Disclosed is a pharmaceutically acceptable oral dosage form comprising fenofibrate, phospholipid, a buffer salt, a water-soluble bulking agent selected from maltodextrin, mannitol, and combinations thereof, a cellulosic additive, beads or crystals of a pharmaceutically acceptable water-soluble excip
Disclosed is a pharmaceutically acceptable oral dosage form comprising fenofibrate, phospholipid, a buffer salt, a water-soluble bulking agent selected from maltodextrin, mannitol, and combinations thereof, a cellulosic additive, beads or crystals of a pharmaceutically acceptable water-soluble excipient support material, a polyvinylpyrrolidone or crospovidone, croscarmellose sodium, granular mannitol, sodium dodecyl sulfate, silicon dioxide, and a stearate, wherein the fenofibrate is in the form of microparticles, and wherein at least a portion of the phospholipid is coated on the surfaces of the fenofibrate microparticles, the phospholipid coated microparticles are embedded in a matrix comprising the water-soluble bulking agent, phospholipid that is not coated on the microparticles, the buffer salt and the cellulosic additive, and the matrix is coated on up to 100% of the surfaces of the beads or crystals of the excipient support material.
대표청구항▼
1. A pharmaceutically acceptable oral dosage form of fenofibrate comprising fenofibrate present in an amount of from about 15% w/w to about 20% w/w of the dosage form; phospholipid present in an amount of from about 1% w/w to about 8% w/w of the dosage form;a buffer salt present in an amount of from
1. A pharmaceutically acceptable oral dosage form of fenofibrate comprising fenofibrate present in an amount of from about 15% w/w to about 20% w/w of the dosage form; phospholipid present in an amount of from about 1% w/w to about 8% w/w of the dosage form;a buffer salt present in an amount of from about 0.1% w/w to about 0.5% w/w of the dosage forth;one or more water-soluble bulking agent selected from maltodextrin and mannitol present in an amount of from about 7% w/w to about 20% w/w of the dosage form;a cellulosic additive present in an amount of from about 3% w/w to about 8% w/w of the dosage form;beads or crystals of a pharmaceutically acceptable water-soluble excipient support material present in an amount of from about 12% w/w to 16% w/w of the dosage form;a polyvinylpyrrolidone or crospovidone present in an amount of from about 5% w/w to about 30% w/w of the dosage form;croscarmellose sodium present in an amount of from about 1% w/w to about 6% w/w of the dosage form;granular mannitol present in an amount of from about 3% w/w to about 30% w/w of the dosage form;sodium dodecyl sulfate present in an amount of from about 1% w/w to about 4% of the dosage form;silicon dioxide present in an amount of up to about 1% w/w of the dosage form; anda stearate present in an amount of up to about 1% w/w of the dosage form;wherein the fenofibrate is in the form of microparticles coated with phospholipid,wherein the phospholipid coated microparticles are embedded in a matrix comprising the water-soluble bulking agent, phospholipid that is not coated on the microparticles, the buffer salt and the cellulosic additive, andwherein the surface of the beads or crystals of the pharmaceutically acceptable water-soluble excipient is coated with the matrix. 2. The dosage form of claim 1, wherein the fenofibrate is present in an amount of from about 18% w/w to about 19.5% w/w of the tablet. 3. The dosage form of claim 1, wherein the phospholipid is present in an amount of from about 2% w/w to about 6% w/w of the tablet. 4. The dosage form of claim 1, wherein the buffer salt is present in an amount of from 0.1% w/w to about 0.2% w/w of the tablet. 5. The dosage form of claim 1, wherein the bulking agent is maltodextrin present in an amount of from about 9% w/w to about 20% w/w of the tablet. 6. The dosage form of claim 1, wherein the bulking agent is mannitol present in an amount of from about 7% w/w to about 20% w/w of the tablet. 7. The dosage form of claim 1, wherein the cellulosic additive is a carboxymethylcellulose. 8. The dosage form of claim 1, wherein the cellulosic additive is sodium carboxymethylcellulose. 9. The dosage form of claim 1, wherein the cellulosic additive is present in an amount of from about 4% w/w to about 6% w/w of the tablet. 10. The dosage form of claim 1, wherein the water-soluble excipient support material present is present in an amount of from about 14% w/w to about 15% w/w of the tablet. 11. The dosage form of claim 1, wherein the polyvinylpyrrolidone or crospovidone is present in an amount of from about 6% w/w to about 26% w/w of the tablet. 12. The dosage form of claim 1, wherein the croscarmellose sodium is present in an amount of from about 2% w/w to about 5% w/w of the tablet. 13. The dosage form of claim 1, wherein the granular mannitol is present in an amount of from about 5% w/w to about 27% w/w of the tablet. 14. The dosage form of claim 1, wherein the sodium dodecyl sulfate is present in an amount of from about 2% w/w to about 3% w/w of the tablet. 15. The dosage form of claim 1, wherein the silicon dioxide is colloidal silicon dioxide present in an amount of from about 0.5% w/w to about 0.8% w/w of the tablet. 16. The dosage form of claim 1, wherein the stearate is magnesium stearate present in an amount of from about 0.2% w/w to about 0.5% w/w of the tablet. 17. A method of treating dislipidemia or dislipoproteinemia in a mammal comprising administering to said mammal a therapeutically effective oral dosage form of claim 1. 18. The method of claim 17, wherein the dosage form provides into the blood of said mammal in a fasted state a therapeutically effective amount of said fenofibrate that is at least 90% of the area under the curve (AUC) amount of the fenofibrate provided by the dosage form into the blood of said mammal in a fed state. 19. The dosage form of claim 1, wherein fenofibrate is present in an amount of from 45 to 51 mg per tablet dosage form. 20. The dosage form of claim 19, wherein fenofibrate is present in an amount of 48 mg per tablet dosage form. 21. The dosage form of claim 1, wherein fenofibrate is present in an amount of from 135 to 155 mg per tablet dosage form. 22. The dosage form of claim 21, wherein fenofibrate is present in an amount of 144 or 145 mg per tablet dosage form. 23. The dosage form of claim 1, wherein fenofibrate is present in an amount of from 120 to 130 mg per tablet dosage form. 24. The dosage form of claim 1, which is free of food effect. 25. A suspension of microparticles consisting of 9%-10% fenofibrate,2.7%-3% Lipoid E80,10%-19% sucrose, and0%-5% sorbitol. 26. A powder comprising a lyophilized preparation of the suspension of claim 25, wherein said lypophilized preparation has a moisture content of between 0.1% and 0.3%. 27. A pharmaceutically acceptable tablet dosage form comprising the powder of claim 26, blended with 0.5% sucrose, 0.2% magnesium stearate, and 0.2% colloidal silica.
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Glamkowski Edward J. (Warren NJ) Fortunato James M. (North Wales PA), 1-(Aminoalkylphenyl and aminoalkylbenzyl)-indoles and indolines and analgesic method of use thereof.
Joshua Henry (Staten Island NY) Wilson Kenneth E. (Westfield NJ) Schwartz Michael S. (Glenside PA) Lee Ta J. (Lansdale PA) Stokker Gerald E. (Gwynedd Valley PA), 3-keto HMG-COA reductase inhibitors.
Joshua Henry (Staten Island NY) Wilson Kenneth E. (Westfield NJ) Schwartz Michael S. (Glenside PA) Lee Ta J. (Lansdale PA) Stokker Gerald E. (Gwynedd Valley PA), 3-keto HMG-CoA reductase inhibitors.
Chucholowski Alexander W. (Ypsilanti MI) Roth Bruce D. (Ann Arbor MI) Sliskovic Drago R. (Ypsilanti MI), 5-pyrimidinyl-3,5-dihydroxy-6-heptenoic acid compounds useful as inhibitors of cholesterol biosynthesis.
Chucholowski Alexander W. (Ypsilanti MI) Creswell Mark W. (Chelsea MI) Roth Bruce D. (Ann Arbor MI) Sliskovic Drago R. (Ypsilanti MI), 6-(((Substituted)pyridin-3-yl)alkyl)-and alkenyl)-tetrahydro-4-hydroxypyran-2-one inhibitors of cholesterol biosynthesis.
Chucholowski Alexander W. (Ypsilanti MI) Creswell Mark W. (Chelsea MI) Roth Bruce D. (Ann Arbor MI) Sliskovic Drago R. (Ypsilanti MI), 6-(((substituted)pyridin-3-yl)alkyl)-and alkenyl)-tetrahydro-4-hydroxypyran-2-one inhibitors of cholesterol biosynthesis.
Picard Joseph A. (Ann Arbor MI) Sliskovic Drago R. (Ypsilanti MI), 6-(2-(2-(Substituted amino)-3-quinolinyl) ethenyl and ethyl) tetrahydro-4-hydroxypyran-2-one inhibitors of cholesterol b.
Jendralla Heiner (Frankfurt am Main DEX) Wess Gnther (Erlensee DEX) Bartmann Wilhelm (Bad Soden am Taunus DEX) Beck Gerhard (Frankfurt am Main DEX), 6-phenoxymethyl-4-hydroxytetrahydropyran-2-ones and 6-thiphenoxymethyl-4-hydroxytetrahydropyran-2-ones and the correspon.
Kesseler Kurt (Soden am Taunus DEX) Bartmann Wilhelm (Soden am Taunus DEX) Wess Gnther (Erlensee DEX) Granzer Ernold (Kelkheim DEX), 7-substituted derivatives of 3,5-dihydroxyhept-6-ynoic acids and corresponding lactones and their use as hypercholeserol.
Bertolini Giorgio (Sesto San Giovanni ITX) Casagrande Cesare (Arese ITX) Santangelo Francesco (Milano ITX), Beazimidazole compounds active as inhibitors of the cholesterol biosynthesis.
Couvreur Patrick (8 ; Avenue de la Foret 1970 Wezembeek-Oppem BEX) Roland Michel (38 ; rue Tomberg 1150 Bruxelles BEX) Speiser Peter (26Wassbergerstrasse 8127 Forch CHX), Biodegradable submicroscopic particles containing a biologically active substance and compositions containing them.
Helms Gregory L. (Fanwood NJ) Horn Wendy S. (Westfield NJ) Jones E. Tracy T. (Edison NJ) Linemeyer David L. (Westfield NJ), Cholesterol lowering agents.
MacConnell John G. (Watchung NJ) Arison Byron H. (Watchung NJ) Doss George A. (Westfield NJ) Monaghan Richard L. (Somerset NJ), Cholesterol lowering compounds.
Byrne Kevin M. (West Trenton NJ) Chen Shieh-Shung T. (Morganville NJ) Kaplan Louis (New City NY) MacConnell John G. (Westfield NJ) Petuch Brian R. (Florence NJ) White Raymond F. (Palmyia VA) Arison B, Cholesterol lowering compounds produced by directed biosynthesis.
Berger Gregory D. (Belle Mead NJ) Bergstrom James D. (Neshanic NJ) Biftu Tesfaye (Westfield NJ) Bugianesi Robert L. (Colonia NJ) Burk Robert M. (Laguna Beach CA) Girotra Narindar N. (Old Bridge NJ) K, Cholesterol-lowering agents.
Dufresne Claude (East Brunswick NJ) Guarro Josep (Tarragona NJ ESX) Huang Leeyuan (Watchung NJ) Kong Yu L. (Edison NJ) Lingham Russell B. (Watchung NJ) Meinz Maria S. (Somerset NJ) Silverman Keith C., Cholesterol-lowering agents.
Bertolini Giorgio (Sesto San Giovanni) Casagrande Cesare (Arese) Santangelo Francesco (Milan ITX), Compounds active as inhibitors of the cholesterol biosynthesis.
Na George C. (Fort Washington PA) Rajagopalan Natarajan (Phoenixville PA), Formulations for nanoparticulate x-ray blood pool contrast agents using high molecular weight nonionic surfactants.
Regan John R. (Princeton NJ) Bruno Joseph G. (Sellersville PA) Neuenschwander Kent W. (Ambler PA) Kuhla Donald E. (Doylestown PA), HMG-COA reductase inhibitors.
Smith Robert L. (Lansdale PA) Halczenko Wasyl (Hatfield PA) Hartman George D. (Lansdale PA) Stokker Gerald E. (Gwynedd Valley PA) Inamine Edward S. (Rahway NJ) Hensens Otto D. (Red Bank NJ) Houck Dav, HMG-CoA reductase inhibitors.
Smith Robert L. ; Halczenko Wasyl ; Hartman George D. ; Stokker Gerald E. ; Inamine Edward S. ; Hensens Otto D. ; Houck David R. ; Lee Ta Jyh, HMG-CoA reductase inhibitors.
Monaghan Richard L. (Somerset NJ) Alberts Alfred W. (Short Hills NJ) Hoffman Carl H. (Scotch Plains NJ) Albers-Schonberg George (Princeton NJ), Hypocholesteremic fermentation products and process of preparation.
Oppenheim ; Richard Charles ; Marty ; Jennifer Joy ; Speiser ; Peter, Injectable compositions, nanoparticles useful therein, and process of manufacturing same.
Fountain Michael W. (Plainsboro NJ) Weiss Steven J. (Lawrenceville NJ) Kearns John J. (Princeton NJ) Weiner Alan L. (Plainsboro NJ) Popescu Mircea C. (Plainsboro NJ), Lipid matrix carriers for use in drug delivery systems.
Olukotun Adeove Y. (Hopewell NJ) Alexander John C. (Winnetka IL), Method for preventing a second heart attack employing an HMG CoA reductase inhibitor.
Papahadjopoulos Demetrios P. (78 Heathwood Williamsville NY 14221) Szoka ; Jr. Francis C. (375 Leroy Ave. Buffalo NY 14214), Method of encapsulating biologically active materials in lipid vesicles.
Papahadjopoulos Demetrios P. (78 Heathwood Williamsville NY 14221) Szoka ; Jr. Francis C. (375 Leroy Ave. Buffalo NY 14214), Method of encapsulating biologically active materials in lipid vesicles.
Mezei Michael (Halifax CAX) Nugent Fredric J. (Halifax CAX), Method of encapsulating biologically active materials in multilamellar lipid vesicles (MLV).
Wretlind ; Karl A. J. ; Ljungberg ; Stellan ; Hakansson ; Ivan ; Ajaxon ; Bengt M., Method of enhancing the administration of pharmalogically active agents.
Na George C. (Fort Washington PA) Rajagopalan Natarajan (Phoenixville PA), Method of making nanoparticulate X-ray blood pool contrast agents using high molecular weight nonionic surfactants.
Na George C. (Fort Washington PA) Rajagopalan Natarajan (Phoenixville PA), Method of preparing nanoparticle compositions containing charged phospholipids to reduce aggregation.
Liversidge Gary G. (West Chester PA) Phillips Christopher P. (Brandamore PA) Cundy Kenneth C. (Belmont CA), Method to reduce particle size growth during lyophilization.
Baurain Roger (Wezembeek BEX) Trouet Andre B. L. (Winksele BEX), Microcrystals comprising an active substance having an affinity for phospholipids, and at least one phospholipid, proces.
Cover William H. (Lansdale PA) Dabora Rebecca L. (Andover MA) Hong Anderson (Taipei WA TWX) Reeves Christopher (Mill Creek WA) Stieber Robert W. (Harrisonburg VA) Vinci Victor A. (Charlottesville VA), Mutant strains of Aspergillus terreus for producing 7-[1,2,6,7,8,8a(R)-hexa-hydro-2(S),6(R)-dimethyl-8(S)-hydr.
Inamine Edward S. (Rahway NJ) Hensens Otto D. (Red Bank NJ) Houck David R. (Los Alamos NM) Lee Ta J. (Lansdale PA) Smith Robert L. (Lansdale PA) Halczenko Wasyl (Hatfield PA) Hartman George D. (Lansd, Novel HMG-CoA reductase inhibitors.
Szab Anna Z. (Budapest HUX) Gal Joszef (Budapest HUX) Mrmarosi Katalin (Budapest HUX) Sebestyn Gyula (Budapest HUX) Miholics Gizella (Budapest HUX) Kovcs Mrta (Budapest HUX), Pharmaceutical composition and process for the preparation thereof.
Dingle John T. (Whittlesford GB2) Gordon John L. (Cambridge GB2) Jones Geraint (Macclesfield GB2) Knight Clive G. (Huntingdon GB2) Lowe John S. (Wilmslow GB2), Pharmaceutical compositions.
List Paul H. (Marburg DEX) Schmidt Peter C. (Marburg DEX) Steffens Klaus-Jrgen (Marburg DEX) Perschbacher Harald (Bad Homburg DEX) Kraemer Hans P. (Marburg DEX) Sedlacek Hans H. (Marburg DEX), Pharmaceutical formulation and process for its preparation.
Dietl Hans (Eichendorffstrasse 33 Bad Aibling DEX 8202), Pharmaceutical preparation containing cyclosporine(s) for intravenous administration and a process for its production.
Karanewsky Donald S. (East Windsor NJ) Biller Scott A. (Ewing NJ) Gordon Eric M. (Pennington NJ), Phosphorous-containing HMG-CoA reductase inhibitors, new intermediates and method.
Karanewsky Donald S. (East Windsor NJ) Badia Michael C. (Lawrenceville NJ) Biller Scott A. (Ewing NJ) Gordon Eric M. (Pennington NJ) Sofia Michael J. (Lawrenceville NJ), Phosphorus-containing HMG-COA reductase inhibitors, new intermediates and method.
Karanewsky Donald S. (East Windsor NJ) Badia Michael C. (Lawrenceville NJ) Biller Scott A. (Ewing NJ) Gordon Eric M. (Pennington NJ) Sofia Michael J. (Lawrenceville NJ), Phosphorus-containing HMG-CoA reductase inhibitors, new intermediates and method.
Postle Stephen R. (Brentwood GB2) Psaila Alexander (Chelmsford GB2), Photographic silver halide material containing a dye filter or a dye anti-halation layer.
Growdon John H. (Brookline MA) Wurtman Richard J. (Boston MA), Process and composition for treating disorders by administering isoxsurpine and choline.
Leclef Brigitte (Brussels BEX) Cerfontaine Patrick (Brussels BEX) Nicolas Jean-Marie (Overijse BEX) Wantier Henri (Dour BEX) Trouet Andr (Winksele Herent BEX), Process for preparing lipid microparticles.
Engh Kevin R. ; Qiu Yihong ; Reiland Thomas L., Process for preparing solid formulations of lipid-regulating agents with enhanced dissolution and absorption.
Bosch H. William (Bryn Mawr PA) Marcera Donna M. (Collegeville PA) Mueller Ronald L. (Downingtown PA) Swanson Jon R. (Macungie PA) Mishra Dinesh S. (Harleysville PA), Process for preparing therapeutic compositions containing nanoparticles.
Chagnon Mark S. (Pelham NH) Ferris John R. (Newburyport MA) Hamilton Tracy J. (Salem NH) Rudd Edwin A. (Salem NH) Carter Michelle J. (Derry NH), Solid care therapeutic compositions and methods for making same.
Kabadi Mohan B. (Marlboro NJ) Vivilecchia Richard V. (Rockaway NJ), Stabilized pharmaceutical compositions comprising an HMG-CoA reductase inhibitor compound.
Lenk Robert P. (Lambertville NJ) Fountain Michael W. (Griggstown NJ) Janoff Andrew S. (Yardley PA) Popescu Mircea C. (Plainsboro NJ) Weiss Steven J. (Hightstown NJ) Ginsberg Richard S. (Monroe Townsh, Stable plurilamellar vesicles.
Regan John R. (Princeton NJ) Bruno Joseph G. (Sellersville PA) Neuenschwander Kent W. (Ambler PA), Substituted cyclohexene derivatives as HMG-CoA reductase inhibitors.
Wong Sui-Ming (Collegeville PA) Newington Ian M. (Hazlemere GB2) Liversidge Elaine M. (West Chester PA) McIntire Gregory L. (West Chester PA) Pitt Alan R. (Sandridge GBX) Shaw Jack M. (Aberdeen MD), Sulfated nonionic block copolymer surfactants as stabilizer coatings for nanoparticle compositions.
Liversidge Gary G. (West Chester PA) Cundy Kenneth C. (Pottstown PA) Bishop John F. (Rochester NY) Czekai David A. (Honeoye Falls NY), Surface modified drug nanoparticles.
Kerc Janez,SIX ; Rebic Ljubomira Barbara,SIX ; Kofler Bojan,SIX, Three-phase pharmaceutical form with constant and controlled release of amorphous active ingredient for single daily application.
Na George C. (Fort Washington PA) Rajagopalan Natarajan (Phoenixville PA), Use of ionic cloud point modifiers to prevent particle aggregation during sterilization.
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