d,l-Lactide-co-glycolide microsphere composition for sustained release of water-soluble drug, e.g. peptide, obtained by encapsulation process using water-in-oil-in-water double emulsion

d,l-Lactide-co-glycolide microsphere composition for sustained release of water-soluble drug, e.g. peptide, obtained by encapsulation process using water-in-oil-in-water double emulsion

Production of microsphere composition for sustained release of water-soluble drug (I) involves: (a) emulsifying aqueous solution of (I) in solution of d,l-lactide-co-glycolide matrix copolymer (II) in chlorinated hydrocarbon; (b) emulsifying obtained fine, homogeneous first emulsion in aqueous exter...

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Hauptverfasser: TARIN PERE, ASIN MIGUEL ANGEL, GARCIA JESUS, FERRET EULALIA, RUTLLAN MONTSERRAT, AROLA ROSA
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HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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creator TARIN PERE
ASIN MIGUEL ANGEL
GARCIA JESUS
FERRET EULALIA
RUTLLAN MONTSERRAT
AROLA ROSA
description Production of microsphere composition for sustained release of water-soluble drug (I) involves: (a) emulsifying aqueous solution of (I) in solution of d,l-lactide-co-glycolide matrix copolymer (II) in chlorinated hydrocarbon; (b) emulsifying obtained fine, homogeneous first emulsion in aqueous external phase containing surfactant, thickener and osmotic agent; and (c) extracting/evaporating solvent. Production of a microsphere composition for sustained release of a water-soluble drug (I) involves: (a) emulsifying an aqueous solution of (I) in a solution of d,l-lactide-co-glycolide matrix copolymer (II) (average molecular weight 40-80 kDa; lactic/glycolic acid ratio 50/50 to 80/20) in a chlorinated hydrocarbon; (b) emulsifying the obtained fine, homogeneous first emulsion in an aqueous external phase containing surfactant, thickener and osmotic agent; and (c) extracting/evaporating the solvent to give microspheres, which are filtered off, washed and dried. An Independent claim is included for microspheres obtained by the process, which release (I) continuously over a period of more than 2 (preferably at least 3) months. Production of microsphere composition for sustained release of water-soluble drug (I) involves: (a) emulsifying aqueous solution of (I) in solution of d,l-lactide-co-glycolide matrix copolymer (II) in chlorinated hydrocarbon (b) emulsifying obtained fine, homogeneous first emulsion in aqueous external phase containing surfactant, thickener and osmotic agent and (c) extracting/evaporating solvent. Production of a microsphere composition for sustained release of a water-soluble drug (I) involves: (a) emulsifying an aqueous solution of (I) in a solution of d,l-lactide-co-glycolide matrix copolymer (II) (average molecular weight 40-80 kDa lactic/glycolic acid ratio 50/50 to 80/20) in a chlorinated hydrocarbon (b) emulsifying the obtained fine, homogeneous first emulsion in an aqueous external phase containing surfactant, thickener and osmotic agent and (c) extracting/evaporating the solvent to give microspheres, which are filtered off, washed and dried. An Independent claim is included for microspheres obtained by the process, which release (I) continuously over a period of more than 2 (preferably at least 3) months. La presente invención se refiere a un procedimiento de preparación de una composición farmacéutica en forma de microesferas con liberación prolongada de un principio activo hidrosoluble y microesferas obtenidas, que comprende la suce
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Production of a microsphere composition for sustained release of a water-soluble drug (I) involves: (a) emulsifying an aqueous solution of (I) in a solution of d,l-lactide-co-glycolide matrix copolymer (II) (average molecular weight 40-80 kDa; lactic/glycolic acid ratio 50/50 to 80/20) in a chlorinated hydrocarbon; (b) emulsifying the obtained fine, homogeneous first emulsion in an aqueous external phase containing surfactant, thickener and osmotic agent; and (c) extracting/evaporating the solvent to give microspheres, which are filtered off, washed and dried. An Independent claim is included for microspheres obtained by the process, which release (I) continuously over a period of more than 2 (preferably at least 3) months. Production of microsphere composition for sustained release of water-soluble drug (I) involves: (a) emulsifying aqueous solution of (I) in solution of d,l-lactide-co-glycolide matrix copolymer (II) in chlorinated hydrocarbon (b) emulsifying obtained fine, homogeneous first emulsion in aqueous external phase containing surfactant, thickener and osmotic agent and (c) extracting/evaporating solvent. Production of a microsphere composition for sustained release of a water-soluble drug (I) involves: (a) emulsifying an aqueous solution of (I) in a solution of d,l-lactide-co-glycolide matrix copolymer (II) (average molecular weight 40-80 kDa lactic/glycolic acid ratio 50/50 to 80/20) in a chlorinated hydrocarbon (b) emulsifying the obtained fine, homogeneous first emulsion in an aqueous external phase containing surfactant, thickener and osmotic agent and (c) extracting/evaporating the solvent to give microspheres, which are filtered off, washed and dried. An Independent claim is included for microspheres obtained by the process, which release (I) continuously over a period of more than 2 (preferably at least 3) months. La presente invención se refiere a un procedimiento de preparación de una composición farmacéutica en forma de microesferas con liberación prolongada de un principio activo hidrosoluble y microesferas obtenidas, que comprende la sucesión de las etapas siguientes: - disolución del principio activo en una cantidad apropiada de agua, - emulsionado de la solución acuosa de principio activo así obtenida con una solución de un copolímero matricial d,l-lactida-co-glicolida, de peso molecular medio comprendido entre 40.000 y 80.000 y que tiene una proporción ácido láctico/ácido glicólico comprendida entre 50/50 y 80/20, disuelto en un hidrocarburo clorado, que conduce a una primera emulsión microfina y homogénea, - emulsionado de dicha primera emulsión así obtenida en una fase acuosa externa, que contiene un surfactante, un agente que aumenta la viscosidad y un agente osmótico, - extracción-evaporación del solvente para obtener unas microesferas que se recuperan después de filtración, lavado y secado, así como las microesferas obtenidas.</description><edition>7</edition><language>eng ; spa</language><subject>HUMAN NECESSITIES ; HYGIENE ; MEDICAL OR VETERINARY SCIENCE ; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES ; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS</subject><creationdate>2003</creationdate><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&amp;date=20031116&amp;DB=EPODOC&amp;CC=ES&amp;NR=2194590A1$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,776,881,25542,76289</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&amp;date=20031116&amp;DB=EPODOC&amp;CC=ES&amp;NR=2194590A1$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>TARIN PERE</creatorcontrib><creatorcontrib>ASIN MIGUEL ANGEL</creatorcontrib><creatorcontrib>GARCIA JESUS</creatorcontrib><creatorcontrib>FERRET EULALIA</creatorcontrib><creatorcontrib>RUTLLAN MONTSERRAT</creatorcontrib><creatorcontrib>AROLA ROSA</creatorcontrib><title>d,l-Lactide-co-glycolide microsphere composition for sustained release of water-soluble drug, e.g. peptide, obtained by encapsulation process using water-in-oil-in-water double emulsion</title><description>Production of microsphere composition for sustained release of water-soluble drug (I) involves: (a) emulsifying aqueous solution of (I) in solution of d,l-lactide-co-glycolide matrix copolymer (II) in chlorinated hydrocarbon; (b) emulsifying obtained fine, homogeneous first emulsion in aqueous external phase containing surfactant, thickener and osmotic agent; and (c) extracting/evaporating solvent. Production of a microsphere composition for sustained release of a water-soluble drug (I) involves: (a) emulsifying an aqueous solution of (I) in a solution of d,l-lactide-co-glycolide matrix copolymer (II) (average molecular weight 40-80 kDa; lactic/glycolic acid ratio 50/50 to 80/20) in a chlorinated hydrocarbon; (b) emulsifying the obtained fine, homogeneous first emulsion in an aqueous external phase containing surfactant, thickener and osmotic agent; and (c) extracting/evaporating the solvent to give microspheres, which are filtered off, washed and dried. An Independent claim is included for microspheres obtained by the process, which release (I) continuously over a period of more than 2 (preferably at least 3) months. Production of microsphere composition for sustained release of water-soluble drug (I) involves: (a) emulsifying aqueous solution of (I) in solution of d,l-lactide-co-glycolide matrix copolymer (II) in chlorinated hydrocarbon (b) emulsifying obtained fine, homogeneous first emulsion in aqueous external phase containing surfactant, thickener and osmotic agent and (c) extracting/evaporating solvent. Production of a microsphere composition for sustained release of a water-soluble drug (I) involves: (a) emulsifying an aqueous solution of (I) in a solution of d,l-lactide-co-glycolide matrix copolymer (II) (average molecular weight 40-80 kDa lactic/glycolic acid ratio 50/50 to 80/20) in a chlorinated hydrocarbon (b) emulsifying the obtained fine, homogeneous first emulsion in an aqueous external phase containing surfactant, thickener and osmotic agent and (c) extracting/evaporating the solvent to give microspheres, which are filtered off, washed and dried. An Independent claim is included for microspheres obtained by the process, which release (I) continuously over a period of more than 2 (preferably at least 3) months. 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Production of a microsphere composition for sustained release of a water-soluble drug (I) involves: (a) emulsifying an aqueous solution of (I) in a solution of d,l-lactide-co-glycolide matrix copolymer (II) (average molecular weight 40-80 kDa; lactic/glycolic acid ratio 50/50 to 80/20) in a chlorinated hydrocarbon; (b) emulsifying the obtained fine, homogeneous first emulsion in an aqueous external phase containing surfactant, thickener and osmotic agent; and (c) extracting/evaporating the solvent to give microspheres, which are filtered off, washed and dried. An Independent claim is included for microspheres obtained by the process, which release (I) continuously over a period of more than 2 (preferably at least 3) months. Production of microsphere composition for sustained release of water-soluble drug (I) involves: (a) emulsifying aqueous solution of (I) in solution of d,l-lactide-co-glycolide matrix copolymer (II) in chlorinated hydrocarbon (b) emulsifying obtained fine, homogeneous first emulsion in aqueous external phase containing surfactant, thickener and osmotic agent and (c) extracting/evaporating solvent. Production of a microsphere composition for sustained release of a water-soluble drug (I) involves: (a) emulsifying an aqueous solution of (I) in a solution of d,l-lactide-co-glycolide matrix copolymer (II) (average molecular weight 40-80 kDa lactic/glycolic acid ratio 50/50 to 80/20) in a chlorinated hydrocarbon (b) emulsifying the obtained fine, homogeneous first emulsion in an aqueous external phase containing surfactant, thickener and osmotic agent and (c) extracting/evaporating the solvent to give microspheres, which are filtered off, washed and dried. An Independent claim is included for microspheres obtained by the process, which release (I) continuously over a period of more than 2 (preferably at least 3) months. La presente invención se refiere a un procedimiento de preparación de una composición farmacéutica en forma de microesferas con liberación prolongada de un principio activo hidrosoluble y microesferas obtenidas, que comprende la sucesión de las etapas siguientes: - disolución del principio activo en una cantidad apropiada de agua, - emulsionado de la solución acuosa de principio activo así obtenida con una solución de un copolímero matricial d,l-lactida-co-glicolida, de peso molecular medio comprendido entre 40.000 y 80.000 y que tiene una proporción ácido láctico/ácido glicólico comprendida entre 50/50 y 80/20, disuelto en un hidrocarburo clorado, que conduce a una primera emulsión microfina y homogénea, - emulsionado de dicha primera emulsión así obtenida en una fase acuosa externa, que contiene un surfactante, un agente que aumenta la viscosidad y un agente osmótico, - extracción-evaporación del solvente para obtener unas microesferas que se recuperan después de filtración, lavado y secado, así como las microesferas obtenidas.</abstract><edition>7</edition><oa>free_for_read</oa></addata></record>
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subjects HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
title d,l-Lactide-co-glycolide microsphere composition for sustained release of water-soluble drug, e.g. peptide, obtained by encapsulation process using water-in-oil-in-water double emulsion
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