# US 8,772,303 B2 · Pharmaceutical formulation > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 8,772,303 B2 - Document ID: US8772303B2 - Status: Granted - Kind: B2 - Application number: 12/478,934 - Filed: 2009-06-05 - Published: 2009-12-10 - Granted: 2014-07-08 - Earliest claimed: 2009-06-05 - Assignees: Glaxo Group Limited - Applicants: Dirk Marinus Johannes Van Schie - Inventors: Dirk Marinus Johannes Van Schie - Web page: https://patentgrep.com/patent/US8772303B2 ## CPC - A61K 9/2077: {Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets} - A61K 31/513: having oxo groups directly attached to the heterocyclic ring, e.g. cytosine - A61P 9/00: Drugs for disorders of the cardiovascular system - A61P 9/10: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis - A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 - A61K 9/2846: {Poly(meth)acrylates} - A61K 9/2886: {having two or more different drug-free coatings; Tablets of the type inert core-drug layer-inactive layer (of the type active core-drug layer-inactive layer A61K9/209)} - A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D) - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS ## Abstract The present invention provides enteric polymer coated tablet formulations for oral administration which comprise a phospholipase A2 enzyme Lipoprotein Associated Phospholipase A2 (Lp-PLA2) inhibitor, processes for preparing such formulations and their use in therapy, in particular the treatment of atherosclerosis. ## Claims ### Claim 1 A pharmaceutical formulation comprising a core which includes a pharmaceutically active ingredient which is 1-(N-(2-(diethylamino)ethyl)-N-(4-(4-trifluoromethylphenyl)benzyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5,6-trimethylenepyrimidin-4-one and a casing which comprises an enteric polymer. ### Claim 2 (depends on 1) A pharmaceutical formulation according to claim 1 wherein said core further comprises a disintegrant. ### Claim 3 (depends on 2) A pharmaceutical formulation according to claim 2 wherein said disintegrant is croscarmellose sodium. ### Claim 4 (depends on 1) A pharmaceutical formulation according to claim 1 wherein said core further comprises a diluent. ### Claim 5 (depends on 4) A pharmaceutical formulation according to claim 4 wherein said diluent is lactose. ### Claim 6 (depends on 1) A pharmaceutical formulation according to claim 1 wherein said core further comprises a binder. ### Claim 7 (depends on 6) A pharmaceutical formulation according to claim 6 wherein said binder is hydroxypropylmethyl cellulose. ### Claim 8 (depends on 1) A pharmaceutical formulation according to claim 1 wherein said core comprises microcrystalline cellulose. ### Claim 9 (depends on 1) A pharmaceutical formulation according to claim 1 wherein said enteric polymer is an Eudragit® enteric polymer which is a methyl acrylate methacrylic acid copolymer. ### Claim 10 (depends on 1) A pharmaceutical formulation according to claim 1 wherein said casing further comprises an anti tack agent. ### Claim 11 (depends on 1) A pharmaceutical formulation according to claim 1 wherein said casing further comprises a surfactant. ### Claim 12 (depends on 1) A pharmaceutical formulation according to claim 1 wherein said active ingredient is micronised. ### Claim 13 (depends on 1) A process for making a pharmaceutical formulation according to claim 1 comprising wet bead milling. ### Claim 14 (depends on 5) A pharmaceutical formulation according to claim 5 wherein said diluent is anhydrous lactose, lactose monohydrate or a mixture thereof. ### Claim 15 (depends on 9) A pharmaceutical formulation according to claim 9 wherein said casing further comprises a plasticizer. ### Claim 16 (depends on 15) A pharmaceutical formulation according to claim 15 wherein said plasticizer is triethyl citrate. ### Claim 17 (depends on 1) A pharmaceutical formulation according to claim 1 further comprising a seal coat between said core and said casing. ### Claim 18 A pharmaceutical formulation comprising: (i) a core which comprises: a pharmaceutically active ingredient, which is 1-(N-(2-(diethylamino)ethyl)-N-(4-(4-trifluoromethylphenyl)benzyl(aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5,6-trimethylenepyrimidin-4-one, a disintegrant which is croscarmellose sodium, a diluent, which is anhydrous lactose, lactose monohydrate, or a mixture thereof, a binder, which is hydroxypropylmethyl cellulose, microcrystalline cellulose, and a lubricant; and (ii) a casing which comprises an enteric polymer, an anti-tack agent, and a surfactant. ### Claim 19 (depends on 18) The formulation of claim 18 wherein the lubricant is magnesium stearate. ### Claim 20 (depends on 18) The formulation of claim 18 wherein the anti-tack agent is glyceryl monostearate and the surfactant is polysorbate 80. ### Claim 21 (depends on 18) A pharmaceutical formulation according to claim 18 wherein said casing further comprises a plasticizer. ### Claim 22 (depends on 21) A pharmaceutical formulation according to claim 21 wherein said plasticizer is triethyl citrate. ### Claim 23 (depends on 18) The formulation of claim 18 further comprising a seal coat between said core and said casing. ### Claim 24 (depends on 18) The formulation of claim 18 wherein the enteric polymer is a methacrylic acid copolymer. ### Claim 25 (depends on 1) The formulation of claim 1 where the enteric polymer is a methacrylic acid copolymer.