JP7499252B2 - エチニルエストラジオール－β－シクロデキストリン複合体およびその製造方法 - Google Patents

エチニルエストラジオール－β－シクロデキストリン複合体およびその製造方法 Download PDF

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JP7499252B2
JP7499252B2 JP2021534321A JP2021534321A JP7499252B2 JP 7499252 B2 JP7499252 B2 JP 7499252B2 JP 2021534321 A JP2021534321 A JP 2021534321A JP 2021534321 A JP2021534321 A JP 2021534321A JP 7499252 B2 JP7499252 B2 JP 7499252B2
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ethinyl estradiol
amorphous
cyclodextrin
complex
tetrahydrofolic acid
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JPWO2020120548A5 (enExample
JP2022513237A (ja
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アンドレサ、マリア、リベイロ
マリア、ドロレス、モジャ、オルテガ
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Laboratorios Leon Farma SA
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Laboratorios Leon Farma SA
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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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1682—Processes
    • A61K9/1694—Processes resulting in granules or microspheres of the matrix type containing more than 5% of excipient
    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • 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
    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • A61K31/567—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in position 17 alpha, e.g. mestranol, norethandrolone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/40—Cyclodextrins; Derivatives 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
    • A61K47/50—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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
    • A61K9/146—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic macromolecular 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; 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
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/18—Feminine contraceptives

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Reproductive Health (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Endocrinology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Inorganic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Steroid Compounds (AREA)
JP2021534321A 2018-12-13 2019-12-11 エチニルエストラジオール－β－シクロデキストリン複合体およびその製造方法 Active JP7499252B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP18382921.7 2018-12-13
EP18382921.7A EP3666260A1 (en) 2018-12-13 2018-12-13 Ethinyl estradiol-beta-cyclodextrin complex and process for preparing thereof
PCT/EP2019/084591 WO2020120548A1 (en) 2018-12-13 2019-12-11 ETHINYL ESTRADIOL-β-CYCLODEXTRIN COMPLEX AND PROCESS FOR PREPARING THEREOF

Publications (3)

Publication Number Publication Date
JP2022513237A JP2022513237A (ja) 2022-02-07
JPWO2020120548A5 JPWO2020120548A5 (enExample) 2022-12-19
JP7499252B2 true JP7499252B2 (ja) 2024-06-13

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JP2021534321A Active JP7499252B2 (ja) 2018-12-13 2019-12-11 エチニルエストラジオール－β－シクロデキストリン複合体およびその製造方法

Country Status (5)

Country Link
US (1) US12318395B2 (enExample)
EP (1) EP3666260A1 (enExample)
JP (1) JP7499252B2 (enExample)
ES (1) ES2850278B2 (enExample)
WO (1) WO2020120548A1 (enExample)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3666260A1 (en) 2018-12-13 2020-06-17 Laboratorios Leon Farma SA Ethinyl estradiol-beta-cyclodextrin complex and process for preparing thereof
CN114225050B (zh) * 2022-01-29 2022-12-13 国家卫生健康委科学技术研究所 炔雌醇环糊精复合物的制备及应用
CN116617157B (zh) * 2023-05-25 2025-02-18 国家卫生健康委科学技术研究所 一种制备pH响应性炔雌醇复合水凝胶的方法

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2004518656A (ja) 2000-12-20 2004-06-24 シエーリング アクチエンゲゼルシャフト エストロゲン−シクロデキストリン複合体の組成物
JP2015536353A (ja) 2012-10-10 2015-12-21 ザ ユニバーシティ オブ クイーンズランドＴｈｅ Ｕｎｉｖｅｒｓｉｔｙ Ｏｆ Ｑｕｅｅｎｓｌａｎｄ シクロデキストリン内へのガスのカプセル化
US20170368197A1 (en) 2014-12-19 2017-12-28 Synthon B.V. Pharmaceutical Composition Comprising Amorphous Lenalidomide

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4727064A (en) * 1984-04-25 1988-02-23 The United States Of America As Represented By The Department Of Health And Human Services Pharmaceutical preparations containing cyclodextrin derivatives
DE4426709A1 (de) 1994-07-20 1996-01-25 Schering Ag Steroidale Sexualhormone enthaltende feste Arzneiformen
IT1304190B1 (it) * 1998-12-18 2001-03-08 Euphar Group Srl Clatrati di deidroepiandrosterone e relative composizionifarmaceutiche
CH693905A5 (de) 1999-04-15 2004-04-15 Eprova Ag Stabile kristalline Salze von 5-Methyltetrahydrofolsäure.
EP2781214A1 (en) 2013-03-22 2014-09-24 Chemo Research, S.L. Formulation of amorphous calcium L-5-methyltetrahydrofolate (L-5-MTHF-Ca)
EP3666260A1 (en) 2018-12-13 2020-06-17 Laboratorios Leon Farma SA Ethinyl estradiol-beta-cyclodextrin complex and process for preparing thereof

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2004518656A (ja) 2000-12-20 2004-06-24 シエーリング アクチエンゲゼルシャフト エストロゲン−シクロデキストリン複合体の組成物
JP2015536353A (ja) 2012-10-10 2015-12-21 ザ ユニバーシティ オブ クイーンズランドＴｈｅ Ｕｎｉｖｅｒｓｉｔｙ Ｏｆ Ｑｕｅｅｎｓｌａｎｄ シクロデキストリン内へのガスのカプセル化
US20170368197A1 (en) 2014-12-19 2017-12-28 Synthon B.V. Pharmaceutical Composition Comprising Amorphous Lenalidomide

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Publication number Publication date
US20220040200A1 (en) 2022-02-10
WO2020120548A1 (en) 2020-06-18
US12318395B2 (en) 2025-06-03
ES2850278R1 (es) 2022-12-02
EP3666260A1 (en) 2020-06-17
ES2850278B2 (es) 2023-09-15
ES2850278A2 (es) 2021-08-26
JP2022513237A (ja) 2022-02-07

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