Unlock all Features See Plans and Pricing

Serving leading biopharmaceutical companies globally:

McKinsey
Johnson and Johnson
Mallinckrodt
Colorcon
Medtronic
Boehringer Ingelheim

Last Updated: January 29, 2022

DrugPatentWatch Database Preview

Claims for Patent: 8,475,842


Email this page to a colleague

« Back to Dashboard

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 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.

Make Better Decisions: Try a trial or see plans & pricing

Serving leading biopharmaceutical companies globally:

AstraZeneca
Mallinckrodt
Boehringer Ingelheim
McKesson
Express Scripts
Johnson and Johnson

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.