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1. RU0002565668 - POLYMERS CAPABLE OF RECOVERY AND REVERSIBLE THERMAL GEL-FORMATION

Office Russian Federation
Application Number 2012111986/04
Application Date 20.09.2010
Publication Number 0002565668
Publication Date 20.10.2015
Grant Number
Grant Date 20.10.2015
Publication Kind C2
IPC
A61K 47/34
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
34Macromolecular 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
C08G 63/08
CCHEMISTRY; METALLURGY
08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
GMACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING CARBON-TO-CARBON UNSATURATED BONDS
63Macromolecular compounds obtained by reactions forming a carboxylic ester link in the main chain of the macromolecule
02Polyesters derived from hydroxy carboxylic acids or from polycarboxylic acids and polyhydroxy compounds
06derived from hydroxy carboxylic acids
08Lactones or lactides
C08L 67/04
CCHEMISTRY; METALLURGY
08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
LCOMPOSITIONS OF MACROMOLECULAR COMPOUNDS
67Compositions of polyesters obtained by reactions forming a carboxylic ester link in the main chain; Compositions of derivatives of such polymers
04Polyesters derived from hydroxy carboxylic acids, e.g. lactones
A61K 47/30
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
CPC
C08G 63/664
CCHEMISTRY; METALLURGY
08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
GMACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
63Macromolecular compounds obtained by reactions forming a carboxylic ester link in the main chain of the macromolecule
66Polyesters containing oxygen in the form of ether groups
664derived from hydroxy carboxylic acids
A61K 9/0024
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
0012Galenical forms characterised by the site of application
0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
0024Solid, semi-solid or solidifying implants, which are implanted or injected in body tissue
A61K 47/34
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
34Macromolecular 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
C08G2261/126
CCHEMISTRY; METALLURGY
08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
GMACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
2261Macromolecular compounds obtained by reactions forming a carbon-to-carbon link in the main chain of the macromolecule
10Definition of the polymer structure
12Copolymers
126block
C08J 3/12
CCHEMISTRY; METALLURGY
08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
JWORKING-UP; GENERAL PROCESSES OF COMPOUNDING; AFTER-TREATMENT NOT COVERED BY SUBCLASSES C08B, C08C, C08F, C08G
3Processes of treating or compounding macromolecular substances
12Powdering or granulating
C08J2367/04
CCHEMISTRY; METALLURGY
08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
JWORKING-UP; GENERAL PROCESSES OF COMPOUNDING; AFTER-TREATMENT NOT COVERED BY SUBCLASSES C08B, C08C, C08F, C08G
2367Characterised by the use of polyesters obtained by reactions forming a carboxylic ester link in the main chain
04Polyesters derived from hydroxy carboxylic acids, e.g. lactones
Inventors ФОВЕРС Кирк Д. (US)
РАТИ Рамеш (US)
ПЬЯО Ай-Жи (US)
FOVERS Kirk D. (US)
RATI Ramesh (US)
P'JaO Aj-Zhi (US)
Priority Data 12/562,653 18.09.2009 US
61/275,717 18.09.2009 US
Title
(EN) POLYMERS CAPABLE OF RECOVERY AND REVERSIBLE THERMAL GEL-FORMATION
(RU) ПОЛИМЕРЫ, СПОСОБНЫЕ К ВОССТАНОВЛЕНИЮ И ОБРАТИМОМУ ТЕРМИЧЕСКОМУ ГЕЛЕОБРАЗОВАНИЮ
Abstract
(EN)
FIELD: chemistry. SUBSTANCE: claimed invention relates to biodegradable and bioabsorbable block-copolymers in form of solid powder or wax-like powder. Described is composition of block-copolymer of AB, ABA or BAB type for introduction of medication, with said block-copolymer containing: at least first block-copolymer component of AB, ABA or BAB type, containing first hydrophobic A-block and first hydrophilic B-block, with first hydrophobic A-block representing biodegradable polyester, containing at least 60% of caprolacton and at least one second polyester-forming monomer, with said first hydrophilic B-block having first average molecular weight and containing polyethylene glycol; at least second block-copolymer component of AB, ABA or BAB type, containing second hydrophobic A-block and second hydrophilic B-block, with said second hydrophobic A-block containing biodegradable polyester, and second hydrophilic B-block having second average molecular weight and containing polyethylene glycol, with second average molecular weight being different from first average molecular weight; and total weight average molecular weight of block-copolymer composition constitutes from 1500 to 10000 Dalton, total content of A-block in composition constitutes approximately from 60 to 85% by weigh, and total content of B-block in composition constitutes approximately from 15 to 40% by weight, with total weight average molecular weight of B-block in composition constituting from 300 to 2000 Dalton, and said block-copolymer composition is solid at room temperature, is capable of reversible thermal gel-formation with obtaining in form of water polymer solution and is capable of converting into water polymer solution in less than thirty minutes with mixing without application of additives or heating above 60°C. Also claimed is method of introduction to warm-blooded animal of at least one medication in form with controlled release, including (1) provision of composition of block-copolymer of AB, ABA or BAB type mentioned above, (2) obtaining water polymer solution of said solid composition by combination of copolymer with water without impact of temperature above 60°C; and (3) introduction of said water polymer solution to said warm-blooded animal. Described is method of obtaining composition described above. EFFECT: obtaining compositions for introduction of medication, possessing improved stability, which have required characteristics of medication release, swelling and dissolution. 15 cl, 4 dwg, 3 tbl, 9 ex

(RU)
Настоящее изобретение относится к биоразлагаемым и биоабсорбируемым блок-сополимерам в виде твердого порошка или воскообразного порошка. Описана композиция блок-сополимера типа АВ, ABA или ВАВ для введения лекарственного средства, при этом указанный блок-сополимер содержит: по меньшей мере первый блок-сополимерный компонент типа АВ, ABA или ВАВ, содержащий первый гидрофобный А-блок и первый гидрофильный В-блок, причем первый гидрофобный А-блок представляет собой биоразлагаемый сложный полиэфир, содержащий по меньшей мере 60% капролактона и по меньшей мере один второй полиэфир-образующий мономер, при этом указанный первый гидрофильный В-блок имеет первую среднюю молекулярную массу и содержит полиэтиленгликоль; по меньшей мере второй блок-сополимерный компонент типа АВ, ABA или ВАВ, содержащий второй гидрофобный А-блок и второй гидрофильный В-блок, при этом второй гидрофобный А-блок содержит биоразлагаемый сложный полиэфир, а второй гидрофильный В-блок имеет вторую среднюю молекулярную массу и содержит полиэтиленгликоль, причем вторая средняя молекулярная масса отличается от первой средней молекулярной массы; при этом общая средневесовая молекулярная масса блок-сополимерной композиции составляет от 1500 до 10000 Дальтон, общее содержание А-блока в композиции составляет примерно от 60 до 85% по массе, а общее содержание В-блока в композиции составляет примерно от 15 до 40% по массе, причем общая средневесовая молекулярная масса В-блока в композиции составляет от 300 до 2000 Дальтон, при этом указанная композиция блок-сополимера является твердой при комнатной температуре, способна к обратимому термическому гелеобразованию при получении в виде водного полимерного раствора и способна превращаться в водный полимерный раствор менее чем за тридцать минут при перемешивании без применения добавок или нагревания свыше 60°C. Также описан способ введения теплокровному животному по меньшей мере одного лекарственного средства в форме с контролируемым высвобождением, включающий: (1) обеспечение композиции блок-сополимера типа АВ, ABA или ВАВ указанной выше, (2) получение водного полимерного раствора указанной твердой композиции путем объединения сополимера с водой без воздействия температуры свыше 60°C; и (3) введение указанного водного полимерного раствора указанному теплокровному животному. Описан способ получения указанной выше композиции. Технический результат - получение композиций для введения лекарственного средства, обладающих улучшенной стабильностью, имеющих требуемые характеристики высвобождения лекарственного средства, набухания и растворения. 3 н. и 12 з.п. ф-лы, 4 ил., 3 табл., 9 пр.