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filingDate 2004-08-31-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 2005-11-02-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber AR-045547-A1
titleOfInvention PHARMACEUTICAL FORMULATION FOR ORAL ADMINISTRATION THAT INCLUDES AN INHIBITOR COMPOSITE OF PHOSPHOLIPASE A2 ENZYME ASSOCIATED WITH LIPOPROTEINS (LP-PLA2) AND PROCEDURE TO PREPARE IT
abstract A pharmaceutical tablet formulation for oral administration comprising a core that includes a pharmaceutically active material that is a compound that inhibits the phospholipase A2 enzyme associated with lipoproteins (Lp-PLA2) of formula (1) in which Ra and Rb are together - (CH2) n is that n is 3 or 4, to form, with the C atoms of the pyrimidine ring to which they are attached, a fused carbocyclic ring of 5 or 6 members; R1 is phenyl optionally substituted with halogen; R2 is C1-3 alkyl substituted with NR5R6; R3 and R4 form a 4- (4-trifluoromethylphenyl) phenyl moiety; and each of R5 and R6, which may be the same or different, is selected from H and C1-6 alkyl, and a shell comprising an enteric polymer. Preferably, said active ingredient is 1- (N- (2- (diethylamino) ethyl) -N- (4- (4-trifluoromethylphenyl) -benzyl) aminocarbonylmethyl) -2- (4-fluorobenzyl) thio-5,6-trimethylene pyrimidine -4-one. The core of the pharmaceutical formulation may further comprise a disintegrating agent, a diluting agent, a binding agent, and microcrystalline cellulose. The enteric polymer may be methacrylic acid. The cover may further comprise a non-stick agent and a surfactant. The active ingredient may be micronized. Process for preparing the preceding pharmaceutical formulation comprising milling in the wet state by means of a ball mill. The pharmaceutical formulation is for use in therapy, in particular in the treatment of atherosclerosis.
priorityDate 2003-09-02-04:00^^<http://www.w3.org/2001/XMLSchema#date>
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