Injectable formulation

Abstract

An object of the present invention is to provide a sustained-release injectable preparation which is in a medication administration form that can provide the effect of 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one for a prolonged period of time, the preparation releasing a therapeutically effective amount of 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one for at least one week. The present invention provides an injectable preparation containing 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or a salt thereof as an active ingredient, which releases the active ingredient in such a manner that its blood concentration is maintained for at least one week.

1 . An aqueous suspension comprising secondary particles formed by the aggregation of particles of 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or a salt thereof, the secondary particles having a mean particle diameter (a mean secondary particle diameter) of 1 to 50 μm and being contained in a dispersed state. 
     
     
         2 . The aqueous suspension according to  claim 1 , wherein the particles of 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or a salt thereof have a mean primary particle diameter of 0.1 to 20 μm. 
     
     
         3 . The aqueous suspension according to  claim 1  or  2 , comprising 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one in an amount of 0.1 to 40 wt %. 
     
     
         4 . An injectable preparation comprising the aqueous suspension according to  claim 3 . 
     
     
         5 . An injectable preparation comprising 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or a salt thereof, a particle binder, and water for injection, the particle binder being at least one member selected from the group consisting of sodium chloride, polyvinylpyrrolidones (PVP), polyoxyethylene (160) polyoxypropylene (30) glycol, tocopherol, tocotrienol and esters thereof, tocopherol acetate, tocopherol succinate, benzyl alcohol, poorly water-soluble polyoxyethylene diol dibenzoate, poorly water-soluble polyoxyethylene diol dimethylsulfonic acid and esters thereof, and benzyl benzoate. 
     
     
         6 . The injectable preparation according to  claim 5 , wherein the 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or a salt thereof forms secondary particles and the secondary particles have a mean secondary particle diameter of 1 to 50 μm. 
     
     
         7 . The injectable preparation according to  claim 5  or  6 , comprising a suspension of the 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or a salt thereof in water for injection. 
     
     
         8 . The injectable preparation according to  claim 5  or  6 , comprising a precipitate of the 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or a salt thereof. 
     
     
         9 . The injectable preparation according to  claim 5  or  6 , wherein the particle binder is at least one member selected from the group consisting of sodium chloride, polyoxyethylene (160) polyoxypropylene (30) glycol, benzyl alcohol, and benzyl benzoate. 
     
     
         10 . The injectable preparation according to  claim 4 , having a pH of 5 to 8. 
     
     
         11 . The injectable preparation according to  claim 9 , having a pH of 5 to 8. 
     
     
         12 . The injectable preparation according to  claim 11 , wherein the 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or a salt thereof is a dihydrate of 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one. 
     
     
         13 . A prefilled syringe that is prefilled with the injectable preparation according to  claim 12 .