CA2877901A1 - Formulation de fenofibrate - Google Patents
Formulation de fenofibrate Download PDFInfo
- Publication number
- CA2877901A1 CA2877901A1 CA2877901A CA2877901A CA2877901A1 CA 2877901 A1 CA2877901 A1 CA 2877901A1 CA 2877901 A CA2877901 A CA 2877901A CA 2877901 A CA2877901 A CA 2877901A CA 2877901 A1 CA2877901 A1 CA 2877901A1
- Authority
- CA
- Canada
- Prior art keywords
- granules
- fenofibrate
- weight
- beads
- surfactant
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Abandoned
Links
- YMTINGFKWWXKFG-UHFFFAOYSA-N fenofibrate Chemical compound C1=CC(OC(C)(C)C(=O)OC(C)C)=CC=C1C(=O)C1=CC=C(Cl)C=C1 YMTINGFKWWXKFG-UHFFFAOYSA-N 0.000 title claims abstract description 311
- 229960002297 fenofibrate Drugs 0.000 title claims abstract description 264
- 239000000203 mixture Substances 0.000 title claims abstract description 126
- 238000009472 formulation Methods 0.000 title description 73
- 239000008187 granular material Substances 0.000 claims abstract description 101
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 66
- 239000004094 surface-active agent Substances 0.000 claims abstract description 65
- 229920002678 cellulose Polymers 0.000 claims abstract description 39
- 239000001913 cellulose Substances 0.000 claims abstract description 39
- 238000001727 in vivo Methods 0.000 claims abstract description 16
- 239000002775 capsule Substances 0.000 claims description 119
- 229940074323 antara Drugs 0.000 claims description 62
- 239000002552 dosage form Substances 0.000 claims description 42
- 229960000701 fenofibric acid Drugs 0.000 claims description 42
- MQOBSOSZFYZQOK-UHFFFAOYSA-N fenofibric acid Chemical compound C1=CC(OC(C)(C)C(O)=O)=CC=C1C(=O)C1=CC=C(Cl)C=C1 MQOBSOSZFYZQOK-UHFFFAOYSA-N 0.000 claims description 42
- 239000008194 pharmaceutical composition Substances 0.000 claims description 29
- 230000000052 comparative effect Effects 0.000 claims description 18
- 230000036470 plasma concentration Effects 0.000 claims description 13
- 239000011248 coating agent Substances 0.000 claims description 12
- 238000000576 coating method Methods 0.000 claims description 12
- 239000012729 immediate-release (IR) formulation Substances 0.000 claims description 12
- 238000012360 testing method Methods 0.000 claims description 10
- 239000000651 prodrug Substances 0.000 claims description 5
- 229940002612 prodrug Drugs 0.000 claims description 5
- 150000002148 esters Chemical class 0.000 claims description 4
- 150000003839 salts Chemical class 0.000 claims description 3
- 239000011324 bead Substances 0.000 description 188
- 239000003814 drug Substances 0.000 description 121
- 229940079593 drug Drugs 0.000 description 119
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 description 95
- 235000019333 sodium laurylsulphate Nutrition 0.000 description 95
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 description 57
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 57
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 57
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 description 49
- 239000000725 suspension Substances 0.000 description 42
- 239000011230 binding agent Substances 0.000 description 33
- 239000011162 core material Substances 0.000 description 31
- 239000002245 particle Substances 0.000 description 26
- 239000008213 purified water Substances 0.000 description 23
- 239000010410 layer Substances 0.000 description 21
- 235000000346 sugar Nutrition 0.000 description 20
- 235000010980 cellulose Nutrition 0.000 description 19
- 238000004090 dissolution Methods 0.000 description 19
- 238000000034 method Methods 0.000 description 19
- 238000004519 manufacturing process Methods 0.000 description 17
- 238000010521 absorption reaction Methods 0.000 description 14
- 239000003826 tablet Substances 0.000 description 12
- 239000008185 minitablet Substances 0.000 description 11
- AMTWCFIAVKBGOD-UHFFFAOYSA-N dioxosilane;methoxy-dimethyl-trimethylsilyloxysilane Chemical compound O=[Si]=O.CO[Si](C)(C)O[Si](C)(C)C AMTWCFIAVKBGOD-UHFFFAOYSA-N 0.000 description 10
- 229960003943 hypromellose Drugs 0.000 description 10
- 239000000546 pharmaceutical excipient Substances 0.000 description 10
- 238000012545 processing Methods 0.000 description 10
- 229940083037 simethicone Drugs 0.000 description 10
- 239000000463 material Substances 0.000 description 9
- 239000003945 anionic surfactant Substances 0.000 description 8
- 239000007963 capsule composition Substances 0.000 description 8
- 239000007903 gelatin capsule Substances 0.000 description 8
- 239000007787 solid Substances 0.000 description 8
- 238000005507 spraying Methods 0.000 description 8
- 239000000454 talc Substances 0.000 description 8
- 229910052623 talc Inorganic materials 0.000 description 8
- 239000002518 antifoaming agent Substances 0.000 description 6
- 239000002736 nonionic surfactant Substances 0.000 description 6
- 239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 description 6
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 description 6
- 229920000053 polysorbate 80 Polymers 0.000 description 6
- 229940068968 polysorbate 80 Drugs 0.000 description 6
- -1 polyvinylpyrolidone Polymers 0.000 description 6
- 239000002904 solvent Substances 0.000 description 6
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- 238000005538 encapsulation Methods 0.000 description 5
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- 238000000338 in vitro Methods 0.000 description 5
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- 239000000843 powder Substances 0.000 description 5
- 239000011734 sodium Substances 0.000 description 5
- 229910052708 sodium Inorganic materials 0.000 description 5
- 238000007906 compression Methods 0.000 description 4
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- 229920003125 hypromellose 2910 Polymers 0.000 description 4
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- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 4
- 239000000758 substrate Substances 0.000 description 4
- 230000001225 therapeutic effect Effects 0.000 description 4
- ZWEHNKRNPOVVGH-UHFFFAOYSA-N 2-Butanone Chemical compound CCC(C)=O ZWEHNKRNPOVVGH-UHFFFAOYSA-N 0.000 description 3
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 description 3
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 description 3
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 3
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 3
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 3
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 description 3
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 3
- LRHPLDYGYMQRHN-UHFFFAOYSA-N N-Butanol Chemical compound CCCCO LRHPLDYGYMQRHN-UHFFFAOYSA-N 0.000 description 3
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 description 3
- BTANRVKWQNVYAZ-UHFFFAOYSA-N butan-2-ol Chemical compound CCC(C)O BTANRVKWQNVYAZ-UHFFFAOYSA-N 0.000 description 3
- 239000003093 cationic surfactant Substances 0.000 description 3
- 239000007931 coated granule Substances 0.000 description 3
- 239000004205 dimethyl polysiloxane Substances 0.000 description 3
- 235000013870 dimethyl polysiloxane Nutrition 0.000 description 3
- 238000001035 drying Methods 0.000 description 3
- 230000000694 effects Effects 0.000 description 3
- 238000011156 evaluation Methods 0.000 description 3
- 235000020937 fasting conditions Nutrition 0.000 description 3
- 239000013022 formulation composition Substances 0.000 description 3
- 229920000435 poly(dimethylsiloxane) Polymers 0.000 description 3
- 230000000291 postprandial effect Effects 0.000 description 3
- 238000002360 preparation method Methods 0.000 description 3
- BDERNNFJNOPAEC-UHFFFAOYSA-N propan-1-ol Chemical compound CCCO BDERNNFJNOPAEC-UHFFFAOYSA-N 0.000 description 3
- 238000012216 screening Methods 0.000 description 3
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 description 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 2
- 229920002134 Carboxymethyl cellulose Polymers 0.000 description 2
- 229920001661 Chitosan Polymers 0.000 description 2
- 102100028717 Cytosolic 5'-nucleotidase 3A Human genes 0.000 description 2
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 2
- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 description 2
- 229920000663 Hydroxyethyl cellulose Polymers 0.000 description 2
- 239000004354 Hydroxyethyl cellulose Substances 0.000 description 2
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 description 2
- 241000219745 Lupinus Species 0.000 description 2
- AMQJEAYHLZJPGS-UHFFFAOYSA-N N-Pentanol Chemical compound CCCCCO AMQJEAYHLZJPGS-UHFFFAOYSA-N 0.000 description 2
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 description 2
- PVNIIMVLHYAWGP-UHFFFAOYSA-N Niacin Chemical compound OC(=O)C1=CC=CN=C1 PVNIIMVLHYAWGP-UHFFFAOYSA-N 0.000 description 2
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 2
- 238000005054 agglomeration Methods 0.000 description 2
- 230000002776 aggregation Effects 0.000 description 2
- RDOXTESZEPMUJZ-UHFFFAOYSA-N anisole Chemical compound COC1=CC=CC=C1 RDOXTESZEPMUJZ-UHFFFAOYSA-N 0.000 description 2
- 238000013459 approach Methods 0.000 description 2
- 239000007900 aqueous suspension Substances 0.000 description 2
- 238000003556 assay Methods 0.000 description 2
- FUFJGUQYACFECW-UHFFFAOYSA-L calcium hydrogenphosphate Chemical compound [Ca+2].OP([O-])([O-])=O FUFJGUQYACFECW-UHFFFAOYSA-L 0.000 description 2
- 239000001768 carboxy methyl cellulose Substances 0.000 description 2
- 235000010948 carboxy methyl cellulose Nutrition 0.000 description 2
- 239000008112 carboxymethyl-cellulose Substances 0.000 description 2
- 230000001419 dependent effect Effects 0.000 description 2
- LRCFXGAMWKDGLA-UHFFFAOYSA-N dioxosilane;hydrate Chemical compound O.O=[Si]=O LRCFXGAMWKDGLA-UHFFFAOYSA-N 0.000 description 2
- 229960003499 fenofibrate micronized Drugs 0.000 description 2
- 238000005243 fluidization Methods 0.000 description 2
- 235000019447 hydroxyethyl cellulose Nutrition 0.000 description 2
- 239000001863 hydroxypropyl cellulose Substances 0.000 description 2
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 description 2
- PHTQWCKDNZKARW-UHFFFAOYSA-N isoamylol Chemical compound CC(C)CCO PHTQWCKDNZKARW-UHFFFAOYSA-N 0.000 description 2
- 238000010902 jet-milling Methods 0.000 description 2
- XZWYZXLIPXDOLR-UHFFFAOYSA-N metformin Chemical compound CN(C)C(=N)NC(N)=N XZWYZXLIPXDOLR-UHFFFAOYSA-N 0.000 description 2
- 229960003105 metformin Drugs 0.000 description 2
- 125000005395 methacrylic acid group Chemical group 0.000 description 2
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- 239000006186 oral dosage form Substances 0.000 description 2
- 239000000825 pharmaceutical preparation Substances 0.000 description 2
- 229920001223 polyethylene glycol Polymers 0.000 description 2
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- 239000002002 slurry Substances 0.000 description 2
- DGSDBJMBHCQYGN-UHFFFAOYSA-M sodium;2-ethylhexyl sulfate Chemical compound [Na+].CCCCC(CC)COS([O-])(=O)=O DGSDBJMBHCQYGN-UHFFFAOYSA-M 0.000 description 2
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 description 1
- WSVLPVUVIUVCRA-KPKNDVKVSA-N Alpha-lactose monohydrate Chemical compound O.O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O WSVLPVUVIUVCRA-KPKNDVKVSA-N 0.000 description 1
- GUBGYTABKSRVRQ-DCSYEGIMSA-N Beta-Lactose Chemical compound OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)[C@H](O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-DCSYEGIMSA-N 0.000 description 1
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 description 1
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 description 1
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 description 1
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- 108010010803 Gelatin Proteins 0.000 description 1
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- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 1
- 229930195725 Mannitol Natural products 0.000 description 1
- NTIZESTWPVYFNL-UHFFFAOYSA-N Methyl isobutyl ketone Chemical compound CC(C)CC(C)=O NTIZESTWPVYFNL-UHFFFAOYSA-N 0.000 description 1
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- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 description 1
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- 229910000019 calcium carbonate Inorganic materials 0.000 description 1
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- 239000001506 calcium phosphate Substances 0.000 description 1
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- NOLXQSVNNIIHMV-UHFFFAOYSA-L disodium;2,2-diethyl-3-hexyl-3-sulfobutanedioate Chemical compound [Na+].[Na+].CCCCCCC(C([O-])=O)(S(O)(=O)=O)C(CC)(CC)C([O-])=O NOLXQSVNNIIHMV-UHFFFAOYSA-L 0.000 description 1
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- CPLXHLVBOLITMK-UHFFFAOYSA-N magnesium oxide Inorganic materials [Mg]=O CPLXHLVBOLITMK-UHFFFAOYSA-N 0.000 description 1
- AXZKOIWUVFPNLO-UHFFFAOYSA-N magnesium;oxygen(2-) Chemical compound [O-2].[Mg+2] AXZKOIWUVFPNLO-UHFFFAOYSA-N 0.000 description 1
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- 239000004800 polyvinyl chloride Substances 0.000 description 1
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- OSBHHMFHRYTYAV-UHFFFAOYSA-M sodium;4-(2-methylheptan-2-yloxy)-4-oxo-3-sulfobutanoate Chemical compound [Na+].CCCCCC(C)(C)OC(=O)C(S(O)(=O)=O)CC([O-])=O OSBHHMFHRYTYAV-UHFFFAOYSA-M 0.000 description 1
- PVGBHEUCHKGFQP-UHFFFAOYSA-N sodium;n-[5-amino-2-(4-aminophenyl)sulfonylphenyl]sulfonylacetamide Chemical compound [Na+].CC(=O)NS(=O)(=O)C1=CC(N)=CC=C1S(=O)(=O)C1=CC=C(N)C=C1 PVGBHEUCHKGFQP-UHFFFAOYSA-N 0.000 description 1
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- 231100000721 toxic potential Toxicity 0.000 description 1
- 230000009466 transformation Effects 0.000 description 1
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 description 1
- 235000019731 tricalcium phosphate Nutrition 0.000 description 1
- 238000005550 wet granulation Methods 0.000 description 1
- 238000009736 wetting Methods 0.000 description 1
- 239000000080 wetting agent Substances 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1617—Organic compounds, e.g. phospholipids, fats
- A61K9/1623—Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4808—Preparations in capsules, e.g. of gelatin, of chocolate characterised by the form of the capsule or the structure of the filling; Capsules containing small tablets; Capsules with outer layer for immediate drug release
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/5005—Wall or coating material
- A61K9/5021—Organic macromolecular compounds
- A61K9/5036—Polysaccharides, e.g. gums, alginate; Cyclodextrin
- A61K9/5042—Cellulose; Cellulose derivatives, e.g. phthalate or acetate succinate esters of hydroxypropyl methylcellulose
- A61K9/5047—Cellulose ethers containing no ester groups, e.g. hydroxypropyl methylcellulose
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/5073—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals having two or more different coatings optionally including drug-containing subcoatings
- A61K9/5078—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals having two or more different coatings optionally including drug-containing subcoatings with drug-free core
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
Landscapes
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Obesity (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
Abstract
La présente invention concerne diverses compositions de fénofibrate comprenant une pluralité de premiers granules présentant une biodisponibilité élevée in vivo, et une pluralité de seconds granules présentant une faible biodisponibilité in vivo. Les premiers granules peuvent comprendre du fénofibrate, de 0,3 % à 10 % en poids des premiers granules d'un premier tensioactif, et un premier dérivé cellulosique hydrodispersable ou hydrosoluble, et les seconds granules peuvent comprendre du fénofibrate, de 0 % à 0,25 % en poids des seconds granules d'un second tensioactif, et un second dérivé cellulosique hydrodispersable ou hydrosoluble.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PCT/US2012/043971 WO2014003706A1 (fr) | 2012-06-25 | 2012-06-25 | Formulation de fénofibrate |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA2877901A1 true CA2877901A1 (fr) | 2014-01-03 |
Family
ID=49783663
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2877901A Abandoned CA2877901A1 (fr) | 2012-06-25 | 2012-06-25 | Formulation de fenofibrate |
Country Status (5)
| Country | Link |
|---|---|
| EP (1) | EP2863890A4 (fr) |
| BR (1) | BR112014032579A2 (fr) |
| CA (1) | CA2877901A1 (fr) |
| IN (1) | IN2014DN11044A (fr) |
| WO (1) | WO2014003706A1 (fr) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR101925590B1 (ko) * | 2016-08-30 | 2018-12-05 | 대원제약 주식회사 | 개선된 생체이용률을 갖는 페노피브릭산 제제 |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2627696B1 (fr) | 1988-02-26 | 1991-09-13 | Fournier Innovation Synergie | Nouvelle forme galenique du fenofibrate |
| US7374779B2 (en) * | 1999-02-26 | 2008-05-20 | Lipocine, Inc. | Pharmaceutical formulations and systems for improved absorption and multistage release of active agents |
| US7863331B2 (en) * | 1999-07-09 | 2011-01-04 | Ethypharm | Pharmaceutical composition containing fenofibrate and method for the preparation thereof |
| US8586094B2 (en) * | 2000-09-20 | 2013-11-19 | Jagotec Ag | Coated tablets |
| US20080241070A1 (en) * | 2000-09-21 | 2008-10-02 | Elan Pharma International Ltd. | Fenofibrate dosage forms |
| RU2007133601A (ru) * | 2005-02-10 | 2009-03-20 | Лайфсайкл Фарма А/С (Dk) | УСТОЙЧИВАЯ ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, СОДЕРЖАЩАЯ ФИКСИРОВАННУЮ ДОЗУ КОМБИНАЦИИ ФЕНОФИБРАТА И ИНГИБИТОРА HMG-CoA-РЕДУКТАЗЫ |
| EP2068837A2 (fr) * | 2006-07-28 | 2009-06-17 | Dr. Reddy's Laboratories Ltd. | Compositions pharmaceutiques granulaires |
| FR2940118B1 (fr) * | 2008-12-24 | 2013-08-09 | Ethypharm Sa | Formulation pharmaceutique de fenofibrate nanonise |
| WO2010078429A1 (fr) | 2008-12-30 | 2010-07-08 | Impax Laboratories, Inc. | Formes galéniques et procédés de fabrication de celles-ci |
| US20110217369A1 (en) * | 2009-09-03 | 2011-09-08 | Ranbaxy Laboratories Limited | Fenofibrate compositions |
-
2012
- 2012-06-25 WO PCT/US2012/043971 patent/WO2014003706A1/fr not_active Ceased
- 2012-06-25 CA CA2877901A patent/CA2877901A1/fr not_active Abandoned
- 2012-06-25 EP EP12880074.5A patent/EP2863890A4/fr not_active Withdrawn
- 2012-06-25 IN IN11044DEN2014 patent/IN2014DN11044A/en unknown
- 2012-06-25 BR BR112014032579A patent/BR112014032579A2/pt not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| EP2863890A4 (fr) | 2015-12-09 |
| EP2863890A1 (fr) | 2015-04-29 |
| WO2014003706A1 (fr) | 2014-01-03 |
| IN2014DN11044A (fr) | 2015-09-25 |
| BR112014032579A2 (pt) | 2017-06-27 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| EEER | Examination request |
Effective date: 20170608 |
|
| FZDE | Discontinued |
Effective date: 20200107 |
|
| FZDE | Discontinued |
Effective date: 20200107 |