WO2001028530A1 - Microcapsulas para la estabilizacion de productos cosmeticos, farmaceuticos o de alimentacion - Google Patents
Microcapsulas para la estabilizacion de productos cosmeticos, farmaceuticos o de alimentacion Download PDFInfo
- Publication number
- WO2001028530A1 WO2001028530A1 PCT/ES2000/000403 ES0000403W WO0128530A1 WO 2001028530 A1 WO2001028530 A1 WO 2001028530A1 ES 0000403 W ES0000403 W ES 0000403W WO 0128530 A1 WO0128530 A1 WO 0128530A1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- microcapsules
- cosmetic
- pharmaceutical
- stabilization
- food
- Prior art date
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- 239000003094 microcapsule Substances 0.000 title claims abstract description 35
- 239000002537 cosmetic Substances 0.000 title claims abstract description 34
- 235000013305 food Nutrition 0.000 title claims abstract description 30
- 230000000087 stabilizing effect Effects 0.000 title abstract 2
- 239000000463 material Substances 0.000 claims abstract description 29
- 239000003463 adsorbent Substances 0.000 claims abstract description 17
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- 150000001875 compounds Chemical class 0.000 claims description 15
- 230000006641 stabilisation Effects 0.000 claims description 13
- 238000011105 stabilization Methods 0.000 claims description 13
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- 238000001035 drying Methods 0.000 description 2
- 239000004005 microsphere Substances 0.000 description 2
- 150000004804 polysaccharides Chemical class 0.000 description 2
- 238000003756 stirring Methods 0.000 description 2
- 229920000856 Amylose Polymers 0.000 description 1
- 229920002261 Corn starch Polymers 0.000 description 1
- AEMRFAOFKBGASW-UHFFFAOYSA-N Glycolic acid Chemical class OCC(O)=O AEMRFAOFKBGASW-UHFFFAOYSA-N 0.000 description 1
- 229920002683 Glycosaminoglycan Polymers 0.000 description 1
- 108010058846 Ovalbumin Proteins 0.000 description 1
- 241000736029 Ruvettus pretiosus Species 0.000 description 1
- BUGBHKTXTAQXES-UHFFFAOYSA-N Selenium Chemical compound [Se] BUGBHKTXTAQXES-UHFFFAOYSA-N 0.000 description 1
- JXLYSJRDGCGARV-WWYNWVTFSA-N Vinblastine Natural products O=C(O[C@H]1[C@](O)(C(=O)OC)[C@@H]2N(C)c3c(cc(c(OC)c3)[C@]3(C(=O)OC)c4[nH]c5c(c4CCN4C[C@](O)(CC)C[C@H](C3)C4)cccc5)[C@@]32[C@H]2[C@@]1(CC)C=CCN2CC3)C JXLYSJRDGCGARV-WWYNWVTFSA-N 0.000 description 1
- 239000002250 absorbent Substances 0.000 description 1
- 230000002745 absorbent Effects 0.000 description 1
- 239000013543 active substance Substances 0.000 description 1
- 235000010443 alginic acid Nutrition 0.000 description 1
- 239000000783 alginic acid Substances 0.000 description 1
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- 229960001126 alginic acid Drugs 0.000 description 1
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- 239000003963 antioxidant agent Substances 0.000 description 1
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- OKHHGHGGPDJQHR-YMOPUZKJSA-L calcium;(2s,3s,4s,5s,6r)-6-[(2r,3s,4r,5s,6r)-2-carboxy-6-[(2r,3s,4r,5s,6r)-2-carboxylato-4,5,6-trihydroxyoxan-3-yl]oxy-4,5-dihydroxyoxan-3-yl]oxy-3,4,5-trihydroxyoxane-2-carboxylate Chemical compound [Ca+2].O[C@@H]1[C@H](O)[C@H](O)O[C@@H](C([O-])=O)[C@H]1O[C@H]1[C@@H](O)[C@@H](O)[C@H](O[C@H]2[C@H]([C@@H](O)[C@H](O)[C@H](O2)C([O-])=O)O)[C@H](C(O)=O)O1 OKHHGHGGPDJQHR-YMOPUZKJSA-L 0.000 description 1
- 230000015556 catabolic process Effects 0.000 description 1
- 239000003638 chemical reducing agent Substances 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 235000012000 cholesterol Nutrition 0.000 description 1
- 239000008120 corn starch Substances 0.000 description 1
- 235000018417 cysteine Nutrition 0.000 description 1
- XUJNEKJLAYXESH-UHFFFAOYSA-N cysteine Natural products SCC(N)C(O)=O XUJNEKJLAYXESH-UHFFFAOYSA-N 0.000 description 1
- 238000006731 degradation reaction Methods 0.000 description 1
- 230000000593 degrading effect Effects 0.000 description 1
- 229960004679 doxorubicin Drugs 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 239000000796 flavoring agent Substances 0.000 description 1
- 235000019634 flavors Nutrition 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 229910010272 inorganic material Inorganic materials 0.000 description 1
- 239000011147 inorganic material Substances 0.000 description 1
- 238000011835 investigation Methods 0.000 description 1
- 239000004310 lactic acid Substances 0.000 description 1
- 230000000873 masking effect Effects 0.000 description 1
- 239000011159 matrix material Substances 0.000 description 1
- 239000012528 membrane Substances 0.000 description 1
- 239000011859 microparticle Substances 0.000 description 1
- RNTIBYGPJVJCCJ-UHFFFAOYSA-N n,n-dimethylmethanamine;ethyl 2-methylprop-2-enoate Chemical compound CN(C)C.CCOC(=O)C(C)=C RNTIBYGPJVJCCJ-UHFFFAOYSA-N 0.000 description 1
- 229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 description 1
- 235000016709 nutrition Nutrition 0.000 description 1
- 235000019645 odor Nutrition 0.000 description 1
- 229940092253 ovalbumin Drugs 0.000 description 1
- 239000002245 particle Substances 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- 239000011148 porous material Substances 0.000 description 1
- 229910052895 riebeckite Inorganic materials 0.000 description 1
- 150000003342 selenium Chemical class 0.000 description 1
- 239000011669 selenium Substances 0.000 description 1
- 229910052711 selenium Inorganic materials 0.000 description 1
- 229960003048 vinblastine Drugs 0.000 description 1
- JXLYSJRDGCGARV-XQKSVPLYSA-N vincaleukoblastine Chemical compound C([C@@H](C[C@]1(C(=O)OC)C=2C(=CC3=C([C@]45[C@H]([C@@]([C@H](OC(C)=O)[C@]6(CC)C=CCN([C@H]56)CC4)(O)C(=O)OC)N3C)C=2)OC)C[C@@](C2)(O)CC)N2CCC2=C1NC1=CC=CC=C21 JXLYSJRDGCGARV-XQKSVPLYSA-N 0.000 description 1
- 229960004528 vincristine Drugs 0.000 description 1
- OGWKCGZFUXNPDA-XQKSVPLYSA-N vincristine Chemical compound C([N@]1C[C@@H](C[C@]2(C(=O)OC)C=3C(=CC4=C([C@]56[C@H]([C@@]([C@H](OC(C)=O)[C@]7(CC)C=CCN([C@H]67)CC5)(O)C(=O)OC)N4C=O)C=3)OC)C[C@@](C1)(O)CC)CC1=C2NC2=CC=CC=C12 OGWKCGZFUXNPDA-XQKSVPLYSA-N 0.000 description 1
- OGWKCGZFUXNPDA-UHFFFAOYSA-N vincristine Natural products C1C(CC)(O)CC(CC2(C(=O)OC)C=3C(=CC4=C(C56C(C(C(OC(C)=O)C7(CC)C=CCN(C67)CC5)(O)C(=O)OC)N4C=O)C=3)OC)CN1CCC1=C2NC2=CC=CC=C12 OGWKCGZFUXNPDA-UHFFFAOYSA-N 0.000 description 1
- 238000009736 wetting Methods 0.000 description 1
Classifications
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- A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
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- A61K2800/412—Microsized, i.e. having sizes between 0.1 and 100 microns
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Definitions
- the present invention deals with a new type of microcapsules for the stabilization of active ingredients, for application in the cosmetic, pharmaceutical or food field, as well as their method of preparation.
- microcapsules microparticles, microspheres, microspheres.
- microspheres a term that can be encompassed within the term microcapsules.
- it will be treated in terms of microcapsules.
- physiological actions For example: cholesterol reducers, relaxants, stimulants, antioxidants, contribution of vitamins, enzymes, etc .
- the use of these substances dissolved freely in the entire product can result in the presence of strange flavors or odors of difficult masking, or instability and degradation of the substance of interest.
- the incorporation or occlusion of these substances inside microcapsules can help solve these problems.
- amylose milliccapsules (WO 89/11269), glycolic lactic acid microcapsules (EP 0202159), gelatin microcapsules and alginic acid (WO 87/01587), ateloglycan microcapsules (WO 92/02254), calcium alginate millicapsules (EP 0391803).
- products of interest in the cosmetic, pharmaceutical and food field can be advantageously encapsulated, inside microcapsules formed by a core of adsorbent material and a coating of polymeric material.
- the products encapsulated in this type of microcapsules have a high degree of stability against degrading agents, although the environment in which the microcapsules are found is aqueous, fatty or emulsion.
- the present invention comprises the preparation and use of microcapsules smaller than 500 ⁇ m formed of a core of adsorbent material in which the active substance or product of interest is incorporated, and all covered by a membrane of polymeric material.
- the incorporation of the active product in the core of the microcapsules is carried out according to the following procedure a) Dissolution of the product to be encapsulated in a suitable solvent (water, ethanol,) b) Incorporation of the product to be encapsulated in the adsorbent material by wetting the absorbent material with the product dissolution obtained in the previous step c) Drying of the core of adsorbent material obtained in the previous step, by conventional processes to remove the solvent. d) Coating of the core of adsorbent material incorporating the product to be encapsulated with a solution of polymeric material.
- a suitable solvent water, ethanol,
- Adsorbent material means all materials of natural or synthetic origin insoluble in water with the ability to incorporate products into the pores of its particles. More specifically, the following products are understood as adsorbent material: - Natural or modified water-insoluble polysaccharides
- Adsorbent inorganic materials more specifically talc, silica, diatomaceous earth, activated carbon and mixtures thereof.
- Polymeric coating material is understood as the following materials:
- Synthetic polymers suitable for use in the cosmetic, pharmaceutical or food field capable of forming films by evaporation of their solutions such as for example polymers of methylacrylic acid (Eudragit L and S), copolymers of dimethylaminoethyl methacrylate (Eudragit E), the copolymers of trimethylammonium ethyl methacrylate (Eudragit RL and RS) and mixtures thereof, polymers and copolymers of lactic and glycolic acids and mixtures thereof.
- Compounds of interest in the field of cosmetics, pharmacy and food that can be incorporated into the preparation object of the present invention include, but are not limited to
- Antibactenan drugs such as gentamicin, - Antiviral agents such as ⁇ fampacin or acyclovir,
- Antifungal compounds such as amphotericin B, miconazole, terconazole, econazole, isoconazole, thioconazole, bifonazole, clotrimazole, ketoconazole, butaconazole, itraconazole, oxyonazole, fenticonazole, nystatin, naftifine, zinoconazole, cytopyroxylamine derivatives, asbestos compounds ,
- Antitumor and antineoplastic compounds such as ad ⁇ amycin, vinblastine, vincristine, mitomycin C, doxorubicin, daunorubicin, methotrexate, cisplatin and others,
- - Peptides such as cyclosponne A, hirudin, somatostatma or thimopentine.
- - Peptide hormones such as human growth hormone, swine growth hormone, bovine growth hormone, human calcitonin, salmon calcitonin, carbocalcitonin and insulin,
- - Hormonal antagonists such as acetylcholine,
- Lipoprotems such as alpha-lipoprotem Immunoglobulms such as IgG Immunomodulators such as interferon or mterleukin
- Vasodilators - Dyes such as Arsenazo III
- Fluorescent compounds such as carboxyfluorescema, - Cellular receptors such as estrogen receptor protein
- Nonsteroidal anti-inflammatory drugs such as indomethacin, ibuprofen, sulindac, piroxicam and naproxen,
- Anti-inflammatories such as dexamethasone, - Antiglaucoma agents such as pilocarpine or timolol, - Midchtatic compounds,
- Vitamins such as alpha-tocopherol
- RNA - Nucleic acids such as thymine
- Polynucleotides such as RNA
- Glycosaminoglycans such as unfractionated hepannas, low molecular weight hepannas, very low molecular weight hepannas, pentasacá do, dermatan sulfate, heparan sulfate, chondro ⁇ t ⁇ n-4-sulfate, chondro ⁇ t ⁇ n-6-sulfate and derivatives,
- - Cardiovascular agents such as beta-blocker alpha-blockers, calcium channel blockers, ACE inhibitors,
- - Prostaglandins such as evening primrose oil, borage oil, castor oil, olive oil, sunflower oil, and the like,
- Animal oils such as cod liver oil fish oils EPA 18 DHA-22 and similar, Silicones for cosmetic use Vegetable extracts such as ginseng, arnica, marigold and similar - Enzymes and coenzymes such as ubidecarenone, and the like;
- Yeasts such as selenium yeast, beer yeast, and the like
- Vitamins and their derivatives such as vitamin E, vitamin E acetate, vitamin A palmitate, and the like
- - Proteins of animal origin such as ovalbumin, gelatin, and the like
- - Proteins of vegetable origin such as gluten, and the like
- microcapsules of the preparation described above can be used in:
- - cosmetic products such as gels, creams, lotions, emulsions, bath gels, shampoos;
- Example 1 Obtaining microcapsules containing docosahexenoic acid (DHA):
- step 1 Repeat step 1 until the whole ethyl cellulose solution is consumed.
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Birds (AREA)
- Engineering & Computer Science (AREA)
- Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Mycology (AREA)
- Pharmacology & Pharmacy (AREA)
- Microbiology (AREA)
- Medicinal Chemistry (AREA)
- Botany (AREA)
- Biotechnology (AREA)
- Emergency Medicine (AREA)
- Polymers & Plastics (AREA)
- Food Science & Technology (AREA)
- Dermatology (AREA)
- Nutrition Science (AREA)
- Cosmetics (AREA)
- Manufacturing Of Micro-Capsules (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- General Preparation And Processing Of Foods (AREA)
- Jellies, Jams, And Syrups (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Microcápsulas para la estabilización de productos cosméticos, farmacéuticos o de alimentación, de tamaño inferior a los 500 νm, constituidas por un núcleo de material adsorbente -polisacárido natural o modificado insoluble en agua o un material inorgánico adsorbente-, en el que están incluidos los ingredientes activos y recubierto por material polimérico -polímero natural o natural modificado o polímero sintético apto para su uso en el campo cosmético, farmacéutico o alimentario, capaz de formar films-. Uso de las microcápsulas, caracterizado por su incorporación en productos cosméticos tales como geles, cremas, lociones, emulsiones, geles de baño, champús, y similares; incorporación en productos farmacéuticos y veterinarios por vía tópica, oral o parenteral; incorporación en productos para la alimentación humana o animal y en productos dietéticos.
Description
MICROCÁPSULAS PARA LA ESTABILIZACIÓN DE PRODUCTOS COSMÉTICOS, FARMACÉUTICOS O DE ALIMENTACIÓN
La presente invención trata de un nuevo tipo de microcápsulas para la estabilización de principios activos, de aplicación en el campo cosmético, farmacéutico o de alimentación, así como su método de preparación.
Según el contexto de la presente invención se puede englobar dentro del termino microcápsulas, los siguientes términos: micropartículas, miliesferas, microesferas. Sin embargo para los fines de la presente invención y para facilitar la comprensión de la misma, se tratará en términos de microcápsulas.
Un punto de creciente interés en el mundo de la cosmética, farmacia y de la alimentación, es la utilización en la formulación de los productos cosméticos, farmacéuticos, alimenticios o dietéticos, de sustancias con diferentes propiedades nutricionales, farmacológicas o con capacidad de provocar acciones fisiológicas (por ejemplo: reductores de colesterol, relajantes, estimulantes, antioxidantes, aporte de vitaminas, de enzimas, etc,...) Sin embargo la utilización de estas sustancias disueltas de forma libre en la totalidad del producto, puede traer como consecuencia la presencia de sabores u olores extraños de difícil enmascaramiento, o la inestabilidad y degradación de la sustancia de interés. La incorporación u oclusión de estas sustancias en el interior de microcápsulas puede ayudar a solucionar estos inconvenientes. Dicha solución ha sido ampliamente utilizada en los campos farmacéutico y cosmético, utilizando milicápsulas de amilosa (WO 89/11269), milicápsulas de láctico glicólico (EP 0202159), microcápsulas de gelatina y ácido algínico (WO
87/01587), microcápsulas de ateloglicanos (WO 92/02254), milicápsulas de alginato calcico (EP 0391803).
Como resultado de las investigaciones, se ha descubierto que se pueden encapsular ventajosamente productos de interés en el campo cosmético, farmacéutico y alimentario, en el interior de microcápsulas formadas por un núcleo de material adsorbente y un recubrimiento de material polimérico. Los productos encapsulados en este tipo de microcápsulas presentan un elevado grado de estabilidad frente a agentes degradantes, pese a que el entorno en que se encuentran las milicápsulas sea acuoso, graso o emulsión.
Es por tanto objeto de la presente invención una preparación cosmética, farmacéutica y alimentaria, para incorporar principios activos de interés en artículos cosméticos, farmacéuticos o alimentarios, caracterizada porque el producto de interés está encapsulado en el interior de microcápsulas compuestas de una matriz o núcleo de material adsorbente y un recubrimiento de material polimérico.
La presente invención comprende la preparación y utilización de microcápsulas de tamaño inferior a 500 μm formadas de un núcleo de material adsorbente en el cual está incorporada la sustancia activa o producto de interés, y todo ello recubierto por una membrana de material polimérico.
La incorporación del producto activo en el núcleo de las microcápsulas se realiza según el siguiente procedimiento a) Disolución del producto a encapsular en un disolvente adecuado (agua, etanol, ) b) Incorporación del producto a encapsular en el material adsorbente mediante humectación del material absorbente con la disolución de producto obtenida en el paso anterior
c) Secado del núcleo de material adsorbente obtenido en el paso anterior, mediante procesos convencionales para eliminar el disolvente. d) Recubrimiento del núcleo de material adsorbente incorporando el producto a encapsular con una disolución de material polimérico.
Se entiende por material adsorbente todos los materiales de origen natural o sintético insolubles en agua con capacidad de incorporar productos en el interior de los poros de sus partículas. Más concretamente se entiende como material adsorbente los siguientes productos: - Los polisacáridos naturales o modificados insolubles en agua
(más concretamente el almidón, la agarosa, la celulosa, celulosas modificadas y sus mezclas)
- Los materiales inorgánicos adsorbentes (más concretamente talco, sílice, tierra de diatomeas, carbón activo y sus mezclas)
Se entiende por material polimérico de recubrimiento los siguientes materiales:
- Los polímeros naturales o naturales modificados, capaces de formar films por evaporación de sus disoluciones, como por ejemplo la etilcelulosa, la hidroxipropilmetil celulosa, el acetoftalato de celulosa, el hidroxipropilmetilftalato de celulosa, y similares;
- Los polímeros sintéticos aptos para su uso en el campo cosmético, farmacéutico o alimentario capaces de formar films por evaporación de sus disoluciones, como por ejemplo los polímeros del ácido metilacrílico (Eudragit L y S), los copolímeros del dimetilaminoetilmetacrilato (Eudragit E), los copolímeros del trimetilamonioetilmetacrilato (Eudragit RL y RS) y sus mezclas, los polímeros y copolímeros de los ácidos láctico y glicólico y sus mezclas.
Los compuestos de interés en el campo de la cosmética, la farmacia y la alimentación que se pueden incorporar en la preparación objeto de la presente invención incluyen, pero no se limitan a
- Drogas antibactenanas como la gentamicina, - Agentes antivirales como la πfampacina o el aciclovir,
- Compuestos antifúngicos como la anfotencina B, miconazol, terconazol, econazol, isoconazol, tioconazol, bifonazol, clotrimazol, ketoconazol, butaconazol, itraconazol, oxiconazol, fenticonazol, nystatin, naftifine, zinoconazol, ciciopiroxolamina, - Compuestos anti-parásitanos como los derivados de antimonio,
- Compuestos antitumorales y antineoplásicos como la adπamicina, la vinblastina, la vincristina, la mitomicina C, la doxorubicina, la daunorubicina, el methotrexate, el cisplatino y otras,
- Antimetabolitos, - Proteínas como la albúmina,
- Toxinas como la toxina diftérica,
- Enzimas como la catalasa,
- Peptidos como la ciclosponna A, la hirudina, la somatostatma o la timopentina, - Hormonas como el estrógeno,
- Hormonas peptídicas como la hormona de crecimiento humano, la hormona de crecimiento porcina, la hormona de crecimiento bovina, la calcitonina humana la calcitonina de salmón, la carbocalcitonina y la insulina,
- Antagonistas hormonales, - Neurotransmisores como la acetilcolma,
- Antagonistas de neurotransmisores
- Glicoprotemas como el acido hialuronico
- Lipoprotemas como la alfa-lipoprotema Inmunoglobulmas como IgG Inmunomoduladores como son el interferon o la mterleukina
Vasodilatadores
- Colorantes como el Arsenazo III,
- Marcadores radiactivos como el 14C,
- Compuestos radio-opacos como el 90Te,
- Compuestos fluorescentes como la carboxifluorescema, - Receptores celulares como la proteína receptora de estrógenos
- Anti-inflamatonos no esteroideos como la indometacina, el ibuprofeno, el sulindac, el piroxicam y el naproxen,
- Anti-inflamatorios como la dexametasona, - Agentes antiglaucoma como la pilocarpina o el timolol, - Compuestos midπáticos,
- Anestésicos locales como la lidocaína,
- Narcóticos como la codeína,
- Vitaminas como el alfa-tocoferol,
- Ácidos nucleicos como la timina, - Polinucleótidos como el RNA,
- Compuestos psicoactivos o ansiolíticos como el diazepam,
- Mono-, di-, y polisacándos como el glicógeno,
- Glicosaminoglicanos como hepannas no fraccionadas, hepannas de bajo peso molecular, hepannas de muy bajo peso molecular, pentasacá do, dermatan sulfato, heparan sulfato, chondroιtιn-4-sulfato, chondroιtιn-6-sulfato y derivados,
- Agentes cardiovasculares como los alfa-bloqueadores beta- bloqueadores, bloqueadores de los canales de calcio, inhibidores de ACE,
- Prostaglandinas, - Aceites vegetales como el aceite de onagra, aceite de borraja aceite de ricino aceite de oliva, aceite de girasol, y similares,
Aceites animales como el aceite de hígado de bacalao aceites de pescado EPA 18 DHA-22 y similares, Siliconas de uso cosmético Extractos vegetales como el de ginseng el de árnica el de caléndula y similares
- Enzimas y coenzimas como la ubidecarenona, y similares;
- Extractos animales;
- Levaduras como la levadura de selenio, la levadura de cerveza, y similares; - Vitaminas y sus derivados como la vitamina E, el acetato de vitamina E, el palmitato de vitamina A, y similares;
- Aminoácidos, como la cisteina, y similares;
- Proteínas de origen animal como la ovoalbúmina, la gelatina, y similares; - Proteínas de origen vegetal como el gluten, y similares;
- Hidrolizados de proteínas animales o vegetales como el hidrolizado de colágeno o el hidrolizado de gluten de trigo, y similares;
- Polisacáridos naturales como el ácido hialurónico, y similares;
- Tocoferoles naturales y sus mezclas, como el Lipafra 2050, y similares;
- Estimulantes como la cafeína, y similares;
- Sales minerales y de oligoelementos como las sales de hierro, sales de Zinc, sales de selenio, y similares;
- Colorantes aceptados en el campo de la cosmética, la dermofarmacia o la alimentación.
Las microcápsulas de la preparación anteriormente descrita, pueden ser utilizadas en:
- productos cosméticos tales como geles, cremas, lociones, emulsiones, geles de baño, champús;
- productos farmacéuticos y veterinarios por vía tópica, oral o parenteral,
- productos para la alimentación humana o animal y en productos dietéticos
A continuación se presentan varios ejemplos de realización practica de la presente invención
Ejemplo 1 : Obtención de microcápsulas conteniendo ácido docosahexenoico (DHA):
En un recipiente adecuado se disuelven 5 g de DHA en 10 mL CH2CI2, de la disolución resultante se adiciona bajo agitación sobre 95 g de almidón de maíz. Posteriormente se eliminan los disolventes, para obtener un polvo de almidón conteniendo DHA.
Se disuelven en 25 mL de etanol 3 g de etilcelulosa, la disolución resultante se adiciona en cinco fracciones diferentes sobre el polvo de almidón conteniendo DHA anteriormente preparado, según los siguientes pasos:
1) Adición de alícuota de disolución de etilcelulosa sobre el polvo de almidón;
2) Agitación durante diez minutos para obtener un sistema homogéneo;
3) Secado del producto resultante;
4) Repetición del paso n°1 hasta consumir toda la disolución de etilcelulosa.
Claims
REIVINDICACIONES
1.- Microcápsulas para la estabilización de productos cosméticos, farmacéuticos o de alimentación, caracterizadas porque están constituidas por un núcleo de material adsorbente, en el que están incluidos los ingredientes activos y recubierto por material polimérico.
2 - Microcápsulas para la estabilización de productos cosméticos, farmacéuticos o de alimentación según la reivindicación 1 , caracterizadas porque son de tamaño inferior a los 500 μm
3.- Microcápsulas para la estabilización de productos cosméticos, farmacéuticos o de alimentación según las reivindicaciones 1 y 2, caracterizadas porque el material adsorbente es un polisacárido natural o modificado insoluble en agua.
4.- Microcápsulas para la estabilización de productos cosméticos, farmacéuticos o de alimentación según las reivindicaciones 1 a 3, caracterizadas porque el material adsorbente es almidón, agarosa, celulosa, celulosas modificadas, y sus mezclas.
5.- Microcápsulas para la estabilización de productos cosméticos, farmacéuticos o de alimentación según las reivindicaciones 1 y 2, caracterizadas porque el material adsorbente es un material inorgánico adsorbente.
6.- Microcápsulas para la estabilización de productos cosméticos, farmacéuticos o de alimentación según las reivindicaciones 1 y 5, caracterizadas porque el material adsorbente es talco, sílice, tierra de diatomeas, carbón activo y sus mezclas 7.- Microcápsulas para la estabilización de productos cosméticos, farmacéuticos o de alimentación según las reivindicaciones 1 a 6, caracterizadas porque el material poliméπco de recubrimiento utilizado es un polímero natural o natural modificado apto para su uso en el campo cosmético, farmacéutico o alimentario, capaz de formar films 8 - Microcápsulas para la estabilización de productos cosméticos, farmacéuticos o de alimentación según las reivindicaciones 1 a 7,
caracterizadas porque el material polimérico de recubrimiento es la etilcelulosa, la hidroxipropilmetilcelulosa, el acetoftalato de celulosa y el hidroxipropilmetil ftalato de celulosa.
9.- Microcápsulas para la estabilización de productos cosméticos, farmacéuticos o de alimentación según las reivindicaciones 1 a 6, caracterizadas porque el material polimérico de recubrimiento utilizado es un polímero sintético apto para su uso en el campo cosmético, farmacéutico o alimentario capaz de formar films por evaporación de sus disoluciones.
10.- Microcápsulas para la estabilización de productos cosméticos, farmacéuticos o de alimentación según las reivindicaciones 1 a 6 y 9, caracterizadas porque el material polimérico de recubrimiento son los polímeros del ácido metilacrílico (Eudragit L y S), los copolímeros del dimetilaminoetilmetacrilato (Eudragit E) los copolímeros del dimetilamonioetílmetacrilato (Eudragit RL y RS) y sus mezclas, los copolímeros de los ácidos glicólíco y láctico y sus mezclas.
11.- Microcápsulas para la estabilización de productos cosméticos, farmacéuticos o de alimentación según las reivindicaciones 1 a 10, caracterizadas porque los ingredientes activos de interés cosmético, farmacéutico y alimentario son: - Drogas antibacterianas como la gentamicina;
- Agentes antivirales como la rifampacina o el aciclovir;
- Compuestos antifúngicos como la anfotericina B, miconazol, terconazol, econazol, isoconazol, tioconazol, bifonazol, clotrimazol, ketoconazol butaconazol, itraconazol, oxiconazol, fenticonazol, nystatin, naftifine, zinoconazol, ciclopiroxolamina;
- Compuestos anti-parásitaπos como los derivados de antimonio;
- Compuestos antitumorales y antineoplásicos como la adπamicma, la vínblastina, la vincπstina, la mitomicina C, la doxorubicma, la daunorubicina, el methotrexate, el cisplatino y otras, - Antimetabolitos
- Proteínas como la albúmina
- Toxinas como la toxina diftérica;
- Enzimas como la catalasa;
- Péptidos como la ciclosporina A, la hirudina, la somatostatina o la timopentina; - Hormonas como el estrógeno;
- Hormonas peptídicas como la hormona de crecimiento humano, la hormona de crecimiento porcina, la hormona de crecimiento bovina, la calcitonina humana, la calcitonina de salmón, la carbocalcitonina y la insulina;
- Antagonistas hormonales; - Neurotransmisores como la acetilcolina;
- Antagonistas de neurotransmisores;
- Glicoproteinas como el ácido hialuróníco;
- Lipoproteínas como la alfa-lipoproteína;
- Inmunoglobulinas como IgG; - Inmunomoduladores como son el interferón o la interleukina;
- Vasodilatadores;
- Colorantes como el Arsenazo III;
- Marcadores radiactivos como el 14C;
- Compuestos radio-opacos como el 90Te; - Compuestos fluorescentes como la carboxifluoresceina;
- Receptores celulares como la proteína receptora de estrógenos.
- Anti-inflamatoríos no esteroideos como la indometacina, el ibuprofeno, el sulindac, el piroxicam y el naproxen;
- Anti-inflamatoríos como la dexametasona; - Agentes antiglaucoma como la pilocarpina o el timolol;
- Compuestos midriáticos;
- Anestésicos locales como la lidocaína;
- Narcóticos como la codeína;
- Vitaminas como el alfa-tocoferol; - Ácidos nucleicos como la timina:
- Polinucleótidos como el RNA;
- Compuestos psicoactivos o ansiolíticos como el diazepam,
- Mono-, di-, y polisacándos como el glicógeno,
- Glicosaminog canos como hepannas no fraccionadas, hepannas de bajo peso molecular, hepaπnas de muy bajo peso molecular, pentasacáπdo, dermatan sulfato, heparan sulfato, chondroιtιn-4-sulfato, chondroιtιn-6-sulfato y derivados;
- Agentes cardiovasculares como los alfa-bloqueadores, beta- bloqueadores, bloqueadores de los canales de calcio, inhibidores de ACE,
- Prostaglandinas; - Aceites vegetales como el aceite de onagra, aceite de borraja, aceite de ricino, aceite de oliva, aceite de girasol, y similares,
- Aceites animales como el aceite de hígado de bacalao, aceites de pescado, EPA-18, DHA-22, y similares,
- Siliconas de uso cosmético, - Extractos vegetales como el de ginseng, el de árnica, el de caléndula, y similares,
- Enzimas y coenzimas como la ubidecarenona, y similares,
- Extractos animales,
- Levaduras como la levadura de setenio, la levadura de cerveza, y similares,
- Vitaminas y sus derivados como la vitamina E, el acetato de vitamina E, el palmitato de vitamina A, y similares,
- Aminoácidos, como la cisterna, y similares,
- Proteínas de origen animal como la ovoalbumma, la gelatina, y similares,
- Proteínas de origen vegetal como el gluten y similares
- Hidro zados de proteínas animales o vegetales como el hidrolizado de colágeno o el hidrolizado de gluten de trigo y similares
- Polisacaπdos naturales como el acido hialuronico y similares Tocoferoles naturales y sus mezclas como el Lipafra 2050, y similares
- Estimulantes como la cafeína, y similares;
- Sales minerales y de oligoelementos como las sales de hierro, sales de Zinc, sales de selenio, y similares;
- Colorantes aceptados en el campo de la cosmética, la dermofarmacia o la alimentación.
12.- Uso de las microcápsulas según las reivindicaciones 1 a 11 , caracterizado por su incorporación en productos cosméticos tales como geles, cremas, lociones, emulsiones, geles de baño, champús, y similares.
13.- Uso de las microcápsulas según las reivindicaciones 1 a 11, caracterizado por su incorporación en productos farmacéuticos y veterinarios por vía tópica, oral o parenteral.
14.- Uso de las microcápsulas según las reivindicaciones 1 a 11, caracterizado por su incorporación en productos para la alimentación humana o animal y en productos dietéticos.
Priority Applications (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| MXPA02003933A MXPA02003933A (es) | 1999-10-21 | 2000-10-19 | Microcapsulas para la estabilizacion de productos cosmeticos, farmaceuticos o de alimentacion. |
| JP2001531360A JP2003535032A (ja) | 1999-10-21 | 2000-10-19 | 化粧品、医薬品、食品の安定化用マイクロカプセル |
| BR0014836-9A BR0014836A (pt) | 1999-10-21 | 2000-10-19 | Microcápsulas para a estabilização de produtos cosméticos, farmacêuticos ou alimentìcios |
| EP00971451A EP1222918A1 (en) | 1999-10-21 | 2000-10-19 | Microcapsules for stabilizing cosmetic, pharmaceutical or food products |
| CA002388166A CA2388166A1 (en) | 1999-10-21 | 2000-10-19 | Microcapsules for stabilizing cosmetic, pharmaceutical or food products |
| AU10305/01A AU1030501A (en) | 1999-10-21 | 2000-10-19 | Microcapsules for stabilizing cosmetic, pharmaceutical or food products |
| US11/265,467 US20060051408A1 (en) | 1999-10-21 | 2005-11-02 | Microcapsules for stabilization of cosmetic, pharmaceutical or food products |
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| ESP9902323 | 1999-10-21 | ||
| ES009902323A ES2162746B1 (es) | 1999-10-21 | 1999-10-21 | Microcapsulas para la estabilizacion de productos cosmeticos, farmaceuticos o de alimentacion. |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| US11/265,467 Division US20060051408A1 (en) | 1999-10-21 | 2005-11-02 | Microcapsules for stabilization of cosmetic, pharmaceutical or food products |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| WO2001028530A1 true WO2001028530A1 (es) | 2001-04-26 |
Family
ID=8310330
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PCT/ES2000/000403 WO2001028530A1 (es) | 1999-10-21 | 2000-10-19 | Microcapsulas para la estabilizacion de productos cosmeticos, farmaceuticos o de alimentacion |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US20060051408A1 (es) |
| EP (1) | EP1222918A1 (es) |
| JP (1) | JP2003535032A (es) |
| AU (1) | AU1030501A (es) |
| BR (1) | BR0014836A (es) |
| CA (1) | CA2388166A1 (es) |
| ES (1) | ES2162746B1 (es) |
| MX (1) | MXPA02003933A (es) |
| WO (1) | WO2001028530A1 (es) |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1284127A1 (de) * | 2001-08-17 | 2003-02-19 | Cognis Iberia, S.L. | Mikrokapseln (XV) |
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| EP0635261A1 (en) * | 1993-07-21 | 1995-01-25 | Lipotec, S.A. | Coated microparticles with improved drug absorption |
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| US5997905A (en) * | 1998-09-04 | 1999-12-07 | Mcneil-Ppc | Preparation of pharmaceutically active particles |
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2000
- 2000-10-19 CA CA002388166A patent/CA2388166A1/en not_active Abandoned
- 2000-10-19 WO PCT/ES2000/000403 patent/WO2001028530A1/es not_active Application Discontinuation
- 2000-10-19 JP JP2001531360A patent/JP2003535032A/ja not_active Withdrawn
- 2000-10-19 MX MXPA02003933A patent/MXPA02003933A/es unknown
- 2000-10-19 EP EP00971451A patent/EP1222918A1/en not_active Withdrawn
- 2000-10-19 BR BR0014836-9A patent/BR0014836A/pt not_active IP Right Cessation
- 2000-10-19 AU AU10305/01A patent/AU1030501A/en not_active Abandoned
-
2005
- 2005-11-02 US US11/265,467 patent/US20060051408A1/en not_active Abandoned
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| WO1987001587A1 (en) * | 1985-09-17 | 1987-03-26 | Biocompatibles Limited | Microcapsules |
| EP0635261A1 (en) * | 1993-07-21 | 1995-01-25 | Lipotec, S.A. | Coated microparticles with improved drug absorption |
| US5792477A (en) * | 1996-05-07 | 1998-08-11 | Alkermes Controlled Therapeutics, Inc. Ii | Preparation of extended shelf-life biodegradable, biocompatible microparticles containing a biologically active agent |
| WO1998014179A1 (en) * | 1996-10-01 | 1998-04-09 | Cima Labs Inc. | Taste-masked microcapsule compositions and methods of manufacture |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1284127A1 (de) * | 2001-08-17 | 2003-02-19 | Cognis Iberia, S.L. | Mikrokapseln (XV) |
| WO2003015721A1 (de) * | 2001-08-17 | 2003-02-27 | Cognis Iberia, S.L. | Mikrokapseln (xv) |
Also Published As
| Publication number | Publication date |
|---|---|
| CA2388166A1 (en) | 2001-04-26 |
| ES2162746A1 (es) | 2002-01-01 |
| US20060051408A1 (en) | 2006-03-09 |
| ES2162746B1 (es) | 2003-02-16 |
| BR0014836A (pt) | 2002-06-11 |
| MXPA02003933A (es) | 2003-09-22 |
| EP1222918A1 (en) | 2002-07-17 |
| JP2003535032A (ja) | 2003-11-25 |
| AU1030501A (en) | 2001-04-30 |
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