DE60221795T2 - Orale zusammensetzungen von itraconazol und verfahren zu herstellung derselbigen - Google Patents
Orale zusammensetzungen von itraconazol und verfahren zu herstellung derselbigen Download PDFInfo
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- DE60221795T2 DE60221795T2 DE60221795T DE60221795T DE60221795T2 DE 60221795 T2 DE60221795 T2 DE 60221795T2 DE 60221795 T DE60221795 T DE 60221795T DE 60221795 T DE60221795 T DE 60221795T DE 60221795 T2 DE60221795 T2 DE 60221795T2
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- itraconazole
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- acid
- oral
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- 239000011230 binding agent Substances 0.000 description 1
- 229960000074 biopharmaceutical Drugs 0.000 description 1
- 239000000872 buffer Substances 0.000 description 1
- VTYYLEPIZMXCLO-UHFFFAOYSA-L calcium carbonate Substances [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 description 1
- 229910000019 calcium carbonate Inorganic materials 0.000 description 1
- 239000001506 calcium phosphate Substances 0.000 description 1
- 229910000389 calcium phosphate Inorganic materials 0.000 description 1
- 235000011010 calcium phosphates Nutrition 0.000 description 1
- 238000004364 calculation method Methods 0.000 description 1
- 235000010948 carboxy methyl cellulose Nutrition 0.000 description 1
- 239000008112 carboxymethyl-cellulose Substances 0.000 description 1
- 229920001525 carrageenan Polymers 0.000 description 1
- 235000010418 carrageenan Nutrition 0.000 description 1
- 239000000969 carrier Substances 0.000 description 1
- 239000002738 chelating agent Substances 0.000 description 1
- 238000006243 chemical reaction Methods 0.000 description 1
- 230000001684 chronic effect Effects 0.000 description 1
- 235000015165 citric acid Nutrition 0.000 description 1
- ZPUCINDJVBIVPJ-LJISPDSOSA-N cocaine Chemical compound O([C@H]1C[C@@H]2CC[C@@H](N2C)[C@H]1C(=O)OC)C(=O)C1=CC=CC=C1 ZPUCINDJVBIVPJ-LJISPDSOSA-N 0.000 description 1
- 230000000536 complexating effect Effects 0.000 description 1
- 239000008139 complexing agent Substances 0.000 description 1
- 238000001816 cooling Methods 0.000 description 1
- 239000013256 coordination polymer Substances 0.000 description 1
- 239000002537 cosmetic Substances 0.000 description 1
- 229960005168 croscarmellose Drugs 0.000 description 1
- 229960000913 crospovidone Drugs 0.000 description 1
- 239000001767 crosslinked sodium carboxy methyl cellulose Substances 0.000 description 1
- 229940075894 denatured ethanol Drugs 0.000 description 1
- 239000000645 desinfectant Substances 0.000 description 1
- 238000001514 detection method Methods 0.000 description 1
- 235000019425 dextrin Nutrition 0.000 description 1
- 239000008121 dextrose Substances 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- BNIILDVGGAEEIG-UHFFFAOYSA-L disodium hydrogen phosphate Chemical compound [Na+].[Na+].OP([O-])([O-])=O BNIILDVGGAEEIG-UHFFFAOYSA-L 0.000 description 1
- 229910000397 disodium phosphate Inorganic materials 0.000 description 1
- 235000019800 disodium phosphate Nutrition 0.000 description 1
- 239000012738 dissolution medium Substances 0.000 description 1
- 239000012153 distilled water Substances 0.000 description 1
- 238000012377 drug delivery Methods 0.000 description 1
- 239000003792 electrolyte Substances 0.000 description 1
- CCIVGXIOQKPBKL-UHFFFAOYSA-M ethanesulfonate Chemical compound CCS([O-])(=O)=O CCIVGXIOQKPBKL-UHFFFAOYSA-M 0.000 description 1
- 239000000945 filler Substances 0.000 description 1
- 239000000706 filtrate Substances 0.000 description 1
- 210000004905 finger nail Anatomy 0.000 description 1
- 239000000796 flavoring agent Substances 0.000 description 1
- 235000019634 flavors Nutrition 0.000 description 1
- 235000003599 food sweetener Nutrition 0.000 description 1
- 239000001530 fumaric acid Substances 0.000 description 1
- 235000011087 fumaric acid Nutrition 0.000 description 1
- 229930182830 galactose Natural products 0.000 description 1
- 239000003365 glass fiber Substances 0.000 description 1
- 239000008103 glucose Substances 0.000 description 1
- 235000010417 guar gum Nutrition 0.000 description 1
- 239000000665 guar gum Substances 0.000 description 1
- 229960002154 guar gum Drugs 0.000 description 1
- 229940093915 gynecological organic acid Drugs 0.000 description 1
- 238000010438 heat treatment Methods 0.000 description 1
- 230000002209 hydrophobic effect Effects 0.000 description 1
- 229920013821 hydroxy alkyl cellulose Polymers 0.000 description 1
- 235000019447 hydroxyethyl cellulose Nutrition 0.000 description 1
- 229910052588 hydroxylapatite Inorganic materials 0.000 description 1
- 229920003063 hydroxymethyl cellulose Polymers 0.000 description 1
- 229940031574 hydroxymethyl cellulose Drugs 0.000 description 1
- 239000012729 immediate-release (IR) formulation Substances 0.000 description 1
- 238000011065 in-situ storage Methods 0.000 description 1
- 230000004054 inflammatory process Effects 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 150000002484 inorganic compounds Chemical class 0.000 description 1
- 229910010272 inorganic material Inorganic materials 0.000 description 1
- 238000011835 investigation Methods 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 238000011068 loading method Methods 0.000 description 1
- ZLNQQNXFFQJAID-UHFFFAOYSA-L magnesium carbonate Chemical compound [Mg+2].[O-]C([O-])=O ZLNQQNXFFQJAID-UHFFFAOYSA-L 0.000 description 1
- 239000001095 magnesium carbonate Substances 0.000 description 1
- 229910000021 magnesium carbonate Inorganic materials 0.000 description 1
- 235000009973 maize Nutrition 0.000 description 1
- 229940035034 maltodextrin Drugs 0.000 description 1
- 239000012528 membrane Substances 0.000 description 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 description 1
- 229920000609 methyl cellulose Polymers 0.000 description 1
- 229940050176 methyl chloride Drugs 0.000 description 1
- 239000001923 methylcellulose Substances 0.000 description 1
- 229910052757 nitrogen Inorganic materials 0.000 description 1
- 239000011824 nuclear material Substances 0.000 description 1
- 229920001542 oligosaccharide Polymers 0.000 description 1
- 150000002482 oligosaccharides Chemical class 0.000 description 1
- 150000007524 organic acids Chemical class 0.000 description 1
- 235000005985 organic acids Nutrition 0.000 description 1
- 239000001814 pectin Substances 0.000 description 1
- 229920001277 pectin Polymers 0.000 description 1
- 235000010987 pectin Nutrition 0.000 description 1
- XYJRXVWERLGGKC-UHFFFAOYSA-D pentacalcium;hydroxide;triphosphate Chemical compound [OH-].[Ca+2].[Ca+2].[Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O XYJRXVWERLGGKC-UHFFFAOYSA-D 0.000 description 1
- 230000035699 permeability Effects 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 125000004193 piperazinyl group Chemical group 0.000 description 1
- 239000004033 plastic Substances 0.000 description 1
- 229920003023 plastic Polymers 0.000 description 1
- 239000004014 plasticizer Substances 0.000 description 1
- 229920000233 poly(alkylene oxides) Polymers 0.000 description 1
- 229920005606 polypropylene copolymer Polymers 0.000 description 1
- 229920001451 polypropylene glycol Polymers 0.000 description 1
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 description 1
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 description 1
- 239000001103 potassium chloride Substances 0.000 description 1
- 235000011164 potassium chloride Nutrition 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 238000000746 purification Methods 0.000 description 1
- 239000008213 purified water Substances 0.000 description 1
- 238000001953 recrystallisation Methods 0.000 description 1
- 229920005989 resin Polymers 0.000 description 1
- 239000011347 resin Substances 0.000 description 1
- 235000009566 rice Nutrition 0.000 description 1
- 239000000377 silicon dioxide Substances 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- FAPWRFPIFSIZLT-UHFFFAOYSA-M sodium chloride Inorganic materials [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 1
- 239000012064 sodium phosphate buffer Substances 0.000 description 1
- 239000007909 solid dosage form Substances 0.000 description 1
- 239000006104 solid solution Substances 0.000 description 1
- 238000001694 spray drying Methods 0.000 description 1
- 150000008163 sugars Chemical class 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 239000003765 sweetening agent Substances 0.000 description 1
- 239000011975 tartaric acid Substances 0.000 description 1
- 235000002906 tartaric acid Nutrition 0.000 description 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 201000005882 tinea unguium Diseases 0.000 description 1
- 210000004906 toe nail Anatomy 0.000 description 1
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 description 1
- 235000010487 tragacanth Nutrition 0.000 description 1
- 239000000196 tragacanth Substances 0.000 description 1
- 229940116362 tragacanth Drugs 0.000 description 1
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 1
- 150000003852 triazoles Chemical class 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
- 238000009423 ventilation Methods 0.000 description 1
- 239000011782 vitamin Substances 0.000 description 1
- 229940088594 vitamin Drugs 0.000 description 1
- 229930003231 vitamin Natural products 0.000 description 1
- 235000013343 vitamin Nutrition 0.000 description 1
- 239000003643 water by type Substances 0.000 description 1
- 238000009736 wetting Methods 0.000 description 1
- 229920001285 xanthan gum Polymers 0.000 description 1
- 235000010493 xanthan gum Nutrition 0.000 description 1
- 239000000230 xanthan gum Substances 0.000 description 1
- 229940082509 xanthan gum 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
- A61K9/14—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
- A61K9/167—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction with an outer layer or coating comprising drug; with chemically bound drugs or non-active substances on their surface
- A61K9/1676—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction with an outer layer or coating comprising drug; with chemically bound drugs or non-active substances on their surface having a drug-free core with discrete complete coating layer containing drug
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/10—Antimycotics
Landscapes
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US26665301P | 2001-02-06 | 2001-02-06 | |
| US266653P | 2001-02-06 | ||
| US933032 | 2001-08-20 | ||
| US09/933,032 US6663897B2 (en) | 2001-02-06 | 2001-08-20 | Oral itraconazole formulations and methods of making the same |
| PCT/NL2002/000080 WO2002062318A2 (en) | 2001-02-06 | 2002-02-01 | Oral itraconazole formulations and methods of making the same |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| DE60221795D1 DE60221795D1 (de) | 2007-09-27 |
| DE60221795T2 true DE60221795T2 (de) | 2007-12-27 |
Family
ID=26951964
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DE60221795T Expired - Fee Related DE60221795T2 (de) | 2001-02-06 | 2002-02-01 | Orale zusammensetzungen von itraconazol und verfahren zu herstellung derselbigen |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US6663897B2 (enExample) |
| EP (1) | EP1357899B1 (enExample) |
| JP (1) | JP2004521897A (enExample) |
| AT (1) | ATE369840T1 (enExample) |
| AU (1) | AU2002233822A1 (enExample) |
| CA (1) | CA2437372A1 (enExample) |
| DE (1) | DE60221795T2 (enExample) |
| MX (1) | MXPA03006980A (enExample) |
| WO (1) | WO2002062318A2 (enExample) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0015239D0 (en) * | 2000-06-21 | 2000-08-16 | Biochemie Gmbh | Organic compounds |
| US8071133B2 (en) | 2001-08-20 | 2011-12-06 | Stiefel Laboratories, Inc. | Oral dosage forms of water insoluble drugs and methods of making the same |
| US20040115266A1 (en) * | 2002-02-01 | 2004-06-17 | Namburi Ranga Raju | Oral itraconazole formulations and methods of making the same |
| US20050025791A1 (en) | 2002-06-21 | 2005-02-03 | Julius Remenar | Pharmaceutical compositions with improved dissolution |
| US7446107B2 (en) | 2002-02-15 | 2008-11-04 | Transform Pharmaceuticals, Inc. | Crystalline forms of conazoles and methods of making and using the same |
| US7790905B2 (en) | 2002-02-15 | 2010-09-07 | Mcneil-Ppc, Inc. | Pharmaceutical propylene glycol solvate compositions |
| US7927613B2 (en) | 2002-02-15 | 2011-04-19 | University Of South Florida | Pharmaceutical co-crystal compositions |
| US7078526B2 (en) | 2002-05-31 | 2006-07-18 | Transform Pharmaceuticals, Inc. | CIS-itraconazole crystalline forms and related processes, pharmaceutical compositions and methods |
| JP4906233B2 (ja) | 2002-03-01 | 2012-03-28 | ユニバーシティー オブ サウス フロリダ | 少なくとも１種の有効薬剤成分を含有する多構成要素固相 |
| GB0205253D0 (en) * | 2002-03-06 | 2002-04-17 | Univ Gent | Immediate release pharmaceutical granule compositions and a continuous process for making them |
| EP1539111A1 (en) * | 2002-08-05 | 2005-06-15 | DSM IP Assets B.V. | Oral dosage forms of water insoluble drugs and methods of making the same |
| US8183290B2 (en) | 2002-12-30 | 2012-05-22 | Mcneil-Ppc, Inc. | Pharmaceutically acceptable propylene glycol solvate of naproxen |
| US20050074494A1 (en) * | 2003-10-06 | 2005-04-07 | Xiu-Xiu Cheng | Itraconazole immediate release formulation |
| US20050118265A1 (en) * | 2003-11-28 | 2005-06-02 | Anandi Krishnan | Antifungal oral dosage forms and the methods for preparation |
| GB0612695D0 (en) * | 2006-06-27 | 2006-08-09 | Univ Gent | Process for preparing a solid dosage form |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4791111A (en) | 1985-12-23 | 1988-12-13 | Janssen Pharmaceutica, N.V. | [[4-[4-(4-phenyl-1-piperazinyl)phenoxymethyl]-1,3-dioxolan-2-yl]methyl]-1H-imidazoles and 1H-1,2,4-triazoles having anti-microbial properties |
| PH30929A (en) | 1992-09-03 | 1997-12-23 | Janssen Pharmaceutica Nv | Beads having a core coated with an antifungal and a polymer. |
| IT1263831B (it) | 1993-01-29 | 1996-09-04 | Paolo Chiesi | Complessi di inclusione multicomponente ad elevata solubilita' costituiti da un farmaco di tipo basico, un acido ed una ciclodestrina |
| TR199802718T2 (xx) * | 1996-06-28 | 1999-03-22 | Schering Corporation | Bir triazol mantara kar�� bile�i�ini i�eren a��zdan al�nan bile�im. |
| FR2758461A1 (fr) | 1997-01-17 | 1998-07-24 | Pharma Pass | Composition pharmaceutique presentant une biodisponibilite elevee et son procede de preparation |
| TR199900990T2 (xx) * | 1997-03-26 | 1999-10-21 | Janssen Pharmaceutica N.V. | Antifungal ve polimer ile kaplanm�� �ekirde�e haiz peletler. |
| DE69927163T2 (de) * | 1998-07-17 | 2006-06-29 | Janssen Pharmaceutica N.V. | Granulat mit einem fungizid und einem polymer umhüllten kern |
| RU2233654C2 (ru) | 1998-11-20 | 2004-08-10 | Ртп Фарма Инк. | Диспергируемые стабилизированные фосфолипидом микрочастицы |
| EP1163234B1 (en) | 1999-03-24 | 2005-10-26 | R.P. Scherer Technologies, Inc. | Pharmaceutical formulations with improved aqueous solubility |
| US6383471B1 (en) * | 1999-04-06 | 2002-05-07 | Lipocine, Inc. | Compositions and methods for improved delivery of ionizable hydrophobic therapeutic agents |
| KR100331529B1 (ko) | 1999-06-16 | 2002-04-06 | 민경윤 | 난용성 항진균제의 경구투여용 조성물 및 그의 제조 방법 |
-
2001
- 2001-08-20 US US09/933,032 patent/US6663897B2/en not_active Expired - Lifetime
-
2002
- 2002-02-01 CA CA002437372A patent/CA2437372A1/en not_active Abandoned
- 2002-02-01 AT AT02700887T patent/ATE369840T1/de not_active IP Right Cessation
- 2002-02-01 MX MXPA03006980A patent/MXPA03006980A/es active IP Right Grant
- 2002-02-01 JP JP2002562325A patent/JP2004521897A/ja active Pending
- 2002-02-01 EP EP02700887A patent/EP1357899B1/en not_active Expired - Lifetime
- 2002-02-01 WO PCT/NL2002/000080 patent/WO2002062318A2/en not_active Ceased
- 2002-02-01 DE DE60221795T patent/DE60221795T2/de not_active Expired - Fee Related
- 2002-02-01 AU AU2002233822A patent/AU2002233822A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| MXPA03006980A (es) | 2004-10-15 |
| ATE369840T1 (de) | 2007-09-15 |
| WO2002062318A3 (en) | 2002-11-21 |
| DE60221795D1 (de) | 2007-09-27 |
| JP2004521897A (ja) | 2004-07-22 |
| CA2437372A1 (en) | 2002-08-15 |
| WO2002062318A2 (en) | 2002-08-15 |
| AU2002233822A1 (en) | 2002-08-19 |
| US20020150620A1 (en) | 2002-10-17 |
| US6663897B2 (en) | 2003-12-16 |
| EP1357899B1 (en) | 2007-08-15 |
| EP1357899A2 (en) | 2003-11-05 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| 8364 | No opposition during term of opposition | ||
| 8339 | Ceased/non-payment of the annual fee |