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 sand 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, as measured.
Inventor(s):	Kaneko Daiki, Matsuda Takakuni, Hoshika Yusuke
Assignee:	OTSUKA PHARMACEUTICAL CO., LTD.
Application Number:	US17108939
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 sand 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 , 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, andK 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 sand having a viscosity of 0.2 Pa·s or less in at least one point in the shear rate range of 900 to 1 claim 1 ,000 s claim 1 , as measured by a rheometer at 25° C.3. The injectable preparation according to 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 comprisinga 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, andsuspending 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, andK 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 claim 8 , 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 sand 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 claim 6 ,000 s claim 6 , as measured by a rheometer at 5° C. claim 6 , 25° C. or 40° C.12. The composition according to 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 sand 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 claim 6 ,000 s claim 6 , as measured by a rheometer at 25° C.13. A sustained release injectable preparation comprising a composition comprisinga 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, andsuspending 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, andK 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, andthe 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 comprisinga 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, andsuspending 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, andK 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, andthe 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 claim 18 , 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 sand has a viscosity of 0.2 Pa·s or less in at least one point in the shear rate range of 900 to 1 claim 13 ,000 s claim 13 , as measured by a rheometer at 5° C. claim 13 , 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 sand has a viscosity of 0.2 Pa·s or less in at least one point in the shear rate range of 900 to 1 claim 13 ,000 s claim 13 , as measured by a rheometer at 25° C.23. A method for treating a recurrence of schizophrenia claim 1 , bipolar disorder claim 1 , or depression claim 1 , the method comprising administering the injectable preparation according to .24. The method according to claim 23 , wherein the injectable preparation is administered intramuscularly or subcutaneously.