AR078951A1 - Esferoides de farmacos revestidos y usos de los mismos para la eliminacion o reduccion de afecciones tales como emesis y diarrea - Google Patents
Esferoides de farmacos revestidos y usos de los mismos para la eliminacion o reduccion de afecciones tales como emesis y diarreaInfo
- Publication number
- AR078951A1 AR078951A1 ARP100104154A AR078951A1 AR 078951 A1 AR078951 A1 AR 078951A1 AR P100104154 A ARP100104154 A AR P100104154A AR 078951 A1 AR078951 A1 AR 078951A1
- Authority
- AR
- Argentina
- Prior art keywords
- percent
- weight
- pharmaceutically acceptable
- spheroidal particles
- spheroids
- Prior art date
Links
- 206010012735 Diarrhoea Diseases 0.000 title 1
- 206010047700 Vomiting Diseases 0.000 title 1
- 239000003814 drug Substances 0.000 title 1
- 229940079593 drug Drugs 0.000 title 1
- 230000008030 elimination Effects 0.000 title 1
- 238000003379 elimination reaction Methods 0.000 title 1
- 239000000203 mixture Substances 0.000 abstract 6
- 239000002245 particle Substances 0.000 abstract 3
- 238000009472 formulation Methods 0.000 abstract 2
- 229940043355 kinase inhibitor Drugs 0.000 abstract 2
- 239000003757 phosphotransferase inhibitor Substances 0.000 abstract 2
- 238000009498 subcoating Methods 0.000 abstract 2
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 229920003174 cellulose-based polymer Polymers 0.000 abstract 1
- 239000011248 coating agent Substances 0.000 abstract 1
- 238000000576 coating method Methods 0.000 abstract 1
- 239000002702 enteric coating Substances 0.000 abstract 1
- 238000009505 enteric coating Methods 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- ZNHPZUKZSNBOSQ-BQYQJAHWSA-N neratinib Chemical compound C=12C=C(NC\C=C\CN(C)C)C(OCC)=CC2=NC=C(C#N)C=1NC(C=C1Cl)=CC=C1OCC1=CC=CC=N1 ZNHPZUKZSNBOSQ-BQYQJAHWSA-N 0.000 abstract 1
- 229950008835 neratinib Drugs 0.000 abstract 1
- 239000008203 oral pharmaceutical composition Substances 0.000 abstract 1
- 229920000642 polymer Polymers 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000000080 wetting agent Substances 0.000 abstract 1
Classifications
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- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/5073—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals having two or more different coatings optionally including drug-containing subcoatings
-
- 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
-
- 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
- A61K31/495—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
-
- 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
- A61K31/495—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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/5005—Wall or coating material
- A61K9/5021—Organic macromolecular compounds
- A61K9/5026—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
-
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/5005—Wall or coating material
- A61K9/5021—Organic macromolecular compounds
- A61K9/5036—Polysaccharides, e.g. gums, alginate; Cyclodextrin
- A61K9/5042—Cellulose; Cellulose derivatives, e.g. phthalate or acetate succinate esters of hydroxypropyl methylcellulose
-
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/5005—Wall or coating material
- A61K9/5021—Organic macromolecular compounds
- A61K9/5036—Polysaccharides, e.g. gums, alginate; Cyclodextrin
- A61K9/5042—Cellulose; Cellulose derivatives, e.g. phthalate or acetate succinate esters of hydroxypropyl methylcellulose
- A61K9/5047—Cellulose ethers containing no ester groups, e.g. hydroxypropyl methylcellulose
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/12—Antidiarrhoeals
-
- 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
- A61P35/00—Antineoplastic agents
Landscapes
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Hospice & Palliative Care (AREA)
- Oncology (AREA)
- Otolaryngology (AREA)
- Communicable Diseases (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medical Preparation Storing Or Oral Administration Devices (AREA)
Abstract
Una formulacion farmacéutica oral que comprende esferoides revestidos de un inhibidor de quinasa tal como neratinib, estando disenada dicha formulacion para reducir o eliminar efectos secundarios asociados con formulaciones orales existentes de inhibidores de quinasa. Reivindicacion 1: Una composicion farmacéuticamente aceptable de (i) partículas esferoides que comprenden: (a) un 30-70 por ciento en peso de (E)-N-(4-(3-cloro-4-(piridin-2-ilmetoxi)fenilamino)-3-ciano-7-etoxiquinolin-6-iI)-4-(dimetilamino)but-2-enamida o una sal farmacéuticamente aceptable de la misma; (b) un 20-30 por ciento en peso de una o más cargas; y (c) un 5-15 por ciento en peso de uno o más agentes humectantes, comprendiendo dichas partículas esferoides el 70-83 por ciento en peso de la composicion total; (ii) un sub-revestimiento aplicado a dichas partículas esferoides que comprende adicionalmente un 1-4 por ciento en peso de uno o más polímeros basados en celulosa farmacéuticamente aceptables y (iii) un 16-30 por ciento en peso de uno o más polímeros farmacéuticamente aceptables como revestimiento entérico aplicado a dicho sub-revestimiento, comprendiendo dichos componentes de revestimiento (ii) y (iii) el 17-30 por ciento en peso de la composicion total. Reivindicacion 11: Un procedimiento para tratar cáncer, que comprende administrar una cantidad eficaz de una composicion de acuerdo con la reivindicacion 2.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US25938709P | 2009-11-09 | 2009-11-09 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR078951A1 true AR078951A1 (es) | 2011-12-14 |
Family
ID=43828063
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP100104154 AR078951A1 (es) | 2009-11-09 | 2010-11-09 | Esferoides de farmacos revestidos y usos de los mismos para la eliminacion o reduccion de afecciones tales como emesis y diarrea |
Country Status (11)
Country | Link |
---|---|
US (2) | US8524281B2 (es) |
EP (1) | EP2498751B1 (es) |
JP (3) | JP5866116B2 (es) |
CN (4) | CN102724962B (es) |
AR (1) | AR078951A1 (es) |
AU (1) | AU2010315362B2 (es) |
CA (1) | CA2780332C (es) |
ES (1) | ES2729677T3 (es) |
NZ (1) | NZ599762A (es) |
TW (1) | TWI429437B (es) |
WO (1) | WO2011056741A2 (es) |
Families Citing this family (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
PT1848414E (pt) | 2005-02-03 | 2011-05-25 | Gen Hospital Corp | M?todo para tratamento de cancro resistente a gefitinib |
AR057854A1 (es) | 2005-11-04 | 2007-12-19 | Wyeth Corp | Combinaciones antineoplasicas con inhibidor de mtor, herceptina y/o hki-272 (e)-n-{4-[3-cloro-4-(2-piridinilmetoxi) anilino]-3-ciano-7-etoxi-6-quinolinil}-4-(dimetilamino)-2-butenamida |
US8022216B2 (en) | 2007-10-17 | 2011-09-20 | Wyeth Llc | Maleate salts of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide and crystalline forms thereof |
KR20180128078A (ko) | 2008-06-17 | 2018-11-30 | 와이어쓰 엘엘씨 | Hki-272 및 비노렐빈을 함유하는 항신생물성 조합물 |
KR20140069340A (ko) | 2008-08-04 | 2014-06-09 | 와이어쓰 엘엘씨 | 4-아닐리노-3-사이아노퀴놀린과 카페시타빈의 항신생물성 조합물 |
CN102369010A (zh) | 2009-04-06 | 2012-03-07 | 惠氏有限责任公司 | 用于乳腺癌的利用奈拉替尼的治疗方案 |
EP2498751B1 (en) | 2009-11-09 | 2019-04-03 | Wyeth LLC | Coated drug spheroids and uses thereof for eliminating or reducing conditions such as emesis and diarrhea |
CN102675287A (zh) * | 2011-03-11 | 2012-09-19 | 江苏恒瑞医药股份有限公司 | (e)-n-[4-[[3-氯-4-(2-吡啶基甲氧基)苯基]氨基]-3-氰基-7-乙氧基-6-喹啉基]-3-[(2r)-1-甲基吡咯烷-2-基]丙-2-烯酰胺的可药用的盐、其制备方法及其在医药上的应用 |
US9301957B2 (en) * | 2011-11-14 | 2016-04-05 | Novartis Ag | Immediate release 4-methyl-3-4[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-N-[5-(4-methyl-1H-imidazol-1-YL)-3-(trifluoromethyl)phenyl] benzamide formulation |
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KR20180128078A (ko) | 2008-06-17 | 2018-11-30 | 와이어쓰 엘엘씨 | Hki-272 및 비노렐빈을 함유하는 항신생물성 조합물 |
KR20140069340A (ko) | 2008-08-04 | 2014-06-09 | 와이어쓰 엘엘씨 | 4-아닐리노-3-사이아노퀴놀린과 카페시타빈의 항신생물성 조합물 |
WO2010048477A2 (en) | 2008-10-24 | 2010-04-29 | Wyeth Llc | Improved process for preparation of coupled products from 4-amino-3-cyanoquinolines using stabilized intermediates |
CN102369010A (zh) | 2009-04-06 | 2012-03-07 | 惠氏有限责任公司 | 用于乳腺癌的利用奈拉替尼的治疗方案 |
CA2766067A1 (en) | 2009-07-02 | 2011-01-06 | Wyeth Llc | 3-cyanoquinoline tablet formulations and uses thereof |
KR20110007985A (ko) | 2009-07-17 | 2011-01-25 | 한올바이오파마주식회사 | N,n―디메틸 이미도디카르본이미딕 디아미드의 부틸산염, 이의 제조방법, 이를 포함하는 약제학적 조성물 및 이를 포함하는 복합제제 |
KR20110007984A (ko) | 2009-07-17 | 2011-01-25 | 한올바이오파마주식회사 | N,n―디메틸 이미도디카르본이미딕 디아미드의 프로피온산염, 이의 제조방법, 이를 포함하는 약제학적 조성물 및 이를 포함하는 복합제제 |
WO2011025269A2 (ko) | 2009-08-25 | 2011-03-03 | 한올바이오파마주식회사 | 메트포르민 타우린염, 그의 제조방법, 그를 포함하는 약학 조성물 및 그를 포함하는 복합제제 |
WO2011025271A2 (ko) | 2009-08-25 | 2011-03-03 | 한올바이오파마주식회사 | 메트포르민 아스코르브산염, 그의 제조방법, 그를 포함하는 약학 조성물 및 그를 포함하는 복합제제 |
WO2011025267A2 (ko) | 2009-08-25 | 2011-03-03 | 한올바이오파마주식회사 | 메트포르민 메탄설폰산염, 그의 제조방법, 그를 포함하는 약학 조성물 및 그를 포함하는 복합제제 |
EP2498751B1 (en) | 2009-11-09 | 2019-04-03 | Wyeth LLC | Coated drug spheroids and uses thereof for eliminating or reducing conditions such as emesis and diarrhea |
AU2010316683B2 (en) | 2009-11-09 | 2015-10-08 | Wyeth Llc | Tablet formulations of neratinib maleate |
CA2783743C (en) | 2009-12-11 | 2022-10-04 | Wyeth Llc | Phosphatidylinositol-3-kinase pathway biomarkers |
US8338456B2 (en) | 2010-01-13 | 2012-12-25 | Wyeth Llc | Cut-point in PTEN protein expression that accurately identifies tumors and is predictive of drug response to a pan-ErbB inhibitor |
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2010
- 2010-11-01 EP EP10787212.9A patent/EP2498751B1/en active Active
- 2010-11-01 WO PCT/US2010/054934 patent/WO2011056741A2/en active Application Filing
- 2010-11-01 CA CA2780332A patent/CA2780332C/en active Active
- 2010-11-01 CN CN201080060547.0A patent/CN102724962B/zh active Active
- 2010-11-01 ES ES10787212T patent/ES2729677T3/es active Active
- 2010-11-01 CN CN201710247663.7A patent/CN107441058A/zh active Pending
- 2010-11-01 CN CN201610509189.6A patent/CN106074445B/zh active Active
- 2010-11-01 AU AU2010315362A patent/AU2010315362B2/en active Active
- 2010-11-01 CN CN201710247590.1A patent/CN107308130B/zh active Active
- 2010-11-01 NZ NZ59976210A patent/NZ599762A/en unknown
- 2010-11-05 US US12/940,797 patent/US8524281B2/en active Active
- 2010-11-09 AR ARP100104154 patent/AR078951A1/es not_active Application Discontinuation
- 2010-11-09 JP JP2010250815A patent/JP5866116B2/ja active Active
- 2010-11-09 TW TW99138517A patent/TWI429437B/zh active
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2013
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Also Published As
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JP5982020B2 (ja) | 2016-08-31 |
JP2011098965A (ja) | 2011-05-19 |
ES2729677T3 (es) | 2019-11-05 |
US8524281B2 (en) | 2013-09-03 |
US20140004203A1 (en) | 2014-01-02 |
CA2780332C (en) | 2018-01-30 |
EP2498751B1 (en) | 2019-04-03 |
JP2016094478A (ja) | 2016-05-26 |
CN102724962A (zh) | 2012-10-10 |
CN107441058A (zh) | 2017-12-08 |
NZ599762A (en) | 2014-07-25 |
CN106074445A (zh) | 2016-11-09 |
US20110165257A1 (en) | 2011-07-07 |
TW201138775A (en) | 2011-11-16 |
JP2015078240A (ja) | 2015-04-23 |
CN107308130A (zh) | 2017-11-03 |
CN102724962B (zh) | 2017-05-17 |
EP2498751A2 (en) | 2012-09-19 |
JP5866116B2 (ja) | 2016-02-17 |
CA2780332A1 (en) | 2011-05-12 |
WO2011056741A2 (en) | 2011-05-12 |
CN107308130B (zh) | 2021-06-15 |
CN106074445B (zh) | 2018-12-21 |
US9211264B2 (en) | 2015-12-15 |
WO2011056741A3 (en) | 2011-06-30 |
TWI429437B (zh) | 2014-03-11 |
AU2010315362A1 (en) | 2012-05-24 |
AU2010315362B2 (en) | 2015-01-22 |
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