WO2020189886A3 - 스테로이드계 약물을 포함하는 생분해성 고분자 미세입자 및 이의 제조 방법 - Google Patents

스테로이드계 약물을 포함하는 생분해성 고분자 미세입자 및 이의 제조 방법 Download PDF

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WO2020189886A3
WO2020189886A3 PCT/KR2020/000413 KR2020000413W WO2020189886A3 WO 2020189886 A3 WO2020189886 A3 WO 2020189886A3 KR 2020000413 W KR2020000413 W KR 2020000413W WO 2020189886 A3 WO2020189886 A3 WO 2020189886A3
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steroid
based drug
drug
biodegradable polymer
preparation
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PCT/KR2020/000413
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English (en)
French (fr)
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WO2020189886A2 (ko
WO2020189886A9 (ko
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김정용
이원천
강미연
최항제
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(주)리젠바이오텍
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Priority claimed from KR1020190031072A external-priority patent/KR102377975B1/ko
Priority claimed from KR1020190179090A external-priority patent/KR102404224B1/ko
Application filed by (주)리젠바이오텍 filed Critical (주)리젠바이오텍
Priority to EP20774762.7A priority Critical patent/EP3943073A4/en
Priority to JP2022504490A priority patent/JP7296520B2/ja
Priority to CN202080000471.6A priority patent/CN112955129A/zh
Priority to US16/756,306 priority patent/US11376226B2/en
Publication of WO2020189886A2 publication Critical patent/WO2020189886A2/ko
Publication of WO2020189886A3 publication Critical patent/WO2020189886A3/ko
Publication of WO2020189886A9 publication Critical patent/WO2020189886A9/ko

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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
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/51—Nanocapsules; Nanoparticles
    • A61K9/5192—Processes
    • 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
    • A61K31/56—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
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
    • A61K31/573—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
    • 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
    • A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • 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
    • 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
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • 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
    • A61K9/1641—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers
    • A61K9/1647—Polyesters, e.g. poly(lactide-co-glycolide)
    • 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
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/51—Nanocapsules; Nanoparticles
    • A61K9/5107—Excipients; Inactive ingredients
    • A61K9/513—Organic macromolecular compounds; Dendrimers
    • A61K9/5146—Organic macromolecular compounds; Dendrimers obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyamines, polyanhydrides
    • A61K9/5153—Polyesters, e.g. poly(lactide-co-glycolide)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01J—CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
    • B01J37/00—Processes, in general, for preparing catalysts; Processes, in general, for activation of catalysts
    • B01J37/32—Freeze drying, i.e. lyophilisation

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
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  • Physics & Mathematics (AREA)
  • Diabetes (AREA)
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  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Materials Engineering (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

본 발명은 스테로이드계 약물을 포함하는 생분해성 고분자 미세입자 및 이의 제조 방법에 관한 것으로, 스테로이드계 약물과 생분해성 폴리에스테르계 고분자를 적당한 유기용매에 용해시키고 저온의 탄화수소 용액에 분사시켜 냉동된 미세입자를 만든 후, 이를 저온의 염 수용액에 넣어 미세입자에 포함되어 있는 유기용매를 용해시키는 제조 방법을 통해 스테로이드계 약물을 포함하는 생분해성 고분자 미세입자를 제조하였고, 제조된 스테로이드계 또는 스테로이드계인 성호르몬계 약물을 포함하는 생분해성 고분자 미세입자가 우수한 생체적합성, 생분해성, 다공성 및 기계적 강도 등을 가지며, 스테로이드계 또는 스테로이드계인 성호르몬계 약물이 서서히 장기간 방출되는 것을 확인함으로써, 본 발명의 스테로이드계 또는 스테로이드계인 성호르몬계 약물을 포함하는 생분해성 고분자 미세입자를 이용하여 일정하게 장기간 지속적으로 약물을 방출하여 스테로이드계 약물 또는 스테로이드계인, 성호르몬의 감소 또는 결핍에 의해 발생하는 증상 및 질환을 치료할 수 있는 제제를 개발할 수 있을 것으로 기대된다.
PCT/KR2020/000413 2019-03-19 2020-01-09 스테로이드계 약물을 포함하는 생분해성 고분자 미세입자 및 이의 제조 방법 WO2020189886A2 (ko)

Priority Applications (4)

Application Number Priority Date Filing Date Title
EP20774762.7A EP3943073A4 (en) 2019-03-19 2020-01-09 BIODEGRADABLE POLYMERIC MICROPARTICLE WITH A STEROID-BASED DRUG AND PROCESS FOR ITS PRODUCTION
JP2022504490A JP7296520B2 (ja) 2019-03-19 2020-01-09 ステロイド系薬物を含む生分解性高分子微細粒子及びその製造方法
CN202080000471.6A CN112955129A (zh) 2019-03-19 2020-01-09 包含类固醇类药物的生物降解性高分子微粒及其制备方法
US16/756,306 US11376226B2 (en) 2019-03-19 2020-01-09 Biodegradable polymer microparticle containing steroid drug and preparation method therefor

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
KR10-2019-0031072 2019-03-19
KR1020190031072A KR102377975B1 (ko) 2019-03-19 2019-03-19 스테로이드계 약물을 포함하는 생분해성 고분자 미세입자 및 이의 제조 방법
KR1020190179090A KR102404224B1 (ko) 2019-12-31 2019-12-31 성호르몬계 약물을 포함하는 생분해성 고분자 미세입자 및 이의 제조 방법
KR10-2019-0179090 2019-12-31

Publications (3)

Publication Number Publication Date
WO2020189886A2 WO2020189886A2 (ko) 2020-09-24
WO2020189886A3 true WO2020189886A3 (ko) 2021-04-22
WO2020189886A9 WO2020189886A9 (ko) 2021-07-15

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PCT/KR2020/000413 WO2020189886A2 (ko) 2019-03-19 2020-01-09 스테로이드계 약물을 포함하는 생분해성 고분자 미세입자 및 이의 제조 방법

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US (1) US11376226B2 (ko)
EP (1) EP3943073A4 (ko)
JP (1) JP7296520B2 (ko)
CN (1) CN112955129A (ko)
WO (1) WO2020189886A2 (ko)

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JP2005525403A (ja) * 2002-05-03 2005-08-25 ピーアール ファーマシューティカルズ， インコーポレイテッド エストラジオール代謝産物の徐放性組成物
KR20090131975A (ko) * 2008-06-19 2009-12-30 한국과학기술연구원 서방형 약물전달 및 조직재생용 덮인 다공성 생분해성고분자 미립구의 제조 방법
KR20100131244A (ko) * 2009-06-05 2010-12-15 주식회사 리젠 바이오텍 생분해성 고분자 미세입자와 그의 제조방법
KR20170001403A (ko) * 2015-06-26 2017-01-04 주식회사 엘지화학 폴리머 입자의 제조방법
KR20180018892A (ko) * 2016-08-09 2018-02-22 단국대학교 천안캠퍼스 산학협력단 안정한 결정형 약물을 포함하는 고분자 미립구 및 그 제조방법

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Publication number Publication date
US11376226B2 (en) 2022-07-05
US20210212956A1 (en) 2021-07-15
EP3943073A2 (en) 2022-01-26
CN112955129A (zh) 2021-06-11
EP3943073A4 (en) 2023-01-04
JP7296520B2 (ja) 2023-06-22
JP2022525705A (ja) 2022-05-18
WO2020189886A2 (ko) 2020-09-24
WO2020189886A9 (ko) 2021-07-15

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