ES2527193T3 - Copolímeros multibloque segmentados de fases separadas biodegradables y liberación de polipéptidos biológicamente activos - Google Patents

Copolímeros multibloque segmentados de fases separadas biodegradables y liberación de polipéptidos biológicamente activos Download PDF

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Publication number
ES2527193T3
ES2527193T3 ES11741302.1T ES11741302T ES2527193T3 ES 2527193 T3 ES2527193 T3 ES 2527193T3 ES 11741302 T ES11741302 T ES 11741302T ES 2527193 T3 ES2527193 T3 ES 2527193T3
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Spain
Prior art keywords
prepolymer
copolymer
biologically active
poly
segments
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
ES11741302.1T
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English (en)
Inventor
Rob Steendam
Theodorus Adrianus Cornelius Flipsen
Christine Hiemstra
Johan Zuidema
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Innocore Technologies BV
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Innocore Technologies BV
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    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/38—Albumins
    • A61K38/385—Serum albumin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/43—Enzymes; Proenzymes; Derivatives thereof
    • A61K38/46—Hydrolases (3)
    • A61K38/47—Hydrolases (3) acting on glycosyl compounds (3.2), e.g. cellulases, lactases
    • 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
    • A61K9/0024—Solid, semi-solid or solidifying implants, which are implanted or injected in body tissue
    • 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
    • A61K9/70—Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
    • A61K9/7007—Drug-containing films, membranes or sheets
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2203/00—Investigating strength properties of solid materials by application of mechanical stress
    • G01N2203/02—Details not specific for a particular testing method
    • G01N2203/026—Specifications of the specimen
    • G01N2203/0262—Shape of the specimen
    • G01N2203/0278—Thin specimens
    • G01N2203/0282—Two dimensional, e.g. tapes, webs, sheets, strips, disks or membranes

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Immunology (AREA)
  • Zoology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Dermatology (AREA)
  • Inorganic Chemistry (AREA)
  • Materials For Medical Uses (AREA)
  • Polyesters Or Polycarbonates (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Biological Depolymerization Polymers (AREA)

Abstract

Una composición para la liberación controlada de al menos un polipéptido biológicamente activo que tiene un peso molecular igual o mayor que 10,000 en el hospedero, que comprende al menos un polipéptido biológicamente activo encapsulado en una matriz que comprende al menos un copolímero multibloque biodegradable, termoplástico y de fases separadas, donde el copolímero se caracteriza porque : (i) comprende al menos dos segmentos hidrolizables seleccionados de un prepolímero (A) y un prepolímero (B), el prepolímero (A) tiene una Tg menor que 37°C y el prepolímero (B) tiene una Tm de 40°C - 100°C en condiciones del cuerpo humano; (ii) el copolímero de fases separadas tiene al menos dos transiciones de fase, cada una de las cuales está relacionada con los valores correspondientes de Tg o Tm de los prepolímeros que están comprendidos en el copolímero; (iii) el prepolímero (A) comprende productos de reacción de monómeros cíclicos seleccionados de glicolida, lactida, ε-caprolactona, δ-valerolactona, trimetilen carbonato, tetrametilencarbonato, 1,5-dioxepan-2-ona, 1,4- dioxan-2-ona (para-dioxanona) y/o anhídridos cíclicos tales como oxepan-2,7- diona; y en donde el prepolímero (A) contiene un segmento que se deriva de un polímero soluble en agua, preferentemente en donde dicho polímero soluble en agua se deriva de un diol, diamina o diácido; (iv) un prepolímero (B) que comprende poli(ε-caprolactona) con un Mn de más de 3000; (v) segmentos que están enlazados mediante un extensor de cadena de diisocianato; (vi) los segmentos están aleatoriamente distribuidos a lo largo de la cadena polimérica; y (vii) dicho copolímero contiene poli(etilenglicol), como segmento del pre polímero (A) y/o como prepolímero adicional, y en donde dicho poli(etilenglicol) a) tiene un peso molecular de 600 a 5000 g/mol, y b) está presente en una cantidad de 5 % en peso a 70 % en peso.

Description

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Claims (1)

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ES11741302.1T 2010-07-09 2011-07-08 Copolímeros multibloque segmentados de fases separadas biodegradables y liberación de polipéptidos biológicamente activos Active ES2527193T3 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US36271010P 2010-07-09 2010-07-09
US362710P 2010-07-09
PCT/NL2011/050502 WO2012005594A2 (en) 2010-07-09 2011-07-08 Biodegradable phase separated segmented multi block co-polymers and release of biologically active polypeptides

Publications (1)

Publication Number Publication Date
ES2527193T3 true ES2527193T3 (es) 2015-01-21

Family

ID=44629868

Family Applications (2)

Application Number Title Priority Date Filing Date
ES11741302.1T Active ES2527193T3 (es) 2010-07-09 2011-07-08 Copolímeros multibloque segmentados de fases separadas biodegradables y liberación de polipéptidos biológicamente activos
ES14195906.4T Active ES2628931T3 (es) 2010-07-09 2011-07-08 Copolímeros multibloque segmentados de fases separadas biodegradables y liberación de polipétidos biológicamente activos

Family Applications After (1)

Application Number Title Priority Date Filing Date
ES14195906.4T Active ES2628931T3 (es) 2010-07-09 2011-07-08 Copolímeros multibloque segmentados de fases separadas biodegradables y liberación de polipétidos biológicamente activos

Country Status (8)

Country Link
US (1) US9364442B2 (es)
EP (2) EP2859887B1 (es)
CA (1) CA2804601C (es)
DK (2) DK2590629T3 (es)
ES (2) ES2527193T3 (es)
HU (1) HUE033386T2 (es)
PL (2) PL2859887T3 (es)
WO (1) WO2012005594A2 (es)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL2859887T3 (pl) 2010-07-09 2017-10-31 Innocore Tech B V Biodegradowalne segmentowane kopolimery wieloblokowe z rozdziałem faz oraz uwalnianie biologicznie czynnych polipeptydów
FI128487B (en) * 2013-05-06 2020-06-15 Teknologian Tutkimuskeskus Vtt Oy Glycolic acid polymers and process for their preparation
GB201405874D0 (en) * 2014-04-01 2014-05-14 Aga Nanotech Ltd A therapeutic agent for use in the treatment of infections
EP3804698B1 (en) 2015-08-03 2024-01-31 Tolmar International Limited Liquid polymer delivery system for extended administration of drugs
US10353503B2 (en) * 2015-10-29 2019-07-16 Texas Instruments Incorporated Integrated force sensing element
CN110234336A (zh) 2017-01-31 2019-09-13 维鲁公司 用于促性腺激素释放激素(GnRH)拮抗剂的长效释放的组合物和方法
KR20200040776A (ko) * 2017-07-25 2020-04-20 뻬까 메드 에스아에스 약물 전달 조성물을 제조하기 위한 방법
EP3628698B1 (en) 2018-09-26 2024-11-20 Covidien LP Biodegradable triblock copolymers and implantable medical devices made therefrom
CA3116438C (en) * 2018-10-29 2023-08-22 Pujing Chemical Industry Co., Ltd Polyglycolide copolymer and preparation thereof
WO2020087203A1 (en) * 2018-10-29 2020-05-07 Pujing Chemical Industry Co., Ltd Heat and aging resistant polyglycolide copolymer and composition thereof
WO2021062079A1 (en) 2019-09-25 2021-04-01 Carbon, Inc. Particle coating methods for additively manufactured products
WO2021064550A1 (en) * 2019-09-30 2021-04-08 Tolmar International Limited Liquid polymer compositions and systems for extended delivery of peptides as active pharmaceutical ingredients
MX2022003975A (es) 2019-10-01 2022-07-19 Innocore Tech Holding B V Copolímero de bloques múltiples termoplástico, separado en fases, biodegradable.
US20220331258A1 (en) 2019-10-01 2022-10-20 Allergan Sales, Llc Poly-Dioxanone Multi-Block Copolymer for Ocular Protein Delivery
JP7737983B2 (ja) * 2019-11-01 2025-09-11 インノコア テクノロジーズ ビー．ブイ． 抗体又は巨大タンパク質の延長された放出の為の剤形物
CN114621450B (zh) * 2021-04-07 2023-05-05 江苏睿安应用生物技术股份有限公司 一种扩链改性生物降解聚酯的方法及其应用
JP2025509813A (ja) 2022-03-17 2025-04-11 イノコア テクノロジーズ ホールディング ビー．ブイ． 生分解性熱可塑性ポリ（オルトエステル）ベースのマルチブロック共重合体
WO2026015019A1 (en) 2024-07-08 2026-01-15 InnoCore Technologies Holding B.V. Biodegradable thermoplastic polyoxazoline based copolymers

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Also Published As

Publication number Publication date
EP2859887A1 (en) 2015-04-15
EP2590629A2 (en) 2013-05-15
US9364442B2 (en) 2016-06-14
WO2012005594A2 (en) 2012-01-12
PL2590629T3 (pl) 2015-04-30
EP2859887B1 (en) 2017-03-22
CA2804601A1 (en) 2012-01-12
DK2859887T3 (en) 2017-06-26
CA2804601C (en) 2020-05-19
DK2590629T3 (en) 2015-01-12
PL2859887T3 (pl) 2017-10-31
HUE033386T2 (en) 2017-11-28
WO2012005594A3 (en) 2012-07-05
US20130209568A1 (en) 2013-08-15
ES2628931T3 (es) 2017-08-04
EP2590629B1 (en) 2014-12-03

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