Claims for Patent: 11,097,007

Summary for Patent: 11,097,007

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 and 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:	US17/108,939
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 11,097,007
Patent Claims:	1. An injectable preparation comprising a composition comprising a poorly soluble drug, a dispersion medium, and a suspending agent, the suspending agent containing polyvinylpyrrolidone, the composition having a viscosity of 40 Pa·s or more in at least one point in the shear rate range of 0.01 to 0.02 s−1 and having a viscosity of 0.2 Pa·s or less in at least one point in the shear rate range of 900 to 1,000 s−1, as measured by a rheometer at 5° C., 25° C. or 40° C., wherein the poorly soluble drug is aripiprazole or a salt thereof, or 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or a salt thereof, the poorly soluble drug has a mean primary particle diameter of 30 μm or less and is contained in a concentration of 200 to 600 mg/mL, and K value of polyvinylpyrrolidone is 12 to 30, and the concentration of polyvinylpyrrolidone is 0.1 to 100 mg/mL. 2. The injectable preparation according to claim 1, wherein the composition has a viscosity of 40 Pa·s or more in at least one point in the shear rate range of 0.01 to0.02 s−1 and having a viscosity of 0.2 Pa·s or less in at least one point in the shear rate range of 900 to 1,000 s−1, as measured by a rheometer at 25° C. 3. The injectable preparation according to claim 1 comprising a composition comprising at least water as a dispersion medium. 4. The injectable preparation according to claim 1, wherein the suspending agent further contains polyethylene glycol. 5. The injectable preparation according to claim 1, wherein the suspending agent further contains polyethylene glycol and carboxymethyl cellulose or a salt thereof. 6. A gel composition comprising a poorly soluble drug which is aripiprazole or a salt thereof, or 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or a salt thereof, water, and suspending agent, wherein the suspending agent contains polyvinylpyrrolidone, the poorly soluble drug has a mean primary particle diameter of 0.5 to 30 μm and is contained in a concentration of 200 to 600 mg/mL, and K value of polyvinylpyrrolidone is 12 to 30, and the concentration of polyvinylpyrrolidone is 0.1 to 100 mg/mL. 7. The composition according to claim 6, wherein the suspending agent further contains polyethylene glycol. 8. The composition according to claim 6, wherein the suspending agent further contains polyethylene glycol and carboxymethyl cellulose or a salt thereof. 9. The composition according to claim 8, wherein the concentration of polyethylene glycol is 0.05 to 2 mg/mL, and the concentration of carboxymethyl cellulose or a salt thereof is 0.5 to 50 mg/m L. 10. The composition according to claim 6, wherein the poorly soluble drug has a mean secondary particle diameter that is up to but not exceeding three times the mean primary particle diameter thereof. 11. The composition according to claim 6, which has a viscosity of 40 Pa·s or more in at least one point in the shear rate range of 0.01 to 0.02 s−1 and which has a viscosity of 0.2 Pa·s or less in at least one point in the shear rate range of 900 to 1,000 s−1, as measured by a rheometer at 5° C., 25° C. or 40° C. 12. The composition according to claim 6 which has a viscosity of 40 Pa·s or more in at least one point in the shear rate range of 0.01 to 0.02 s−1 and which has a viscosity of 0.2 Pa·s or less in at least one point in the shear rate range of 900 to 1,000 s−1, as measured by a rheometer at 25° C. 13. A sustained release injectable preparation comprising a composition comprising a poorly soluble drug which is aripiprazole or a salt thereof, or 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or a salt thereof, water, and suspending agent, wherein the suspending agent contains polyvinylpyrrolidone, the poorly soluble drug has a mean primary particle diameter of 1 to 10 μm and is contained in a concentration of 200 to 400 mg/mL, and K value of polyvinylpyrrolidone is 12 to 30, and the concentration of polyvinylpyrrolidone is 0.1 to 100 mg/mL, the composition being in the form of a gel when allowed to stand, and changing to a sol when subjected to an impact, and the preparation being administered once per month. 14. The injectable preparation according to claim 13, wherein the poorly soluble drug has a mean primary particle diameter of 2 to 7 μm. 15. A sustained release injectable preparation comprising a composition comprising a poorly soluble drug which is aripiprazole or a salt thereof, or 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or a salt thereof, water, and suspending agent, wherein the suspending agent contains polyvinylpyrrolidone, the poorly soluble drug has a mean primary particle diameter of 4 to 30 μm and is contained in a concentration of 300 to 600 mg/mL, and K value of polyvinylpyrrolidone is 12 to 30, and the concentration of polyvinylpyrrolidone is 0.1 to 100 mg/mL, the composition being in the form of a gel when allowed to stand, and changing to a sol when subjected to an impact, and the preparation being administered once every two to three months. 16. The injectable preparation according to claim 15, wherein the poorly soluble drug has a mean primary particle diameter of 5 to 20 μm. 17. The injectable preparation according to claim 13, wherein the suspending agent further contains polyethylene glycol. 18. The injectable preparation according to claim 13, wherein the suspending agent further contains polyethylene glycol and carboxymethyl cellulose or a salt thereof. 19. The injectable preparation according to claim 18, wherein the concentration of polyethylene glycol is 0.05 to 2 mg/mL, and the concentration of carboxymethyl cellulose or a salt thereof is 0.5 to 50 mg/mL. 20. The injectable preparation according to claim 13, wherein the poorly soluble drug has a mean secondary particle diameter that is up to but not exceeding three times the mean primary particle diameter thereof. 21. The injectable preparation according to claim 13, wherein the composition has a viscosity of 40 Pa·s or more in at least one point in the shear rate range of 0.01 to 0.02 s−1 and has a viscosity of 0.2 Pa·s or less in at least one point in the shear rate range of 900 to 1,000 s−1, as measured by a rheometer at 5° C., 25° C. or 40° C. 22. The injectable preparation according to claim 13, wherein the composition has a viscosity of 40 Pa·s or more in at least one point in the shear rate range of 0.01 to 0.02 s−1 and has a viscosity of 0.2 Pa·s or less in at least one point in the shear rate range of 900 to 1,000 s−1, as measured by a rheometer at 25° C. 23. A method for treating a recurrence of schizophrenia, bipolar disorder, or depression, the method comprising administering the injectable preparation according to claim 1. 24. The method according to claim 23, wherein the injectable preparation is administered intramuscularly or subcutaneously.