IMMEDIATE RELEASE PHARMACEUTICAL FORMULATION OF 4-[3-(4-CYCLOPROPANECARBONYL-PIPERAZINE-1-CARBONYL)-4-FLUORO-BENZYL]-2H-PHTHALAZIN-1-ONE

The present invention relates to a pharmaceutical formulation comprising the drug 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one in a solid dispersion with a matrix polymer that exhibits low hygroscopicity and high softening temperature, such as copovidone. The invention also relates to a daily pharmaceutical dose of the drug provided by such a formulation. In addition, the invention relates to the use of a matrix polymer that exhibits low hygroscopicity and high softening temperature in solid dispersion with 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one for increasing the bioavailability of the drug. 1. An extrudate for use in an immediate release pharmaceutical formulation , the extrudate formed during melt extrusion and comprising an active agent in solid dispersion with a matrix polymer , wherein the active agent is 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one or a salt or solvate thereof , and the matrix polymer is copovidone , wherein the ratio by weight of the active agent and matrix polymer is in the range from about 1:2 to about 1:4.2. The extrudate as claimed in claim 1 , wherein the active agent is in stable amorphous form.3. The extrudate as claimed in claim 2 , wherein at least 90% by weight of the active agent is in amorphous form.4. The extrudate as claimed in claim 1 , wherein the copovidone is a co-polymer of 1-vinyl-2-pyrollidone and vinyl acetate in a ratio of 6:4 by mass.5. The extrudate as claimed in claim 1 , wherein the solid dispersion includes a surface-active agent and/or plasticiser.6. The extrudate as claimed in claim 5 , wherein the surface-active agent is selected from: sodium dodecyl sulphate (sodium lauryl sulphate); docusate sodium; cetrimide; benzethonium chloride; cetylpyridinium chloride; lauric acid; polyoxyethylene alkyl ethers; polyoxyethylene sorbitan fatty acid esters claim 5 , e.g. polysorbates 20 ...

IMMEDIATE RELEASE PHARMACEUTICAL FORMULATION OF 4-[3-(4-CYCLOPROPANECARBONYL-PIPERAZINE-1-CARBONYL)-4-FLUORO-BENZYL]-2H-PHTHALAZIN-1-ONE

The present invention relates to a pharmaceutical formulation comprising the drug 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one in a solid dispersion with a matrix polymer that exhibits low hygroscopicity and high softening temperature, such as copovidone. The invention also relates to a daily pharmaceutical dose of the drug provided by such a formulation. In addition, the invention relates to the use of a matrix polymer that exhibits low hygroscopicity and high softening temperature in solid dispersion with 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one for increasing the bioavailability of the drug. 1. A pharmaceutical formulation comprising and active agent in solid dispersion with a matrix polymer , wherein the active agent is 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one or a salt or solvate thereof , and the matrix polymer exhibits low hygroscopicity and high softening temperature.2. The formulation as claimed in claim 1 , wherein the active agent is in stable amorphous form.3. The formulation as claimed in claim 2 , wherein at least 90% of the active agent is in amorphous form.4. The formulation as claimed in any one of to claim 2 , wherein the matrix polymer is selected from: copovidone claim 2 , hydroxypropyl methylcellulose phthalate (HPMCP) claim 2 , hydroxypropyl methylcellulose acetate succinate (HPMCAS) claim 2 , 2-hydroxypropyl-β-cyclodextrin (HPBCD) claim 2 , hydroxypropyl methylcellulose (Hypromellose claim 2 , HPMC) claim 2 , polymethacrylates claim 2 , hydroxypropyl cellulose (HPC) claim 2 , and cellulose acetate phthalate (CAP).5. The formulation as claimed in any one of to claim 2 , wherein the matrix polymer is copovidone.6. The formulation as claimed in claim 5 , wherein the copovidone is a co-polymer of 1-vinyl-2-pyrollidone and vinyl acetate in a ratio of 6:4 by mass.7. The formulation as claimed in claim 6 , ...

IMMEDIATE RELEASE PHARMACEUTICAL FORMULATION OF 4-[3-(4-CYCLOPROPANECARBONYL-PIPERAZINE-1-CARBONYL)-4-FLUORO-BENZYL]-2H-PHTHALAZIN-1-ONE

The present invention relates to a pharmaceutical formulation comprising the drug 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one in a solid dispersion with a matrix polymer that exhibits low hygroscopicity and high softening temperature, such as copovidone. The invention also relates to a daily pharmaceutical dose of the drug provided by such a formulation. In addition, the invention relates to the use of a matrix polymer that exhibits low hygroscopicity and high softening temperature in solid dispersion with 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one for increasing the bioavailability of the drug. 1. A pharmaceutical formulation comprising and active agent in solid dispersion with a matrix polymer , wherein the active agent is 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one or a salt or solvate thereof , and the matrix polymer exhibits low hygroscopicity and high softening temperature.2. The formulation as claimed in claim 1 , wherein the active agent is in stable amorphous form.3. The formulation as claimed in claim 2 , wherein at least 90% of the active agent is in amorphous form.4. The formulation as claimed in any one of to claim 2 , wherein the matrix polymer is selected from: copovidone claim 2 , hydroxypropyl methylcellulose phthalate (HPMCP) claim 2 , hydroxypropyl methylcellulose acetate succinate (HPMCAS) claim 2 , 2-hydroxypropyl-β-cyclodextrin (HPBCD) claim 2 , hydroxypropyl methylcellulose (Hypromellose claim 2 , HPMC) claim 2 , polymethacrylates claim 2 , hydroxypropyl cellulose (HPC) claim 2 , and cellulose acetate phthalate (CAP).5. The formulation as claimed in any one of to claim 2 , wherein the matrix polymer is copovidone.6. The formulation as claimed in claim 5 , wherein the copovidone is a co-polymer of 1-vinyl-2-pyrollidone and vinyl acetate in a ratio of 6:4 by mass.7. The formulation as claimed in claim 6 , ...

IMMEDIATE RELEASE PHARMACEUTICAL FORMULATION OF 4-[3-(4-CYCLOPROPANECARBONYL-PIPERAZINE-1-CARBONYL)-4-FLUORO-BENZYL]-2H-PHTHALAZIN-1-ONE

The present invention relates to a pharmaceutical formulation comprising the drug 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one in a solid dispersion with a matrix polymer that exhibits low hygroscopicity and high softening temperature, such as copovidone. The invention also relates to a daily pharmaceutical dose of the drug provided by such a formulation. In addition, the invention relates to the use of a matrix polymer that exhibits low hygroscopicity and high softening temperature in solid dispersion with 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one for increasing the bioavailability of the drug. 1. An extrudate for use in an immediate release pharmaceutical formulation , the extrudate formed during melt extrusion and comprising an active agent in solid dispersion with a matrix polymer , wherein the active agent is 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one or a salt or solvate thereof , and the matrix polymer is copovidone , wherein the ratio by weight of the active agent and matrix polymer is in the range from 1:2 to 1:4.2. The extrudate as claimed in claim 1 , wherein the active agent is in stable amorphous form.3. The extrudate as claimed in claim 2 , wherein at least 90% by weight of the active agent is in amorphous form.4. The extrudate as claimed in claim 1 , wherein the copovidone is a co-polymer of 1-vinyl-2-pyrollidone and vinyl acetate in a ratio of 6:4 by mass.5. The extrudate as claimed in claim 1 , wherein the solid dispersion includes a surface-active agent and/or plasticiser.6. The extrudate as claimed in claim 5 , wherein the surface-active agent is selected from: sodium dodecyl sulphate (sodium lauryl sulphate); docusate sodium; cetrimide; benzethonium chloride; cetylpyridinium chloride; lauric acid; polyoxyethylene alkyl ethers; polyoxyethylene sorbitan fatty acid esters polysorbates 20 claim 5 , 40 claim 5 , 60 ...

IMMEDIATE RELEASE PHARMACEUTICAL FORMULATION OF 4-[3-(4-CYCLOPROPANECARBONYL-PIPERAZINE-1-CARBONYL)-4-FLUORO-BENZYL]-2H-PHTHALAZIN-1-ONE

The present invention relates to a pharmaceutical formulation comprising the drug 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one in a solid dispersion with a matrix polymer that exhibits low hygroscopicity and high softening temperature, such as copovidone. The invention also relates to a daily pharmaceutical dose of the drug provided by such a formulation. In addition, the invention relates to the use of a matrix polymer that exhibits low hygroscopicity and high softening temperature in solid dispersion with 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one for increasing the bioavailability of the drug. 1. An extrudate for use in an immediate release pharmaceutical formulation , the extrudate formed during melt extrusion and comprising an active agent in solid dispersion with a matrix polymer , wherein the active agent is 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one or a salt or solvate thereof , and the matrix polymer is copovidone , wherein the ratio by weight of the active agent and matrix polymer is in the range from about 1:2 to about 1:4.2. The extrudate as claimed in claim 1 , wherein the active agent is in stable amorphous form.3. The extrudate as claimed in claim 2 , wherein at least 90% by weight of the active agent is in amorphous form.4. The extrudate as claimed in claim 1 , wherein the copovidone is a co-polymer of 1-vinyl-2-pyrollidone and vinyl acetate in a ratio of 6:4 by mass.5. The extrudate as claimed in claim 1 , wherein the solid dispersion includes a surface-active agent and/or plasticiser.6. The extrudate as claimed in claim 5 , wherein the surface-active agent is selected from: sodium dodecyl sulphate (sodium lauryl sulphate); docusate sodium; cetrimide; benzethonium chloride; cetylpyridinium chloride; lauric acid; polyoxyethylene alkyl ethers; polyoxyethylene sorbitan fatty acid esters polysorbates 20 claim 5 , 40 ...

Immediate release pharmaceutical formulation of 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2h-phthalazin-1-one

The present invention relates to a pharmaceutical formulation comprising the drug 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one in a solid dispersion with a matrix polymer that exhibits low hygroscopicity and high softening temperature, such as copovidone. The invention also relates to a daily pharmaceutical dose of the drug provided by such a formulation. In addition, the invention relates to the use of a matrix polymer that exhibits low hygroscopicity and high softening temperature in solid dispersion with 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one for increasing the bioavailability of the drug.

Pharmaceutical formulation 514

Pharmaceutical formulation 514

The present invention relates to a pharmaceutical formulation comprising the drug 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one in a solid dispersion with a matrix polymer that exhibits low hygroscopicity and high softening temperature, such as copovidone. The invention also relates to a daily pharmaceutical dose of the drug provided by such a formulation. In addition, the invention relates to the use of a matrix polymer that exhibits low hygroscopicity and high softening temperature in solid dispersion with 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one for increasing the bioavailability of the drug.

Immediate release pharmaceutical formulation of 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one

The present invention relates to a pharmaceutical formulation comprising the drug 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one in a solid dispersion with a matrix polymer that exhibits low hygroscopicity and high softening temperature, such as copovidone. The invention also relates to a daily pharmaceutical dose of the drug provided by such a formulation. In addition, the invention relates to the use of a matrix polymer that exhibits low hygroscopicity and high softening temperature in solid dispersion with 4-[3-(4-cyclopropanecarbonyl-piperazine-1 -carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one for increasing the bioavailability of the drug.

Pharmaceutical formulation 514

The present invention relates to a pharmaceutical formulation comprising the drug 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one in a solid dispersion with a matrix polymer that exhibits low hygroscopicity and high softening temperature, such as copovidone. The invention also relates to a daily pharmaceutical dose of the drug provided by such a formulation. In addition, the invention relates to the use of a matrix polymer that exhibits low hygroscopicity and high softening temperature in solid dispersion with 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H- phthalazin-1-one for increasing the bioavailability of the drug.

A PHARMACEUTICAL FORMULATION THAT INCLUDES 4- [3- (4-CICLOPROPANOCARBONIL-PIPERAZINA-1-CARBONIL) -4-FLUOROBENCIL] -2h-FTALAZIN-1-ONA IN SOLID DISPERSION WITH COPOVIDONA

La presente invención se refiere a una formulación farmacéutica que contiene el fármaco 4-[3-(4-ciclopropanocarbonil-piperazina-1-carbonil)-4-fluorobencil]-2H-ftalazin-1-ona en una dispersión sólida con un polímero de matriz que tiene baja higroscopicidad y elevada temperatura de ablandamiento, como copovidona. La invención también se refiere a una dosis farmacéutica diaria del fármaco provisto por dicha formulación. Además, la invención se refiere al uso de un polímero de matriz que tiene baja higroscopicidad y elevada temperatura de ablandamiento en una dispersión sólida con 4-[3-(4-ciclopropanocarbonil-piperazina-1-carbonil)-4-fluorobencil]-2H-ftalazin-1-ona para aumentar la biodisponibilidad del fármaco. The present invention relates to a pharmaceutical formulation containing the drug 4- [3- (4-cyclopropanecarbonyl-piperazine-1-carbonyl) -4-fluorobenzyl] -2H-phthalazin-1-one in a solid dispersion with a polymer of matrix that has low hygroscopicity and high softening temperature, such as copovidone. The invention also relates to a daily pharmaceutical dose of the drug provided by said formulation. Furthermore, the invention relates to the use of a matrix polymer that has low hygroscopicity and high softening temperature in a solid dispersion with 4- [3- (4-cyclopropanecarbonyl-piperazine-1-carbonyl) -4-fluorobenzyl] -2H -ftalazin-1-one to increase the bioavailability of the drug.

PHARMACEUTICAL FORMULATION 514 comprising 4-[3-( 4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one

PHARMACEUTICAL FORMULATION 514

Pharmaceutical formulations comprising 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2h-phthalazin-1-one or salt or solvate thereof in solid dispersion with a matrix polymer, medicaments comprising the same and methods of producing said solid dispersion

Pharmaceutical formulation 514

The present invention relates to a pharmaceutical formulation comprising the drug 4-[3-(4-cyclopropanecarbonyl--piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one in a solid dispersion with a matrix polymer that exhibits low hygroscopicity and high softening temperature, such as copovidone. The invention also relates to a daily pharmaceutical dose of the drug provided by such a formulation. In addition, the invention relates to the use of a matrix polymer that exhibits low hygroscop-icity and high softening temperature in solid dispersion with 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-ben-zyl]-2H-phthalazin-1-one for increasing the bioavailability of the drug.

Farmacevtska formulacija 514

Farmaceutska formulacija 514

Immediate release pharmaceutical formulation of 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2h-phthalazin-1-one

The present invention relates to a pharmaceutical formulation comprising the drug 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one in a solid dispersion with a matrix polymer that exhibits low hygroscopicity and high softening temperature, such as copovidone. The invention also relates to a daily pharmaceutical dose of the drug provided by such a formulation. In addition, the invention relates to the use of a matrix polymer that exhibits low hygroscopicity and high softening temperature in solid dispersion with 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one for increasing the bioavailability of the drug.

Immediate release pharmaceutical formulation of 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2h-phthalazin-1-one

The present invention relates to a pharmaceutical formulation comprising the drug 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one in a solid dispersion with a matrix polymer that exhibits low hygroscopicity and high softening temperature, such as copovidone. The invention also relates to a daily pharmaceutical dose of the drug provided by such a formulation. In addition, the invention relates to the use of a matrix polymer that exhibits low hygroscopicity and high softening temperature in solid dispersion with 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one for increasing the bioavailability of the drug.

Immediate release pharmaceutical formulation of 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one

The present invention relates to a pharmaceutical formulation comprising the drug 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one in a solid dispersion with a matrix polymer that exhibits low hygroscopicity and high softening temperature, such as copovidone. The invention also relates to a daily pharmaceutical dose of the drug provided by such a formulation. In addition, the invention relates to the use of a matrix polymer that exhibits low hygroscopicity and high softening temperature in solid dispersion with 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one for increasing the bioavailability of the drug.

Farmaceutska formulacija 514

Immediate release pharmaceutical formulation of 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one

The present invention relates to a pharmaceutical formulation comprising the drug 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one in a solid dispersion with a matrix polymer that exhibits low hygroscopicity and high softening temperature, such as copovidone. The invention also relates to a daily pharmaceutical dose of the drug provided by such a formulation. In addition, the invention relates to the use of a matrix polymer that exhibits low hygroscopicity and high softening temperature in solid dispersion with 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one for increasing the bioavailability of the drug.

Preparat farmaceutyczny 514