AR102101A2 - Formulación y método de complejo de aripiprazol - Google Patents
Formulación y método de complejo de aripiprazolInfo
- Publication number
- AR102101A2 AR102101A2 ARP150103114A ARP150103114A AR102101A2 AR 102101 A2 AR102101 A2 AR 102101A2 AR P150103114 A ARP150103114 A AR P150103114A AR P150103114 A ARP150103114 A AR P150103114A AR 102101 A2 AR102101 A2 AR 102101A2
- Authority
- AR
- Argentina
- Prior art keywords
- cyclodextrin
- formulation
- aripiprazole
- complex
- sbecd
- Prior art date
Links
- CEUORZQYGODEFX-UHFFFAOYSA-N Aripirazole Chemical compound ClC1=CC=CC(N2CCN(CCCCOC=3C=C4NC(=O)CCC4=CC=3)CC2)=C1Cl CEUORZQYGODEFX-UHFFFAOYSA-N 0.000 title abstract 5
- 238000009472 formulation Methods 0.000 title abstract 5
- 239000000203 mixture Substances 0.000 title abstract 5
- 238000000034 method Methods 0.000 title abstract 3
- WHGYBXFWUBPSRW-FOUAGVGXSA-N beta-cyclodextrin Chemical compound OC[C@H]([C@H]([C@@H]([C@H]1O)O)O[C@H]2O[C@@H]([C@@H](O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O3)[C@H](O)[C@H]2O)CO)O[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@@H]3O[C@@H]1CO WHGYBXFWUBPSRW-FOUAGVGXSA-N 0.000 abstract 5
- 229960004372 aripiprazole Drugs 0.000 abstract 4
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 abstract 3
- NZAQRZWBQUIBSF-UHFFFAOYSA-N 4-(4-sulfobutoxy)butane-1-sulfonic acid Chemical compound OS(=O)(=O)CCCCOCCCCS(O)(=O)=O NZAQRZWBQUIBSF-UHFFFAOYSA-N 0.000 abstract 2
- 238000010255 intramuscular injection Methods 0.000 abstract 2
- 239000007927 intramuscular injection Substances 0.000 abstract 2
- 230000007794 irritation Effects 0.000 abstract 2
- ODLHGICHYURWBS-FOSILIAISA-N molport-023-220-444 Chemical compound CC(O)COC[C@@H]([C@@H]([C@H]([C@@H]1O)O)O[C@@H]2O[C@H]([C@H](O[C@@H]3O[C@@H](COCC(C)O)[C@@H]([C@H]([C@@H]3O)O)O[C@@H]3O[C@@H](COCC(C)O)[C@@H]([C@H]([C@@H]3O)O)O[C@@H]3O[C@@H](COCC(C)O)[C@@H]([C@H]([C@@H]3O)O)O[C@@H]3O[C@@H](COCC(C)O)[C@@H]([C@H]([C@@H]3O)O)O3)[C@@H](O)[C@@H]2O)COCC(O)C)O[C@H]1O[C@@H]1[C@@H](O)[C@H](O)[C@H]3O[C@H]1COCC(C)O ODLHGICHYURWBS-FOSILIAISA-N 0.000 abstract 2
- 229920000858 Cyclodextrin Polymers 0.000 abstract 1
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 abstract 1
- 239000003795 chemical substances by application Substances 0.000 abstract 1
- 201000000980 schizophrenia Diseases 0.000 abstract 1
- 235000002906 tartaric acid Nutrition 0.000 abstract 1
- 239000011975 tartaric acid Substances 0.000 abstract 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 abstract 1
Classifications
-
- 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
- A61K47/02—Inorganic 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
- A61K31/495—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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/715—Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
- A61K31/716—Glucans
- A61K31/724—Cyclodextrins
-
- 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
- A61K47/12—Carboxylic acids; Salts or anhydrides thereof
-
- 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
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
- A61K47/40—Cyclodextrins; Derivatives thereof
-
- 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
- A61K47/50—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/69—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit
- A61K47/6949—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit inclusion complexes, e.g. clathrates, cavitates or fullerenes
- A61K47/6951—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit inclusion complexes, e.g. clathrates, cavitates or fullerenes using cyclodextrin
-
- 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
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
-
- 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
-
- 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
-
- B—PERFORMING OPERATIONS; TRANSPORTING
- B82—NANOTECHNOLOGY
- B82Y—SPECIFIC USES OR APPLICATIONS OF NANOSTRUCTURES; MEASUREMENT OR ANALYSIS OF NANOSTRUCTURES; MANUFACTURE OR TREATMENT OF NANOSTRUCTURES
- B82Y5/00—Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nanotechnology (AREA)
- Molecular Biology (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Dermatology (AREA)
- Biotechnology (AREA)
- Inorganic Chemistry (AREA)
- Biophysics (AREA)
- General Engineering & Computer Science (AREA)
- Medical Informatics (AREA)
- Crystallography & Structural Chemistry (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Psychiatry (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Se proporciona una formulación de aripiprazol que incluye un agente antisicótico en la forma de un complejo de inclusión en una b-ciclodextrina, preferiblemente b-ciclodextrina de éter sulfobutilo (SBECD), que en la forma de un inyectable produce generalmente reversible irritación mínima a moderada en el sitio de inyección intramuscular. Se proporciona un método para minimizar o reducir la irritación causada por el aripiprazol en un sitio de inyección intramuscular y un método para tratar esquizofrenia mediante el empleo de la formulación anterior. Reivindicación 1: Un complejo de inclusión de aripiprazol en una b-ciclodextrina. Reivindicación 2: El complejo como se definió en la reivindicación 1 en donde la b-ciclodextrina es b-ciclodextrina de éter sulfobutilo (SBECD) o hidroxipropil-b-ciclodextrina (HPBCD). Reivindicación 18: La formulación como se definió en la reivindicación 11 que comprende aripiprazol en una cantidad para proveer de aproximadamente 1.5 a aproximadamente 8 mg/mL de formulación, SBECD en una cantidad en la escala de 100 a aproximadamente 200 mg/mL; ácido tartárico en una cantidad dentro de la escala de aproximadamente 7 a aproximadamente 9 mg/mL de hidróxido de sodio cs para ajustar el pH dentro de la escala de aproximadamente 4 a aproximadamente 4.6 y agua cs para 1 mL.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US40471302P | 2002-08-20 | 2002-08-20 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR102101A2 true AR102101A2 (es) | 2017-02-01 |
Family
ID=31946748
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
AR20030102990A AR040887A1 (es) | 2002-08-20 | 2003-08-19 | Formulacion y metodo de complejo de aripiprazol |
ARP150103114A AR102101A2 (es) | 2002-08-20 | 2015-09-28 | Formulación y método de complejo de aripiprazol |
Family Applications Before (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
AR20030102990A AR040887A1 (es) | 2002-08-20 | 2003-08-19 | Formulacion y metodo de complejo de aripiprazol |
Country Status (32)
Country | Link |
---|---|
US (8) | US7115587B2 (es) |
EP (1) | EP1542668B1 (es) |
JP (1) | JP4729306B2 (es) |
KR (1) | KR101043866B1 (es) |
CN (1) | CN100335047C (es) |
AR (2) | AR040887A1 (es) |
AT (1) | ATE428423T1 (es) |
AU (1) | AU2003269965B2 (es) |
BR (1) | BR0313602A (es) |
CA (1) | CA2495864C (es) |
CY (1) | CY1110331T1 (es) |
DE (1) | DE60327225D1 (es) |
DK (1) | DK1542668T3 (es) |
ES (1) | ES2322953T3 (es) |
GE (1) | GEP20063996B (es) |
HR (1) | HRP20050149B1 (es) |
IL (1) | IL166623A (es) |
IS (1) | IS2878B (es) |
MX (1) | MXPA05001865A (es) |
MY (1) | MY140793A (es) |
NO (1) | NO333458B1 (es) |
NZ (1) | NZ537995A (es) |
PE (1) | PE20040895A1 (es) |
PL (1) | PL212428B1 (es) |
PT (1) | PT1542668E (es) |
RS (1) | RS51903B (es) |
RU (1) | RU2342931C2 (es) |
SI (1) | SI1542668T1 (es) |
TW (1) | TWI307626B (es) |
UA (1) | UA79984C2 (es) |
WO (1) | WO2004017897A2 (es) |
ZA (1) | ZA200501064B (es) |
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US20040170705A1 (en) * | 2001-03-08 | 2004-09-02 | Dusan Miljkovic | Compositions and methods for non-insulin glucose uptake |
RU2342931C2 (ru) * | 2002-08-20 | 2009-01-10 | Бристол-Маерс Сквибб Компани | Состав на основе комплекса арипипразола |
CN1870980B (zh) * | 2003-10-23 | 2010-06-23 | 大冢制药株式会社 | 控释无菌阿立哌唑注射剂和方法 |
US7714129B2 (en) | 2003-12-16 | 2010-05-11 | Teva Pharmaceutical Industries Ltd. | Methods of preparing anhydrous aripiprazole form II |
TW200529850A (en) * | 2003-12-16 | 2005-09-16 | Teva Pharma | Methods of preparing aripiprazole crystalline forms |
UA89513C2 (uk) * | 2004-12-03 | 2010-02-10 | Элан Фарма Интернешнл Лтд. | Стабільна композиція з наночастинок ралоксифену гідрохлориду |
JP2008536856A (ja) * | 2005-04-13 | 2008-09-11 | エラン・ファルマ・インターナショナル・リミテッド | プロスタグランジン誘導体を含んでなるナノ粒子状且つ徐放性の組成物 |
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US8501740B2 (en) * | 2007-10-09 | 2013-08-06 | Board Of Regents, The University Of Texas System | Methods of treatment of opioid tolerance, physical dependence, pain and addiction with inhibitors of certain growth factor receptors |
KR20110007095A (ko) * | 2008-03-21 | 2011-01-21 | 엘란 파마 인터내셔널 리미티드 | 이마티니브의 부위-특이적 전달을 위한 조성물 및 사용방법 |
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CA2867123C (en) | 2012-03-19 | 2021-02-16 | Alkermes Pharma Ireland Limited | Pharmaceutical compositions comprising water-insoluble antipsychotic agents and glycerol esters |
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JP2022543837A (ja) | 2019-08-05 | 2022-10-14 | マリナス ファーマシューティカルズ, インコーポレイテッド | てんかん重積状態の治療に使用するためのガナキソロン |
JP2023503928A (ja) | 2019-12-06 | 2023-02-01 | マリナス ファーマシューティカルズ, インコーポレイテッド | 結節性硬化症の治療での使用のためのガナキソロン |
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US5376645A (en) | 1990-01-23 | 1994-12-27 | University Of Kansas | Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof |
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