BRPI0412329A - dispersão sólida de tacrolimus e método de processar a mesma - Google Patents
dispersão sólida de tacrolimus e método de processar a mesmaInfo
- Publication number
- BRPI0412329A BRPI0412329A BRPI0412329-8A BRPI0412329A BRPI0412329A BR PI0412329 A BRPI0412329 A BR PI0412329A BR PI0412329 A BRPI0412329 A BR PI0412329A BR PI0412329 A BRPI0412329 A BR PI0412329A
- Authority
- BR
- Brazil
- Prior art keywords
- tacrolimus
- processing
- solid
- solid dispersion
- same
- Prior art date
Links
- QJJXYPPXXYFBGM-LFZNUXCKSA-N Tacrolimus Chemical compound C1C[C@@H](O)[C@H](OC)C[C@@H]1\C=C(/C)[C@@H]1[C@H](C)[C@@H](O)CC(=O)[C@H](CC=C)/C=C(C)/C[C@H](C)C[C@H](OC)[C@H]([C@H](C[C@H]2C)OC)O[C@@]2(O)C(=O)C(=O)N2CCCC[C@H]2C(=O)O1 QJJXYPPXXYFBGM-LFZNUXCKSA-N 0.000 title abstract 4
- 229960001967 tacrolimus Drugs 0.000 title abstract 4
- QJJXYPPXXYFBGM-SHYZHZOCSA-N tacrolimus Natural products CO[C@H]1C[C@H](CC[C@@H]1O)C=C(C)[C@H]2OC(=O)[C@H]3CCCCN3C(=O)C(=O)[C@@]4(O)O[C@@H]([C@H](C[C@H]4C)OC)[C@@H](C[C@H](C)CC(=C[C@@H](CC=C)C(=O)C[C@H](O)[C@H]2C)C)OC QJJXYPPXXYFBGM-SHYZHZOCSA-N 0.000 title abstract 4
- 238000000034 method Methods 0.000 title abstract 2
- 239000007962 solid dispersion Substances 0.000 title abstract 2
- 238000004090 dissolution Methods 0.000 abstract 2
- 239000007787 solid Substances 0.000 abstract 2
- 239000004094 surface-active agent Substances 0.000 abstract 2
- 238000010521 absorption reaction Methods 0.000 abstract 1
- 239000006185 dispersion Substances 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 239000003623 enhancer Substances 0.000 abstract 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
-
- 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
- A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
- A61K9/145—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/12—Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
- A61K38/13—Cyclosporins
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- 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
- A61K47/14—Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
-
- 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
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
Landscapes
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Molecular Biology (AREA)
- Gastroenterology & Hepatology (AREA)
- Biophysics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Transplantation (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
"DISPERSãO SóLIDA DE TACROLIMUS E MéTODO DE PROCESSAR A MESMA". A presente invenção se refere ao veículo da dispersão sólida de tacrolimus, o qual é preparado através de uso de um tensoativo sólido tendo uma propriedade de valor de HLB maior do que ou igual a cerca de 7. O tensoativo desempenha uma função de um veículo e uma função de um intensificador de dissolução, simultaneamente. Como um resultado, a taxa de dissolução do tacrolimus é aperfeiçoada e a capacidade de absorção oral e a biodisponibilidade podem ser aumentada em virtude da rápida liberação de droga.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| KR20030046550 | 2003-07-09 | ||
| PCT/KR2004/001684 WO2005004848A1 (en) | 2003-07-09 | 2004-07-09 | The solid dispersion of tacrolimus |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BRPI0412329A true BRPI0412329A (pt) | 2006-09-05 |
Family
ID=36587202
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI0412329-8A BRPI0412329A (pt) | 2003-07-09 | 2004-07-09 | dispersão sólida de tacrolimus e método de processar a mesma |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US20060177500A1 (pt) |
| EP (1) | EP1641437A4 (pt) |
| JP (1) | JP2007527383A (pt) |
| KR (1) | KR100486016B1 (pt) |
| CN (1) | CN1819817A (pt) |
| BR (1) | BRPI0412329A (pt) |
| MX (1) | MXPA06000370A (pt) |
| NO (1) | NO20060631L (pt) |
| WO (1) | WO2005004848A1 (pt) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2376238T3 (es) * | 2003-08-29 | 2012-03-12 | Veloxis Pharmaceuticals A/S | Composiciones de liberación modificada comprendiendo tacrolimus. |
| US7994214B2 (en) | 2003-08-29 | 2011-08-09 | Lifecycle Pharma A/S | Solid dispersions comprising tacrolimus |
| KR100539706B1 (ko) * | 2005-01-25 | 2005-12-28 | 지엘팜텍 주식회사 | 타크로리무스 및 장용성 고분자를 함유하는 고체분산체 |
| KR100678824B1 (ko) * | 2005-02-04 | 2007-02-05 | 한미약품 주식회사 | 용해성이 증가된 무정형 타크로리무스 고체분산체 및 이를포함하는 약제학적 조성물 |
| KR100711220B1 (ko) * | 2005-06-14 | 2007-04-24 | 삼천당제약주식회사 | 타크로리무스를 함유하는 경구용 조성물 및 그의 제조방법 |
| KR100693461B1 (ko) * | 2005-07-29 | 2007-03-12 | 동국제약 주식회사 | 마크로라이드계 항생물질을 유효성분으로 함유하는약제학적 조성물 및 이의 제조방법과, 상기 약제학적조성물을 함유하는 서방성 제제 |
| MXPA05010457A (es) * | 2005-09-28 | 2007-03-27 | Fernando Ahumada Ayala | Preparacion para el tratamiento de enfermedades inflamatorias de la piel, que contiene tacrolimus. |
| DE102005047561A1 (de) * | 2005-10-04 | 2007-04-05 | Bayer Healthcare Ag | Feste, oral applizierbare pharmazeutische Darreichungsformen mit schneller Wirkstofffreisetzung |
| WO2008033023A2 (en) * | 2006-09-15 | 2008-03-20 | Echo Pharmaceuticals B.V. | Granulate containing a pharmaceutically active substance and anemulsifier and method for its manufacture |
| CA2664315C (en) | 2006-09-15 | 2016-01-19 | Echo Pharmaceuticals B.V. | Dosage unit for sublingual, buccal or oral administration of water-insoluble pharmaceutically active substances |
| US20080181947A1 (en) * | 2006-09-26 | 2008-07-31 | Astellas Pharma Inc. | Controlled release dosage form of tacrolimus |
| JP2010515753A (ja) | 2007-01-10 | 2010-05-13 | ボード・オブ・リージエンツ,ザ・ユニバーシテイ・オブ・テキサス・システム | 肺内送達用免疫抑制剤組成物の送達の増強 |
| PL2167033T4 (pl) | 2007-05-30 | 2018-08-31 | Veloxis Pharmaceuticals A/S | Podawana raz dziennie doustna postać dawkowania zawierająca takrolimus |
| US12083103B2 (en) | 2007-05-30 | 2024-09-10 | Veloxis Pharmaceuticals, Inc. | Tacrolimus for improved treatment of transplant patients |
| US12403095B2 (en) | 2008-05-30 | 2025-09-02 | Veloxis Pharmaceuticals, Inc. | Stabilized tacrolimus composition |
| ES2739352T3 (es) | 2009-02-26 | 2020-01-30 | Glaxo Group Ltd | Formulaciones farmacéuticas que comprenden 4-{(1R)-2-[(6-{2-[(2,6-diclorobencil)oxi]etoxi}hexil)amino]-1-hidroxietil}-2-(hidroximetil)fenol |
| GB0921075D0 (en) | 2009-12-01 | 2010-01-13 | Glaxo Group Ltd | Novel combination of the therapeutic agents |
| ES2591352T3 (es) | 2010-02-17 | 2016-11-28 | Veloxis Pharmaceuticals A/S | Composición de tacrolimus estabilizada |
| KR20130028824A (ko) * | 2011-09-09 | 2013-03-20 | 주식회사 삼양바이오팜 | 타크로리무스를 포함하는 고체 분산체 및 이의 제조방법 |
| ES2600465T3 (es) | 2012-05-07 | 2017-02-09 | Echo Pharmaceuticals B.V. | Granulado que contiene cannabinoide, método para su producción y unidad de dosificación oral que comprende tal granulado |
| CN104415054A (zh) * | 2013-08-20 | 2015-03-18 | 哈药集团三精制药股份有限公司 | 一种速释复方氨酚烷胺片的制备方法 |
| CN110639020B (zh) * | 2019-08-15 | 2022-07-08 | 浙江工业大学 | 一种固体分散体基质及其制备方法和应用 |
| CN113577032A (zh) * | 2021-08-27 | 2021-11-02 | 国药集团川抗制药有限公司 | 他克莫司固体分散体的制备方法、速释药物组合物和应用 |
| WO2025220686A1 (ja) * | 2024-04-16 | 2025-10-23 | 中外製薬株式会社 | ペプチド、糖脂肪酸エステル構造を有する界面活性剤及び(メタ)アクリル酸系ポリマーを含む医薬組成物 |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4894366A (en) * | 1984-12-03 | 1990-01-16 | Fujisawa Pharmaceutical Company, Ltd. | Tricyclo compounds, a process for their production and a pharmaceutical composition containing the same |
| GB8608080D0 (en) * | 1986-04-02 | 1986-05-08 | Fujisawa Pharmaceutical Co | Solid dispersion composition |
| FR2736550B1 (fr) * | 1995-07-14 | 1998-07-24 | Sandoz Sa | Composition pharmaceutique sous la forme d'une dispersion solide comprenant un macrolide et un vehicule |
| CZ267796A3 (cs) * | 1996-09-12 | 1998-04-15 | Galena A.S. | Léčivé přípravky, zejména pro vnitřní aplikaci, ve formě samomikroemulgujících terapeutických systémů |
| ZA9710927B (en) * | 1996-12-06 | 1998-06-15 | Fujisawa Pharmaceutical Co | Pharmaceutical composition. |
| JP4221762B2 (ja) * | 1997-04-11 | 2009-02-12 | アステラス製薬株式会社 | 医薬組成物 |
| AU749623B2 (en) * | 1998-03-26 | 2002-06-27 | Astellas Pharma Inc. | Sustained release preparations |
| US6248363B1 (en) * | 1999-11-23 | 2001-06-19 | Lipocine, Inc. | Solid carriers for improved delivery of active ingredients in pharmaceutical compositions |
| US20010036959A1 (en) * | 2000-04-03 | 2001-11-01 | Gabel Rolf Dieter | Carvedilol-hydrophilic solutions |
| US7994214B2 (en) * | 2003-08-29 | 2011-08-09 | Lifecycle Pharma A/S | Solid dispersions comprising tacrolimus |
-
2004
- 2004-07-09 BR BRPI0412329-8A patent/BRPI0412329A/pt not_active IP Right Cessation
- 2004-07-09 CN CNA2004800193916A patent/CN1819817A/zh active Pending
- 2004-07-09 KR KR10-2004-0053269A patent/KR100486016B1/ko not_active Expired - Lifetime
- 2004-07-09 JP JP2006518554A patent/JP2007527383A/ja active Pending
- 2004-07-09 EP EP04774097A patent/EP1641437A4/en not_active Withdrawn
- 2004-07-09 WO PCT/KR2004/001684 patent/WO2005004848A1/en not_active Ceased
- 2004-07-09 US US10/563,972 patent/US20060177500A1/en not_active Abandoned
- 2004-07-09 MX MXPA06000370A patent/MXPA06000370A/es unknown
-
2006
- 2006-02-09 NO NO20060631A patent/NO20060631L/no not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| US20060177500A1 (en) | 2006-08-10 |
| EP1641437A4 (en) | 2009-06-03 |
| EP1641437A1 (en) | 2006-04-05 |
| WO2005004848A1 (en) | 2005-01-20 |
| MXPA06000370A (es) | 2006-03-28 |
| NO20060631L (no) | 2006-04-05 |
| KR100486016B1 (ko) | 2005-04-29 |
| KR20050007173A (ko) | 2005-01-17 |
| JP2007527383A (ja) | 2007-09-27 |
| CN1819817A (zh) | 2006-08-16 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B08F | Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette] |
Free format text: REFERENTE A 5A,6A E 7A ANUIDADE(S) |
|
| B08K | Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette] |
Free format text: REFERENTE AO DESPACHO 8.6 PUBLICADO NA RPI 2129 DE 25/10/2011. |