CN111565712A - 一种固体微粒及其制备方法和含其的药物组合物 - Google Patents

一种固体微粒及其制备方法和含其的药物组合物 Download PDF

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CN111565712A
CN111565712A CN201880085921.9A CN201880085921A CN111565712A CN 111565712 A CN111565712 A CN 111565712A CN 201880085921 A CN201880085921 A CN 201880085921A CN 111565712 A CN111565712 A CN 111565712A
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solid particles
hydrophobic
propylene glycol
dutasteride
weight percentage
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CN111565712B (zh
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董良昶
马文博
王琳
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Shanghai Wd Pharmaceutical Co ltd
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Shanghai Wd Pharmaceutical Co ltd
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    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/473—Quinolines; Isoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
    • 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
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    • 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
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    • 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
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    • A61K47/44—Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
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    • 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
    • A61K9/143—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 inorganic compounds
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    • 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
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    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate

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  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

一种固体微粒及其制备方法和药物组合物。该固体微粒包括多孔固体颗粒和非水性液体配方，所述非水性液体配方包括0.10‑4.00重量％疏水性药物活性成分、28.00‑99.90重量％疏水性增溶液体、0‑70.00重量％非离子表面活性剂和0‑1.00重量％抗氧化剂，所述疏水性增溶液体包括中链甘油单/双酯和/或丙二醇脂肪酸单酯。

Description

PCT国内申请，说明书已公开。

Claims (10)

  1. PCT国内申请，权利要求书已公开。
CN201880085921.9A 2018-01-10 2018-11-27 一种固体微粒及其制备方法和含其的药物组合物 Active CN111565712B (zh)

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CN2018100236968 2018-01-10
CN201810023696.8A CN110013467B (zh) 2018-01-10 2018-01-10 一种固体微粒及其制备方法和含其的药物组合物
PCT/CN2018/117622 WO2019137103A1 (zh) 2018-01-10 2018-11-27 一种固体微粒及其制备方法和含其的药物组合物

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CN110013467B (zh) 2018-01-10 2021-09-17 上海汉都医药科技有限公司 一种固体微粒及其制备方法和含其的药物组合物
CN110559185A (zh) * 2019-09-30 2019-12-13 上海汉都医药科技有限公司 固体口服制剂的药物容置装置及含其的口服给药递送装置

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003063835A1 (en) * 2002-01-28 2003-08-07 Phares Pharmaceutical Research N.V. Composition comprising low water soluble compounds within porous carriers
CN102413813B (zh) * 2009-03-24 2014-11-12 Adds制药有限责任公司 用于口服递送的稳定化的溶解性增强的制剂

Family Cites Families (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9405304D0 (en) * 1994-03-16 1994-04-27 Scherer Ltd R P Delivery systems for hydrophobic drugs
US20150374826A1 (en) * 1999-06-30 2015-12-31 Lipocine Inc. Pharmaceutical compositions and dosage forms for administration of hydrophobic drugs
US20030236236A1 (en) * 1999-06-30 2003-12-25 Feng-Jing Chen Pharmaceutical compositions and dosage forms for administration of hydrophobic drugs
US20060003002A1 (en) 2003-11-03 2006-01-05 Lipocine, Inc. Pharmaceutical compositions with synchronized solubilizer release
MY142989A (en) 2004-03-10 2011-02-14 Bayer Schering Pharma Ag Stabilised supersaturated solids of lipophilic drugs
KR100669497B1 (ko) * 2005-08-17 2007-01-16 보람제약주식회사 안정성과 용출률이 뛰어난 약리학적 조성물 및 그 제조방법
MX2011006012A (es) * 2008-12-09 2011-11-18 Synthon Bv Granulos de tamsulosina para combinacion de dosis fija.
WO2010092596A1 (en) 2009-02-10 2010-08-19 Genepharm India Private Limited An oral pharmaceutical composition of dutasteride
EP2468262A1 (en) 2010-12-06 2012-06-27 Krka Tovarna Zdravil, D.D., Novo Mesto Pharmaceutical composition comprising dutasteride
US9622981B2 (en) 2011-11-17 2017-04-18 Mylan Inc. Liquid-filled hard gel capsule pharmaceutical formulations
CA2931086C (en) * 2012-12-20 2020-11-03 Solural Pharma ApS Solid oral dosage form of testosterone derivative
KR102382963B1 (ko) 2015-01-14 2022-04-05 동아에스티 주식회사 안정성이 개선된 정제형태의 두타스테리드 조성물
EP3257511B1 (en) * 2015-02-10 2018-10-24 FUJIFILM Corporation Orally disintegrating tablet and method for manufacturing same
JP7116277B2 (ja) 2017-06-12 2022-08-10 富士化学工業株式会社 顆粒剤、並びに錠剤及びその製造方法
US11633409B2 (en) * 2017-09-01 2023-04-25 Jw Pharmaceutical Corporation Solid preparation comprising dutasteride and method for preparing same
CN110013467B (zh) 2018-01-10 2021-09-17 上海汉都医药科技有限公司 一种固体微粒及其制备方法和含其的药物组合物

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003063835A1 (en) * 2002-01-28 2003-08-07 Phares Pharmaceutical Research N.V. Composition comprising low water soluble compounds within porous carriers
CN102413813B (zh) * 2009-03-24 2014-11-12 Adds制药有限责任公司 用于口服递送的稳定化的溶解性增强的制剂

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
黄可龙: "《精细化学品技术手册》", 30 June 1994, 中南工业大学出版社 *

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JP7072929B2 (ja) 2022-05-23
CN110013467B (zh) 2021-09-17
JP2021511371A (ja) 2021-05-06
CN110013467A (zh) 2019-07-16
US11771690B2 (en) 2023-10-03
CN111565712B (zh) 2023-01-13
WO2019137103A1 (zh) 2019-07-18
EP3738582A1 (en) 2020-11-18
US20200368221A1 (en) 2020-11-26
EP3738582A4 (en) 2021-03-17

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