a syringe with the injectable preparation. The present invention provides an injectable preparation comprising a composition comprising a poorly soluble drug, a dispersion medium, and a specific suspending agent, the composition having a viscosity of 40 pascal-seconds or more in at least one point in the shear rate range of 0.01 to 0.02 s−1 end having a viscosity of 0.2 pascal-seconds or less in at least one point in the shear rate range of 900 to 1.000 s−1, as measured.
Inventor(s):	Daiki Kaneko, Takakuni Matsuda, Yusuke Hoshika
Assignee:	Otsuka Pharmaceutical Co Ltd
Application Number:	US18/148,860
Patent Claims:	1. A gel composition comprising: aripiprazole or a salt thereof, water, and polyvinylpyrrolidone with a K value ranging from 12 to 30, wherein a concentration of the polyvinylpyrrolidone ranges from 0.1 mg/mL to 100 mg/mL, and the aripiprazole or a salt thereof has a mean primary particle diameter ranging from 0.5 μm to 30 μm, and a concentration of the aripiprazole or a salt thereof ranges from 200 mg/mL to 600 mg/mL, which is calculated as an anhydrate. 2. The gel composition according to claim 1, wherein K value of the polyvinylpyrrolidone ranges from 12 to 20. 3. The gel composition according to claim 2, wherein K value of the polyvinylpyrrolidone is 17. 4. The gel composition according to claim 1, further comprising polyethylene glycol. 5. The gel composition according to claim 1, further comprising polyethylene glycol and carboxymethyl cellulose or a salt thereof. 6. The gel composition according to claim 5, wherein a concentration of the polyethylene glycol ranges from 0.1 mg/mL to 100 mg/mL, and a concentration of the carboxymethyl cellulose or a salt thereof ranges from 0.5 mg/mL to 50 mg/m L. 7. The gel composition according to claim 6, wherein the concentration of the polyvinylpyrrolidone ranges from 2 mg/mL to 20 mg/mL, the concentration of the polyethylene glycol ranges from 0.1 mg/mL to 50 mg/mL, and the concentration of the carboxymethyl cellulose or a salt thereof ranges from 2 mg/mL to 20 mg/m L. 8. The gel composition according to claim 5, wherein the polyethylene glycol is polyethylene glycol 4000, and the concentration of the polyethylene glycol ranges from 0.1 mg/mL to 40 mg/m L. 9. The gel composition according to claim 1, wherein the concentration of the aripiprazole or salt thereof ranges from 250 mg/mL to 450 mg/m L. 10. The gel composition according to claim 1, wherein the aripiprazole or a salt thereof is a monohydrate of aripiprazole or a salt thereof. 11. The gel composition according to claim 1, wherein the mean primary particle diameter ranges from 1 μm to 10 μm. 12. The gel composition according to claim 11, wherein the mean primary particle diameter ranges from 2 μm to 7 μm. 13. The gel composition according to claim 1, wherein the aripiprazole or a salt thereof has a mean secondary particle diameter up to but not exceeding three times the mean primary particle diameter thereof. 14. The gel composition according to claim 1, wherein the composition has a viscosity of 40 Pa·s or more in at least one point in a shear rate ranging from 0.01 s−1 to 0.02 s−1 and viscosity of 0.2 Pa·s or less in at least one point in a shear rate ranging from 900 s−1 to 1,000 s−1, as measured by a rheometer at 25° C. 15. The gel composition according to claim 1, wherein the composition is disposed within a prefilled syringe in gel form for storage and forms a sol when subjected to an impact. 16. The gel composition according to claim 1, wherein the composition is administered once every two to three months. 17. A method for treating schizophrenia, bipolar disorder, or depression, the method comprising administering the gel composition according to claim 1 to a patient in need thereof. 18. A method for treating schizophrenia, bipolar disorder, or depression in a subject in need thereof, comprising administering a pharmaceutical composition, wherein the method comprising preparing the pharmaceutical composition comprising; aripiprazole or a salt thereof, water, and polyvinylpyrrolidone, wherein a K value of the polyvinylpyrrolidone ranges from 12 to 30, a concentration of the polyvinylpyrrolidone ranges from 0.1 mg/mL to 100 mg/mL, the aripiprazole or a salt thereof has a mean primary particle diameter of ranging from 0.5 μm to 30 μm, and a concentration of the aripiprazole or a salt thereof ranges from 200 mg/mL to 600 mg/mL, which is calculated as an anhydrate. 19. The method according to claim 18, wherein the pharmaceutical composition is an injectable preparation in a gel form for storage and forms a sol when subjected to an impact. 20. The method according to claim 19, wherein the pharmaceutical composition is an injectable preparation in a gel form for storage and is administered to a patient in need thereof in a sol form. 21. The method according to claim 19, wherein the pharmaceutical composition is administered once every two months. 22. The method according to claim 20, wherein the pharmaceutical composition is administered once every two months. 23. The method according to claim 21, wherein the pharmaceutical composition is administered intramuscularly. 24. The method according to claim 22, wherein the pharmaceutical composition is administered intramuscularly. 25. A pharmaceutical composition comprising: aripiprazole or a salt thereof, water, polyvinylpyrrolidone with a K value ranging from 12 to 20, carboxymethyl cellulose or a salt thereof with a concentration ranging from 2 mg/mL to 20 mg/mL, and polyethylene glycol with a concentration ranging from 0.1 mg/mL to 50 mg/mL, wherein a concentration of the polyvinylpyrrolidone ranges from 0.1 mg/mL to 50 mg/mL, the aripiprazole or a salt thereof has a mean primary particle diameter ranging from 1 μm to 10 μm and a concentration of the aripiprazole or a salt thereof ranges from 250 mg/mL to 450 mg/mL, which is calculated as an anhydrate, and wherein the pharmaceutical composition is disposed within a container in gel form for storage and changes to a sol when subjected to an impact, and the pharmaceutical composition is administered once every two months. 26. The pharmaceutical composition according to claim 25, wherein K value of polyvinylpyrrolidone is 17. 27. The pharmaceutical composition according to claim 25, wherein the polyethylene glycol is polyethylene glycol 400, and the polyethylene glycol 400, and a concentration of the polyethylene glycol ranges from 0.5 mg/mL to 5 mg/m L. 28. The pharmaceutical composition according to claim 25, wherein the polyethylene glycol is polyethylene glycol 4000, and the polyethylene glycol 4000, and a concentration of the polyethylene glycol ranges from 0.1 mg/mL to 40 mg/m L. 29. A method for treating schizophrenia, bipolar disorder, or depression in a subject in need thereof, comprising administering a pharmaceutical composition, wherein the pharmaceutical composition comprises; aripiprazole or a salt thereof, water, polyvinylpyrrolidone with a K value ranging from 12 to 20, carboxymethyl cellulose or a salt thereof with a concentration ranging from 2 mg/mL to 20 mg/mL, and polyethylene glycol with a concentration ranging from 0.1 mg/mL to 50 mg/mL, wherein a concentration of the polyvinylpyrrolidone ranges from 0.1 mg/mL to 50 mg/mL, the aripiprazole or a salt thereof has a mean primary particle diameter ranging from 1 μm to 10 μm, and a concentration of the aripiprazole or a salt thereof ranges from 250 mg/mL to 450 mg/mL, which is calculated as an anhydrate, and wherein the pharmaceutical composition changes to a sol when subjected to an impact, and the pharmaceutical composition is administered once every two months. 30. The method according to claim 29, wherein the pharmaceutical composition is administered intramuscularly. 31. A gel composition comprising: aripiprazole monohydrate or a salt thereof, water, polyvinylpyrrolidone with a K value ranging from 12 to 20, carboxymethyl cellulose or a salt thereof with a concentration ranging from 2 mg/mL to 20 mg/mL, and polyethylene glycol with a concentration ranging from 0.1 mg/mL to 50 mg/mL, wherein a concentration of the polyvinylpyrrolidone ranges from 0.1 mg/mL to 50 mg/mL, the aripiprazole monohydrate or a salt thereof has a mean primary particle diameter ranging from 0.5 μm to 30 μm, and a concentration of the aripiprazole monohydrate or a salt thereof ranges from 208 mg/mL to 416 mg/m L. 32. The gel composition according to claim 31, wherein K value of the polyvinylpyrrolidone is 17. 33. The gel composition according to claim 31, wherein the polyethylene glycol is polyethylene glycol 400, and the concentration of the polyethylene glycol ranges from 0.5 mg/mL to 5 mg/mL. 34. The gel composition according to claim 31, wherein the polyethylene glycol is polyethylene glycol 4000, and the concentration of the polyethylene glycol ranges from 0.1 mg/mL to 40 mg/m L. 35. A method for treating schizophrenia, bipolar disorder, or depression in a subject in need thereof, comprising administering a pharmaceutical composition, wherein the pharmaceutical composition comprises: aripiprazole monohydrate or a salt thereof, water, polyvinylpyrrolidone with a K value ranging from 12 to 20, carboxymethyl cellulose or a salt thereof with a concentration of the carboxymethyl cellulose or a salt thereof ranges from 2 mg/mL to 20 mg/mL, and polyethylene glycol with a concentration of the polyethylene glycol ranges from 0.1 mg/m L to 50 mg/mL, wherein a concentration of the polyvinylpyrrolidone ranges from 0.1 mg/mL to 50 mg/mL, the aripiprazole monohydrate or a salt thereof has a mean primary particle diameter ranging from 0.5 μm to 30 μm, and a concentration of the aripiprazole monohydrate or a salt thereof ranges from 208 mg/mL to 416 mg/m L. 36. The method according to claim 35, wherein the pharmaceutical composition is an injectable preparation in a gel form for storage and forms a sol when subjected to an impact, and the composition is administered once every two months. 37. The method according to claim 35, wherein the pharmaceutical composition is administered intramuscularly. 38. The gel composition according to claim 5, wherein the polyethylene glycol is polyethylene glycol 400, and the concentration of the polyethylene glycol ranges from 0.5 mg/mL to 5 mg/mL.