KR101982482B1 - 메틸날트렉손의 경구 제형 및 친유성 염 - Google Patents

메틸날트렉손의 경구 제형 및 친유성 염 Download PDF

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KR101982482B1
KR101982482B1 KR1020187030676A KR20187030676A KR101982482B1 KR 101982482 B1 KR101982482 B1 KR 101982482B1 KR 1020187030676 A KR1020187030676 A KR 1020187030676A KR 20187030676 A KR20187030676 A KR 20187030676A KR 101982482 B1 KR101982482 B1 KR 101982482B1
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pharmaceutical composition
certain embodiments
methylnaltrexone
bromide
dissolved
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Korean (ko)
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KR20180118260A (ko
Inventor
시에드 엠. 샤
크리스토퍼 리차드 다이오리오
에릭 씨. 에른스퍼거
쉬 멍
샤레피 카둠 에이. 알
조나단 마크 코헨
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와이어쓰 엘엘씨
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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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806—Coating materials
    • A61K9/2833—Organic macromolecular compounds
    • A61K9/284—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/485—Morphinan derivatives, e.g. morphine, codeine
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • 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
    • 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
    • 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
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2009—Inorganic compounds
    • 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
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • 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
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • 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
    • A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
    • A61K9/2077—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
    • 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
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • 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
    • 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
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • 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
    • A61P1/10—Laxatives
    • 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
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D489/00—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula:
    • C07D489/06—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: with a hetero atom directly attached in position 14
    • C07D489/08—Oxygen atom

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Emergency Medicine (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Inorganic Chemistry (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Neurology (AREA)
  • Otolaryngology (AREA)
  • Neurosurgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
KR1020187030676A 2010-03-11 2011-03-10 메틸날트렉손의 경구 제형 및 친유성 염 Active KR101982482B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US31301810P 2010-03-11 2010-03-11
US61/313,018 2010-03-11
PCT/US2011/027913 WO2011112816A1 (en) 2010-03-11 2011-03-10 Oral formulations and lipophilic salts of methylnaltrexone

Related Parent Applications (1)

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KR1020127026488A Division KR101913102B1 (ko) 2010-03-11 2011-03-10 메틸날트렉손의 경구 제형 및 친유성 염

Publications (2)

Publication Number Publication Date
KR20180118260A KR20180118260A (ko) 2018-10-30
KR101982482B1 true KR101982482B1 (ko) 2019-05-27

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KR1020127026488A Active KR101913102B1 (ko) 2010-03-11 2011-03-10 메틸날트렉손의 경구 제형 및 친유성 염
KR1020187030676A Active KR101982482B1 (ko) 2010-03-11 2011-03-10 메틸날트렉손의 경구 제형 및 친유성 염

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Country Status (32)

Country Link
US (8) US8524276B2 (enExample)
EP (2) EP2371357B1 (enExample)
JP (4) JP6143409B2 (enExample)
KR (2) KR101913102B1 (enExample)
CN (2) CN107308125B (enExample)
AR (1) AR080491A1 (enExample)
AU (1) AU2011224275B2 (enExample)
BR (1) BR112012022873B1 (enExample)
CA (1) CA2789798C (enExample)
CL (1) CL2012002192A1 (enExample)
CO (1) CO6630134A2 (enExample)
CR (1) CR20120476A (enExample)
EA (1) EA029096B1 (enExample)
EC (1) ECSP12012208A (enExample)
ES (1) ES2623926T3 (enExample)
GE (1) GEP201606550B (enExample)
GT (1) GT201200247A (enExample)
HU (1) HUE033133T2 (enExample)
IL (1) IL221452A (enExample)
MA (1) MA34146B1 (enExample)
MX (2) MX349145B (enExample)
MY (1) MY160727A (enExample)
NZ (3) NZ702826A (enExample)
PE (1) PE20130063A1 (enExample)
PH (1) PH12012501622A1 (enExample)
PL (2) PL3178472T3 (enExample)
SG (3) SG10201501821RA (enExample)
TN (1) TN2012000392A1 (enExample)
TW (2) TWI589293B (enExample)
UA (2) UA123856C2 (enExample)
WO (1) WO2011112816A1 (enExample)
ZA (1) ZA201808498B (enExample)

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IL221452A0 (en) 2012-10-31
GT201200247A (es) 2013-09-11
JP2019034958A (ja) 2019-03-07
US20200121673A1 (en) 2020-04-23
EP3178472A1 (en) 2017-06-14
JP2016029054A (ja) 2016-03-03
CN102918039B (zh) 2017-06-09
US20190314365A1 (en) 2019-10-17
US20190117645A1 (en) 2019-04-25
WO2011112816A1 (en) 2011-09-15
BR112012022873A2 (pt) 2016-08-30
KR20130010900A (ko) 2013-01-29
TWI605814B (zh) 2017-11-21
UA123856C2 (uk) 2021-06-16
PE20130063A1 (es) 2013-02-11
CN107308125B (zh) 2021-07-16
TN2012000392A1 (en) 2014-01-30
US20130330407A1 (en) 2013-12-12
US9314461B2 (en) 2016-04-19
JP2017206553A (ja) 2017-11-24
HK1245673A1 (zh) 2018-08-31
PH12012501622A1 (en) 2012-11-05
US8524276B2 (en) 2013-09-03
TW201141479A (en) 2011-12-01
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US20120070495A1 (en) 2012-03-22
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