AU2001255515A1 - Stabilised fibrate microparticles - Google Patents
Stabilised fibrate microparticlesInfo
- Publication number
- AU2001255515A1 AU2001255515A1 AU2001255515A AU5551501A AU2001255515A1 AU 2001255515 A1 AU2001255515 A1 AU 2001255515A1 AU 2001255515 A AU2001255515 A AU 2001255515A AU 5551501 A AU5551501 A AU 5551501A AU 2001255515 A1 AU2001255515 A1 AU 2001255515A1
- Authority
- AU
- Australia
- Prior art keywords
- fenofibrate
- microparticles
- composition
- dosage form
- phospholipid
- 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
- 239000011859 microparticle Substances 0.000 title claims abstract description 128
- 229940125753 fibrate Drugs 0.000 title claims abstract description 81
- 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 claims abstract description 468
- 229960002297 fenofibrate Drugs 0.000 claims abstract description 452
- 239000000203 mixture Substances 0.000 claims abstract description 272
- 238000000034 method Methods 0.000 claims abstract description 202
- 150000003904 phospholipids Chemical class 0.000 claims abstract description 194
- 239000004094 surface-active agent Substances 0.000 claims abstract description 153
- 239000002552 dosage form Substances 0.000 claims abstract description 118
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- 238000011282 treatment Methods 0.000 claims abstract description 41
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- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 26
- 239000006186 oral dosage form Substances 0.000 claims abstract description 17
- 241000124008 Mammalia Species 0.000 claims abstract description 16
- 239000002245 particle Substances 0.000 claims description 331
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 142
- 230000008569 process Effects 0.000 claims description 131
- 239000006185 dispersion Substances 0.000 claims description 115
- 239000000725 suspension Substances 0.000 claims description 103
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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 claims description 43
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- 239000000126 substance Substances 0.000 claims description 42
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 39
- 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 claims description 35
- 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 claims description 35
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- 235000000346 sugar Nutrition 0.000 claims description 23
- 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 claims description 22
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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 claims description 12
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- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 9
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- 229930091371 Fructose Natural products 0.000 claims description 8
- RFSUNEUAIZKAJO-ARQDHWQXSA-N Fructose Chemical compound OC[C@H]1O[C@](O)(CO)[C@@H](O)[C@@H]1O RFSUNEUAIZKAJO-ARQDHWQXSA-N 0.000 claims description 8
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- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 claims description 8
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 claims description 8
- 239000008121 dextrose Substances 0.000 claims description 8
- BPHQZTVXXXJVHI-UHFFFAOYSA-N dimyristoyl phosphatidylglycerol Chemical compound CCCCCCCCCCCCCC(=O)OCC(COP(O)(=O)OCC(O)CO)OC(=O)CCCCCCCCCCCCC BPHQZTVXXXJVHI-UHFFFAOYSA-N 0.000 claims description 8
- 150000002016 disaccharides Chemical class 0.000 claims description 8
- 150000002402 hexoses Chemical class 0.000 claims description 8
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 claims description 8
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- 235000010447 xylitol Nutrition 0.000 claims description 8
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 claims description 8
- 229960002675 xylitol Drugs 0.000 claims description 8
- 229910019142 PO4 Inorganic materials 0.000 claims description 7
- MUPFEKGTMRGPLJ-RMMQSMQOSA-N Raffinose Natural products O(C[C@H]1[C@@H](O)[C@H](O)[C@@H](O)[C@@H](O[C@@]2(CO)[C@H](O)[C@@H](O)[C@@H](CO)O2)O1)[C@@H]1[C@H](O)[C@@H](O)[C@@H](O)[C@@H](CO)O1 MUPFEKGTMRGPLJ-RMMQSMQOSA-N 0.000 claims description 7
- MUPFEKGTMRGPLJ-UHFFFAOYSA-N UNPD196149 Natural products OC1C(O)C(CO)OC1(CO)OC1C(O)C(O)C(O)C(COC2C(C(O)C(O)C(CO)O2)O)O1 MUPFEKGTMRGPLJ-UHFFFAOYSA-N 0.000 claims description 7
- 239000010452 phosphate Substances 0.000 claims description 7
- 229920000642 polymer Polymers 0.000 claims description 7
- MUPFEKGTMRGPLJ-ZQSKZDJDSA-N raffinose 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[C@@H]2[C@@H]([C@@H](O)[C@@H](O)[C@@H](CO)O2)O)O1 MUPFEKGTMRGPLJ-ZQSKZDJDSA-N 0.000 claims description 7
- 208000031226 Hyperlipidaemia Diseases 0.000 claims description 6
- JLPULHDHAOZNQI-JLOPVYAASA-N [(2r)-3-hexadecanoyloxy-2-[(9e,12e)-octadeca-9,12-dienoyl]oxypropyl] 2-(trimethylazaniumyl)ethyl phosphate Chemical class CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCCCCCC\C=C\C\C=C\CCCCC JLPULHDHAOZNQI-JLOPVYAASA-N 0.000 claims description 6
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- 208000035150 Hypercholesterolemia Diseases 0.000 claims description 3
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- 125000002467 phosphate group Chemical group [H]OP(=O)(O[H])O[*] 0.000 claims 4
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- 230000008901 benefit Effects 0.000 description 16
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- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 16
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Landscapes
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| US60241761 | 2000-10-20 | ||
| PCT/US2001/012826 WO2002024193A1 (en) | 2000-09-20 | 2001-04-20 | Stabilised fibrate microparticles |
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| US20070231402A1 (en) * | 1994-08-02 | 2007-10-04 | Immunopath Profile, Inc. | Therapeutic stem cell composition and stimulant, facilitator, accelerator, and synergizer thereof, growth factor, anti-inflammatory composition and uses thereof |
| US20050004049A1 (en) * | 1997-03-11 | 2005-01-06 | Elan Pharma International Limited | Novel griseofulvin compositions |
| US20080113025A1 (en) * | 1998-11-02 | 2008-05-15 | Elan Pharma International Limited | Compositions comprising nanoparticulate naproxen and controlled release hydrocodone |
| US20070160675A1 (en) * | 1998-11-02 | 2007-07-12 | Elan Corporation, Plc | Nanoparticulate and controlled release compositions comprising a cephalosporin |
| US20070037777A1 (en) * | 2005-08-12 | 2007-02-15 | Immunopath Profile, Inc. | Lipid-containing compositions and methods of using them |
| US20090274660A1 (en) * | 1999-08-17 | 2009-11-05 | Immunopath Profile, Inc. | Pluripotent therapeutic compositions and uses thereof |
| US7790678B1 (en) * | 1999-08-17 | 2010-09-07 | Immunopath Profile, Inc. | Composition with anti-inflammatory, protein synthesizing, enzyme deficiency activating genetic therapy and anti-cancer activity and methods of use |
| 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 |
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-
2001
- 2001-04-20 TW TW090109549A patent/TWI354568B/zh not_active IP Right Cessation
- 2001-04-20 JP JP2002528263A patent/JP2004509146A/ja active Pending
- 2001-04-20 CA CA2423336A patent/CA2423336C/en not_active Expired - Fee Related
- 2001-04-20 WO PCT/US2001/012826 patent/WO2002024193A1/en not_active Ceased
- 2001-04-20 ES ES01928684T patent/ES2372746T3/es not_active Expired - Lifetime
- 2001-04-20 EP EP01928684A patent/EP1320362B1/en not_active Expired - Lifetime
- 2001-04-20 AT AT01928684T patent/ATE522211T1/de not_active IP Right Cessation
- 2001-04-20 US US09/838,541 patent/US20020058065A1/en not_active Abandoned
- 2001-04-20 AU AU2001255515A patent/AU2001255515A1/en not_active Abandoned
- 2001-04-20 NZ NZ525231A patent/NZ525231A/en not_active IP Right Cessation
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2003
- 2003-05-19 US US10/440,368 patent/US20030194442A1/en not_active Abandoned
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| Publication number | Publication date |
|---|---|
| CA2423336A1 (en) | 2002-03-28 |
| CA2423336C (en) | 2011-03-08 |
| JP2004509146A (ja) | 2004-03-25 |
| ATE522211T1 (de) | 2011-09-15 |
| WO2002024193A1 (en) | 2002-03-28 |
| AU2007201953A1 (en) | 2007-05-24 |
| ES2372746T3 (es) | 2012-01-26 |
| AU2007201953B2 (en) | 2009-08-13 |
| US20020058065A1 (en) | 2002-05-16 |
| EP1320362B1 (en) | 2011-08-31 |
| EP1320362A1 (en) | 2003-06-25 |
| NZ525231A (en) | 2004-08-27 |
| US20030194442A1 (en) | 2003-10-16 |
| TWI354568B (en) | 2011-12-21 |
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