US20170354592A1 - Parenteral sustained-release delivery of carvedilol disperse systems - Google Patents

Parenteral sustained-release delivery of carvedilol disperse systems Download PDF

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Publication number
US20170354592A1
US20170354592A1 US15/621,844 US201715621844A US2017354592A1 US 20170354592 A1 US20170354592 A1 US 20170354592A1 US 201715621844 A US201715621844 A US 201715621844A US 2017354592 A1 US2017354592 A1 US 2017354592A1
Authority
US
United States
Prior art keywords
carvedilol
composition
nanoparticles
microparticles
preferably less
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.)
Abandoned
Application number
US15/621,844
Other languages
English (en)
Inventor
Vera Ivanova
Kaoru Maeda
Wan Wang
Dongwei GUO
Jingjun Huang
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.)
ASCENDIA PHARMACEUTICALS LLC
Original Assignee
ASCENDIA PHARMACEUTICALS LLC
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
Priority to US15/621,844 priority Critical patent/US20170354592A1/en
Priority to JP2018565290A priority patent/JP2019521979A/ja
Priority to CN201780036949.9A priority patent/CN110381929A/zh
Priority to BR112018075984-8A priority patent/BR112018075984A2/pt
Priority to CA3027368A priority patent/CA3027368A1/fr
Priority to PCT/US2017/037311 priority patent/WO2017218576A1/fr
Application filed by ASCENDIA PHARMACEUTICALS LLC filed Critical ASCENDIA PHARMACEUTICALS LLC
Priority to KR1020197000045A priority patent/KR102474392B1/ko
Publication of US20170354592A1 publication Critical patent/US20170354592A1/en
Assigned to ASCENDIA PHARMACEUTICALS, LLC reassignment ASCENDIA PHARMACEUTICALS, LLC ASSIGNMENT OF ASSIGNORS INTEREST (SEE DOCUMENT FOR DETAILS). Assignors: HUANG, JINGJUN, IVANOVA, VERA, MAEDA, KAORU, GUO, Dongwei, WANG, WAN
Priority to US16/429,693 priority patent/US10792244B2/en
Priority to JP2022081399A priority patent/JP2022103337A/ja
Abandoned legal-status Critical Current

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0002Galenical forms characterised by the drug release technique; Application systems commanded by energy
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404Indoles, e.g. pindolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/24Organic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/28Steroids, e.g. cholesterol, bile acids or glycyrrhetinic acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/10Dispersions; Emulsions
    • A61K9/127Liposomes
    • A61K9/1271Non-conventional liposomes, e.g. PEGylated liposomes, liposomes coated with polymers
    • A61K9/1272Non-conventional liposomes, e.g. PEGylated liposomes, liposomes coated with polymers with substantial amounts of non-phosphatidyl, i.e. non-acylglycerophosphate, surfactants as bilayer-forming substances, e.g. cationic lipids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2072Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50Microcapsules 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
    • A61K9/5005Wall or coating material
    • A61K9/5021Organic macromolecular compounds
    • A61K9/5031Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poly(lactide-co-glycolide)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50Microcapsules 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
    • A61K9/51Nanocapsules; Nanoparticles
    • A61K9/5107Excipients; Inactive ingredients
    • A61K9/513Organic macromolecular compounds; Dendrimers
    • A61K9/5146Organic macromolecular compounds; Dendrimers obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyamines, polyanhydrides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50Microcapsules 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
    • A61K9/51Nanocapsules; Nanoparticles
    • A61K9/5107Excipients; Inactive ingredients
    • A61K9/513Organic macromolecular compounds; Dendrimers
    • A61K9/5146Organic macromolecular compounds; Dendrimers obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyamines, polyanhydrides
    • A61K9/5153Polyesters, e.g. poly(lactide-co-glycolide)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nanotechnology (AREA)
  • Optics & Photonics (AREA)
  • Biomedical Technology (AREA)
  • Physics & Mathematics (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Dermatology (AREA)
  • Dispersion Chemistry (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
US15/621,844 2016-06-13 2017-06-13 Parenteral sustained-release delivery of carvedilol disperse systems Abandoned US20170354592A1 (en)

Priority Applications (9)

Application Number Priority Date Filing Date Title
JP2018565290A JP2019521979A (ja) 2016-06-13 2017-06-13 カルベジロール分散系の非経口徐放送達
CN201780036949.9A CN110381929A (zh) 2016-06-13 2017-06-13 卡维地洛分散系统的肠胃外缓释传递
BR112018075984-8A BR112018075984A2 (pt) 2016-06-13 2017-06-13 composição de distribuição de fármaco parenteral para liberação sustentada
CA3027368A CA3027368A1 (fr) 2016-06-13 2017-06-13 Administration a liberation prolongee par voie parenterale de systemes de dispersion de carvedilol
PCT/US2017/037311 WO2017218576A1 (fr) 2016-06-13 2017-06-13 Administration à libération prolongée par voie parentérale de systèmes de dispersion de carvédilol
US15/621,844 US20170354592A1 (en) 2016-06-13 2017-06-13 Parenteral sustained-release delivery of carvedilol disperse systems
KR1020197000045A KR102474392B1 (ko) 2016-06-13 2017-06-21 카르베딜롤 분산 시스템의 비경구 지속-방출 전달
US16/429,693 US10792244B2 (en) 2016-06-13 2019-06-03 Parenteral sustained-release delivery of carvedilol disperse systems
JP2022081399A JP2022103337A (ja) 2016-06-13 2022-05-18 カルベジロール分散系の非経口徐放送達

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201662349390P 2016-06-13 2016-06-13
US15/621,844 US20170354592A1 (en) 2016-06-13 2017-06-13 Parenteral sustained-release delivery of carvedilol disperse systems

Related Child Applications (1)

Application Number Title Priority Date Filing Date
US16/429,693 Continuation US10792244B2 (en) 2016-06-13 2019-06-03 Parenteral sustained-release delivery of carvedilol disperse systems

Publications (1)

Publication Number Publication Date
US20170354592A1 true US20170354592A1 (en) 2017-12-14

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Family Applications (2)

Application Number Title Priority Date Filing Date
US15/621,844 Abandoned US20170354592A1 (en) 2016-06-13 2017-06-13 Parenteral sustained-release delivery of carvedilol disperse systems
US16/429,693 Active US10792244B2 (en) 2016-06-13 2019-06-03 Parenteral sustained-release delivery of carvedilol disperse systems

Family Applications After (1)

Application Number Title Priority Date Filing Date
US16/429,693 Active US10792244B2 (en) 2016-06-13 2019-06-03 Parenteral sustained-release delivery of carvedilol disperse systems

Country Status (8)

Country Link
US (2) US20170354592A1 (fr)
EP (1) EP3468539A4 (fr)
JP (2) JP2019521979A (fr)
KR (1) KR102474392B1 (fr)
CN (1) CN110381929A (fr)
BR (1) BR112018075984A2 (fr)
CA (1) CA3027368A1 (fr)
WO (1) WO2017218576A1 (fr)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2021063813A1 (fr) * 2019-10-01 2021-04-08 Evonik Operations Gmbh Procédé de préparation de nanoparticules sous forme de poudre comprenant un polyester biorésorbable
CN114159405A (zh) * 2020-09-10 2022-03-11 上海中医药大学 一种在胃肠道内稳定的口服纳米粒子及其制备方法和应用
CN115297849A (zh) * 2020-03-16 2022-11-04 株式会社理光 用于生产颗粒的方法

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR112018075984A2 (pt) 2016-06-13 2019-04-02 Ascendia Pharmaceuticals, Llc composição de distribuição de fármaco parenteral para liberação sustentada

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US5308862A (en) * 1993-03-05 1994-05-03 Boehringer Mannheim Pharmaceuticals Corporation - Smithkline Beecham Corp., Ltd. Partnership No. 1 Use of, and method of treatment using, carbazolyl-(4)-oxypropanolamine compounds for inhibition of smooth muscle cell proliferation
US5576016A (en) * 1993-05-18 1996-11-19 Pharmos Corporation Solid fat nanoemulsions as drug delivery vehicles
US5760069A (en) * 1995-02-08 1998-06-02 Boehringer Mannheim Pharmaceuticals Corporation-Smithkline Beecham Corporation Limited Partnership #1 Method of treatment for decreasing mortality resulting from congestive heart failure
US5891467A (en) * 1997-01-31 1999-04-06 Depotech Corporation Method for utilizing neutral lipids to modify in vivo release from multivesicular liposomes
JP2002510045A (ja) * 1998-03-30 2002-04-02 バイオシャフ リミテッド 細胞および体液における一般的診断要因を分析するためのフロー式細胞数計算器
US6664284B2 (en) 1998-07-23 2003-12-16 Roche Diagnostics Gmbh Stabilized carvedilol injection solution
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Cited By (5)

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Publication number Priority date Publication date Assignee Title
WO2021063813A1 (fr) * 2019-10-01 2021-04-08 Evonik Operations Gmbh Procédé de préparation de nanoparticules sous forme de poudre comprenant un polyester biorésorbable
CN114555064A (zh) * 2019-10-01 2022-05-27 赢创有限公司 制备包含生物可再吸收的聚酯的粉末形式的纳米颗粒的方法
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CN115297849A (zh) * 2020-03-16 2022-11-04 株式会社理光 用于生产颗粒的方法
CN114159405A (zh) * 2020-09-10 2022-03-11 上海中医药大学 一种在胃肠道内稳定的口服纳米粒子及其制备方法和应用

Also Published As

Publication number Publication date
US10792244B2 (en) 2020-10-06
EP3468539A1 (fr) 2019-04-17
CA3027368A1 (fr) 2017-12-21
WO2017218576A1 (fr) 2017-12-21
KR20190109376A (ko) 2019-09-25
JP2019521979A (ja) 2019-08-08
BR112018075984A2 (pt) 2019-04-02
KR102474392B1 (ko) 2022-12-07
US20200000706A1 (en) 2020-01-02
EP3468539A4 (fr) 2020-01-15
CN110381929A (zh) 2019-10-25
JP2022103337A (ja) 2022-07-07

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