US 8,475,842 B2 · Immediate release pharmaceutical formulation of 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one

Abstract

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.

Claims10

Dependent claims

An immediate-release pharmaceutical composition in the form of a solid dispersion, the composition comprising:

an active agent phase comprising 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one (Compound 1) or a salt thereof;
and
a carrier phase comprising copovidone;
and
wherein the active agent phase is dispersed in the carrier phase:
wherein the total concentration of Compound 1 in the composition is in the range of from 20% by weight to 30% by weight;
wherein the total amount of Compound 1 in the composition is in the range of from 25 mg to 400 mg;
and
wherein the weight ratio of Compound 1 to copovidone is in the range of from 1:2 to 1:4.

6 more elements

Dependencies are inferred from the claim text.

Facts

Application

12/574,801Filed 7 Oct 2009 · us provisional application

Priority

7 Oct 2008

Published

US 2010/0098763 A122 Apr 2010

Granted

2 Jul 2013

Term ends

Not estimatedThe source records don’t support an estimate.

Classification12 codes

A61K 31/502
Pyridazines; Hydrogenated pyridazines: ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
A61K 9/2009
Excipients; Inactive ingredients: inorganic compounds
A61K 9/2013
Excipients; Inactive ingredients: organic compounds, e.g. phospholipids, fats
A61K 9/2027
Organic macromolecular compounds: obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, polyacrylates

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

Life of this patent

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

Life of this patent

Abstract

Claims10