BR112013010190B1 - composição farmacêutica - Google Patents
composição farmacêutica Download PDFInfo
- Publication number
- BR112013010190B1 BR112013010190B1 BR112013010190A BR112013010190A BR112013010190B1 BR 112013010190 B1 BR112013010190 B1 BR 112013010190B1 BR 112013010190 A BR112013010190 A BR 112013010190A BR 112013010190 A BR112013010190 A BR 112013010190A BR 112013010190 B1 BR112013010190 B1 BR 112013010190B1
- Authority
- BR
- Brazil
- Prior art keywords
- alcohol
- pharmaceutical composition
- aripiprazole
- carbopol
- piv
- Prior art date
Links
- 239000008194 pharmaceutical composition Substances 0.000 title claims abstract description 12
- CEUORZQYGODEFX-UHFFFAOYSA-N Aripirazole Chemical compound ClC1=CC=CC(N2CCN(CCCCOC=3C=C4NC(=O)CCC4=CC=3)CC2)=C1Cl CEUORZQYGODEFX-UHFFFAOYSA-N 0.000 claims abstract description 39
- 229960004372 aripiprazole Drugs 0.000 claims abstract description 39
- 239000007788 liquid Substances 0.000 claims abstract description 8
- 239000000203 mixture Substances 0.000 claims description 26
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 claims description 24
- SECXISVLQFMRJM-UHFFFAOYSA-N N-Methylpyrrolidone Chemical compound CN1CCCC1=O SECXISVLQFMRJM-UHFFFAOYSA-N 0.000 claims description 22
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 16
- 235000019441 ethanol Nutrition 0.000 claims description 16
- 229920002125 Sokalan® Polymers 0.000 claims description 13
- ZMXDDKWLCZADIW-UHFFFAOYSA-N N,N-Dimethylformamide Chemical compound CN(C)C=O ZMXDDKWLCZADIW-UHFFFAOYSA-N 0.000 claims description 12
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 12
- POULHZVOKOAJMA-UHFFFAOYSA-N dodecanoic acid ester group Chemical group C(CCCCCCCCCCC)(=O)O POULHZVOKOAJMA-UHFFFAOYSA-N 0.000 claims description 8
- -1 polyethylene Polymers 0.000 claims description 8
- 235000014113 dietary fatty acids Nutrition 0.000 claims description 6
- 239000000194 fatty acid Substances 0.000 claims description 6
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- 239000002502 liposome Substances 0.000 claims description 5
- 239000003961 penetration enhancing agent Substances 0.000 claims description 5
- FXHOOIRPVKKKFG-UHFFFAOYSA-N N,N-Dimethylacetamide Chemical compound CN(C)C(C)=O FXHOOIRPVKKKFG-UHFFFAOYSA-N 0.000 claims description 4
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 claims description 4
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- WEEGYLXZBRQIMU-WAAGHKOSSA-N Eucalyptol Chemical compound C1C[C@H]2CC[C@]1(C)OC2(C)C WEEGYLXZBRQIMU-WAAGHKOSSA-N 0.000 description 1
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- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 1
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- BHQCQFFYRZLCQQ-OELDTZBJSA-N cholic acid Chemical compound C([C@H]1C[C@H]2O)[C@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H]([C@@H](CCC(O)=O)C)[C@@]2(C)[C@@H](O)C1 BHQCQFFYRZLCQQ-OELDTZBJSA-N 0.000 description 1
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Classifications
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- 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
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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
- A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
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- 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
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- 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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- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
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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
- A61K47/44—Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
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- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0014—Skin, i.e. galenical aspects of topical compositions
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- A61K9/06—Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
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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
- A61K9/08—Solutions
-
- 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
- A61K9/70—Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
- A61K9/7023—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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Abstract
Description
PIV | PIV | |
N-metil-2-pirrolidona (NMP) | 40% | 40% |
Dimetil Sulfóxido (DMSO) | 40% | 40% |
Alcool Etilico | 15% | 15% |
Carbopol 971P | - | 0,5% |
Água | 5% | 4,5% |
Total | 100,00% | 100,00% |
Formulação | NMP | DMSO | Álcool | Água |
1. | 50 | 50 | - | — |
2. | 40 | 40 | 20 | — |
3. | 40 | 40 | — | 20 |
4. | 40 | 40 | 15 | 5 |
5. | 40 | 40 | 10 | 10 |
6. | 40 | 40 | 5 | 15 |
7. | 30 | 30 | 20 | 20 |
8. | 30 | 30 | 30 | 10 |
9. | 30 | 40 | 25 | 5 |
10. | 40 | 30 | 25 | 5 |
11. | 45 | 45 | 10 | 0 |
12. | 45 | 40 | 10 | 5 |
Claims (6)
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
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US40759110P | 2010-10-28 | 2010-10-28 | |
PCT/US2011/057080 WO2012058091A2 (en) | 2010-10-28 | 2011-10-20 | Aripiprazole compositions and methods for its transdermal delivery |
Publications (2)
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BR112013010190A2 BR112013010190A2 (pt) | 2016-09-13 |
BR112013010190B1 true BR112013010190B1 (pt) | 2019-12-31 |
Family
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BR112013010190A BR112013010190B1 (pt) | 2010-10-28 | 2011-10-20 | composição farmacêutica |
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US (2) | US9138402B2 (pt) |
EP (1) | EP2632463B1 (pt) |
JP (2) | JP5966228B2 (pt) |
CN (2) | CN107929239B (pt) |
AU (1) | AU2011320758B2 (pt) |
BR (1) | BR112013010190B1 (pt) |
CA (1) | CA2816203C (pt) |
ES (1) | ES2675913T3 (pt) |
MX (1) | MX339196B (pt) |
RU (1) | RU2589689C2 (pt) |
WO (1) | WO2012058091A2 (pt) |
Families Citing this family (8)
Publication number | Priority date | Publication date | Assignee | Title |
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US9757374B2 (en) | 2010-10-28 | 2017-09-12 | Aequus Pharmaceuticals Inc. | Aripiprazole compositions and methods for its transdermal delivery |
WO2014172344A1 (en) * | 2013-04-16 | 2014-10-23 | Alpha To Omega Pharmaceutical Consultants, Inc. | Pharmaceutical compositions |
US10356018B2 (en) * | 2014-01-31 | 2019-07-16 | Vivint, Inc. | User management methods and systems |
CN107920989A (zh) * | 2015-06-08 | 2018-04-17 | 考里安国际公司 | 用于透皮递送阿立哌唑的制剂 |
WO2017025912A1 (en) * | 2015-08-13 | 2017-02-16 | Aequus Pharmaceuticals Inc. | Aripiprazole compositions and methods for its transdermal delivery |
JP2019515032A (ja) * | 2016-04-25 | 2019-06-06 | 大塚製薬株式会社 | 摂取型イベントマーカーを有する医薬品の組成物 |
EP3441068A4 (en) * | 2016-05-12 | 2019-04-10 | FUJIFILM Corporation | TRANSDERMALES PREPARATION |
WO2018117125A1 (ja) * | 2016-12-19 | 2018-06-28 | 富士フイルム株式会社 | 経皮製剤 |
Family Cites Families (24)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
IL101492A0 (en) | 1992-04-03 | 1992-12-30 | Shalom Levy | Anti-skin rash preparation |
US5616602A (en) * | 1993-07-09 | 1997-04-01 | Ciba-Geigy Corporation | Topically administrable zinc phthalocyanine compositions |
ATE200979T1 (de) * | 1994-02-18 | 2001-05-15 | Drossapharm Ag | Transdermales therapeutisches system |
US5558071A (en) * | 1994-03-07 | 1996-09-24 | Combustion Electromagnetics, Inc. | Ignition system power converter and controller |
IL134830A0 (en) * | 2000-03-01 | 2001-05-20 | Chay 13 Medical Res Group N V | Peptides and immunostimulatory and anti-bacterial pharmaceutical compositions containing them |
DE10030716A1 (de) * | 2000-06-23 | 2002-01-03 | Degussa | Tieftemperaturschlagzähe Polymerlegierung |
DE10110953A1 (de) * | 2001-03-07 | 2002-09-19 | Lohmann Therapie Syst Lts | Transdermales therapeutisches System zur Verabreichung von partiellen Dopamin-D2-Agonisten |
US20040170672A1 (en) * | 2001-03-07 | 2004-09-02 | Thorsten Selzer | Transdermal therapeutic system for administration of partial dopamine-d2 agonists |
CA2428237C (en) | 2003-05-08 | 2010-07-20 | Delmar Chemicals Inc. | Process for the preparation of carbostyril derivatives |
JP4836797B2 (ja) * | 2003-10-23 | 2011-12-14 | 大塚製薬株式会社 | 放出制御性無菌注射アリピプラゾール製剤および方法 |
PT1613598E (pt) | 2003-12-16 | 2012-01-13 | Teva Pharma | Métodos para preparar formas cristalinas de aripiprazol |
CA2622758A1 (en) * | 2005-09-15 | 2007-03-29 | Elan Pharma International, Limited | Nanoparticulate aripiprazole formulations |
KR101329658B1 (ko) * | 2006-09-25 | 2013-11-14 | 아처 다니엘 미드랜드 캄파니 | 초흡수성 표면처리된 카르복시알킬화 다당류 및 그 제조방법 |
CA2665105A1 (en) * | 2006-10-05 | 2008-04-10 | Panacea Biotec Ltd. | Injectable depot composition and its' process of preparation |
US20130084243A1 (en) * | 2010-01-27 | 2013-04-04 | Liliane Goetsch | Igf-1r specific antibodies useful in the detection and diagnosis of cellular proliferative disorders |
CL2008003305A1 (es) * | 2007-11-06 | 2009-06-05 | M/S Panacea Biotec Ltd | Composicion inyectable que comprende un agente activo seleccionado de un grupo definido; al menos un polimero bioerosionable, al menos un solvente no toxico y opcionalmente uno o mas excipientes; proceso de preparacion; uso para tratar enfermedades mentales o cancer. |
EP2889029A1 (en) * | 2008-09-25 | 2015-07-01 | Cephalon, Inc. | Liquid formulations of bendamustine |
GB0905365D0 (en) * | 2009-03-27 | 2009-05-13 | Norbrook Lab Ltd | A topical parasiticide composition |
EP2238976B1 (en) * | 2009-04-03 | 2012-06-27 | Hexal AG | Oral films comprising 7-[4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butoxy]-3,4-dihydro- 1H-quinolin-2-one base or salts or hydrates thereof |
US8815261B2 (en) * | 2009-06-19 | 2014-08-26 | Medrx Co., Ltd. | Composition for external application comprising aripiprazole and organic acid as active ingredients |
US20110028412A1 (en) * | 2009-08-03 | 2011-02-03 | Cappellos, Inc. | Herbal enhanced analgesic formulations |
US9358261B2 (en) * | 2011-10-25 | 2016-06-07 | U.S. Phytotherapy, Inc. | Additional artemisinin and berberine compositions and methods of making |
US9968740B2 (en) * | 2014-03-25 | 2018-05-15 | Surefire Medical, Inc. | Closed tip dynamic microvalve protection device |
US9468206B2 (en) * | 2014-12-31 | 2016-10-18 | Valent U.S.A., Corporation | Lactofen and dicamba diglycol amine liquid formulations |
-
2011
- 2011-10-20 JP JP2013536677A patent/JP5966228B2/ja active Active
- 2011-10-20 AU AU2011320758A patent/AU2011320758B2/en not_active Ceased
- 2011-10-20 ES ES11836886.9T patent/ES2675913T3/es active Active
- 2011-10-20 CN CN201711272197.4A patent/CN107929239B/zh not_active Expired - Fee Related
- 2011-10-20 WO PCT/US2011/057080 patent/WO2012058091A2/en active Application Filing
- 2011-10-20 RU RU2013124401/15A patent/RU2589689C2/ru active
- 2011-10-20 CA CA2816203A patent/CA2816203C/en active Active
- 2011-10-20 CN CN201180052667.0A patent/CN103491961B/zh not_active Expired - Fee Related
- 2011-10-20 US US13/879,485 patent/US9138402B2/en active Active
- 2011-10-20 BR BR112013010190A patent/BR112013010190B1/pt not_active IP Right Cessation
- 2011-10-20 EP EP11836886.9A patent/EP2632463B1/en active Active
- 2011-10-20 MX MX2013004693A patent/MX339196B/es active IP Right Grant
-
2012
- 2012-11-05 US US13/668,500 patent/US20130171237A1/en not_active Abandoned
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2016
- 2016-06-16 JP JP2016119741A patent/JP2016164204A/ja active Pending
Also Published As
Publication number | Publication date |
---|---|
CN107929239A (zh) | 2018-04-20 |
US20130171237A1 (en) | 2013-07-04 |
EP2632463A2 (en) | 2013-09-04 |
EP2632463A4 (en) | 2016-04-20 |
AU2011320758A1 (en) | 2013-05-09 |
CN107929239B (zh) | 2021-06-01 |
RU2013124401A (ru) | 2014-12-10 |
MX2013004693A (es) | 2013-11-01 |
JP2016164204A (ja) | 2016-09-08 |
CA2816203C (en) | 2017-02-21 |
JP5966228B2 (ja) | 2016-08-10 |
US9138402B2 (en) | 2015-09-22 |
ES2675913T3 (es) | 2018-07-13 |
JP2014503479A (ja) | 2014-02-13 |
WO2012058091A3 (en) | 2013-10-17 |
CN103491961B (zh) | 2018-01-02 |
RU2589689C2 (ru) | 2016-07-10 |
US20130209552A1 (en) | 2013-08-15 |
CN103491961A (zh) | 2014-01-01 |
AU2011320758B2 (en) | 2015-09-24 |
WO2012058091A2 (en) | 2012-05-03 |
CA2816203A1 (en) | 2012-05-03 |
BR112013010190A2 (pt) | 2016-09-13 |
MX339196B (es) | 2016-05-16 |
EP2632463B1 (en) | 2018-04-04 |
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