CN109996787A - 难溶性复合物或其溶剂合物、药物组合物及其应用 - Google Patents

难溶性复合物或其溶剂合物、药物组合物及其应用 Download PDF

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Publication number
CN109996787A
CN109996787A CN201880002853.5A CN201880002853A CN109996787A CN 109996787 A CN109996787 A CN 109996787A CN 201880002853 A CN201880002853 A CN 201880002853A CN 109996787 A CN109996787 A CN 109996787A
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China
Prior art keywords
bupivacaine
solvate
compound
compound according
crystal form
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CN201880002853.5A
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CN109996787B (zh
Inventor
张善春
汪贻华
彭家仕
程开生
汪潇
高署
孙宏张
鲁晓蓉
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Hefei Nomin Drug Safety Research Co ltd
Hefei Co Source Pharmaceuticals Co ltd
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Hefei Nomin Drug Safety Research Co ltd
Hefei Co Source Pharmaceuticals Co ltd
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/235—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group
    • A61K31/24—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group having an amino or nitro group
    • A61K31/245—Amino benzoic acid types, e.g. procaine, novocaine
    • 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
    • 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
    • A61K47/50—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/542—Carboxylic acids, e.g. a fatty acid or an amino acid
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P23/00—Anaesthetics
    • A61P23/02—Local anaesthetics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C65/00—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C65/01—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups
    • C07C65/105—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups polycyclic
    • C07C65/11—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups polycyclic with carboxyl groups on a condensed ring system containing two rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Anesthesiology (AREA)
  • Neurology (AREA)
  • Pain & Pain Management (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Emergency Medicine (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

本发明提供式(I)的复合物或其溶剂合物(其中n为1至4)、药物组合物以及所述药物组合物用于预防或治疗手术、手术中和手术后疼痛中的应用。根据本发明的技术方案，提供了一种生产工艺简单、可在体内长时间稳定释放出局麻药物的药物，其至少能够持续释放三天以上，既能延长手术后疼痛的镇痛作用，也能方便医生和患者使用，具有良好的用药依从性。

Description

PCT国内申请，说明书已公开。

Claims (25)

  1. PCT国内申请，权利要求书已公开。
CN201880002853.5A 2017-03-27 2018-03-26 难溶性复合物或其溶剂合物、药物组合物及其应用 Active CN109996787B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN2017101880017 2017-03-27
CN201710188001 2017-03-27
PCT/CN2018/080424 WO2018177232A1 (zh) 2017-03-27 2018-03-26 难溶性复合物或其溶剂合物、药物组合物及其应用

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CN109996787A true CN109996787A (zh) 2019-07-09
CN109996787B CN109996787B (zh) 2022-07-05

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US (1) US11084790B2 (zh)
EP (1) EP3486233B1 (zh)
JP (1) JP6923122B2 (zh)
KR (1) KR102248445B1 (zh)
CN (1) CN109996787B (zh)
AU (1) AU2018241564B2 (zh)
CA (1) CA3049220C (zh)
DK (1) DK3486233T3 (zh)
EA (1) EA039449B1 (zh)
ES (1) ES2866401T3 (zh)
HU (1) HUE053472T2 (zh)
PH (1) PH12019501560A1 (zh)
PL (1) PL3486233T3 (zh)
PT (1) PT3486233T (zh)
SG (1) SG11201906132UA (zh)
TW (1) TWI740045B (zh)
WO (1) WO2018177232A1 (zh)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110483372A (zh) * 2018-05-14 2019-11-22 南京诺瑞特医药科技有限公司 布比卡因的盐
CN111983052A (zh) * 2020-07-24 2020-11-24 合肥诺明药物安全研究有限公司 一种hyr-pb21有效成分血药浓度的定量分析方法

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20230133595A (ko) 2022-03-11 2023-09-19 한국한의약진흥원 등검은말벌독에 함유된 세로토닌의 안정성을 유지하기 위한 조성물

Citations (3)

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WO2004112713A2 (en) * 2003-06-20 2004-12-29 Royer Biomedical, Inc. Drug polymer complexes
CN104370934A (zh) * 2013-08-13 2015-02-25 上海科胜药物研发有限公司 一种普拉格雷盐及其制备方法
WO2017036408A1 (zh) * 2015-09-01 2017-03-09 四川海思科制药有限公司 S-(-)-1-丙基-2',6'-二甲苯胺甲酰基哌啶晶体及其缓释制剂

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AU2003227517A1 (en) * 2002-05-23 2003-12-12 Danmarks Farmaceutiske Universitet Pharmacologically active salts
CA2581287C (en) * 2004-09-17 2015-08-25 Durect Corporation Sustained local anesthetic composition containing bupivacaine and saib
WO2009061497A1 (en) 2007-11-07 2009-05-14 Svip5 Llc Slow release of organic salts of local anesthetics for pain relief
EP2398468B1 (en) 2009-02-17 2016-11-30 KRKA, D.D., Novo Mesto Pharmaceutical compositions comprising prasugrel base or its pharmaceutically acceptable acid addition salts and processes for their preparation
CZ2009762A3 (cs) 2009-11-16 2011-05-25 Zentiva, K. S. Nové soli 5-[2-cyklopropyl-1-(2-fluorfenyl)-2-oxoethyl]-4,5,6,7-tetrahydrothieno[3,2-c]pyridin-2-yl acetátu známého pod nechráneným názvem prasugrel a zpusob jejich výroby
RU2021114918A (ru) * 2016-12-26 2021-07-09 Целликс Био Прайвет Лимитед Композиции и способы лечения хронической боли

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004112713A2 (en) * 2003-06-20 2004-12-29 Royer Biomedical, Inc. Drug polymer complexes
CN104370934A (zh) * 2013-08-13 2015-02-25 上海科胜药物研发有限公司 一种普拉格雷盐及其制备方法
WO2017036408A1 (zh) * 2015-09-01 2017-03-09 四川海思科制药有限公司 S-(-)-1-丙基-2',6'-二甲苯胺甲酰基哌啶晶体及其缓释制剂

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110483372A (zh) * 2018-05-14 2019-11-22 南京诺瑞特医药科技有限公司 布比卡因的盐
CN111983052A (zh) * 2020-07-24 2020-11-24 合肥诺明药物安全研究有限公司 一种hyr-pb21有效成分血药浓度的定量分析方法

Also Published As

Publication number Publication date
HUE053472T2 (hu) 2021-06-28
KR102248445B1 (ko) 2021-05-04
ES2866401T3 (es) 2021-10-19
EA039449B1 (ru) 2022-01-28
CA3049220A1 (en) 2018-10-04
US20210087144A1 (en) 2021-03-25
PL3486233T3 (pl) 2021-06-28
SG11201906132UA (en) 2019-10-30
EP3486233A4 (en) 2020-04-08
EP3486233A1 (en) 2019-05-22
EP3486233B1 (en) 2021-01-27
PT3486233T (pt) 2021-03-18
AU2018241564B2 (en) 2020-07-02
TWI740045B (zh) 2021-09-21
EA201990419A1 (ru) 2019-09-30
WO2018177232A1 (zh) 2018-10-04
TW201940170A (zh) 2019-10-16
CN109996787B (zh) 2022-07-05
CA3049220C (en) 2022-03-29
JP6923122B2 (ja) 2021-08-18
DK3486233T3 (da) 2021-03-15
KR20190101980A (ko) 2019-09-02
PH12019501560A1 (en) 2020-02-24
JP2020515513A (ja) 2020-05-28
AU2018241564A1 (en) 2019-05-30
US11084790B2 (en) 2021-08-10

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