CN114364386A - 一种抗肿瘤药物组合物以及提高化合物的溶解度的方法 - Google Patents

一种抗肿瘤药物组合物以及提高化合物的溶解度的方法 Download PDF

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CN114364386A
CN114364386A CN202080063242.9A CN202080063242A CN114364386A CN 114364386 A CN114364386 A CN 114364386A CN 202080063242 A CN202080063242 A CN 202080063242A CN 114364386 A CN114364386 A CN 114364386A
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acid
compound
formula
pharmaceutically acceptable
pharmaceutical composition
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CN202080063242.9A
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CN114364386B (zh
Inventor
鹿宁
程智慧
杨红振
胡怀忠
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Beijing Konruns Pharmaceutical Co Ltd
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Beijing Konruns Pharmaceutical Co Ltd
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    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
    • 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
    • A61K31/66—Phosphorus compounds
    • A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • 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
    • A61K47/02—Inorganic compounds
    • 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
    • A61K47/12—Carboxylic acids; Salts or anhydrides 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents

Abstract

本发明提供一种含磷取代基的喹啉类抗肿瘤药物组合物以及提高该药物组合物中的原料药的溶解度的方法，所述药物组合物包括原料药以及药物学上可接受的酸。本发明通过在原料药中加入酸化合物，可以使药物进入胃液之后，释放出酸，从而提高胃液的酸性，降低胃液pH值。胃液pH值的降低为药物的溶解提供了有利的环境，促进了原料药在胃内的溶解和吸收，提高了药物在体内的生物利用度。本发明还提供了一种提高含磷取代基的喹啉类抗肿瘤药物在水中的溶解度的方法。

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。
CN202080063242.9A 2019-12-30 2020-12-25 一种抗肿瘤药物组合物以及提高化合物的溶解度的方法 Active CN114364386B (zh)

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CN2019113990125 2019-12-30
CN201911399012.5A CN113116894A (zh) 2019-12-30 2019-12-30 一种抗肿瘤药物组合物以及提高化合物的溶解度的方法
PCT/CN2020/139414 WO2021136089A1 (zh) 2019-12-30 2020-12-25 一种抗肿瘤药物组合物以及提高化合物的溶解度的方法

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Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1197456A (zh) * 1995-09-21 1998-10-28 帕斯医药股份有限公司 新的含有对酸不稳定的奥美拉唑的组合物及其制备方法
US20100093727A1 (en) * 2008-10-14 2010-04-15 Ning Xi Compounds and methods of use
CN102093421A (zh) * 2011-01-28 2011-06-15 广州盈升生物科技有限公司 一种含磷取代基的喹啉类化合物及其制备方法、以及含有该化合物的药物组合物及其应用
CN102408411A (zh) * 2011-09-19 2012-04-11 广州盈升生物科技有限公司 一种含喹啉基的羟肟酸类化合物及其制备方法、以及含有该化合物的药物组合物及其应用
US20130035344A1 (en) * 2009-12-29 2013-02-07 Kowa Co., Ltd. Pharmaceutical composition for oral administration

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106290600B (zh) * 2015-06-12 2019-01-01 北京康辰药业股份有限公司 一种用液相色谱法分离康尼替尼及有关物质的方法

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1197456A (zh) * 1995-09-21 1998-10-28 帕斯医药股份有限公司 新的含有对酸不稳定的奥美拉唑的组合物及其制备方法
US20100093727A1 (en) * 2008-10-14 2010-04-15 Ning Xi Compounds and methods of use
US20130035344A1 (en) * 2009-12-29 2013-02-07 Kowa Co., Ltd. Pharmaceutical composition for oral administration
CN102093421A (zh) * 2011-01-28 2011-06-15 广州盈升生物科技有限公司 一种含磷取代基的喹啉类化合物及其制备方法、以及含有该化合物的药物组合物及其应用
CN102408411A (zh) * 2011-09-19 2012-04-11 广州盈升生物科技有限公司 一种含喹啉基的羟肟酸类化合物及其制备方法、以及含有该化合物的药物组合物及其应用

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
陈优生等: ""提高难溶性药物溶解度的研究"", 《海峡药学》, vol. 20, no. 7, pages 25 - 26 *

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CN113116894A (zh) 2021-07-16
CN114364386B (zh) 2023-06-16
WO2021136089A1 (zh) 2021-07-08

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