CN113825511A - 一种固体分散体及其制备方法 - Google Patents

一种固体分散体及其制备方法 Download PDF

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Publication number
CN113825511A
CN113825511A CN202080036373.8A CN202080036373A CN113825511A CN 113825511 A CN113825511 A CN 113825511A CN 202080036373 A CN202080036373 A CN 202080036373A CN 113825511 A CN113825511 A CN 113825511A
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China
Prior art keywords
solid dispersion
active ingredient
carrier material
poor solvent
solvent
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Pending
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CN202080036373.8A
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English (en)
Inventor
周先强
杜振兴
王捷
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Jiangsu Hengrui Medicine Co Ltd
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Jiangsu Hengrui Medicine Co Ltd
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Publication of CN113825511A publication Critical patent/CN113825511A/zh
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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
    • A61K9/141—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
    • A61K9/145—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 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
    • A61K9/141—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
    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61K47/14—Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
    • 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
    • A61K47/38—Cellulose; Derivatives thereof
    • 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
    • A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Inorganic Chemistry (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Colloid Chemistry (AREA)

Abstract

一种固体分散体及其制备方法。在具体的实施方案中，固体分散体含有活性成分(R)‑4‑氨基‑1‑(1‑(丁‑2‑炔酰基)吡咯烷‑3‑基)‑3‑(4‑(2,6‑二氟苯氧基)苯基)‑1,6‑二氢‑7H‑吡咯并[2,3‑d]哒嗪‑7‑酮或其盐和载体材料，并调节pH值；采用添加适量酸的方法，有效抑制反向溶剂法过程中乳化现象，进而获得粒径适中、含量均一的固体分散体。

Description

PCT国内申请，说明书已公开。

Claims (24)

  1. PCT国内申请，权利要求书已公开。
CN202080036373.8A 2019-05-31 2020-05-29 一种固体分散体及其制备方法 Pending CN113825511A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201910468254 2019-05-31
CN2019104682549 2019-05-31
PCT/CN2020/093206 WO2020239065A1 (zh) 2019-05-31 2020-05-29 一种固体分散体及其制备方法

Publications (1)

Publication Number Publication Date
CN113825511A true CN113825511A (zh) 2021-12-21

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ID=73553512

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CN202080036373.8A Pending CN113825511A (zh) 2019-05-31 2020-05-29 一种固体分散体及其制备方法

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US (1) US20220233449A1 (zh)
EP (1) EP3977997A4 (zh)
JP (1) JP2022534610A (zh)
KR (1) KR20220016116A (zh)
CN (1) CN113825511A (zh)
AU (1) AU2020282470A1 (zh)
BR (1) BR112021023691A2 (zh)
CA (1) CA3141921A1 (zh)
MX (1) MX2021014402A (zh)
TW (1) TW202100527A (zh)
WO (1) WO2020239065A1 (zh)
ZA (1) ZA202110055B (zh)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2023182332A1 (ja) * 2022-03-22 2023-09-28 株式会社ダイセル 口腔内崩壊錠用の添加剤組成物

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104936589A (zh) * 2013-01-22 2015-09-23 霍夫曼-拉罗奇有限公司 具有改善的生物利用度的药物组合物
CN105640890A (zh) * 2014-11-27 2016-06-08 华东理工大学 一种难溶性活性成分微粒、微粒制剂及其制备方法
WO2019007317A1 (zh) * 2017-07-04 2019-01-10 江苏恒瑞医药股份有限公司 一种药物组合物及其制备方法

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008112722A2 (en) * 2007-03-12 2008-09-18 Dr. Reddy's Laboratories Ltd. Imatinib mesylate
WO2016007185A1 (en) 2014-07-07 2016-01-14 Eternity Bioscience Inc. Aminopyridazinone compounds as protein kinase inhibitors
WO2016088074A1 (en) * 2014-12-03 2016-06-09 Dr. Reddy’S Laboratories Limited Process for the preparation of amorphous ibrutinib
CN106924262A (zh) * 2015-12-31 2017-07-07 常州方楠医药技术有限公司 一种无定型托法替尼枸橼酸盐与药用辅料的固体分散体及其制备方法
US10626116B2 (en) * 2016-01-05 2020-04-21 Jiangsu Hengrui Medicine Co., Ltd. Crystalline form of BTK kinase inhibitor and preparation method thereof
IN201621020494A (zh) * 2016-06-15 2017-12-22

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104936589A (zh) * 2013-01-22 2015-09-23 霍夫曼-拉罗奇有限公司 具有改善的生物利用度的药物组合物
CN105640890A (zh) * 2014-11-27 2016-06-08 华东理工大学 一种难溶性活性成分微粒、微粒制剂及其制备方法
WO2019007317A1 (zh) * 2017-07-04 2019-01-10 江苏恒瑞医药股份有限公司 一种药物组合物及其制备方法

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Publication number Publication date
TW202100527A (zh) 2021-01-01
KR20220016116A (ko) 2022-02-08
US20220233449A1 (en) 2022-07-28
WO2020239065A1 (zh) 2020-12-03
AU2020282470A1 (en) 2022-01-27
EP3977997A4 (en) 2022-07-27
BR112021023691A2 (pt) 2022-04-12
ZA202110055B (en) 2023-04-26
MX2021014402A (es) 2022-02-14
JP2022534610A (ja) 2022-08-02
CA3141921A1 (en) 2020-12-03
EP3977997A1 (en) 2022-04-06

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