KR20060011943A - 향상된 경구 및 경점막 수송용 클라드리빈 제형 - Google Patents

향상된 경구 및 경점막 수송용 클라드리빈 제형 Download PDF

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Publication number
KR20060011943A
KR20060011943A KR1020057018337A KR20057018337A KR20060011943A KR 20060011943 A KR20060011943 A KR 20060011943A KR 1020057018337 A KR1020057018337 A KR 1020057018337A KR 20057018337 A KR20057018337 A KR 20057018337A KR 20060011943 A KR20060011943 A KR 20060011943A
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South Korea
Prior art keywords
cyclodextrin
cladribine
complex
saturated
pharmaceutical formulation
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Ceased
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KR1020057018337A
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English (en)
Korean (ko)
Inventor
니콜라스 에스 보도르
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아이박스 코포레이션
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Publication of KR20060011943A publication Critical patent/KR20060011943A/ko
Ceased legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08L—COMPOSITIONS OF MACROMOLECULAR COMPOUNDS
    • C08L5/00—Compositions of polysaccharides or of their derivatives not provided for in groups C08L1/00 or C08L3/00
    • C08L5/16—Cyclodextrin; Derivatives thereof
    • 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
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • 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
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7076—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • 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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • 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
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • C—CHEMISTRY; METALLURGY
    • C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08B—POLYSACCHARIDES; DERIVATIVES THEREOF
    • C08B37/00—Preparation of polysaccharides not provided for in groups C08B1/00 - C08B35/00; Derivatives thereof
    • C08B37/0006—Homoglycans, i.e. polysaccharides having a main chain consisting of one single sugar, e.g. colominic acid
    • C08B37/0009—Homoglycans, i.e. polysaccharides having a main chain consisting of one single sugar, e.g. colominic acid alpha-D-Glucans, e.g. polydextrose, alternan, glycogen; (alpha-1,4)(alpha-1,6)-D-Glucans; (alpha-1,3)(alpha-1,4)-D-Glucans, e.g. isolichenan or nigeran; (alpha-1,4)-D-Glucans; (alpha-1,3)-D-Glucans, e.g. pseudonigeran; Derivatives thereof
    • C08B37/0012—Cyclodextrin [CD], e.g. cycle with 6 units (alpha), with 7 units (beta) and with 8 units (gamma), large-ring cyclodextrin or cycloamylose with 9 units or more; Derivatives thereof
    • C08B37/0015—Inclusion compounds, i.e. host-guest compounds, e.g. polyrotaxanes
    • 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
    • A61K9/0034—Urogenital system, e.g. vagina, uterus, cervix, penis, scrotum, urethra, bladder; Personal lubricants
    • 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
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A61K9/006—Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Immunology (AREA)
  • Nanotechnology (AREA)
  • Biomedical Technology (AREA)
  • Polymers & Plastics (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Biophysics (AREA)
  • Materials Engineering (AREA)
  • Rheumatology (AREA)
  • Biochemistry (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Medical Informatics (AREA)
  • Oncology (AREA)
  • General Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Biotechnology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Communicable Diseases (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Obesity (AREA)
  • Transplantation (AREA)
KR1020057018337A 2003-03-28 2004-03-26 향상된 경구 및 경점막 수송용 클라드리빈 제형 Ceased KR20060011943A (ko)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US45892203P 2003-03-28 2003-03-28
US60/458,922 2003-03-28
US48475603P 2003-07-02 2003-07-02
US60/484,756 2003-07-02
US54124604P 2004-02-04 2004-02-04
US60/541,246 2004-02-04

Publications (1)

Publication Number Publication Date
KR20060011943A true KR20060011943A (ko) 2006-02-06

Family

ID=33135981

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020057018337A Ceased KR20060011943A (ko) 2003-03-28 2004-03-26 향상된 경구 및 경점막 수송용 클라드리빈 제형

Country Status (16)

Country Link
US (2) US20070065492A1 (https=)
EP (1) EP1608343B1 (https=)
JP (1) JP5412709B2 (https=)
KR (1) KR20060011943A (https=)
CN (1) CN101912615B (https=)
AU (2) AU2004226435B2 (https=)
BR (1) BRPI0408895A (https=)
CA (1) CA2520522C (https=)
EA (1) EA009714B1 (https=)
ES (1) ES2584183T3 (https=)
HR (1) HRP20050924A2 (https=)
IS (1) IS8047A (https=)
ME (1) MEP34508A (https=)
MX (1) MXPA05010330A (https=)
NO (1) NO20054944L (https=)
WO (1) WO2004087100A2 (https=)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3332789B1 (en) 2004-12-22 2022-04-06 Merck Serono SA Cladribine regimen for treating multiple sclerosis
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US7893040B2 (en) 2005-07-22 2011-02-22 Oculis Ehf Cyclodextrin nanotechnology for ophthalmic drug delivery
AU2007253254B2 (en) 2006-05-24 2013-01-17 Merck Serono Sa Cladribine regimen for treating multiple sclerosis
CN100486645C (zh) * 2006-09-12 2009-05-13 南京师范大学 含有环糊精紫杉醇包合物的药物组合物及其制备方法
CN100411688C (zh) * 2006-09-12 2008-08-20 南京师范大学 含有环糊精/多烯紫杉醇包合物的药物组合物及其制备方法
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WO2012097867A1 (en) 2011-01-18 2012-07-26 Synthon Bv Cladribine particles and pharmaceutical compositions comprising them
WO2014075935A1 (de) 2012-11-15 2014-05-22 Sapiotec Gmbh Delphinidinkomplex als antiphlogistischer oder immunsuppressiver wirkstoff
US9949947B2 (en) 2012-12-11 2018-04-24 Sapiotec Gmbh Delphinidin for combating melanoma cells
GB201401465D0 (en) 2014-01-29 2014-03-12 Roach Arthur H Use of cladribine for treating autoimmune inflammatory disease
WO2015140790A1 (en) * 2014-03-17 2015-09-24 Mapi Pharma Ltd. Sublingual delivery of glatiramer acetate
JP7138103B2 (ja) 2016-11-29 2022-09-15 オキュリス エスエー 眼科用活性医薬成分送達のためのシクロデキストリン固体複合体の製造
GB2564717A (en) 2017-07-21 2019-01-23 Chord Therapeutics S A R L Use of cladribine for treating autoimmune neuromuscular disease
EP3713582A1 (en) 2017-11-24 2020-09-30 Merck Patent GmbH Cladribine regimen for use intreating progressive forms of multiple sclerosis
EP4670738A3 (en) 2019-07-01 2026-03-04 Oculis Operations Sàrl Method for stabilizing the ph of an aqueous composition comprising a drug
CA3194812A1 (en) 2020-09-10 2022-03-17 Merck Patent Gmbh Novel treatment regimen for the treatment of autoimmune disorders
GB2601786A (en) 2020-12-10 2022-06-15 Chord Therapeutics S A R L Use of cladribine for treating immune brain disease
US20240077481A1 (en) 2021-03-03 2024-03-07 Ares Trading S.A. Improved treatment methods using dmds for the treatment of autoimmune diseases, and biomarker for predicting and/or optimising said treatment methods
RU2758436C1 (ru) * 2021-04-05 2021-10-28 Общество с ограниченной ответственностью «ФармЭко» Способ получения аморфных ко-эвапоратов кладрибина с циклодекстринами
US20260000606A1 (en) 2022-06-15 2026-01-01 Vektor Pharma Tf Gmbh Sublingual Formulation of Anticancer Compound for Use in the Treatment of Autoimmune Neurodegenerative Diseases
TW202541818A (zh) 2023-12-14 2025-11-01 瑞士商亞利斯貿易公司 用於治療重症肌無力之克拉屈濱(cladribine)療程

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Publication number Publication date
CN101912615A (zh) 2010-12-15
EP1608343A2 (en) 2005-12-28
JP2006526009A (ja) 2006-11-16
JP5412709B2 (ja) 2014-02-12
BRPI0408895A (pt) 2006-04-11
AU2009227811B2 (en) 2012-02-02
ES2584183T3 (es) 2016-09-26
AU2009227811A1 (en) 2009-11-05
IS8047A (is) 2005-09-26
HRP20050924A2 (en) 2006-08-31
MEP34508A (en) 2011-02-10
WO2004087100A2 (en) 2004-10-14
AU2004226435B2 (en) 2009-11-12
NO20054944L (no) 2005-11-24
NO20054944D0 (no) 2005-10-25
US8623408B2 (en) 2014-01-07
EP1608343B1 (en) 2016-04-27
CA2520522A1 (en) 2004-10-14
WO2004087100A3 (en) 2005-03-03
AU2004226435A1 (en) 2004-10-14
CA2520522C (en) 2012-05-29
US20110015145A1 (en) 2011-01-20
CN101912615B (zh) 2013-03-27
US20070065492A1 (en) 2007-03-22
EA200600403A1 (ru) 2006-08-25
MXPA05010330A (es) 2006-05-31
EA009714B1 (ru) 2008-02-28

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