CN111954672B - 丁丙诺啡衍生物的长效注射制剂及结晶形式 - Google Patents

丁丙诺啡衍生物的长效注射制剂及结晶形式 Download PDF

Info

Publication number
CN111954672B
CN111954672B CN201980023678.2A CN201980023678A CN111954672B CN 111954672 B CN111954672 B CN 111954672B CN 201980023678 A CN201980023678 A CN 201980023678A CN 111954672 B CN111954672 B CN 111954672B
Authority
CN
China
Prior art keywords
buprenorphine
crystalline form
diffraction pattern
ray powder
powder diffraction
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Active
Application number
CN201980023678.2A
Other languages
English (en)
Chinese (zh)
Other versions
CN111954672A (zh
Inventor
林东和
文永顺
梁芮玮
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Alar Pharmaceuticals Inc
Original Assignee
Alar Pharmaceuticals Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Alar Pharmaceuticals Inc filed Critical Alar Pharmaceuticals Inc
Publication of CN111954672A publication Critical patent/CN111954672A/zh
Application granted granted Critical
Publication of CN111954672B publication Critical patent/CN111954672B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D489/00—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula:
    • C07D489/02—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: with oxygen atoms attached in positions 3 and 6, e.g. morphine, morphinone
    • C07D489/04—Salts; Organic complexes
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D489/00—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula:
    • C07D489/09—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: containing 4aH-8, 9 c-Iminoethano- phenanthro [4, 5-b, c, d] furan ring systems condensed with carbocyclic rings or ring systems
    • C07D489/10—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: containing 4aH-8, 9 c-Iminoethano- phenanthro [4, 5-b, c, d] furan ring systems condensed with carbocyclic rings or ring systems with a bridge between positions 6 and 14
    • C07D489/12—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: containing 4aH-8, 9 c-Iminoethano- phenanthro [4, 5-b, c, d] furan ring systems condensed with carbocyclic rings or ring systems with a bridge between positions 6 and 14 the bridge containing only two carbon atoms
    • 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
    • A61K31/485—Morphinan derivatives, e.g. morphine, codeine
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • 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
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/34—Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/10—Dispersions; Emulsions
    • 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
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1641—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers
    • A61K9/1647—Polyesters, e.g. poly(lactide-co-glycolide)
    • 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
    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5005—Wall or coating material
    • A61K9/5021—Organic macromolecular compounds
    • A61K9/5031—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poly(lactide-co-glycolide)
    • 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
    • A61P1/10—Laxatives
    • 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
    • A61P25/24—Antidepressants
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36—Opioid-abuse
    • 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]
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Dermatology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Addiction (AREA)
  • Molecular Biology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biochemistry (AREA)
  • Rheumatology (AREA)
  • Dispersion Chemistry (AREA)
  • Emergency Medicine (AREA)
  • Inorganic Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biophysics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CN201980023678.2A 2018-05-11 2019-05-10 丁丙诺啡衍生物的长效注射制剂及结晶形式 Active CN111954672B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862670714P 2018-05-11 2018-05-11
US62/670,714 2018-05-11
PCT/CN2019/086449 WO2019214726A1 (en) 2018-05-11 2019-05-10 Long-acting injectable formulations and crystalline forms of buprenorphine derivatives

Publications (2)

Publication Number Publication Date
CN111954672A CN111954672A (zh) 2020-11-17
CN111954672B true CN111954672B (zh) 2023-09-01

Family

ID=68466685

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201980023678.2A Active CN111954672B (zh) 2018-05-11 2019-05-10 丁丙诺啡衍生物的长效注射制剂及结晶形式

Country Status (14)

Country Link
US (2) US11524965B2 (https=)
EP (1) EP3790881B1 (https=)
JP (3) JP7421804B2 (https=)
KR (2) KR102839314B1 (https=)
CN (1) CN111954672B (https=)
AR (1) AR117426A1 (https=)
AU (1) AU2019266795B2 (https=)
BR (1) BR112020016576A2 (https=)
CA (1) CA3089256C (https=)
MX (1) MX2020008471A (https=)
NZ (1) NZ766474A (https=)
TW (1) TWI838372B (https=)
WO (1) WO2019214726A1 (https=)
ZA (1) ZA202004582B (https=)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR112020016576A2 (pt) 2018-05-11 2020-12-15 Alar Pharmaceuticals Inc. Formulações injetáveis de ação prolongada e formas cristalinas de derivados de buprenorfina
GB202019594D0 (en) * 2020-12-11 2021-01-27 Univ London Queen Mary Sustained release formulations of crystalline drugs
CN117999079A (zh) * 2021-08-20 2024-05-07 苏州恩华生物医药科技有限公司 一种包含塞纳布啡的药物组合物
IL317873A (en) * 2022-06-24 2025-02-01 Alar Pharmaceuticals Inc Stable pharmaceutical composition of buprenorphine and method of preparation and use thereof
CN115317453A (zh) * 2022-09-01 2022-11-11 广东嘉博制药有限公司 一种缓释微球制剂及其制备方法与用途
EP4719414A2 (en) * 2023-06-02 2026-04-08 Board of Regents of the University of Nebraska Compounds, nanoparticles, and pharmaceutical compositions for the treatment of drug addiction

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1500786A (zh) * 2002-11-12 2004-06-02 ���ŷ�������ҽԺ 新颖的丁丙诺啡酯衍生物及其制备方法，以及长效作用镇痛药学组合物
CN103068387A (zh) * 2010-06-08 2013-04-24 Rb医药品有限公司 包含丁丙诺啡的组合物
CN105377301A (zh) * 2013-03-15 2016-03-02 奥克伍德实验室有限责任公司 高药物载量的丁丙诺啡微球和生产其的方法
WO2016142877A1 (en) * 2015-03-10 2016-09-15 Rhodes Technologies Acetate salt of buprenorphine and methods for preparing buprenorphine
WO2018050043A1 (en) * 2016-09-13 2018-03-22 Alar Pharmaceuticals Inc. Sustained-release buprenorphine formulations background of invention

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RO121631B1 (ro) 1999-08-27 2008-01-30 Southern Research Institute Compoziţie cu buprenorfină şi utilizarea acesteia pentru reducerea consumului de heroină şi/sau alcool
DE60329515D1 (de) 2002-10-25 2009-11-12 Euro Celtique Sa Analoga und prodrugs von buprenorphin
DE60224288T2 (de) 2002-11-25 2009-04-16 Chi Mei Foundation Medical Center Buprenorphinesterderivate, Verfahren zu ihrer Herstellung, und langwirksame analgetische Arzneimittel
JP2004175706A (ja) * 2002-11-26 2004-06-24 Chi Mei Foundation Medical Center 新規なブプレノルフィンのエステル誘導体及びそれらの調製方法、及び長時間効力持続性鎮痛薬剤組成物
WO2005117830A1 (en) 2004-06-04 2005-12-15 Camurus Ab Liquid depot formulations
GB0606124D0 (en) 2006-03-28 2006-05-03 Reckitt Benckiser Healthcare Buprenorphine derivatives and uses thereof
US9272044B2 (en) * 2010-06-08 2016-03-01 Indivior Uk Limited Injectable flowable composition buprenorphine
GB2481018B (en) 2010-06-08 2015-03-18 Rb Pharmaceuticals Ltd Injectable flowable composition comprising buprenorphine
FR2975912B1 (fr) * 2011-05-30 2013-06-14 Flamel Tech Sa Composition a liberation controlee de buprenorphine
CA2867121C (en) * 2012-03-19 2021-05-25 Alkermes Pharma Ireland Limited Pharmaceutical compositions comprising fatty acid esters
EP2970188A4 (en) 2013-03-15 2016-10-19 Vm Therapeutics Llc NOVEL CRYSTALLINE FORMS
GB201404139D0 (en) * 2014-03-10 2014-04-23 Rb Pharmaceuticals Ltd Sustained release buprenorphine solution formulations
BR112020016576A2 (pt) 2018-05-11 2020-12-15 Alar Pharmaceuticals Inc. Formulações injetáveis de ação prolongada e formas cristalinas de derivados de buprenorfina

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1500786A (zh) * 2002-11-12 2004-06-02 ���ŷ�������ҽԺ 新颖的丁丙诺啡酯衍生物及其制备方法，以及长效作用镇痛药学组合物
CN103068387A (zh) * 2010-06-08 2013-04-24 Rb医药品有限公司 包含丁丙诺啡的组合物
CN105377301A (zh) * 2013-03-15 2016-03-02 奥克伍德实验室有限责任公司 高药物载量的丁丙诺啡微球和生产其的方法
WO2016142877A1 (en) * 2015-03-10 2016-09-15 Rhodes Technologies Acetate salt of buprenorphine and methods for preparing buprenorphine
WO2018050043A1 (en) * 2016-09-13 2018-03-22 Alar Pharmaceuticals Inc. Sustained-release buprenorphine formulations background of invention

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
A Solubility and Related Physicochemical Property Comparison of Buprenorphine and Its 3-Alkyl Esters;Audra L. Stinchcomb et al.;《Pharmaceutical Research》;第12卷(第10期);第1526-1529页 *

Also Published As

Publication number Publication date
WO2019214726A1 (en) 2019-11-14
US20210122756A1 (en) 2021-04-29
TW202016117A (zh) 2020-05-01
TWI838372B (zh) 2024-04-11
JP2023106478A (ja) 2023-08-01
JP2025121948A (ja) 2025-08-20
JP7421804B2 (ja) 2024-01-25
JP2021522306A (ja) 2021-08-30
US20230002399A1 (en) 2023-01-05
EP3790881A4 (en) 2022-03-09
US11524965B2 (en) 2022-12-13
EP3790881A1 (en) 2021-03-17
CA3089256A1 (en) 2019-11-14
AU2019266795B2 (en) 2023-02-09
ZA202004582B (en) 2023-01-25
CN111954672A (zh) 2020-11-17
AR117426A1 (es) 2021-08-04
US12522610B2 (en) 2026-01-13
AU2019266795A1 (en) 2020-08-13
BR112020016576A2 (pt) 2020-12-15
NZ766474A (en) 2023-03-31
KR20210021459A (ko) 2021-02-26
KR102839314B1 (ko) 2025-07-29
EP3790881B1 (en) 2026-04-15
KR20230093535A (ko) 2023-06-27
MX2020008471A (es) 2020-09-25
CA3089256C (en) 2023-10-10

Similar Documents

Publication Publication Date Title
CN111954672B (zh) 丁丙诺啡衍生物的长效注射制剂及结晶形式
EP2310363B1 (en) Anticancer oral formulation
US10744132B2 (en) Sustained-release buprenorphine formulations
CN113226288B (zh) 纳曲酮注射型缓释制剂
WO2018177232A1 (zh) 难溶性复合物或其溶剂合物、药物组合物及其应用
HK40038905B (zh) 丁丙诺啡衍生物的长效注射制剂及结晶形式
HK40038905A (en) Long-acting injectable formulations and crystalline forms of buprenorphine derivatives
NZ750367B2 (en) Sustained-release buprenorphine formulations
HK40062327B (zh) 氯胺酮双羟萘酸盐的长效注射剂型
HK40004794A (en) Sustained-release buprenorphine formulations

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 40038905

Country of ref document: HK

GR01 Patent grant
GR01 Patent grant