AR066905A1 - Administracion intranasal de asenapina y composiciones farmaceuticas correspondientes - Google Patents
Administracion intranasal de asenapina y composiciones farmaceuticas correspondientesInfo
- Publication number
- AR066905A1 AR066905A1 ARP080102394A ARP080102394A AR066905A1 AR 066905 A1 AR066905 A1 AR 066905A1 AR P080102394 A ARP080102394 A AR P080102394A AR P080102394 A ARP080102394 A AR P080102394A AR 066905 A1 AR066905 A1 AR 066905A1
- Authority
- AR
- Argentina
- Prior art keywords
- agent
- formulation according
- acid
- salt
- polyol
- Prior art date
Links
- VSWBSWWIRNCQIJ-GJZGRUSLSA-N (R,R)-asenapine Chemical compound O1C2=CC=CC=C2[C@@H]2CN(C)C[C@H]2C2=CC(Cl)=CC=C21 VSWBSWWIRNCQIJ-GJZGRUSLSA-N 0.000 title abstract 2
- 229960005245 asenapine Drugs 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 239000003795 chemical substances by application Substances 0.000 abstract 5
- 238000009472 formulation Methods 0.000 abstract 5
- 239000000203 mixture Substances 0.000 abstract 5
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 abstract 3
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 abstract 3
- 229920005862 polyol Polymers 0.000 abstract 3
- 150000003077 polyols Chemical class 0.000 abstract 3
- 150000003839 salts Chemical class 0.000 abstract 3
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 abstract 3
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 abstract 2
- 239000003112 inhibitor Substances 0.000 abstract 2
- 239000007788 liquid Substances 0.000 abstract 2
- 239000003961 penetration enhancing agent Substances 0.000 abstract 2
- HFHDHCJBZVLPGP-UHFFFAOYSA-N schardinger α-dextrin Chemical compound O1C(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(O)C2O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC2C(O)C(O)C1OC2CO HFHDHCJBZVLPGP-UHFFFAOYSA-N 0.000 abstract 2
- 239000003981 vehicle Substances 0.000 abstract 2
- 239000004475 Arginine Substances 0.000 abstract 1
- 229920000858 Cyclodextrin Polymers 0.000 abstract 1
- KCXVZYZYPLLWCC-UHFFFAOYSA-N EDTA Chemical compound OC(=O)CN(CC(O)=O)CCN(CC(O)=O)CC(O)=O KCXVZYZYPLLWCC-UHFFFAOYSA-N 0.000 abstract 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 abstract 1
- XUJNEKJLAYXESH-REOHCLBHSA-N L-Cysteine Chemical compound SC[C@H](N)C(O)=O XUJNEKJLAYXESH-REOHCLBHSA-N 0.000 abstract 1
- ODKSFYDXXFIFQN-BYPYZUCNSA-P L-argininium(2+) Chemical compound NC(=[NH2+])NCCC[C@H]([NH3+])C(O)=O ODKSFYDXXFIFQN-BYPYZUCNSA-P 0.000 abstract 1
- FFEARJCKVFRZRR-BYPYZUCNSA-N L-methionine Chemical compound CSCC[C@H](N)C(O)=O FFEARJCKVFRZRR-BYPYZUCNSA-N 0.000 abstract 1
- AYFVYJQAPQTCCC-GBXIJSLDSA-N L-threonine Chemical compound C[C@@H](O)[C@H](N)C(O)=O AYFVYJQAPQTCCC-GBXIJSLDSA-N 0.000 abstract 1
- RVGRUAULSDPKGF-UHFFFAOYSA-N Poloxamer Chemical compound C1CO1.CC1CO1 RVGRUAULSDPKGF-UHFFFAOYSA-N 0.000 abstract 1
- 239000002202 Polyethylene glycol Substances 0.000 abstract 1
- WCUXLLCKKVVCTQ-UHFFFAOYSA-M Potassium chloride Chemical compound [Cl-].[K+] WCUXLLCKKVVCTQ-UHFFFAOYSA-M 0.000 abstract 1
- AYFVYJQAPQTCCC-UHFFFAOYSA-N Threonine Natural products CC(O)C(N)C(O)=O AYFVYJQAPQTCCC-UHFFFAOYSA-N 0.000 abstract 1
- 239000004473 Threonine Substances 0.000 abstract 1
- 102000004142 Trypsin Human genes 0.000 abstract 1
- 108090000631 Trypsin Proteins 0.000 abstract 1
- 238000010521 absorption reaction Methods 0.000 abstract 1
- 125000000738 acetamido group Chemical group [H]C([H])([H])C(=O)N([H])[*] 0.000 abstract 1
- -1 acetoacetic acid glycerol ester Chemical class 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 239000000654 additive Substances 0.000 abstract 1
- 230000000996 additive effect Effects 0.000 abstract 1
- 230000002776 aggregation Effects 0.000 abstract 1
- 238000004220 aggregation Methods 0.000 abstract 1
- QFAADIRHLBXJJS-ZAZJUGBXSA-N amastatin Chemical compound CC(C)C[C@@H](N)[C@H](O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](C(O)=O)CC(O)=O QFAADIRHLBXJJS-ZAZJUGBXSA-N 0.000 abstract 1
- 108010052590 amastatin Proteins 0.000 abstract 1
- 235000001014 amino acid Nutrition 0.000 abstract 1
- 150000001413 amino acids Chemical class 0.000 abstract 1
- ODKSFYDXXFIFQN-UHFFFAOYSA-N arginine Natural products OC(=O)C(N)CCCNC(N)=N ODKSFYDXXFIFQN-UHFFFAOYSA-N 0.000 abstract 1
- 239000000022 bacteriostatic agent Substances 0.000 abstract 1
- 229960000686 benzalkonium chloride Drugs 0.000 abstract 1
- CADWTSSKOVRVJC-UHFFFAOYSA-N benzyl(dimethyl)azanium;chloride Chemical compound [Cl-].C[NH+](C)CC1=CC=CC=C1 CADWTSSKOVRVJC-UHFFFAOYSA-N 0.000 abstract 1
- 239000003833 bile salt Substances 0.000 abstract 1
- 239000006172 buffering agent Substances 0.000 abstract 1
- 230000015556 catabolic process Effects 0.000 abstract 1
- 230000000536 complexating effect Effects 0.000 abstract 1
- 239000008139 complexing agent Substances 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- XUJNEKJLAYXESH-UHFFFAOYSA-N cysteine Natural products SCC(N)C(O)=O XUJNEKJLAYXESH-UHFFFAOYSA-N 0.000 abstract 1
- 235000018417 cysteine Nutrition 0.000 abstract 1
- 238000006731 degradation reaction Methods 0.000 abstract 1
- 235000014113 dietary fatty acids Nutrition 0.000 abstract 1
- 150000002081 enamines Chemical class 0.000 abstract 1
- 230000002708 enhancing effect Effects 0.000 abstract 1
- 229940125532 enzyme inhibitor Drugs 0.000 abstract 1
- 239000002532 enzyme inhibitor Substances 0.000 abstract 1
- 239000003172 expectorant agent Substances 0.000 abstract 1
- 229930195729 fatty acid Natural products 0.000 abstract 1
- 239000000194 fatty acid Substances 0.000 abstract 1
- 150000004665 fatty acids Chemical class 0.000 abstract 1
- 239000002502 liposome Substances 0.000 abstract 1
- 229930182817 methionine Natural products 0.000 abstract 1
- 239000000693 micelle Substances 0.000 abstract 1
- 229940066491 mucolytics Drugs 0.000 abstract 1
- 210000003097 mucus Anatomy 0.000 abstract 1
- 239000002840 nitric oxide donor Substances 0.000 abstract 1
- 150000003904 phospholipids Chemical class 0.000 abstract 1
- 230000035479 physiological effects, processes and functions Effects 0.000 abstract 1
- 229960000502 poloxamer Drugs 0.000 abstract 1
- 229920001983 poloxamer Polymers 0.000 abstract 1
- 229920000724 poly(L-arginine) polymer Polymers 0.000 abstract 1
- 108010011110 polyarginine Proteins 0.000 abstract 1
- 229920001223 polyethylene glycol Polymers 0.000 abstract 1
- 229960001860 salicylate Drugs 0.000 abstract 1
- YGSDEFSMJLZEOE-UHFFFAOYSA-M salicylate Chemical compound OC1=CC=CC=C1C([O-])=O YGSDEFSMJLZEOE-UHFFFAOYSA-M 0.000 abstract 1
- 150000003872 salicylic acid derivatives Chemical class 0.000 abstract 1
- 239000011780 sodium chloride Substances 0.000 abstract 1
- OABYVIYXWMZFFJ-ZUHYDKSRSA-M sodium glycocholate Chemical compound [Na+].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)NCC([O-])=O)C)[C@@]2(C)[C@@H](O)C1 OABYVIYXWMZFFJ-ZUHYDKSRSA-M 0.000 abstract 1
- 239000004094 surface-active agent Substances 0.000 abstract 1
- 239000012588 trypsin Substances 0.000 abstract 1
- 239000003071 vasodilator agent 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
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0043—Nose
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
-
- 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
- A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Otolaryngology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurosurgery (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Psychiatry (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
La asenapina o una sal farmacéuticamente aceptable de la misma, puede ser administrada intranasalmente, típicamente por medio de una formulacion de dosificacion intranasal con un vehículo líquido con contenido de agua. Reivindicacion 2: La formulacion de acuerdo con la reivindicacion 1, caracterizada porque dicho vehículo líquido que contiene agua comprende agua y un poliol, preferentemente dicho poliol es polietilenglicol o propilenglicol. Reivindicacion 5: La formulacion de acuerdo con las reivindicaciones 1-4, que comprende asimismo un agente bacteriostático y/o un agente buffer. Reivindicacion 6: La formulacion de acuerdo con las reivindicaciones 1-5, que comprende asimismo un agente mejorador de la penetracion, seleccionado dentro del grupo que comprende: (a) un agente mejorador de la absorcion; (b) un agente inhibidor de la agregacion; (c) un agente inhibidor de la enzima de degradacion; (d) un agente mucolítico o liberador de la mucosidad; (e) un agente ciliostático; (f) un agente modulador de la fisiología de la union epitelial; (g) un agente vasodilatador; y (h) una especie formadora de complejos. Reivindicacion 7: La formulacion de acuerdo con la reivindicacion 6, caracterizada porque dicho agente mejorador de la penetracion se selecciona dentro del grupo consistente en un tensioactivo, una sal biliar, un aditivo fosfolípido, una micela mixta, un liposoma, un alcohol, una enamina, un compuesto dador de oxido nítrico, un derivado de ácido salicílico, un gliceroléster de ácido acetoacético, una ciclodextrina, un derivado de ciclodextrina, un ácido graso C1-12, un aminoácido o sal del mismo, un agente formador de complejos, un inhibidor de tripsina, un azucar, y combinaciones de los mismos, tal como un ácido acetilamino o sal del mismo, NaCl, KCl, amastatina, glicocolato de sodio, metionina, cisteína, treonina, cloruro de benzalconio, EDTA, ácido cítrico, un poloxámero, un poliol, un salicilato, arginina, poliarginina, y combinaciones de los mismos.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US94208207P | 2007-06-05 | 2007-06-05 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR066905A1 true AR066905A1 (es) | 2009-09-23 |
Family
ID=39876712
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP080102394A AR066905A1 (es) | 2007-06-05 | 2008-06-05 | Administracion intranasal de asenapina y composiciones farmaceuticas correspondientes |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US20080306133A1 (es) |
| EP (1) | EP2170399A1 (es) |
| AR (1) | AR066905A1 (es) |
| CL (1) | CL2008001605A1 (es) |
| WO (1) | WO2008148515A1 (es) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2010127674A1 (en) * | 2009-05-06 | 2010-11-11 | Sunin K/S | Transdermal compositions of asenapine for the treatment of psychiatric disorders |
| US8779161B2 (en) | 2010-06-18 | 2014-07-15 | Dr. Reddy's Laboratories Limited | Asenapine maleate |
| EP2524920A1 (en) * | 2011-05-17 | 2012-11-21 | Sandoz AG | Novel Crystalline Asenapine Hydrochloride Salt Forms |
| EP2524919A1 (en) | 2011-05-17 | 2012-11-21 | Sandoz AG | Novel crystalline salts of Asenapine with organic Di-acids and Tri-acids |
| JP6014656B2 (ja) * | 2011-05-18 | 2016-10-25 | ラビラトリオス レスビ エス エレ | 化合物の多形体 |
| WO2014127786A1 (en) * | 2013-02-22 | 2014-08-28 | Zentiva, K.S. | Orally disintegrating pharmaceutical composition comprising asenapine |
| US10085971B2 (en) | 2016-08-22 | 2018-10-02 | Navinta Iii Inc | Pharmaceutical solution of asenapine for sublingual or buccal use |
| MX382195B (es) | 2016-12-20 | 2025-03-13 | Lts Lohmann Therapie Systeme Ag | Sistema terapeutico transdermico que contiene asenapina |
| CN110087641B (zh) | 2016-12-20 | 2024-03-12 | 罗曼治疗系统股份公司 | 含有阿塞那平和聚硅氧烷或聚异丁烯的透皮治疗系统 |
| CN110799180A (zh) | 2017-06-26 | 2020-02-14 | 罗曼治疗系统股份公司 | 含阿塞那平和硅氧烷丙烯酸杂化聚合物的经皮治疗系统 |
| PL3810100T3 (pl) | 2018-06-20 | 2025-05-12 | Lts Lohmann Therapie-Systeme Ag | Transdermalny system terapeutyczny zawierający asenapinę |
| US12329862B2 (en) | 2018-06-20 | 2025-06-17 | Lts Lohmann Therapie-Systeme Ag | Transdermal therapeutic system containing asenapine |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NL7605526A (nl) * | 1976-05-24 | 1977-11-28 | Akzo Nv | Nieuwe tetracyclische derivaten. |
| US20030225031A1 (en) * | 2002-05-21 | 2003-12-04 | Quay Steven C. | Administration of acetylcholinesterase inhibitors to the cerebral spinal fluid |
| JP2007519705A (ja) * | 2004-01-29 | 2007-07-19 | ファイザー・プロダクツ・インク | Ｃｎｓ障害を治療するための非定型抗精神病薬とアミノメチルピリジルオキシメチル／ベンゾイソオキサゾールアザビシクロ誘導体の組合せ |
| BRPI0507609A (pt) * | 2004-02-13 | 2007-07-03 | Pfizer Prod Inc | combinações terapêuticas de anti-psicóticos atìpicos com antagonistas de fator de liberação de corticotropina |
| CA2565996A1 (en) * | 2004-05-11 | 2005-11-17 | Pfizer Products Inc. | Combination of atypical antipsychotics and 5-ht1b receptor antagonists |
| US20060039869A1 (en) * | 2004-08-17 | 2006-02-23 | Daniel Wermeling | Intranasal delivery of antipsychotic drugs |
-
2008
- 2008-05-29 EP EP08749503A patent/EP2170399A1/en not_active Withdrawn
- 2008-05-29 WO PCT/EP2008/004394 patent/WO2008148515A1/en not_active Ceased
- 2008-06-02 CL CL2008001605A patent/CL2008001605A1/es unknown
- 2008-06-04 US US12/133,106 patent/US20080306133A1/en not_active Abandoned
- 2008-06-05 AR ARP080102394A patent/AR066905A1/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| WO2008148515A1 (en) | 2008-12-11 |
| EP2170399A1 (en) | 2010-04-07 |
| US20080306133A1 (en) | 2008-12-11 |
| CL2008001605A1 (es) | 2009-05-04 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |