JP2006511536A - 水貧溶性薬物のバイオアベイラビリティーを改善する自由流動性固形製剤およびその製造方法 - Google Patents
水貧溶性薬物のバイオアベイラビリティーを改善する自由流動性固形製剤およびその製造方法 Download PDFInfo
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- OIALAIQRYISUEV-UHFFFAOYSA-N 2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-(2-hydroxyethoxy)ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]e Polymers CCCCCCCCCCCCCCCCCC(=O)OCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCO OIALAIQRYISUEV-UHFFFAOYSA-N 0.000 description 4
- 229920002685 Polyoxyl 35CastorOil Polymers 0.000 description 4
- 235000019359 magnesium stearate Nutrition 0.000 description 4
- 238000012360 testing method Methods 0.000 description 4
- 230000002378 acidificating effect Effects 0.000 description 3
- 239000000839 emulsion Substances 0.000 description 3
- 210000004051 gastric juice Anatomy 0.000 description 3
- 238000011068 loading method Methods 0.000 description 3
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- 239000011782 vitamin Substances 0.000 description 3
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- 229940088594 vitamin Drugs 0.000 description 3
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- LSNNMFCWUKXFEE-UHFFFAOYSA-M Bisulfite Chemical compound OS([O-])=O LSNNMFCWUKXFEE-UHFFFAOYSA-M 0.000 description 2
- 229920000168 Microcrystalline cellulose Polymers 0.000 description 2
- 229920002675 Polyoxyl Polymers 0.000 description 2
- 235000021355 Stearic acid Nutrition 0.000 description 2
- WPMWEFXCIYCJSA-UHFFFAOYSA-N Tetraethylene glycol monododecyl ether Chemical compound CCCCCCCCCCCCOCCOCCOCCOCCO WPMWEFXCIYCJSA-UHFFFAOYSA-N 0.000 description 2
- 239000001506 calcium phosphate Substances 0.000 description 2
- 150000001735 carboxylic acids Chemical class 0.000 description 2
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- 238000004090 dissolution Methods 0.000 description 2
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- 235000013355 food flavoring agent Nutrition 0.000 description 2
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- 238000005469 granulation Methods 0.000 description 2
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- 238000004128 high performance liquid chromatography Methods 0.000 description 2
- 125000000400 lauroyl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 2
- 239000012669 liquid formulation Substances 0.000 description 2
- 239000008108 microcrystalline cellulose Substances 0.000 description 2
- 229940016286 microcrystalline cellulose Drugs 0.000 description 2
- 235000019813 microcrystalline cellulose Nutrition 0.000 description 2
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 2
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 2
- 239000008194 pharmaceutical composition Substances 0.000 description 2
- 239000003755 preservative agent Substances 0.000 description 2
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- OYHQOLUKZRVURQ-NTGFUMLPSA-N (9Z,12Z)-9,10,12,13-tetratritiooctadeca-9,12-dienoic acid Chemical compound C(CCCCCCC\C(=C(/C\C(=C(/CCCCC)\[3H])\[3H])\[3H])\[3H])(=O)O OYHQOLUKZRVURQ-NTGFUMLPSA-N 0.000 description 1
- 235000019739 Dicalciumphosphate Nutrition 0.000 description 1
- 238000010268 HPLC based assay Methods 0.000 description 1
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- 241000124008 Mammalia Species 0.000 description 1
- 235000004443 Ricinus communis Nutrition 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 239000013543 active substance Substances 0.000 description 1
- 125000003277 amino group Chemical group 0.000 description 1
- 239000002260 anti-inflammatory agent Substances 0.000 description 1
- 229940121363 anti-inflammatory agent Drugs 0.000 description 1
- 238000013459 approach Methods 0.000 description 1
- 239000012736 aqueous medium Substances 0.000 description 1
- 229910000389 calcium phosphate Inorganic materials 0.000 description 1
- 235000011010 calcium phosphates Nutrition 0.000 description 1
- 239000000969 carrier Substances 0.000 description 1
- 239000003086 colorant Substances 0.000 description 1
- 238000001816 cooling Methods 0.000 description 1
- 239000002537 cosmetic Substances 0.000 description 1
- NEFBYIFKOOEVPA-UHFFFAOYSA-K dicalcium phosphate Chemical compound [Ca+2].[Ca+2].[O-]P([O-])([O-])=O NEFBYIFKOOEVPA-UHFFFAOYSA-K 0.000 description 1
- 229910000390 dicalcium phosphate Inorganic materials 0.000 description 1
- 229940038472 dicalcium phosphate Drugs 0.000 description 1
- 235000015872 dietary supplement Nutrition 0.000 description 1
- 238000007922 dissolution test Methods 0.000 description 1
- 238000001647 drug administration Methods 0.000 description 1
- 238000012377 drug delivery Methods 0.000 description 1
- 239000008157 edible vegetable oil Substances 0.000 description 1
- 230000037406 food intake Effects 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 239000005414 inactive ingredient Substances 0.000 description 1
- 238000010348 incorporation Methods 0.000 description 1
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- 239000007924 injection Substances 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
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- 239000002609 medium Substances 0.000 description 1
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- 230000004048 modification Effects 0.000 description 1
- 239000003921 oil Substances 0.000 description 1
- 229960000273 oxametacin Drugs 0.000 description 1
- QUANRIQJNFHVEU-UHFFFAOYSA-N oxirane;propane-1,2,3-triol Chemical compound C1CO1.OCC(O)CO QUANRIQJNFHVEU-UHFFFAOYSA-N 0.000 description 1
- 230000035515 penetration Effects 0.000 description 1
- 239000008389 polyethoxylated castor oil Substances 0.000 description 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 1
- 230000003381 solubilizing effect Effects 0.000 description 1
- 150000003431 steroids Chemical group 0.000 description 1
- 230000001839 systemic circulation 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
- 235000019155 vitamin A Nutrition 0.000 description 1
- 239000011719 vitamin A Substances 0.000 description 1
- 235000019165 vitamin E Nutrition 0.000 description 1
- 239000011709 vitamin E Substances 0.000 description 1
- 239000000341 volatile oil Substances 0.000 description 1
- 229940072168 zocor Drugs 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
- A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
- A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
-
- 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
- A61K9/06—Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
-
- 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
- A61K9/1611—Inorganic compounds
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
- A61K9/2077—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
-
- 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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Inorganic Chemistry (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US10/317,657 US20040115226A1 (en) | 2002-12-12 | 2002-12-12 | Free-flowing solid formulations with improved bio-availability of poorly water soluble drugs and process for making the same |
| PCT/US2003/038979 WO2004054540A2 (en) | 2002-12-12 | 2003-12-09 | Solid compositions with improved bio-availability of insoluble or poorly water soluble drugs and a corresponding process for preparing such |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2006511536A true JP2006511536A (ja) | 2006-04-06 |
| JP2006511536A5 JP2006511536A5 (enExample) | 2006-09-21 |
Family
ID=32506185
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2004560372A Pending JP2006511536A (ja) | 2002-12-12 | 2003-12-09 | 水貧溶性薬物のバイオアベイラビリティーを改善する自由流動性固形製剤およびその製造方法 |
Country Status (4)
| Country | Link |
|---|---|
| US (3) | US20040115226A1 (enExample) |
| JP (1) | JP2006511536A (enExample) |
| AU (1) | AU2003300833A1 (enExample) |
| WO (1) | WO2004054540A2 (enExample) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2007191396A (ja) * | 2005-01-07 | 2007-08-02 | Rohto Pharmaceut Co Ltd | 皮膚外用剤 |
| JP2022520361A (ja) * | 2019-02-12 | 2022-03-30 | スミトモ ダイニッポン ファーマ オンコロジー， インコーポレイテッド | 複素環式タンパク質キナーゼ阻害剤を含む製剤 |
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| WO2005016312A1 (en) | 2003-08-13 | 2005-02-24 | Nobex Corporation | Micro-particle fatty acid salt solid dosage formulations for therapeutic agents |
| CA2536283A1 (en) * | 2003-08-20 | 2005-03-03 | Ajinomoto Co., Inc. | Pharmaceutical preparations having an improved solubility |
| US20050220825A1 (en) * | 2004-03-10 | 2005-10-06 | Adrian Funke | Molecular dispersions of drospirenone |
| WO2005105040A2 (en) * | 2004-04-26 | 2005-11-10 | Micelle Products, Inc. | Water-soluble formulations of fat soluble vitamins and pharmaceutical agents and their applications |
| GB0612809D0 (en) * | 2006-06-28 | 2006-08-09 | Univ Sunderland | Formulation |
| US20100061969A1 (en) * | 2006-11-22 | 2010-03-11 | Asahi Kasei Pharma Corporation | Dietary supplement, anti-fatigue agent or physical endurance enhancer, functional food, or cosmetic |
| WO2009070978A1 (fr) * | 2007-11-22 | 2009-06-11 | Yu He | Libération rapide dans la cavité buccale des produits de santé et procédé de préparation associé |
| EP2111854A1 (en) | 2008-04-22 | 2009-10-28 | Lek Pharmaceuticals D.D. | Self-microemulsifying systems incorporated into liquid core microcapsules |
| EP2400840A4 (en) * | 2009-02-24 | 2012-08-01 | Madeira Therapeutics | LIQUID STATINE FORMULATIONS |
| ES2363964B1 (es) | 2009-11-20 | 2012-08-22 | Gp Pharm, S.A. | Cápsulas de principios activos farmacéuticos y ésteres de ácidos grasos poliinsaturados. |
| ES2363965B1 (es) | 2009-11-20 | 2013-01-24 | Gp Pharm S.A. | Cápsulas de principios activos betabloqueantes y ésteres de ácidos grasos poliinsaturados. |
| US20110160168A1 (en) | 2009-12-31 | 2011-06-30 | Differential Drug Development Associates, Llc | Modulation of solubility, stability, absorption, metabolism, and pharmacokinetic profile of lipophilic drugs by sterols |
| CN103228266B (zh) | 2010-10-29 | 2017-11-14 | 健康科学西部大学 | 三元混合物制剂 |
| US20130045958A1 (en) | 2011-05-13 | 2013-02-21 | Trimel Pharmaceuticals Corporation | Intranasal 0.15% and 0.24% testosterone gel formulations and use thereof for treating anorgasmia or hypoactive sexual desire disorder |
| US9757388B2 (en) | 2011-05-13 | 2017-09-12 | Acerus Pharmaceuticals Srl | Intranasal methods of treating women for anorgasmia with 0.6% and 0.72% testosterone gels |
| AR086400A1 (es) | 2011-05-13 | 2013-12-11 | Trimel Pharmaceuticals Corp | Formulaciones en gel intranasal de testosterona en dosis de menor potencia y uso de las mismas para el tratamiento de la anorgasmia o el trastorno de deseo sexual hipoactivo |
| US9301920B2 (en) | 2012-06-18 | 2016-04-05 | Therapeuticsmd, Inc. | Natural combination hormone replacement formulations and therapies |
| RS62297B1 (sr) | 2011-11-23 | 2021-09-30 | Therapeuticsmd Inc | Prirodne kombinovane hormonske supstitucione formulacije i terapije |
| EA201791738A1 (ru) | 2012-05-09 | 2018-03-30 | Вестерн Юниверсити Оф Хелт Сайенсиз | Пролипосомальные композиции тестостерона |
| US10806740B2 (en) | 2012-06-18 | 2020-10-20 | Therapeuticsmd, Inc. | Natural combination hormone replacement formulations and therapies |
| US20150196640A1 (en) | 2012-06-18 | 2015-07-16 | Therapeuticsmd, Inc. | Progesterone formulations having a desirable pk profile |
| US20130338122A1 (en) | 2012-06-18 | 2013-12-19 | Therapeuticsmd, Inc. | Transdermal hormone replacement therapies |
| US10806697B2 (en) | 2012-12-21 | 2020-10-20 | Therapeuticsmd, Inc. | Vaginal inserted estradiol pharmaceutical compositions and methods |
| US11266661B2 (en) | 2012-12-21 | 2022-03-08 | Therapeuticsmd, Inc. | Vaginal inserted estradiol pharmaceutical compositions and methods |
| US10471072B2 (en) | 2012-12-21 | 2019-11-12 | Therapeuticsmd, Inc. | Vaginal inserted estradiol pharmaceutical compositions and methods |
| US10568891B2 (en) | 2012-12-21 | 2020-02-25 | Therapeuticsmd, Inc. | Vaginal inserted estradiol pharmaceutical compositions and methods |
| US11246875B2 (en) | 2012-12-21 | 2022-02-15 | Therapeuticsmd, Inc. | Vaginal inserted estradiol pharmaceutical compositions and methods |
| US9180091B2 (en) | 2012-12-21 | 2015-11-10 | Therapeuticsmd, Inc. | Soluble estradiol capsule for vaginal insertion |
| US10537581B2 (en) | 2012-12-21 | 2020-01-21 | Therapeuticsmd, Inc. | Vaginal inserted estradiol pharmaceutical compositions and methods |
| US11744838B2 (en) | 2013-03-15 | 2023-09-05 | Acerus Biopharma Inc. | Methods of treating hypogonadism with transnasal testosterone bio-adhesive gel formulations in male with allergic rhinitis, and methods for preventing an allergic rhinitis event |
| ES2907284T3 (es) | 2013-03-15 | 2022-04-22 | Marius Pharmaceuticals Llc | Formulaciones de emulsión |
| US20140370084A1 (en) * | 2013-06-18 | 2014-12-18 | Therapeuticsmd, Inc. | Estradiol formulations and therapies |
| JP2017516768A (ja) | 2014-05-22 | 2017-06-22 | セラピューティックスエムディー インコーポレーテッドＴｈｅｒａｐｅｕｔｉｃｓｍｄ， Ｉｎｃ． | 天然の併用ホルモン補充療法剤及び療法 |
| US10328087B2 (en) | 2015-07-23 | 2019-06-25 | Therapeuticsmd, Inc. | Formulations for solubilizing hormones |
| US9931349B2 (en) | 2016-04-01 | 2018-04-03 | Therapeuticsmd, Inc. | Steroid hormone pharmaceutical composition |
| US10286077B2 (en) | 2016-04-01 | 2019-05-14 | Therapeuticsmd, Inc. | Steroid hormone compositions in medium chain oils |
| US12403146B2 (en) | 2019-10-30 | 2025-09-02 | Marius Pharmaceuticals, Inc. | Preferred oral testosterone undecanoate therapy to achieve testosterone replacement treatment |
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| JPS59148718A (ja) * | 1983-02-10 | 1984-08-25 | Fujisawa Pharmaceut Co Ltd | ユビデカレノン組成物 |
| JP2002522473A (ja) * | 1998-08-13 | 2002-07-23 | シーマ・ラブス・インコーポレイテッド | 経口投与の固形投与形態物としてのマイクロエマルション |
| JP2002537317A (ja) * | 1999-02-26 | 2002-11-05 | リポシン インコーポレイテッド | 疎水性治療剤の改善された送達のための組成物および方法 |
| JP2005516991A (ja) * | 2002-02-01 | 2005-06-09 | ミセル・プロダクツ・インコーポレイテッド | 白板症を処置するためのβカロチン澄明ミセル化製剤 |
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2002
- 2002-12-12 US US10/317,657 patent/US20040115226A1/en not_active Abandoned
-
2003
- 2003-12-09 AU AU2003300833A patent/AU2003300833A1/en not_active Abandoned
- 2003-12-09 JP JP2004560372A patent/JP2006511536A/ja active Pending
- 2003-12-09 WO PCT/US2003/038979 patent/WO2004054540A2/en not_active Ceased
-
2006
- 2006-07-27 US US11/494,131 patent/US20060263397A1/en not_active Abandoned
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| JPS59148718A (ja) * | 1983-02-10 | 1984-08-25 | Fujisawa Pharmaceut Co Ltd | ユビデカレノン組成物 |
| JP2002522473A (ja) * | 1998-08-13 | 2002-07-23 | シーマ・ラブス・インコーポレイテッド | 経口投与の固形投与形態物としてのマイクロエマルション |
| JP2002537317A (ja) * | 1999-02-26 | 2002-11-05 | リポシン インコーポレイテッド | 疎水性治療剤の改善された送達のための組成物および方法 |
| JP2005516991A (ja) * | 2002-02-01 | 2005-06-09 | ミセル・プロダクツ・インコーポレイテッド | 白板症を処置するためのβカロチン澄明ミセル化製剤 |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2007191396A (ja) * | 2005-01-07 | 2007-08-02 | Rohto Pharmaceut Co Ltd | 皮膚外用剤 |
| JP2022520361A (ja) * | 2019-02-12 | 2022-03-30 | スミトモ ダイニッポン ファーマ オンコロジー， インコーポレイテッド | 複素環式タンパク質キナーゼ阻害剤を含む製剤 |
| JP7662528B2 (ja) | 2019-02-12 | 2025-04-15 | スミトモ ファーマ アメリカ， インコーポレイテッド | 複素環式タンパク質キナーゼ阻害剤を含む製剤 |
Also Published As
| Publication number | Publication date |
|---|---|
| AU2003300833A1 (en) | 2004-07-09 |
| US20060263397A1 (en) | 2006-11-23 |
| AU2003300833A8 (en) | 2004-07-09 |
| US20070009559A1 (en) | 2007-01-11 |
| WO2004054540A2 (en) | 2004-07-01 |
| WO2004054540A3 (en) | 2004-09-30 |
| US20040115226A1 (en) | 2004-06-17 |
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