CN114980893A - 一种长效罗哌卡因药物组合物及其制备方法和用途 - Google Patents

一种长效罗哌卡因药物组合物及其制备方法和用途 Download PDF

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CN114980893A
CN114980893A CN202180008982.7A CN202180008982A CN114980893A CN 114980893 A CN114980893 A CN 114980893A CN 202180008982 A CN202180008982 A CN 202180008982A CN 114980893 A CN114980893 A CN 114980893A
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ropivacaine
acid
oil
composition
drug
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CN114980893B (zh
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甘勇
郭仕艳
孙银银
朱全垒
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Shanghai Institute of Materia Medica of CAS
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P23/00—Anaesthetics
    • A61P23/02—Local anaesthetics
    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • 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
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • 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
    • A61K9/08—Solutions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • 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
    • A61K47/24—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
    • 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
    • A61K47/44—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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
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  • Oil, Petroleum & Natural Gas (AREA)
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  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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Abstract

提供了一种长效罗哌卡因药物组合物及其制备方法和用途。所述药物组合物包含：罗哌卡因；药物溶剂；药用磷脂；药用油脂；药效增强剂，非必需的抗氧剂及非必需的酸碱调节剂。所述药物组合物具有可控的释放行为和缓释效果，可显著降低药物的血浆峰浓度，维持稳定的体内血药浓度，延长有效治疗时间，降低有效治疗剂量，提高药物利用率，降低神经毒性风险，具有长效镇痛作用，可用于疼痛治疗。

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。
CN202180008982.7A 2020-01-14 2021-01-14 一种长效罗哌卡因药物组合物及其制备方法和用途 Active CN114980893B (zh)

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CN2020100370644 2020-01-14
PCT/CN2021/071647 WO2021143745A1 (zh) 2020-01-14 2021-01-14 一种长效罗哌卡因药物组合物及其制备方法和用途

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US11992483B2 (en) 2021-03-31 2024-05-28 Cali Biosciences Us, Llc Emulsions for local anesthetics
CN113941004B (zh) * 2021-07-26 2022-10-21 南京清普生物科技有限公司 一种高浓度局麻药的缓释组合物
CN113941002B (zh) * 2021-08-27 2022-10-14 南京清普生物科技有限公司 一种小分子药物缓释递药系统
CN114344299A (zh) * 2021-12-17 2022-04-15 佐建锋 一种具有长效缓释作用的脂质释药系统及其制备方法
CN115006533B (zh) * 2021-12-28 2023-07-14 南京清普生物科技有限公司 一种含局麻药的均相水性组合物

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CN108159055A (zh) * 2018-01-04 2018-06-15 西安力邦医药科技有限责任公司 治疗乳腺癌的长效递药系统、其制备方法及应用
CN108743952A (zh) * 2018-06-11 2018-11-06 西安力邦医药科技有限责任公司 局部麻醉药的磷脂-混溶剂-油缓释递药系统组方与制备方法
JP2019520310A (ja) * 2017-05-03 2019-07-18 ファミアナ・ヘルス・サイエンス・インク 癌及び前癌病変に対する治療剤、治療方法、及び治療薬剤製造方法
WO2019144079A1 (en) * 2018-01-22 2019-07-25 Yuhua Li Pharmaceutical composition for sustained release delivery of buprenorphine

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CN108159055A (zh) * 2018-01-04 2018-06-15 西安力邦医药科技有限责任公司 治疗乳腺癌的长效递药系统、其制备方法及应用
WO2019144079A1 (en) * 2018-01-22 2019-07-25 Yuhua Li Pharmaceutical composition for sustained release delivery of buprenorphine
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EP4091612A1 (en) 2022-11-23
CN113116813B (zh) 2022-11-29
US20230080811A1 (en) 2023-03-16
CN113116813A (zh) 2021-07-16
EP4091612A4 (en) 2024-01-24
WO2021143745A1 (zh) 2021-07-22
CN114980893B (zh) 2023-12-29

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