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ES2366886T1 - Composición que presenta estabilidad de formulación potenciada y administración de ingredientes activos tópicos potenciado. - Google Patents

Composición que presenta estabilidad de formulación potenciada y administración de ingredientes activos tópicos potenciado. Download PDF

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Publication number
ES2366886T1
ES2366886T1 ES10182378T ES10182378T ES2366886T1 ES 2366886 T1 ES2366886 T1 ES 2366886T1 ES 10182378 T ES10182378 T ES 10182378T ES 10182378 T ES10182378 T ES 10182378T ES 2366886 T1 ES2366886 T1 ES 2366886T1
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Spain
Prior art keywords
dispersion
solid
surfactant
sol
group
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Pending
Application number
ES10182378T
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English (en)
Inventor
Noa Lapidot
Shlomo Magdassi
David Avnir
Claudio Rottman
Orit Ben Zazon
Alon Seri-Levy
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Sol Gel Technologies Ltd
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Sol Gel Technologies Ltd
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Application filed by Sol Gel Technologies Ltd filed Critical Sol Gel Technologies Ltd
Publication of ES2366886T1 publication Critical patent/ES2366886T1/es
Pending legal-status Critical Current

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
    • A61K8/04—Dispersions; Emulsions
    • A61K8/042—Gels
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
    • A61K8/11—Encapsulated compositions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • A61K8/25—Silicon; Compounds thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/37—Esters of carboxylic acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/38—Percompounds, e.g. peracids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/60—Sugars; Derivatives thereof
    • A61K8/602—Glycosides, e.g. rutin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/67—Vitamins
    • A61K8/671—Vitamin A; Derivatives thereof, e.g. ester of vitamin A acid, ester of retinol, retinol, retinal
    • 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
    • A61K9/51—Nanocapsules; Nanoparticles
    • A61K9/5107—Excipients; Inactive ingredients
    • A61K9/513—Organic macromolecular compounds; Dendrimers
    • A61K9/5138—Organic macromolecular compounds; Dendrimers obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/02—Nutrients, e.g. vitamins, minerals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10—Antimycotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q11/00—Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00—Preparations for care of the skin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q5/00—Preparations for care of the hair
    • A61Q5/02—Preparations for cleaning the hair
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q5/00—Preparations for care of the hair
    • A61Q5/12—Preparations containing hair conditioners
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B82—NANOTECHNOLOGY
    • B82Y—SPECIFIC USES OR APPLICATIONS OF NANOSTRUCTURES; MEASUREMENT OR ANALYSIS OF NANOSTRUCTURES; MANUFACTURE OR TREATMENT OF NANOSTRUCTURES
    • B82Y5/00—Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/40—Chemical, physico-chemical or functional or structural properties of particular ingredients
    • A61K2800/41—Particular ingredients further characterized by their size
    • A61K2800/412—Microsized, i.e. having sizes between 0.1 and 100 microns
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/40—Chemical, physico-chemical or functional or structural properties of particular ingredients
    • A61K2800/56—Compounds, absorbed onto or entrapped into a solid carrier, e.g. encapsulated perfumes, inclusion compounds, sustained release forms
    • 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
    • A61K9/501—Inorganic compounds
    • 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
    • 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
    • A61K9/51—Nanocapsules; Nanoparticles
    • A61K9/5107—Excipients; Inactive ingredients
    • A61K9/5115—Inorganic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q17/00—Barrier preparations; Preparations brought into direct contact with the skin for affording protection against external influences, e.g. sunlight, X-rays or other harmful rays, corrosive materials, bacteria or insect stings
    • A61Q17/04—Topical preparations for affording protection against sunlight or other radiation; Topical sun tanning preparations

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Birds (AREA)
  • Dermatology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Nanotechnology (AREA)
  • Emergency Medicine (AREA)
  • Pain & Pain Management (AREA)
  • General Engineering & Computer Science (AREA)
  • Physics & Mathematics (AREA)
  • Biomedical Technology (AREA)
  • Obesity (AREA)
  • Optics & Photonics (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Dispersion Chemistry (AREA)
  • Nutrition Science (AREA)
  • Virology (AREA)
  • Biophysics (AREA)
  • Biotechnology (AREA)
  • Rheumatology (AREA)
  • Medical Informatics (AREA)
  • Molecular Biology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Oral & Maxillofacial Surgery (AREA)

Abstract

Un procedimiento para la preparación de microcápsulas que tienen una estructura de núcleo-cáscara, en el que dichas microcápsulas tienen un diámetro de aproximadamente 0,1 a 100 micrómetros, en las que cada núcleo incluye al menos un ingrediente activo, dicho núcleo está encapsulado dentro de una cáscara microcapsular y en las que dicha cáscara está comprendida por al menos un polímero inorgánico obtenido por un procedimiento de sol-gel y dicha cáscara microcapsular protege el ingrediente activo antes de la aplicación tópica y libera dicho ingrediente activo después de la aplicación tópica, dicho procedimiento comprende las etapas de: (a) preparar una solución hidrófoba o una dispersión hidrófoba que comprende precursores sol-gel y un ingrediente a encapsular; (b) emulsionar la solución o dispersión hidrófoba de la etapa (a) en una solución acuosa sometida a fuerzas de alto cizallamiento para obtener una emulsión; (c) mezclar y agitar la emulsión obtenida, con una segunda solución acuosa, a un pH seleccionado para obtener las microcápsulas sol-gel.

Claims (15)

1. Un procedimiento para la preparación de microcápsulas que tienen una estructura de núcleo-cáscara, en el que dichas microcápsulas tienen un diámetro de aproximadamente 0,1 a 100 micrómetros, en las que cada núcleo incluye al menos un ingrediente activo, dicho núcleo está encapsulado dentro de una cáscara microcapsular y en las que dicha cáscara está comprendida por al menos un polímero inorgánico obtenido por un procedimiento de sol-gel y dicha cáscara microcapsular protege el ingrediente activo antes de la aplicación tópica y libera dicho ingrediente activo después de la aplicación tópica, dicho procedimiento comprende las etapas de: (a) preparar una solución hidrófoba o una dispersión hidrófoba que comprende precursores sol-gel y un ingrediente a encapsular; (b) emulsionar la solución o dispersión hidrófoba de la etapa (a) en una solución acuosa sometida a fuerzas de alto cizallamiento para obtener una emulsión; (c) mezclar y agitar la emulsión obtenida, con una segunda solución acuosa, a un pH seleccionado para obtener las microcápsulas sol-gel.
2. El procedimiento de la reivindicación 1, en el que dicha solución o dispersión hidrófoba comprende adicionalmente un tensioactivo, un polímero, un tensioactivo polimérico, un agente de suspensión o mezclas de los mismos.
3. El procedimiento de la reivindicación 1, en el que dichos precursores sol-gel se seleccionan a partir del grupo que consiste en un monómero de alcóxido metálico, un monómero de alcóxido semimetálico, un monómero de éster metálico, un monómero de éster semimetálico, un monómero de silazano, un monómero de la fórmula M(R)_{n}(P)_{m}, en la que M es un elemento metálico o un elemento semimetálico, R es un sustituyente hidrolizable, n es un número entero desde 2 hasta 6, P es un sustituyente no polimerizable y m es un número entero desde 0 hasta 6, un polímero parcialmente hidrolizado y parcialmente condensado de los mismos, o cualquier mezcla de los mismos.
4. El procedimiento de la reivindicación 1, en el que dicha dispersión hidrófoba se prepara por un procedimiento que comprende las siguientes etapas: (a) humedecer y mezclar un ingrediente sólido a encapsular con al menos un aditivo seleccionado del grupo que consiste en un líquido, un agente humectante, o una combinación de los mismos; (b) micronizar el sólido por trituración o molienda para obtener una dispersión del sólido en dicho aditivo.
5. El procedimiento de la reivindicación 4, que comprende adicionalmente añadir al menos un aceite en la etapa (a) o en la etapa (b) o en ambas etapas (a) y (b) para obtener una dispersión del sólido en el aceite.
6. El procedimiento de la reivindicación 1, en el que dicha dispersión hidrófoba se prepara por un procedimiento que comprende las siguientes etapas: (a) micronizar un ingrediente sólido para encapsular por trituración o molienda; (b) humedecer y mezclar un ingrediente sólido a encapsular con al menos un aditivo seleccionado del grupo que consiste en un líquido, un agente humectante, o una combinación de los mismos.
7. El procedimiento de la reclamación 6, comprendiendo adicionalmente la etapa de añadir al menos una fase de dispersión seleccionada del grupo que consiste en un aceite, un precursor sol-gel o una combinación de los mismos y su mezcla para obtener una dispersión.
8. El procedimiento de acuerdo con la reivindicación 0-4, en el que la concentración del sólido es aproximadamente 0,001 por ciento al 95 por ciento (peso/peso) en base al peso total del sólido y el aceite.
9. El procedimiento de acuerdo con la reivindicación 4, en el que el tamaño de la partícula del sólido disperso está entre aproximadamente 0,1 aproximadamente 20 micrómetros.
10. El procedimiento de acuerdo con la reivindicación 4, en el que un aceite está presente en la dispersión final a una concentración de entre aproximadamente 5 aproximadamente 99 por ciento (peso/peso).
11. El procedimiento de acuerdo con la reivindicación 4 en el que el líquido está seleccionado del grupo que consiste en un líquido hidrófobo, un líquido hidrófilo, un líquido acuoso, o mezclas de los mismos.
12. El procedimiento de acuerdo con la reivindicación 4 en el que la concentración de los precursores sol-gel en la dispersión final está entre aproximadamente 5 aproximadamente 99 por ciento (peso/peso).
13. El procedimiento de acuerdo con la reivindicación 4 en el que el agente humectante está seleccionado del grupo que consiste en un tensioactivo, un tensioactivo polimérico, o mezclas de los mismos.
14. El procedimiento de acuerdo con la reivindicación 13 en el que el tensioactivo está seleccionado del grupo que consiste en un tensioactivo aniónico, un tensioactivo catiónico, un tensioactivo anfótero, un tensioactivo no iónico, o mezclas de los mismos.
15. El procedimiento de acuerdo con cualquiera de las reivindicaciones precedentes, en el que el aceite está seleccionado a partir de un grupo que consiste en aceite mineral, dimeticona, ciclometicona, alquilsiloxanos, éteres de alquilsiloxanos, copolioles de dimeticona, benzoato de alquilo C12-15, benzoato de isoestearilo, benzoato de éter estearílico PPG-15, benzoato de octildodecilo, benzoato de estearilo, benzoato de metilo Gluceth-20, dibenzoato de Poloxámero 1 82, benzoato de Poloxámero 1 05, Transcutol, éster de Bernel, maleato de dietilhexilo, sebacato de dietilhexilo, adipato d e dietilhexilo, adipato de diisopropilo, sebacato de diisopropilo, maleato de diisopropilo, salicilato de etilhexilo, salicilato de tridecilo, salicilato de butiloctilo, miristato de isopropilo, o mezclas de los mismos.
ES10182378T 2000-04-21 2001-04-20 Composición que presenta estabilidad de formulación potenciada y administración de ingredientes activos tópicos potenciado. Pending ES2366886T1 (es)

Applications Claiming Priority (2)

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US19874900P 2000-04-21 2000-04-21
US198749P 2000-04-21

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ES2366886T1 true ES2366886T1 (es) 2011-10-26

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EP (2) EP1335693A2 (es)
JP (1) JP4979109B2 (es)
AU (1) AU2001252513A1 (es)
BR (1) BR0110600A (es)
CA (1) CA2406008C (es)
DE (1) DE10182378T1 (es)
ES (1) ES2366886T1 (es)
IL (1) IL152339A0 (es)
WO (1) WO2001080823A2 (es)

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