RU2019126497A - Способ получения электроспряденных волокон с высоким содержанием биоадгезивнго вещества - Google Patents

Способ получения электроспряденных волокон с высоким содержанием биоадгезивнго вещества Download PDF

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RU2019126497A
RU2019126497A RU2019126497A RU2019126497A RU2019126497A RU 2019126497 A RU2019126497 A RU 2019126497A RU 2019126497 A RU2019126497 A RU 2019126497A RU 2019126497 A RU2019126497 A RU 2019126497A RU 2019126497 A RU2019126497 A RU 2019126497A
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bioadhesive
fibers
drug
hydrophilic polymer
peo
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RU2019126497A
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Йенс ХАНСЕН
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Афикс Терапьютикс А/С
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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
    • A61K9/70Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/575Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
    • 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
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/32Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
    • 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
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/34Macromolecular 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
    • 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
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38Cellulose; Derivatives thereof
    • 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
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • A61K9/006Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • DTEXTILES; PAPER
    • D01NATURAL OR MAN-MADE THREADS OR FIBRES; SPINNING
    • D01DMECHANICAL METHODS OR APPARATUS IN THE MANUFACTURE OF ARTIFICIAL FILAMENTS, THREADS, FIBRES, BRISTLES OR RIBBONS
    • D01D5/00Formation of filaments, threads, or the like
    • D01D5/0007Electro-spinning
    • D01D5/0015Electro-spinning characterised by the initial state of the material
    • D01D5/003Electro-spinning characterised by the initial state of the material the material being a polymer solution or dispersion
    • DTEXTILES; PAPER
    • D01NATURAL OR MAN-MADE THREADS OR FIBRES; SPINNING
    • D01FCHEMICAL FEATURES IN THE MANUFACTURE OF ARTIFICIAL FILAMENTS, THREADS, FIBRES, BRISTLES OR RIBBONS; APPARATUS SPECIALLY ADAPTED FOR THE MANUFACTURE OF CARBON FILAMENTS
    • D01F6/00Monocomponent artificial filaments or the like of synthetic polymers; Manufacture thereof
    • D01F6/02Monocomponent artificial filaments or the like of synthetic polymers; Manufacture thereof from homopolymers obtained by reactions only involving carbon-to-carbon unsaturated bonds
    • D01F6/16Monocomponent artificial filaments or the like of synthetic polymers; Manufacture thereof from homopolymers obtained by reactions only involving carbon-to-carbon unsaturated bonds from polymers of unsaturated carboxylic acids or unsaturated organic esters, e.g. polyacrylic esters, polyvinyl acetate
    • DTEXTILES; PAPER
    • D01NATURAL OR MAN-MADE THREADS OR FIBRES; SPINNING
    • D01FCHEMICAL FEATURES IN THE MANUFACTURE OF ARTIFICIAL FILAMENTS, THREADS, FIBRES, BRISTLES OR RIBBONS; APPARATUS SPECIALLY ADAPTED FOR THE MANUFACTURE OF CARBON FILAMENTS
    • D01F6/00Monocomponent artificial filaments or the like of synthetic polymers; Manufacture thereof
    • D01F6/02Monocomponent artificial filaments or the like of synthetic polymers; Manufacture thereof from homopolymers obtained by reactions only involving carbon-to-carbon unsaturated bonds
    • D01F6/26Monocomponent artificial filaments or the like of synthetic polymers; Manufacture thereof from homopolymers obtained by reactions only involving carbon-to-carbon unsaturated bonds from other polymers
    • DTEXTILES; PAPER
    • D01NATURAL OR MAN-MADE THREADS OR FIBRES; SPINNING
    • D01FCHEMICAL FEATURES IN THE MANUFACTURE OF ARTIFICIAL FILAMENTS, THREADS, FIBRES, BRISTLES OR RIBBONS; APPARATUS SPECIALLY ADAPTED FOR THE MANUFACTURE OF CARBON FILAMENTS
    • D01F6/00Monocomponent artificial filaments or the like of synthetic polymers; Manufacture thereof
    • D01F6/58Monocomponent artificial filaments or the like of synthetic polymers; Manufacture thereof from homopolycondensation products
    • D01F6/62Monocomponent artificial filaments or the like of synthetic polymers; Manufacture thereof from homopolycondensation products from polyesters
    • D01F6/625Monocomponent artificial filaments or the like of synthetic polymers; Manufacture thereof from homopolycondensation products from polyesters derived from hydroxy-carboxylic acids, e.g. lactones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/57Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
    • A61K31/573Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
    • CCHEMISTRY; METALLURGY
    • C08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08LCOMPOSITIONS OF MACROMOLECULAR COMPOUNDS
    • C08L2203/00Applications
    • C08L2203/02Applications for biomedical use
    • CCHEMISTRY; METALLURGY
    • C08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08LCOMPOSITIONS OF MACROMOLECULAR COMPOUNDS
    • C08L33/00Compositions of homopolymers or copolymers of compounds having one or more unsaturated aliphatic radicals, each having only one carbon-to-carbon double bond, and only one being terminated by only one carboxyl radical, or of salts, anhydrides, esters, amides, imides or nitriles thereof; Compositions of derivatives of such polymers
    • C08L33/04Homopolymers or copolymers of esters
    • C08L33/14Homopolymers or copolymers of esters of esters containing halogen, nitrogen, sulfur, or oxygen atoms in addition to the carboxy oxygen
    • CCHEMISTRY; METALLURGY
    • C08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08LCOMPOSITIONS OF MACROMOLECULAR COMPOUNDS
    • C08L39/00Compositions of homopolymers or copolymers of compounds having one or more unsaturated aliphatic radicals, each having only one carbon-to-carbon double bond, and at least one being terminated by a single or double bond to nitrogen or by a heterocyclic ring containing nitrogen; Compositions of derivatives of such polymers
    • C08L39/04Homopolymers or copolymers of monomers containing heterocyclic rings having nitrogen as ring member
    • C08L39/06Homopolymers or copolymers of N-vinyl-pyrrolidones

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Textile Engineering (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Inorganic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Dispersion Chemistry (AREA)
  • Mechanical Engineering (AREA)
  • Physiology (AREA)
  • Nutrition Science (AREA)
  • Rheumatology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Pain & Pain Management (AREA)
  • Medicinal Preparation (AREA)
  • Materials For Medical Uses (AREA)
  • Spinning Methods And Devices For Manufacturing Artificial Fibers (AREA)
  • Cosmetics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Artificial Filaments (AREA)
  • Nonwoven Fabrics (AREA)

Claims (19)

1. Способ получения электроспряденных волокон, включающий
i) растворение волокнообразующего гидрофильного полимера в спирте, выбранном из C1-C3 спиртов,
ii) растворение биоадгезивного вещества в воде, где биоадгезивное вещество имеет растворимость в воде 3 г/100 мл или более при 25°С или 10 г/100 мл или более при 25°С, и где биоадгезивное вещество имеет растворимость в спирте, выбранном из С1-С3 спиртов, 0,5 г/100 мл или менее при 25°С или 0,1 г/100 мл или менее при 25°С,
iii) добавление при перемешивании полученного раствора с этапа ii) к полученному раствору с этапа i) с осаждением биоадгезивного вещества и формированием гомогенной суспензии, где биоадгезивное вещество суспендировано в виде частиц, и
iv) электропрядение гомогенной суспензии с получением гидрофильных волокон.
2. Способ по п.1, дополнительно включающий растворение или суспендирование лекарственного вещества на этапе i) или на эьапе ii).
3. Способ по п.1 или 2, где гидрофильный полимер выбран из группы, состоящей из поливинилпиррролидона, этилцеллюлозы, гидроксипропилцеллюлозы, акрилатов и акриловых сополимеров (Eudragit®) и их смесей.
4. Способ по любому из предшествующих пунктов, где биоадгезивное вещество выбрано из группы, состоящей из декстранов, полиэтиленоксидов (PEO), альгината, трагаканта, каррагенана, пектина, желатина, гуара, ксантана, геллана, метилцеллюлозы, гидроксипропилметилцеллюлозы (HPMC), поливинилового спирта (PVA), полимеров акриловых кислот (производные PAA), хитозана, лектинов, тиолированных полимеров, polyoxo WSRA, PAA-co-PEG (PEG представляет собой полиэтиленгликоль) и их смесей.
5. Способ по любому из предшествующих пунктов, где биоадгезивное вещество представляет собой PEO.
6. Способ по любому из предшествующих пунктов, где биоадгезивное вещество представляет собой PEO, имеющий молекулярную массу от приблизительно 100000 до приблизительно 500000 дальтон.
7. Способ по любому из предшествующих пунктов, где биоадгезивное вещество представляет собой полиэтиленоксид, имеющий молекулярную массу приблизительно 200000 дальтон.
8. Способ по п.1 или 2, где волокна содержат гидрофильный полимер, выбранный из поливинилпирролидона, акрилатов и акриловых сополимеров и их смесей.
9. Способ по любому из предшествующих пунктов, где концентрация волокнообразующего гидрофильного полимера(ов) в волокнах составляет от приблизительно 40% до приблизительно 70% масс./масс., в частности, от приблизительно 45 до приблизительно 70% масс./масс. или от приблизительно 50% до 70% масс./масс. в расчете на сумму общей сухой массы.
10. Способ по любому из предшествующих пунктов, где концентрация биоадгезивного вещества в волокнах составляет от приблизительно 30% до приблизительно 60% масс./масс., в частности, от приблизительно 35 до приблизительно 60% или от приблизительно 40% до приблизительно 55% масс./масс. в расчете на сумму общей сухой массы.
11. Способ по любому из предшествующих пунктов, где C1-C3 растворитель представляет собой этанол.
12. Способ по любому из предшествующих пунктов, где лекарственное вещество добавляют на этапе i).
13. Способ по любому из предшествующих пунктов, где лекарственное вещество представляет собой противовоспалительное лекарственное вещество.
14. Способ по любому из предшествующих пунктов, где лекарственное вещество представляет собой кортикостероид.
15. Способ по любому из предшествующих пунктов, дополнительно включающий этап контактирования электроспряденного гидрофильного волокна с электроспряденным гидрофобным слоем.
RU2019126497A 2017-01-23 2018-01-22 Способ получения электроспряденных волокон с высоким содержанием биоадгезивнго вещества RU2019126497A (ru)

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DKPA201770043 2017-01-23
DKPA201770043 2017-01-23
PCT/DK2018/050010 WO2018133910A1 (en) 2017-01-23 2018-01-22 Method for preparing electrospun fibers with a high content of a bioadhesive substance

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KR (1) KR102595001B1 (ru)
CN (1) CN110290783A (ru)
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US11045430B2 (en) 2021-06-29
JP7353980B2 (ja) 2023-10-02
EP3570822A1 (en) 2019-11-27
CA3050026A1 (en) 2018-07-26
BR112019014732A2 (pt) 2020-03-10
ES2874787T3 (es) 2021-11-05
US20190254986A1 (en) 2019-08-22
IL268185B1 (en) 2023-09-01
AU2018209592A1 (en) 2019-07-25
EP3570822B1 (en) 2021-05-05
JP2020506307A (ja) 2020-02-27
IL268185A (en) 2019-09-26
RU2019126497A3 (ru) 2021-05-26
KR102595001B1 (ko) 2023-10-26
KR20190126306A (ko) 2019-11-11
AU2018209592B2 (en) 2024-03-21
CN110290783A (zh) 2019-09-27
WO2018133910A1 (en) 2018-07-26
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DK3570822T3 (da) 2021-07-26
MX2019008155A (es) 2019-11-07

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