Claims for Patent: 8,475,842

Summary for Patent: 8,475,842

Title:	Immediate release pharmaceutical formulation of 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-p- hthalazin-1-one
Abstract:	The present invention relates to a pharmaceutical formulation comprising the drug 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-ben- zyl]-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.
Inventor(s):	Bechtold; Michael Karl (Ludwigshafen, DE), Packhaeuser; Claudia Bettina (Ludwigshafen, DE), Fastnacht; Katja Maren (Ludwigshafen, DE), Liepold; Bernd Harald (Ludwigshafen, DE), Steitz; Benedikt (Ludwigshafen, DE), Cahill; Julie Kay (Macclesfield, GB), Lennon; Kieran James (Macclesfield, GB)
Assignee:	Astrazeneca AB (Sodertalje, SE)
Application Number:	12/574,801
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,475,842
Patent Claims:	1. 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-p- hthalazin-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. 2. The composition of claim 1, wherein Compound 1 is in an amorphous form. 3. The composition of claim 1, wherein at least 90% of Compound 1 is in an amorphous form. 4. The composition of claim 1, wherein the composition is made by solvent evaporation or melt extrusion. 5. The composition of claim 4, wherein the composition is made by melt extrusion. 6. 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-p- hthalazin-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 10 mg to 1,000 mg; and wherein the weight ratio of Compound 1 to copovidone is in the range of from 1:2 to 1:4. 7. 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-p- hthalazin-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 25% by weight; and wherein the weight ratio of Compound 1 to copovidone is 1:2.3. 8. The composition of claim 7, further comprising a glidant, a soluble filler, and a lubricant. 9. The composition of claim 7, further comprising colloidal silicon dioxide, mannitol, and sodium stearyl fumarate. 10. The composition of claim 7, further comprising 1.8% by weight colloidal silicon dioxide, 14.7% by weight mannitol, and 1% by weight sodium stearyl fumarate.