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.
Type:
Application
Filed:
October 7, 2009
Publication date:
April 22, 2010
Applicants:
Abbot GmbH & Co. KG
Inventors:
Michael Karl Bechtold, Claudia Bettina Packhaeuser, Katja Maren Fastnacht, Bernd Harald Liepold, Benedikt Steitz, Julie Kay Cahill, Kieran James Lennon
Abstract: The invention relates to pyrimidin 2-one compounds of general formula (I), in addition to the derivatives and tautomers of (I) and the physiologically acceptable salts of said compounds. In said formula, A represents linear or branched C3-C6 alkene, which can have a double bond or triple bond and/or a group Z, which is not adjacent to the nitrogen atom of the pyrimidinone ring and is selected from O, S, C(O), NR3, C(O)NR3, NR3C(O), OC(O) and C(O)O; B represents a group of the formula (II), in which X stands for CH2 or N and Y stands for CH2 or CH2CH2, or X—Y can also jointly represent C?CH, C?CH—CH2 or CH—CH?CH; R1 and R2 are defined as cited in the description and the claims; and Ar represents an optionally substituted aromatic group. The invention also relates to a pharmaceutical agent, containing at least one compound (I) and the tautomers, derivatives and/or acid addition salts of said compound, optionally together with physiologically acceptable carriers and/or auxiliary agents.
Type:
Application
Filed:
March 12, 2004
Publication date:
October 19, 2006
Applicant:
ABBOT GMBH & CO. KG
Inventors:
Herve Geneste, Andreas Kling, Wilfried Braje, Andreas Haupt, Lillian Unger