Patent: Microparticles for Oral Delivery US20080044481A1

Patent DrawingPatent DrawingPatent DrawingPatent DrawingPatent DrawingPatent Drawing
ZUSAMMENFASSUNG
The invention provides microbeads containing oil-associated biologically active compounds and methods for their manufacture and use. The microbeads consist of a soluble complex of non-digestible polymer and emulsifier with oil-associated biologically active compounds embedded in a matrix of digestible polymer. The disclosed microbead complex protects the biologically active compounds, such as vitamins, fish oil and carotenoids, from oxidation, taste and odor degradation. The disclosed microbeads also provide protection from the stomach digestive distraction, and allows for the delivery of the biologically active compounds in the intestine.
Veröffentlichungsnummer US20080044481 A1
Publikationstyp Anmeldung
Anmeldenummer US 11/597,826
PCT-Nummer PCT/US2005/018797
Veröffentlichungsdatum 21. Febr. 2008
Eingetragen 27. Mai 2005
Prioritätsdatum 27. Mai 2004
Auch veröffentlicht unter EP1750674A2EP1750674A4WO2005115341A2WO2005115341A3
Erfinder Mordechai Harel
Ursprünglich Bevollmächtigter Mordechai Harel
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Externe Links: USPTOUSPTO-ZuordnungEspacenet
    DESCRIPTION

  • [0051]
    The invention relates to particles for administering a composition to an animal, including administration to a selected compartment (e.g., stomach, small intestine, or large intestine) of the animal. The particles are of two overlapping and related types, referred to herein as microparticles and microbeads. For the sake of convenience, these two types of particles are described in separate sections herein, after which are discussed the identities and properties of ingredients useful in one, the other, or both, as well as uses for both types of particles.
  • [0052]
    Microparticles
  • [0053]
    The microparticles described herein comprise a matrix that includes at least one substantially indigestible polymer. The composition to be administered to the animal is suspended in the substantially indigestible polymer matrix. A lipid that is dissoluble in the desired compartment of the animal is also suspended in the matrix.
  • [0054]
    Each of the lipid and the composition can be separately enclosed or dispersed in the matrix. Preferably, however, the lipid and the composition are combined prior to suspension in the matrix. If the composition (e.g., a vitamin) is soluble in the lipid, then the composition can be simply dissolved in the lipid. If the composition and the lipid are immiscible, then they can be separately suspended in the matrix, suspended as immiscible droplets, or suspended in the form of an emulsion. If desired, the matrix, the lipid, and the composition can be formed into a single emulsion in which the matrix is present in the continuous phase. In microparticles that include an emulsified component, an emulsifier can be used to facilitate formation or stability of the emulsion.
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  • [0056]
    The microparticles can be as large as 5 millimeters along their largest dimension. There is no lower limit on the size of the microparticles, but microparticles having a maximum dimension not smaller than 10 micrometers are preferred. The maximum desired size of a microparticle can also depend on the use to which it is to be put. For example, very small animals (e.g., rotifers) are not able to consume particles greater than the size of their mouths. Furthermore, when the microparticles are to be used as components of a food product, it can be desirable that the microparticles are not visible. In each of these instances, appropriate sizes for particles would be apparent to a skilled artisan in the corresponding field.
  • [0057]
    In one embodiment, a composition including a bioactive substance (e.g., a nutraceutical, pharmaceutical, vaccine, probiotic, hormone, vitamin, or protein ingredient) is embedded in a solid or waxy lipid matrix. The matrix is immobilized in an substantially indigestible polymer matrix to form a microparticle that releases the bioactive compound in the digestive tract of an animal. Such a microparticle is useful for protecting bioactive materials from humidity and oxidation damage during storage, for decreasing degradation of the bioactive material contained therein by gastric conditions, and for limiting release of the bioactive material from the microparticle when it contacts water below the melting point of the solid lipid. Microparticles are also useful for improved the heat and shear stability of the a composition contained therein during storage and processing (e.g., during preparation of food products into which the microparticles are incorporated).
  • [0058]
    In one embodiment, the invention relates to a method of preparing a composition containing unsaturated oils, such as fish oil, in a complex effective to stabilize the unsaturated oils. The composition comprises the oil mixed with a lipid that is solid or waxy at the temperature at which the microparticles are normally stored, but which is liquid at the body temperature of an animal. The mixture can be embedded in, suspended in, or mixed with a substantially indigestible (e.g., amylose) matrix. Upon delivery to the stomach or intestine of an animal, the lipid becomes liquid, permiting egress of the oil from the microparticles. Mechanical digestive activity, pH, temperature, enzymatic activity, presence of digestive juices, or some combination of these can further enhance release of the oil from the microparticles. Other (e.g., hydrophilic) bioactive agents can be used in place of the oil and can be similarly delivered.
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  • [0084]
    Bioactive Compositions
  • [0085]
    The particles described herein can be used to deliver substantially any chemical species, combination of chemicals, cell, or other piece of matter that can be incorporated into the particle to a component of an animal. All such items are referred to herein as “bioactive” compositions, regardless of what the utility of the composition is. Bioactive compositions include, for example, pharmaceutical compositions or compounds, nutraceutical compositions or compounds, nutritional components, probiotic bacteria, bacteriophages, viruses, flavorants, fragrances, detergents or other surface-active compositions.
  • [0086]
    Examples of these agents include antibiotics, analgesics, vaccines, anti-inflammatory agents, antidepressants, anti-viral agents, anti-tumor agents, enzyme inhibitors, formulations containing zidovudine, proteins or peptides (such as vaccines, antibodies, antimicrobial peptides), enzymes, (e.g., amylases, proteases, lipases, pectinases, cellulases, hemicellulases, pentosanases, xylanases, and phytases), liposomes, aromatic nitro and nitroso compounds and their metabolites, HIV protease inhibitors, viruses, and steroids, hormones or other growth stimulating agents, pesticides, herbicides, germicides, biocides, algicides, rodenticides, fungicides, insecticides, antioxidants, plant and animal growth promoters, plant and animal growth inhibitors, preservatives, nutraceuticals, disinfectants, sterilization agents, catalysts, chemical reactants, fermentation agents, foods, animal feeds, food or animal feed supplements, nutrients, flavors, colors, dyes, cosmetics, drugs, vitamins, sex sterilants, fertility inhibitors, fertility promoters, air purifiers, microorganism attenuators, nucleic acids (e.g., RNA, DNA, PNA, vectors, plasmids, ribozymes, aptamers, dendrimers, and the like), antioxidants, phytochemicals, hormones, vitamins (such as vitamins A, B1, B2, B6, B12; C, D, E, and K, pantothenate, and folic acid), pro-vitamins, carotenoids, minerals (such as calcium, selenium, magnesium salts, available iron, and iron salts), microorganisms (such as bacteria, such as probiotics, lactobacilli, fungi, and yeast), prebiotics, trace elements, essential and/or highly unsaturated fatty acids (such as omega-3 fatty acids, and mid-chain triglycerides), nutritional supplements, enzymes (such as amylases, proteases, lipases, pectinases, cellulases, hemicellulases, pentosanases, xylanases, and phytases), pigments, amino acids, agriculturally useful compositions to either prevent infestation (such as herbicides, pesticides, insecticides, rodenticides, fungicides, mixtures thereof) or to promote growth (such as hormones, fertilizers, or other growth stimulating agents), flavorants, and fragrances.
  • [0087]
    Oil-associated bioactive compounds and/or other bioactive compounds and microbes are added and mixed thoroughly into the complex solution in a final concentration of between about 0.1% to about 80% by weight of the microbead.
  • [0088]
    The particles described herein can be used to deliver organism-based bioactive agents including bacteria (e.g., Bacillus spp., B. licheniformis, B. subtilis, Lactobacillus spp., L. bulgaricus, L. helveticus, L. plantarum, L. paracasei, L. casei, L. rhamnosus, L. lactis, Alteromonas spp., A. media, Camobacterium spp., C. divergens, Vibrio spp., V. alginolyticus, Pseudomonas spp., P. fluorescens, Streptococcus spp., S. lactis, S. thermophilus, Pseudoalteromonas spp., P. undina), yeast (e.g., Saccharomyces spp., S. cerevisiae, S. exiguous, Phaffia spp., P. rhodozoma, Pichia spp., P. pastoris, Kluyveromyces spp., K. aestuarii, K. marxianus, and K. yarrowii., Schizochitrium, Ulkenia, Crypthecodinium, Nannochloropsis, nannochloris, Hematococcus, Pfaffia, Isochrysis and Chlorella) and viruses (e.g., live viruses, heat killed viruses, attenuated viruses, bacteriophages).
  • [0089]
    The particles described herein can also be used to deliver antimicrobial-based bioactive agents including, but not limited to gentamicin, tetracycline, oxytetracycline, doxycycline, ampicillin, ticarcillin, cephalothin, cephaloridine, cefotiam, cefsulodin, cefmenoxime, cefmetazole, cefazolin, cefotaxime, cefoperazone, ceftizoxime, moxolactam, latamoxef, thienamycin, sulfazecin, and azthreonam.
  • [0090]
    The particles described herein can be used to deliver hormone-based bioactive proteins including, but not limited to somatostatin, somatostatin derivatives, growth hormones, prolactin, adrenocorticotropic hormone, melanocyte stimulating hormone, thyroid hormone releasing hormone (TRH), TRH salts, TRH derivatives, thyroid stimulating hormone, leutinizing hormone, oxytocin, calcitonin, gastrin, secretin, pancreaozymin, choecystokinin, interleukins, thymopoeitin, thymosin, thymostimulin, thymic factors, bombesin, neurostensin, lysozyme, protein synthesis stimulating peptides, vasoactive intestinal polypeptide, growth hormone releasing factor, and somatocrinin.

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Advanced BioNutrition Corp

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