KR20180118136A - Nk-1 수용체 길항제를 포함하는 에멀젼 - Google Patents

Nk-1 수용체 길항제를 포함하는 에멀젼 Download PDF

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KR20180118136A
KR20180118136A KR1020187025071A KR20187025071A KR20180118136A KR 20180118136 A KR20180118136 A KR 20180118136A KR 1020187025071 A KR1020187025071 A KR 1020187025071A KR 20187025071 A KR20187025071 A KR 20187025071A KR 20180118136 A KR20180118136 A KR 20180118136A
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South Korea
Prior art keywords
emulsion
oil
receptor antagonist
emulsifier
aqueous phase
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KR1020187025071A
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English (en)
Korean (ko)
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토마스 비. 오토보니
한 한
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헤론 테라퓨틱스 인코포레이티드
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Publication of KR20180118136A publication Critical patent/KR20180118136A/ko

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • 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
    • A61K31/40Heterocyclic 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
    • A61K31/403Heterocyclic 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 carbocyclic rings, e.g. carbazole
    • A61K31/4035Isoindoles, e.g. phthalimide
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/438The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/439Heterocyclic 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 the ring forming part of a bridged ring system, e.g. quinuclidine
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/24Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/10Dispersions; Emulsions
    • A61K9/107Emulsions ; Emulsion preconcentrates; Micelles
    • A61K9/1075Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Otolaryngology (AREA)
  • Hospice & Palliative Care (AREA)
  • Dispersion Chemistry (AREA)
  • Dermatology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
KR1020187025071A 2016-02-01 2016-02-01 Nk-1 수용체 길항제를 포함하는 에멀젼 KR20180118136A (ko)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/US2016/015992 WO2017135923A1 (en) 2016-02-01 2016-02-01 Emulsion comprising an nk-1 receptor antagonist

Publications (1)

Publication Number Publication Date
KR20180118136A true KR20180118136A (ko) 2018-10-30

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Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020187025071A KR20180118136A (ko) 2016-02-01 2016-02-01 Nk-1 수용체 길항제를 포함하는 에멀젼

Country Status (7)

Country Link
EP (1) EP3411013A1 (ja)
JP (1) JP6829257B2 (ja)
KR (1) KR20180118136A (ja)
CN (1) CN108883058A (ja)
AU (1) AU2016391046A1 (ja)
CA (1) CA3013288A1 (ja)
WO (1) WO2017135923A1 (ja)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2019214872A1 (en) * 2018-01-30 2020-08-06 Heron Therapeutics, Inc. Method of administering emulsion formulations of an NK-1 receptor antagonist
US11065265B2 (en) 2018-05-18 2021-07-20 Spes Pharmaceuticals Inc. Compositions of fosaprepitant and methods of preparation
CN108703950B (zh) * 2018-08-27 2021-04-20 辅必成(上海)医药科技有限公司 一种罗拉吡坦的乳剂注射液
CN109453115A (zh) * 2018-12-25 2019-03-12 广州白云山汉方现代药业有限公司 一种罗拉匹坦静脉注射乳剂及其制备方法和应用
CN111388419A (zh) * 2019-01-03 2020-07-10 齐鲁制药有限公司 阿瑞匹坦乳剂
CN110772482A (zh) * 2019-12-02 2020-02-11 广州白云山汉方现代药业有限公司 一种高比例乳化剂的乳剂及其制备方法
JP2023169445A (ja) * 2020-10-08 2023-11-30 丸石製薬株式会社 ホスアプレピタント注射剤希釈液による細胞毒性抑制剤

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2609640T3 (es) * 2009-08-14 2017-04-21 Opko Health, Inc Formulaciones intravenosas de rolapitant
CN102379845A (zh) * 2011-11-03 2012-03-21 南京优科生物医药有限公司 一种注射用阿瑞匹坦微乳剂及其制备方法
CA2874700A1 (en) * 2012-05-24 2013-11-28 Innopharma, Inc. Aprepitant injectable formulations
CN103520725B (zh) * 2012-07-05 2017-10-24 海思科医药集团股份有限公司 一种治疗呕吐的药物组合物
RS60599B1 (sr) * 2012-07-06 2020-08-31 Pharmathen Sa Stabilna injektibilna farmaceutska kompozicija antagonista neurokinin-1-receptora i postupak za njeno dobijanje
KR20160023692A (ko) * 2013-06-24 2016-03-03 타이거캣 파마, 인크. 소양증에서의 nk-1 수용체 길항제 세를로피탄트의 용도
US9808465B2 (en) * 2014-09-19 2017-11-07 Heron Therapeutics, Inc. Emulsion formulations of aprepitant

Also Published As

Publication number Publication date
CA3013288A1 (en) 2017-08-10
AU2016391046A1 (en) 2018-08-16
JP6829257B2 (ja) 2021-02-10
JP2019507131A (ja) 2019-03-14
CN108883058A (zh) 2018-11-23
EP3411013A1 (en) 2018-12-12
WO2017135923A1 (en) 2017-08-10

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