ES2561108T3 - Composiciones inyectables para la liberación controlada de compuesto farmacológicamente activo - Google Patents
Composiciones inyectables para la liberación controlada de compuesto farmacológicamente activo Download PDFInfo
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- ES2561108T3 ES2561108T3 ES02802160.8T ES02802160T ES2561108T3 ES 2561108 T3 ES2561108 T3 ES 2561108T3 ES 02802160 T ES02802160 T ES 02802160T ES 2561108 T3 ES2561108 T3 ES 2561108T3
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- 150000001875 compounds Chemical class 0.000 title abstract 4
- 239000007972 injectable composition Substances 0.000 title abstract 2
- 238000013270 controlled release Methods 0.000 title 1
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 abstract description 9
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 abstract description 6
- 150000003839 salts Chemical class 0.000 abstract description 3
- 239000002253 acid Substances 0.000 abstract 6
- 239000000203 mixture Substances 0.000 abstract 4
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 abstract 3
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 abstract 2
- 150000007513 acids Chemical class 0.000 abstract 2
- CXMXRPHRNRROMY-UHFFFAOYSA-N sebacic acid Chemical compound OC(=O)CCCCCCCCC(O)=O CXMXRPHRNRROMY-UHFFFAOYSA-N 0.000 abstract 2
- URAYPUMNDPQOKB-UHFFFAOYSA-N triacetin Chemical compound CC(=O)OCC(OC(C)=O)COC(C)=O URAYPUMNDPQOKB-UHFFFAOYSA-N 0.000 abstract 2
- FCGXLCNBWYIEAA-UHFFFAOYSA-N 1,3-benzothiazol-6-ylmethanamine Chemical compound NCC1=CC=C2N=CSC2=C1 FCGXLCNBWYIEAA-UHFFFAOYSA-N 0.000 abstract 1
- 208000004998 Abdominal Pain Diseases 0.000 abstract 1
- 208000002881 Colic Diseases 0.000 abstract 1
- 241000124008 Mammalia Species 0.000 abstract 1
- SECXISVLQFMRJM-UHFFFAOYSA-N N-Methylpyrrolidone Chemical compound CN1CCCC1=O SECXISVLQFMRJM-UHFFFAOYSA-N 0.000 abstract 1
- 239000002202 Polyethylene glycol Substances 0.000 abstract 1
- 239000001089 [(2R)-oxolan-2-yl]methanol Substances 0.000 abstract 1
- 150000001991 dicarboxylic acids Chemical class 0.000 abstract 1
- 239000001087 glyceryl triacetate Substances 0.000 abstract 1
- 235000013773 glyceryl triacetate Nutrition 0.000 abstract 1
- 239000003960 organic solvent Substances 0.000 abstract 1
- 229920001223 polyethylene glycol Polymers 0.000 abstract 1
- 239000002244 precipitate Substances 0.000 abstract 1
- HNJBEVLQSNELDL-UHFFFAOYSA-N pyrrolidin-2-one Chemical compound O=C1CCCN1 HNJBEVLQSNELDL-UHFFFAOYSA-N 0.000 abstract 1
- 229920006395 saturated elastomer Polymers 0.000 abstract 1
- 235000003441 saturated fatty acids Nutrition 0.000 abstract 1
- 150000004671 saturated fatty acids Chemical class 0.000 abstract 1
- -1 sebacic acid) Chemical class 0.000 abstract 1
- 239000002904 solvent Substances 0.000 abstract 1
- BSYVTEYKTMYBMK-UHFFFAOYSA-N tetrahydrofurfuryl alcohol Chemical compound OCC1CCCO1 BSYVTEYKTMYBMK-UHFFFAOYSA-N 0.000 abstract 1
- 229960002622 triacetin Drugs 0.000 abstract 1
- 235000021122 unsaturated fatty acids Nutrition 0.000 abstract 1
- 150000004670 unsaturated fatty acids Chemical class 0.000 abstract 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 3
- OYHQOLUKZRVURQ-HZJYTTRNSA-N Linoleic acid Chemical compound CCCCC\C=C/C\C=C/CCCCCCCC(O)=O OYHQOLUKZRVURQ-HZJYTTRNSA-N 0.000 description 2
- 125000003277 amino group Chemical group 0.000 description 2
- OYHQOLUKZRVURQ-IXWMQOLASA-N linoleic acid Natural products CCCCC\C=C/C\C=C\CCCCCCCC(O)=O OYHQOLUKZRVURQ-IXWMQOLASA-N 0.000 description 2
- 235000020778 linoleic acid Nutrition 0.000 description 2
- RXZBMPWDPOLZGW-XMRMVWPWSA-N (E)-roxithromycin Chemical compound O([C@@H]1[C@@H](C)C(=O)O[C@@H]([C@@]([C@H](O)[C@@H](C)C(=N/OCOCCOC)/[C@H](C)C[C@@](C)(O)[C@H](O[C@H]2[C@@H]([C@H](C[C@@H](C)O2)N(C)C)O)[C@H]1C)(C)O)CC)[C@H]1C[C@@](C)(OC)[C@@H](O)[C@H](C)O1 RXZBMPWDPOLZGW-XMRMVWPWSA-N 0.000 description 1
- 241000894006 Bacteria Species 0.000 description 1
- 241000283690 Bos taurus Species 0.000 description 1
- 108090000790 Enzymes Proteins 0.000 description 1
- 102000004190 Enzymes Human genes 0.000 description 1
- 230000000843 anti-fungal effect Effects 0.000 description 1
- 229940121375 antifungal agent Drugs 0.000 description 1
- 108010017796 epoxidase Proteins 0.000 description 1
- 230000008686 ergosterol biosynthesis Effects 0.000 description 1
- 230000002538 fungal effect Effects 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- QQONPFPTGQHPMA-UHFFFAOYSA-N propylene Natural products CC=C QQONPFPTGQHPMA-UHFFFAOYSA-N 0.000 description 1
- 125000004805 propylene group Chemical group [H]C([H])([H])C([H])([*:1])C([H])([H])[*:2] 0.000 description 1
- 208000023504 respiratory system disease Diseases 0.000 description 1
- 229960005224 roxithromycin Drugs 0.000 description 1
- JTSDBFGMPLKDCD-XVFHVFLVSA-N tilmicosin Chemical compound O([C@@H]1[C@@H](C)[C@H](O)CC(=O)O[C@@H]([C@H](/C=C(\C)/C=C/C(=O)[C@H](C)C[C@@H]1CCN1C[C@H](C)C[C@H](C)C1)CO[C@H]1[C@@H]([C@H](OC)[C@H](O)[C@@H](C)O1)OC)CC)[C@@H]1O[C@H](C)[C@@H](O)[C@H](N(C)C)[C@H]1O JTSDBFGMPLKDCD-XVFHVFLVSA-N 0.000 description 1
- 229960000223 tilmicosin Drugs 0.000 description 1
Classifications
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
- A61K31/235—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group
- A61K31/24—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group having an amino or nitro group
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
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- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
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- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
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- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/12—Carboxylic acids; Salts or anhydrides thereof
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- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/14—Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
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- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/20—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
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- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/22—Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
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- A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
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- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
- A61K9/0024—Solid, semi-solid or solidifying implants, which are implanted or injected in body tissue
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Cardiology (AREA)
- Molecular Biology (AREA)
- Heart & Thoracic Surgery (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Neurosurgery (AREA)
- Anesthesiology (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Dermatology (AREA)
- Emergency Medicine (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
Abstract
Una composición para administración de un compuesto farmacológicamente activo a un mamífero que comprende una sal de un compuesto farmacológicamente activo básico y un ácido lipófilo, en la que el ácido lipófilo está seleccionado del grupo que consiste en ácidos grasos saturados o insaturados, ácidos cólicos, ácidos fosfatídicos, ácidos dicarboxílicos (como ácido sebácico), ácido polisebácico y ácido polibenzoico; y un disolvente farmacéuticamente aceptable orgánico, en el que el disolvente farmacéuticamente aceptable está seleccionado del grupo que consiste en uno o una combinación de: pirrolidona, N-metilpirrolidona, polietilenglicol, propilenglicol, glicerol formal, éter dimetílico de isosorbida, etanol, sulfóxido de dimetilo, alcohol tetrahidrofurfurílico y triacetina; combinados juntos para formar una composición inyectable, en la que la composición forma un precipitado cuando la composición se introduce o inyecta en un entorno acuoso y en la que la composición libera el compuesto activo con el tiempo cuando se introduce o inyecta en el entorno acuoso.
Description
Es eficaz contra un amplio intervalo de bacterias, y se usa para el tratamiento de enfermedades respiratorias en el ganado vacuno. El grupo amina de la roxitromicina se neutralizó con ácido linoleico en 10 % de propileno en glicerol 5 formal, produciendo una disolución transparente a 200 mg/ml. Al igual que en el caso de la tilmicosina, la sal precipitó cuando la disolución se enriqueció en agua.
10 La turbinafina es un antifúngico y la estructura es como se muestra a continuación:
La turbinafina es un inhibidor específico de la escualina epoxidasa, una enzima clave en la biosíntesis del ergosterol
15 fúngico. El grupo amina de la turbinafina se neutralizó con ácido linoleico en 10 % de propilenglicol en glicerol formal, produciendo una disolución transparente a 150 mg/ml. La sal resultante fue altamente insoluble en agua, y precipitó cuando se enriqueció en agua.
Otras realizaciones se exponen dentro de las siguientes reivindicaciones. 20
10
Claims (1)
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imagen1 imagen2 imagen3
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US34362501P | 2001-10-19 | 2001-10-19 | |
US343625P | 2001-10-19 | ||
PCT/US2002/033300 WO2003034988A2 (en) | 2001-10-19 | 2002-10-18 | Injectable compositions for the controlled delivery of pharmacologically active compound |
Publications (1)
Publication Number | Publication Date |
---|---|
ES2561108T3 true ES2561108T3 (es) | 2016-02-24 |
Family
ID=23346878
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ES02802160.8T Expired - Lifetime ES2561108T3 (es) | 2001-10-19 | 2002-10-18 | Composiciones inyectables para la liberación controlada de compuesto farmacológicamente activo |
Country Status (16)
Country | Link |
---|---|
US (4) | US6887487B2 (es) |
EP (1) | EP1446103B1 (es) |
JP (1) | JP4850390B2 (es) |
CN (2) | CN1607937A (es) |
AU (1) | AU2002335077B2 (es) |
BG (1) | BG108634A (es) |
BR (1) | BRPI0213425B8 (es) |
CA (1) | CA2463896C (es) |
ES (1) | ES2561108T3 (es) |
IL (1) | IL160282A (es) |
MX (1) | MXPA04003608A (es) |
NZ (1) | NZ531460A (es) |
PL (1) | PL211116B1 (es) |
RU (1) | RU2292871C2 (es) |
WO (1) | WO2003034988A2 (es) |
ZA (1) | ZA200401076B (es) |
Families Citing this family (34)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US6946137B2 (en) * | 2001-10-19 | 2005-09-20 | Idexx Laboratories, Inc. | Methods for the controlled delivery of pharmacologically active compounds |
CN1607937A (zh) * | 2001-10-19 | 2005-04-20 | 爱德士实验室公司 | 用于药理活性化合物的可控释放的可注射组合物 |
US20070060604A1 (en) * | 2002-03-25 | 2007-03-15 | Council Of Scientific And Industrial Research | Antibiotic pharmaceutical composition with lysergol as bio-enhancer and method of treatment |
US20050049210A1 (en) * | 2003-08-27 | 2005-03-03 | Idexx Laboratories, Inc. | Methods for the controlled delivery of pharmacologically active compounds |
US7858115B2 (en) * | 2004-06-24 | 2010-12-28 | Idexx Laboratories | Phospholipid gel compositions for drug delivery and methods of treating conditions using same |
US7618651B2 (en) | 2004-06-24 | 2009-11-17 | Idexx Laboratories | Pharmaceutical compositions for drug delivery and methods of treating or preventing conditions using same |
US7854943B2 (en) | 2004-06-24 | 2010-12-21 | Idexx Laboratories | Phospholipid gel compositions for drug delivery and methods of treating conditions using same |
JP5144267B2 (ja) * | 2004-10-28 | 2013-02-13 | アイデックス ラボラトリーズ,インコーポレイティド | 医薬活性化合物を制御して搬送するための組成物 |
US7282487B2 (en) * | 2004-10-28 | 2007-10-16 | Idexx Laboratories | Method for treating bacterial infections in horses or pigs with tilmicosin |
WO2007016153A2 (en) * | 2005-07-28 | 2007-02-08 | Eli Lilly And Company | Tilmicosin formulation |
US8114440B2 (en) * | 2005-11-16 | 2012-02-14 | Idexx Laboratories Inc. | Pharmaceutical compositions for the administration of aptamers |
US7754679B2 (en) * | 2005-11-16 | 2010-07-13 | Idexx Laboratories, Inc. | Pharmaceutical compositions for the administration of aptamers |
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-
2002
- 2002-10-18 CN CNA028192842A patent/CN1607937A/zh active Pending
- 2002-10-18 AU AU2002335077A patent/AU2002335077B2/en not_active Expired
- 2002-10-18 US US10/274,445 patent/US6887487B2/en not_active Expired - Lifetime
- 2002-10-18 ES ES02802160.8T patent/ES2561108T3/es not_active Expired - Lifetime
- 2002-10-18 PL PL368338A patent/PL211116B1/pl unknown
- 2002-10-18 CN CN201010124253.1A patent/CN101785861B/zh not_active Expired - Lifetime
- 2002-10-18 NZ NZ531460A patent/NZ531460A/en not_active IP Right Cessation
- 2002-10-18 EP EP02802160.8A patent/EP1446103B1/en not_active Expired - Lifetime
- 2002-10-18 WO PCT/US2002/033300 patent/WO2003034988A2/en active IP Right Grant
- 2002-10-18 RU RU2004115103/15A patent/RU2292871C2/ru active
- 2002-10-18 BR BRPI0213425A patent/BRPI0213425B8/pt not_active IP Right Cessation
- 2002-10-18 CA CA2463896A patent/CA2463896C/en not_active Expired - Lifetime
- 2002-10-18 JP JP2003537557A patent/JP4850390B2/ja not_active Expired - Lifetime
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2003
- 2003-03-28 US US10/403,100 patent/US7033599B2/en not_active Expired - Fee Related
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2004
- 2004-02-09 IL IL160282A patent/IL160282A/en active IP Right Grant
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- 2004-03-16 BG BG108634A patent/BG108634A/xx unknown
- 2004-04-16 MX MXPA04003608A patent/MXPA04003608A/es active IP Right Grant
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2005
- 2005-03-25 US US11/088,922 patent/US7404964B2/en active Active
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2007
- 2007-01-31 US US11/700,068 patent/US20070141162A1/en not_active Abandoned
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PL211116B1 (pl) | 2012-04-30 |
WO2003034988A2 (en) | 2003-05-01 |
CN1607937A (zh) | 2005-04-20 |
US20030130211A1 (en) | 2003-07-10 |
CA2463896A1 (en) | 2003-05-01 |
US7404964B2 (en) | 2008-07-29 |
ZA200401076B (en) | 2005-06-29 |
US6887487B2 (en) | 2005-05-03 |
US20050075296A1 (en) | 2005-04-07 |
EP1446103A2 (en) | 2004-08-18 |
EP1446103B1 (en) | 2015-12-23 |
PL368338A1 (en) | 2005-03-21 |
RU2004115103A (ru) | 2005-03-20 |
US7033599B2 (en) | 2006-04-25 |
BRPI0213425B8 (pt) | 2021-05-25 |
BR0213425A (pt) | 2004-12-14 |
JP4850390B2 (ja) | 2012-01-11 |
MXPA04003608A (es) | 2004-07-27 |
RU2292871C2 (ru) | 2007-02-10 |
CN101785861B (zh) | 2014-08-13 |
EP1446103A4 (en) | 2011-01-12 |
AU2002335077B2 (en) | 2006-09-07 |
JP2005506992A (ja) | 2005-03-10 |
BRPI0213425B1 (pt) | 2020-01-28 |
US20050163859A1 (en) | 2005-07-28 |
BG108634A (en) | 2005-04-30 |
WO2003034988A3 (en) | 2003-07-31 |
CA2463896C (en) | 2010-05-04 |
US20070141162A1 (en) | 2007-06-21 |
IL160282A (en) | 2009-11-18 |
CN101785861A (zh) | 2010-07-28 |
NZ531460A (en) | 2005-05-27 |
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