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AR079008A1 - Co-cristales de tramadol y coxibs, proceso de preparacion y composicion farmaceutica - Google Patents

Co-cristales de tramadol y coxibs, proceso de preparacion y composicion farmaceutica

Info

Publication number
AR079008A1
AR079008A1 ARP100103777A ARP100103777A AR079008A1 AR 079008 A1 AR079008 A1 AR 079008A1 AR P100103777 A ARP100103777 A AR P100103777A AR P100103777 A ARP100103777 A AR P100103777A AR 079008 A1 AR079008 A1 AR 079008A1
Authority
AR
Argentina
Prior art keywords
crystal
tramadol
increased
solution
coxib
Prior art date
Application number
ARP100103777A
Other languages
English (en)
Original Assignee
Esteve Labor Dr
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from PCT/EP2009/007451 external-priority patent/WO2010043412A1/en
Application filed by Esteve Labor Dr filed Critical Esteve Labor Dr
Publication of AR079008A1 publication Critical patent/AR079008A1/es

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/13Amines
    • A61K31/135Amines having aromatic rings, e.g. ketamine, nortriptyline
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/63Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide
    • A61K31/635Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide having a heterocyclic ring, e.g. sulfadiazine
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/045Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/045Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
    • A61K31/05Phenols
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/13Amines
    • A61K31/135Amines having aromatic rings, e.g. ketamine, nortriptyline
    • A61K31/137Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/195Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/196Carboxylic acids, e.g. valproic acid having an amino group the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C213/00Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton
    • C07C213/10Separation; Purification; Stabilisation; Use of additives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C217/00Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton
    • C07C217/54Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
    • C07C217/74Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with rings other than six-membered aromatic rings being part of the carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/40Unsaturated compounds
    • C07C59/58Unsaturated compounds containing ether groups, groups, groups, or groups
    • C07C59/64Unsaturated compounds containing ether groups, groups, groups, or groups containing six-membered aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00Systems containing only non-condensed rings
    • C07C2601/12Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14The ring being saturated

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Rheumatology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Biomedical Technology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Emergency Medicine (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicinal Preparation (AREA)

Abstract

La presente solicitud se refiere a co-cristales de tramadol y formadores de co-cristal seleccionados de NSAIDs/coxibs, procesos para preparacion de los mismos y sus usos como medicamentos o en formulaciones farmacéuticas, más particularmente para el tratamiento del dolor. Reivindicacion 1: Un co-cristal que comprende tramadol tanto como una base libre o como una sal fisiologicamente aceptable y por lo menos un coxib. Reivindicacion 2: Un co-cristal de acuerdo con la reivindicacion 1, donde el coxib se elige de tal manera que si se compara tanto con tramadol solo, como una mezcla de tramadol y el correspondiente coxib, como agente/s activo/s: la solubilidad del co-cristal se incrementa; y/o la respuesta de dosis del co-cristal se incrementa; y/o la eficacia del co-cristal se incrementa; y/o la disolucion del co-cristal se incrementa; y/o la biodisponibilidad del co-cristal se incrementa; y/o la estabilidad del co-cristal se incrementa; y/o la higroscopicidad del co-cristal se disminuye; y/o la diversidad de forma del co-cristal se disminuye; y/o la morfología del co-cristal se modula. Reivindicacion 13: Un proceso para la produccion de un co-cristal de acuerdo con reivindicacion 1 que comprende los pasos de: (a) disolver o suspender el coxib en un solvente; opcionalmente calentando la solucion o dispersion a una temperatura por encima de temperatura ambiente y por debajo del punto de ebullicion de la solucion o dispersion; (b) disolver junto con, o después, o antes del paso (a) tramadol ya sea como una base libre o como una sal en un solvente, opcionalmente combinado con el paso (a) mediante disolucion de tramadol ya junto con el coxib en el paso (a), (c) opcionalmente anadir la solucion de (b) a una solucion de (a) y mezclarlos; (d) opcionalmente anadir un solvente a la solucion de (a), (b) o (c) y mezclarlos; (e) enfriar la solucion/dispersion mezclada del paso (a), (b), (c) o (d) a temperatura ambiente o por debajo; (f) opcionalmente evaporar parte o todo el solvente; y (g) recoger mediante filtracion los co-cristales resultantes. Reivindicacion 14: Una composicion farmacéutica caracterizada por cuanto comprende una cantidad terapéuticamente eficaz del co-cristal de acuerdo con cualquiera de las reivindicaciones 1 a 12 en un medio fisiologicamente aceptable.
ARP100103777A 2009-10-16 2010-10-15 Co-cristales de tramadol y coxibs, proceso de preparacion y composicion farmaceutica AR079008A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
PCT/EP2009/007451 WO2010043412A1 (en) 2008-10-17 2009-10-16 Co-crystals of tramadol and nsaids
PCT/EP2010/002385 WO2011044962A1 (en) 2009-10-16 2010-04-19 Co-crystals of tramadol and coxibs

Publications (1)

Publication Number Publication Date
AR079008A1 true AR079008A1 (es) 2011-12-21

Family

ID=42272447

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP100103777A AR079008A1 (es) 2009-10-16 2010-10-15 Co-cristales de tramadol y coxibs, proceso de preparacion y composicion farmaceutica

Country Status (19)

Country Link
US (1) US20230057884A1 (es)
JP (1) JP5399564B2 (es)
KR (1) KR101471585B1 (es)
CN (3) CN104844513B (es)
AR (1) AR079008A1 (es)
AU (1) AU2010306168B2 (es)
BR (1) BR112012005011B8 (es)
CA (1) CA2771665C (es)
CO (1) CO6511248A2 (es)
HR (1) HRP20130316T1 (es)
IL (1) IL218256A (es)
MA (1) MA33742B1 (es)
MX (1) MX2012003050A (es)
NZ (1) NZ598353A (es)
PT (1) PT2488169E (es)
SG (1) SG178835A1 (es)
TW (1) TWI441630B (es)
WO (1) WO2011044962A1 (es)
ZA (1) ZA201201892B (es)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2177215A1 (en) 2008-10-17 2010-04-21 Laboratorios Del. Dr. Esteve, S.A. Co-crystals of tramadol and NSAIDs
EP2311446A1 (en) * 2009-10-16 2011-04-20 Laboratorios Del. Dr. Esteve, S.A. Compositions comprising Tramadol and Celecoxib in the treatment of pain
KR101710792B1 (ko) * 2015-07-14 2017-02-28 주식회사 유영제약 세레콕시브 및 트라마돌을 함유하는 약제학적 조성물
MX2016006464A (es) * 2016-05-18 2017-11-17 Laboratorios Liomont S A De C V Composicion farmaceutica de una combinacion de clorhidrato de tramadol-etoricoxib para el tratamiento del dolor.
CN107648228A (zh) * 2017-10-24 2018-02-02 珠海赛隆药业股份有限公司 一种帕瑞昔布钠与盐酸曲马多组成的复合物及其用途
MX2018013070A (es) 2017-12-29 2019-10-15 Gruenenthal Gmbh Combinación farmacéutica que comprende clorhidrato de tramadol de liberación extendida y etoricoxib de liberación inmediata, y su uso para el tratamiento del dolor.
CA3137381A1 (en) * 2019-05-14 2020-11-19 Esteve Pharmaceuticals, S.A. Use of co-crystals of tramadol and celecoxib for treating pain while reducing the abuse liability of tramadol
CN112007024A (zh) * 2019-05-28 2020-12-01 江苏恒瑞医药股份有限公司 艾瑞昔布与曲马多联合在制备治疗疼痛的药物中的用途

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU661723B2 (en) * 1991-10-30 1995-08-03 Mcneilab, Inc. Composition comprising a tramadol material and a non-steroidal anti-inflammatory drug
WO2008085674A1 (en) * 2007-01-04 2008-07-17 Transform Pharmaceuticals, Inc. Pharmaceutical compositions comprising celecoxib co-crystals
US20080031950A1 (en) * 2007-04-27 2008-02-07 Nectid Inc. Novel anelgesic combination

Also Published As

Publication number Publication date
MX2012003050A (es) 2012-05-29
PT2488169E (pt) 2013-04-03
CO6511248A2 (es) 2012-08-31
CA2771665A1 (en) 2011-04-21
BR112012005011B1 (pt) 2021-01-19
CA2771665C (en) 2015-10-06
CN104844513A (zh) 2015-08-19
AU2010306168B2 (en) 2014-10-30
TW201116273A (en) 2011-05-16
ZA201201892B (en) 2012-11-28
TWI441630B (zh) 2014-06-21
MA33742B1 (fr) 2012-11-01
KR20120099212A (ko) 2012-09-07
BR112012005011B8 (pt) 2021-05-25
JP2013507402A (ja) 2013-03-04
AU2010306168A1 (en) 2012-03-15
HK1173380A1 (en) 2013-05-16
US20230057884A1 (en) 2023-02-23
HRP20130316T1 (en) 2013-05-31
CN102573825A (zh) 2012-07-11
BR112012005011A2 (pt) 2016-05-03
IL218256A (en) 2017-05-29
CN104817501B (zh) 2017-09-22
CN104817501A (zh) 2015-08-05
CN102573825B (zh) 2015-04-22
SG178835A1 (en) 2012-05-30
IL218256A0 (en) 2012-04-30
KR101471585B1 (ko) 2014-12-10
JP5399564B2 (ja) 2014-01-29
CN104844513B (zh) 2018-08-07
WO2011044962A1 (en) 2011-04-21
NZ598353A (en) 2014-01-31

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