Claims for Patent: 10,517,951

Summary for Patent: 10,517,951

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:	US16156958
Patent Claims:	1. An injectable preparation suitable for the treatment of a human patient comprising a composition comprising a poorly soluble drug , a dispersion medium , and a suspending agent ,the poorly soluble drug being 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 suspending agent containing polyvinylpyrrolidone, polyethylene glycol, and carboxymethyl cellulose or a salt thereof,K value of polyvinylpyrrolidone being 17, and the concentration of polyvinylpyrrolidone being 4 mg/mL,the polyethylene glycol being polyethylene glycol 400, and the concentration of polyethylene glycol being 1 mg/mL,the concentration of carboxymethyl cellulose or a salt thereof being 5 mg/mL,the poorly soluble drug being contained in a concentration of 300 mg/mL, and{'sup': −1', '−1, '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 25° C.,'}wherein the injectable preparation is in gel form for storage and forms a sol when subjected to an impact.2. The injectable preparation according to comprising a composition comprising at least water as a dispersion medium.3. The injectable preparation according to wherein the 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one is in the form of a dihydrate.4. The injectable preparation according to wherein the poorly soluble drug has a mean primary particle diameter of 1 to 10 μm.5. The injectable preparation according to wherein the injectable preparation is disposed within a container.6. The injectable preparation according to wherein the container is syringe or vial.8. The composition according to 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.9. 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 7 ,000 s claim 7 , as measured by a rheometer at 25° C.10. The composition according to wherein the 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one is in the form of a dihydrate.11. The composition according to wherein the poorly soluble drug has a mean primary particle diameter of 1 to 10 μm.12. The composition according to wherein the composition is disposed within a container.13. The composition according to wherein the container is syringe or vial.14. A sustained release injectable preparation suitable for the treatment of a human patient 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, anda suspending agent comprising polyvinylpyrrolidone, polyethylene glycol, and carboxymethyl cellulose or a salt thereof,wherein the poorly soluble drug has a mean primary particle diameter of 1 to 10 μm and is contained in a concentration of 300 mg/mL,K value of polyvinylpyrrolidone is 17, and the concentration of polyvinylpyrrolidone is 4 mg/mL,the polyethylene glycol is polyethylene glycol 400, and the concentration of polyethylene glycol is 1 mg/mL, andthe concentration of carboxymethyl cellulose or a salt thereof is 5 mg/mL,the preparation 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.15. The injectable preparation according to wherein the poorly soluble drug has a mean primary particle diameter of 2 to 7 μm.16. 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, anda suspending agent comprising polyvinylpyrrolidone, polyethylene glycol, and carboxymethyl cellulose or a salt thereof,wherein the poorly soluble drug has a mean primary particle diameter of 4 to 30 μm and is contained in a concentration of 300 mg/mL,K value of polyvinylpyrrolidone is 17, and the concentration of polyvinylpyrrolidone is 4 mg/mL,the polyethylene glycol is polyethylene glycol 400, and the concentration of polyethylene glycol is 1 mg/mL, andthe concentration of carboxymethyl cellulose or a salt thereof is 5 mg/mL,the preparation 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.17. The injectable preparation according to wherein the poorly soluble drug has a mean primary particle diameter of 5 to 20 μm.18. The injectable preparation according to 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.19. The injectable preparation according to 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 14 ,000 s claim 14 , as measured by a rheometer at 25° C.20. The injectable preparation according to wherein the 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one is in the form of a dihydrate.21. The injectable preparation according to wherein the preparation being disposed within a container.22. The injectable preparation according to wherein the container is syringe or vial.23. The injectable preparation according to wherein the preparation being disposed within a container.24. The injectable preparation according to wherein the container is syringe or vial.25. A method for treating schizophrenia claim 1 , bipolar disorder claim 1 , or depression claim 1 , the method comprising administering the injectable preparation according to .26. The method according to wherein the injectable preparation is administered intramuscularly or subcutaneously.