US20190133952A1 - Preparation method of sustained-release microparticles - Google Patents

Preparation method of sustained-release microparticles Download PDF

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Publication number
US20190133952A1
US20190133952A1 US16/095,315 US201716095315A US2019133952A1 US 20190133952 A1 US20190133952 A1 US 20190133952A1 US 201716095315 A US201716095315 A US 201716095315A US 2019133952 A1 US2019133952 A1 US 2019133952A1
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Prior art keywords
microparticles
water
sustained
preparation
drug
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US16/095,315
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Inventor
Feng Liu
Shuting LAI
Yang Zheng
Fuchun CAO
Yuanfa LIAN
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AC Pharmaceuticals Co Ltd
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AC Pharmaceuticals Co Ltd
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Assigned to AC PHARMACEUTICALS CO., LTD. reassignment AC PHARMACEUTICALS CO., LTD. ASSIGNMENT OF ASSIGNORS INTEREST (SEE DOCUMENT FOR DETAILS). Assignors: CAO, Fuchun, LAI, Shuting, LIAN, Yuanfa, LIU, FENG, ZHENG, YANG
Publication of US20190133952A1 publication Critical patent/US20190133952A1/en
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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
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1682Processes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605Excipients; Inactive ingredients
    • A61K9/1629Organic macromolecular compounds
    • A61K9/1641Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers
    • A61K9/1647Polyesters, e.g. poly(lactide-co-glycolide)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/08Peptides having 5 to 11 amino acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/08Peptides having 5 to 11 amino acids
    • A61K38/09Luteinising hormone-releasing hormone [LHRH], i.e. Gonadotropin-releasing hormone [GnRH]; Related peptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/08Peptides having 5 to 11 amino acids
    • A61K38/095Oxytocins; Vasopressins; Related peptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/12Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/19Cytokines; Lymphokines; Interferons
    • A61K38/20Interleukins [IL]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/22Hormones
    • A61K38/26Glucagons
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/22Hormones
    • A61K38/31Somatostatins
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/33Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans derived from pro-opiomelanocortin, pro-enkephalin or pro-dynorphin
    • A61K38/35Corticotropin [ACTH]
    • 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
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/34Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0002Galenical forms characterised by the drug release technique; Application systems commanded by energy
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605Excipients; Inactive ingredients
    • A61K9/1629Organic macromolecular compounds
    • A61K9/1635Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605Excipients; Inactive ingredients
    • A61K9/1629Organic macromolecular compounds
    • A61K9/1641Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers

Definitions

  • the solvent removal in step 4) may use the following method:

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Immunology (AREA)
  • Zoology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Inorganic Chemistry (AREA)
  • Medicinal Preparation (AREA)
US16/095,315 2016-04-26 2017-04-24 Preparation method of sustained-release microparticles Pending US20190133952A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201610269834.1A CN105963258B (zh) 2016-04-26 2016-04-26 一种缓释微粒的制备方法
CN201610269834.1 2016-04-26
PCT/CN2017/081640 WO2017186077A1 (fr) 2016-04-26 2017-04-24 Procédé de préparation de microparticules à libération prolongée

Publications (1)

Publication Number Publication Date
US20190133952A1 true US20190133952A1 (en) 2019-05-09

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US16/095,315 Pending US20190133952A1 (en) 2016-04-26 2017-04-24 Preparation method of sustained-release microparticles

Country Status (4)

Country Link
US (1) US20190133952A1 (fr)
EP (1) EP3434263B1 (fr)
CN (1) CN105963258B (fr)
WO (1) WO2017186077A1 (fr)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11865213B2 (en) * 2021-07-05 2024-01-09 Mapi Pharma Ltd. Semaglutide depot systems and use thereof

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105963258B (zh) * 2016-04-26 2021-01-22 广州帝奇医药技术有限公司 一种缓释微粒的制备方法
US11612563B2 (en) 2017-07-17 2023-03-28 Medincell Pharmaceutical composition
US20210154147A1 (en) * 2018-10-19 2021-05-27 Ac Pharmaceuticals Co., Ltd. Preparation method of sustained-release microparticles
CN110498919B (zh) * 2019-07-26 2022-03-01 河南师范大学 一种酯化度可控的γ-PGA-Bn的合成方法
CN111150883A (zh) * 2020-01-14 2020-05-15 北京四环制药有限公司 可生物降解的注射填充物及其制备方法和其应用
KR20220032301A (ko) * 2020-09-07 2022-03-15 (주)인벤티지랩 약물의 지속 방출을 위한 서방형 마이크로입자
CN112354010A (zh) * 2020-11-27 2021-02-12 曲阜师范大学 一种聚γ-谷氨酸/壳聚糖/柠檬酸钙生物材料及其制备方法
CN112603892B (zh) * 2020-12-18 2023-09-05 中国药科大学 一种载药微球及其制备方法

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US5556642A (en) * 1992-07-16 1996-09-17 Tanabe Seiyaku Co., Ltd. Method for producing sustained release microsphere preparation
US6235224B1 (en) * 1995-07-21 2001-05-22 Brown University Research Foundation Process for preparing microparticles through phase inversion phenomena
US20020198315A1 (en) * 1992-05-28 2002-12-26 Hutchinson Francis Gowland Salts of peptides with carboxy-terminated polyesters
US20080131513A1 (en) * 2004-04-30 2008-06-05 Byung Ho Woo Sustained-Release Microspheres and Methods of Making and Using Same
US20100316571A1 (en) * 2007-10-27 2010-12-16 The Trustees Of The University Of Pennsylvania Method and Compositions for Polymer Nanocarriers Containing Therapeutic Molecules

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US5556642A (en) * 1992-07-16 1996-09-17 Tanabe Seiyaku Co., Ltd. Method for producing sustained release microsphere preparation
US6235224B1 (en) * 1995-07-21 2001-05-22 Brown University Research Foundation Process for preparing microparticles through phase inversion phenomena
US20080131513A1 (en) * 2004-04-30 2008-06-05 Byung Ho Woo Sustained-Release Microspheres and Methods of Making and Using Same
US20100316571A1 (en) * 2007-10-27 2010-12-16 The Trustees Of The University Of Pennsylvania Method and Compositions for Polymer Nanocarriers Containing Therapeutic Molecules

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11865213B2 (en) * 2021-07-05 2024-01-09 Mapi Pharma Ltd. Semaglutide depot systems and use thereof

Also Published As

Publication number Publication date
EP3434263A1 (fr) 2019-01-30
EP3434263A4 (fr) 2019-03-27
CN105963258B (zh) 2021-01-22
EP3434263B1 (fr) 2020-07-15
WO2017186077A1 (fr) 2017-11-02
CN105963258A (zh) 2016-09-28

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