CN114916221A - 一种高生物利用度的索拉非尼药物组合物及应用 - Google Patents

一种高生物利用度的索拉非尼药物组合物及应用 Download PDF

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Publication number
CN114916221A
CN114916221A CN202080055010.9A CN202080055010A CN114916221A CN 114916221 A CN114916221 A CN 114916221A CN 202080055010 A CN202080055010 A CN 202080055010A CN 114916221 A CN114916221 A CN 114916221A
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sorafenib
sodium
oral solid
pharmaceutical composition
solid dispersion
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CN202080055010.9A
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CN114916221B (zh
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贾慧娟
张加晏
侯鑫
李衍
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Beijing Creatron Institute Of Pharmaceutical Research Co ltd
Tianjin Ruichuang Kangtai Biotechnology Co ltd
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Beijing Creatron Institute Of Pharmaceutical Research Co ltd
Tianjin Ruichuang Kangtai Biotechnology Co ltd
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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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated 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
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • 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
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • 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
    • 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
    • A61K9/2031—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • 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

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

一种低剂量索拉非尼口服固体制剂，包括：a)索拉非尼固体分散体；b)抑晶剂；c)其他药学上可接受的辅剂。上述低剂量索拉非尼口服固体制剂具有较高的生物利用度，降低了索拉非尼的服用剂量，病人口服多吉美片剂给药剂量的35％～70％即可达到与多吉美片剂相同的治疗效果；同时具有更高的稳定性，更安全、副作用发生率更少；具有更低的Cmax、AUC0‑t变异，更高的溶出度，随胃肠道pH的升高，析晶速率低；片剂体积小，病人易于服用；崩解速度快，溶出效果好；易于实现产业化。

Description

PCT国内申请，说明书已公开。

Claims (17)

  1. PCT国内申请，权利要求书已公开。
CN202080055010.9A 2020-12-07 2020-12-07 一种高生物利用度的索拉非尼药物组合物及应用 Active CN114916221B (zh)

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PCT/CN2020/134164 WO2022120512A1 (zh) 2020-12-07 2020-12-07 一种高生物利用度的索拉非尼药物组合物及应用

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CN114916221B CN114916221B (zh) 2024-01-30

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US (1) US20230310393A1 (zh)
EP (1) EP4032529A4 (zh)
JP (1) JP7428356B2 (zh)
CN (1) CN114916221B (zh)
CA (1) CA3155855A1 (zh)
WO (1) WO2022120512A1 (zh)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN115813861A (zh) * 2022-12-28 2023-03-21 药源生物科技（启东）有限公司 一种提高难溶性药物溶解度的固体分散体及制备方法

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2023155182A1 (zh) * 2022-02-21 2023-08-24 北京睿创康泰医药研究院有限公司 一种低服用剂量高药物暴露量的索拉非尼或多纳非尼口服制剂及其应用

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009100176A2 (en) * 2008-02-07 2009-08-13 Abbott Laboratories Pharmaceutical dosage form for oral administration of tyrosine kinase inhibitor
CN101594851A (zh) * 2006-11-09 2009-12-02 阿伯特有限及两合公司 用于口服给药的酪氨酸激酶抑制剂的药物剂型
CN107115317A (zh) * 2012-01-13 2017-09-01 X喷雾微粒公司 包含稳定的、无定形杂化纳米颗粒的药物组合物
WO2018211336A2 (en) * 2018-09-07 2018-11-22 Alvogen Malta Operations (Row) Ltd Solid dosage form containing sorafenib tosylate

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE395905T1 (de) * 2004-08-27 2008-06-15 Bayer Pharmaceuticals Corp Pharmazeutische zusammensetzungen in form fester dispersionen zur behandlung von krebs
WO2008008733A2 (en) * 2006-07-10 2008-01-17 Elan Pharma International Ltd. Nanoparticulate sorafenib formulations
CN104971045A (zh) 2014-04-11 2015-10-14 上海宣泰医药科技有限公司 泊沙康唑药物组合物及其制备方法和药物制剂
CN105126111A (zh) * 2015-09-30 2015-12-09 清华大学 提高索拉非尼生物利用度的制剂
KR102333609B1 (ko) * 2017-10-31 2021-12-01 주식회사 삼양홀딩스 붕해가 개선된 경구용 고형 제제 조성물 및 이의 제조 방법

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101594851A (zh) * 2006-11-09 2009-12-02 阿伯特有限及两合公司 用于口服给药的酪氨酸激酶抑制剂的药物剂型
WO2009100176A2 (en) * 2008-02-07 2009-08-13 Abbott Laboratories Pharmaceutical dosage form for oral administration of tyrosine kinase inhibitor
CN107115317A (zh) * 2012-01-13 2017-09-01 X喷雾微粒公司 包含稳定的、无定形杂化纳米颗粒的药物组合物
WO2018211336A2 (en) * 2018-09-07 2018-11-22 Alvogen Malta Operations (Row) Ltd Solid dosage form containing sorafenib tosylate

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN115813861A (zh) * 2022-12-28 2023-03-21 药源生物科技（启东）有限公司 一种提高难溶性药物溶解度的固体分散体及制备方法

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WO2022120512A1 (zh) 2022-06-16
JP7428356B2 (ja) 2024-02-06
EP4032529A4 (en) 2022-11-16
EP4032529A1 (en) 2022-07-27
CN114916221B (zh) 2024-01-30
CA3155855A1 (en) 2022-06-07
US20230310393A1 (en) 2023-10-05
JP2023509560A (ja) 2023-03-09

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