Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
  • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
  • A61K31/22—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
• • A—HUMAN NECESSITIES
  • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
  • A23L—FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF
  • A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
  • A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
  • A23L33/115—Fatty acids or derivatives thereof; Fats or oils
• • A—HUMAN NECESSITIES
  • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
  • A23L—FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF
  • A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
  • A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
  • A23L33/15—Vitamins
• • A—HUMAN NECESSITIES
  • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
  • A23L—FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF
  • A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
  • A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
  • A23L33/16—Inorganic salts, minerals or trace elements
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/13—Amines
  • A61K31/14—Quaternary ammonium compounds, e.g. edrophonium, choline
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
  • A61K31/19—Carboxylic acids, e.g. valproic acid
  • A61K31/20—Carboxylic acids, e.g. valproic acid having a carboxyl group bound to a chain of seven or more carbon atoms, e.g. stearic, palmitic, arachidic acids
  • A61K31/202—Carboxylic acids, e.g. valproic acid having a carboxyl group bound to a chain of seven or more carbon atoms, e.g. stearic, palmitic, arachidic acids having three or more double bonds, e.g. linolenic
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
  • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
  • A61K31/22—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
  • A61K31/23—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
  • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P25/00—Drugs for disorders of the nervous system
  • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• • 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
  • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
• • 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
  • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
  • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction

Definitions

• the present invention relates to a mixture, and a composition comprising said mixture, comprising or, alternatively, consisting of: medium-chain triglycerides MCT, omega-3 and choline.
• the present invention relates to a mixture, and a composition comprising said mixture, comprising or, alternatively, consisting of: medium-chain triglycerides MCT, omega-3 and choline for use in a method of treatment, preferably in a preventive method of treatment, of a subjective memory disorder, a mild cognitive decline (MCI), a dementia or an Alzheimer's disease.
• MCI mild cognitive decline
• a first disorder is a subjective memory disorder that results in a deterioration of one's cognitive abilities, in the absence of neuropsychological deficits.
• the most common symptom is a decline in thinking and/or memory to a level that creates a discomfort and relative distress.
• MCI Mild Cognitive Impairment
• Alzheimer's disease is the most common form of dementia characterized by the presence of amyloid plaques in brain tissue and a subsequent loss of cognitive function.
• the symptoms of Alzheimer's disease depend on the degree of cognitive decline. However, initially the patient presents with short-term memory loss with long-term memory episodes.
• the way to maintain healthy mitochondria is also the one that prevents cancer and heart disease or a number of other age-related diseases: exercise and a diet rich in antioxidants.
• Memory consolidation is modulated by endogenous adenosine triphosphate (ATP) acting on purinergic receptors in the hippocampus.
• ATP adenosine triphosphate
• neurons and astrocytes release ATP, which acts on purinergic P2 receptors.
• purines in enhancing mammalian hippocampal activity (LTP) in learning and memory processes.
• a mixture and a composition comprising said mixture, for use in a method of treatment of 1) subjective memory disorder, 2) mild cognitive decline (MCI), 3) dementia, or 4) Alzheimer's disease, having the characteristics as set forth in the united claims.
• composition and “formulation” may be used as terms having the same meaning, and the phrase “composition/formulation of the present invention” also includes foods for special medical purposes (FSMPs) according to Regulation (EU) 609/2013 and regulated by Commission Regulation (EU) 2016/128, and medical devices according to Regulation (EU) 745/2017.
• FSMPs special medical purposes
• EU Regulation
• EU Commission Regulation
• EU Commission Regulation
• the mixture M of the present invention comprises or, alternatively, consists of: I) medium-chain triglycerides- MCT, ii) omega-3 powder, titrated in DHA-docosahexaenoic acid, from about 10% to 15%, and titrated in EPA-eicosapentaenoic acid, from about 1% to about 3%, microencapsulated from fish oil; and ill) a choline bitartrate.
• medium-chain triglycerides MTC may, preferably, be in the form of a dry extract titrated, for example, at 50%, or 60%, or 70%, or 80%.
• choline may be present, preferably, in the form of choline bitartrate, for example, choline bitartrate at 30%, or 35%, or 40%, or 45%, or 50%, or 55%, or 60%, or 70%.
• the mixture M comprising or, alternatively, consisting of: I) medium-chain triglycerides-MCT, ii) omega-3 powder, titrated in DHA -docosahexaenoic acid, from about 10% to 15%, and in to EPA -eicosapentaenoic acid, from about 1% to about 3%, microencapsulated from fish oil, and ill) a choline bitartrate, as an example of a choline source, comprises, in addition, a zinc (II) source, preferably a zinc gluconate having, for example, a CAS No.
• II medium-chain triglycerides-MCT
• omega-3 powder titrated in DHA -docosahexaenoic acid, from about 10% to 15%, and in to EPA -eicosapentaenoic acid, from about 1% to about 3%, microencapsulated from fish oil, and ill) a choline bitartrate
• an iron (III) source preferably an iron pyrophosphate having, for example, a CAS No. 10058-44-3.
• Said zinc gluconate may, for example, have a zinc (II) content from 10% to 15%, e.g., about 13%, while said iron pyrophosphate may, for example, have an iron (III) content from 80 mg/g to 90 mg/g, e.g., 85 mg/g, and may be emulsified with lecithin, maltodextrin, and sodium chloride, and be in micronized form. This mixture is referred to as M*.
• said medium-chain triglycerides-MCT are obtained from a plant of the Arecaceae family such as, for example, from Elaeis guineensis Jacq. also known as the oil palm.
• said MCT are supported in a carrier that may contain, for example, a sodium caseinate, in an amount by weight from about 20% to about 30%, a glycerol acid ester, in an amount by weight from about 2% to about 10%, and a silicon dioxide, in an amount by weight less than about 2%.
• a composition of said medium-chain triglycerides may contain MCT in an amount by weight from about 70% to about 90%; a caprylic acid in an amount by weight from about 50% to about 70%; and a capric acid in an amount by weight from about 35% to about 45%; preferably said composition may have, for example, an acidity value of less than 1 mg KOH/g, a peroxide index of less than 0.13 mEq O2/Kg, a solubility in water, and a density from about 0.35 g/ml to about 0.55 g/ml; preferably said composition may have a particle size of the type 90% at 60 mesh.
• said microencapsulated omega-3 powder from fish oil is titrated at about 12% in DHA and about 3% in EPA, more preferably it is tuna oil in the presence of glucose syrup, milk protein, sodium ascorbate (E301), sodium citrate (E331) and mono and diglycerides of fatty acids (E471).
• said microencapsulated omega-3 powder from fish oil may have, for example, a pH value in the range from 7.3 to 8.3; a peroxide value of less than about 2 mEq/Kg; and a solubility index greater than about 99%; more preferably, said microencapsulated omega-3 powder from fish oil may have, for example, a protein content in an amount by weight from about 6.5 to about 9 g/100 g; a fat content in an amount by weight from about 47% to about 54% g/100 g; a trans acids content in an amount by weight less than about 0.5 g/100 g TG; a DHA content in an amount by weight greater than about 120 mg/g TG; and an EPA content in an amount by weight less than about 30 mg/ g TG.
• Said omega-3 fatty acids are present in the mixture M in a DHA:EPA ratio of about 4:1.
• said choline is present in the mixture preferably in the form of choline bitartrate having, e.g., a CAS No. 87-67-2, and is presented as a white crystalline powder.
• said mixture M comprises, in addition to i), ii) and iii), also iv) at least one vitamin of the B group selected from the group comprising or, alternatively, consisting of:
• vitamin B3 preferably a vitamin B3 (or vitamin PP or niacin) in the form of nicotinamide having, for example, a CAS No. 98-92-0;
• a vitamin B5 preferably a vitamin B5 in the form of D-calcium pantotheate having, for example, a CAS No. 137-08-6;
• vitamin B6 preferably a vitamin B6 in the form of pyridoxine hydrochloride having, for example, a CAS No. 58-56-0;
• vitamin B9 preferably a vitamin B9 in the form of folic acid having, for example, a CAS No. 59-30-3;
• said mixture M also comprises, in addition to i), ii) and iii), also said vitamin B5 and said vitamin B6, or said vitamins B5, B6, B9 and B12 to give a mixture M1.
• said mixture M or M1 comprises, in addition to i), ii), iii) and iv), also v) at least one vitamin of the C group, preferably a vitamin C in the form of (+) ascorbic acid having, for example, CAS No. 50-81-7, to give a mixture M2.
• said mixture M or M* or M1 or M2 or M3 comprises, in addition to i), ii), iii), iv), v) and iv), also vii) at least one vitamin of the E group, preferably a vitamin E in the form of DL-a-tocopheryl acetate having, for
• said mixture M or M* or M1 or M2 or M3 or M4 comprises, in addition to i), ii), iii), iv), v), vi), and vii), also viii) at least one vitamin of the K group, preferably a vitamin K1 having, for example, a CAS No. 81818-54-4, to give a mixture M5.
• said mixture M or M* or M1 or M2 or M3 or M4 or M5 or M6 comprises, in addition to i), ii), iii), iv), v), vi), vii), viii), ix), and x), also xi) a source of potassium (I), preferably a potassium citrate having, for example, a No. CAS 6100-5-6; said potassium citrate may, for example, be present in the form of tripotassium citrate monohydrate, and xii) a source of calcium (II) and phosphorus, preferably a tricalcium phosphate having, for example, a CAS No. 12167-74-7, to give a mixture M7.
• a source of potassium (I) preferably a potassium citrate having, for example, a No. CAS 6100-5-6; said potassium citrate may, for example, be present in the form of tripotassium citrate monohydrate, and xii) a source of calcium (II) and
• said mixture M or M* or M1 or M2 or M3 or M4 or M5 or M6 or M7 comprises, in addition to i), ii), iii), iv), v), vi), vii), viii), ix), x), and xi), also xii) a source of magnesium (II), preferably a magnesium citrate having, for example, a No. CAS 153531-96-5; said magnesium citrate may, for example, have a magnesium (II) content from 12% to 18%, e.g., about 15% on a dry base, to give a mixture M8.
• a source of magnesium (II) preferably a magnesium citrate having, for example, a No. CAS 153531-96-5; said magnesium citrate may, for example, have a magnesium (II) content from 12% to 18%, e.g., about 15% on a dry base, to give a mixture M8.
• a source of selenium preferably a L-seleniomethionine having, for example, a selenium content from 0.5% to 2%, e.g., 1.5%; and/or
• a solid composition comprising a solid mixture selected from the above-described mixtures M or M* or M1 or M2 or M3 or M4 or M5 or M6 or M7 or M8 or M9 and, optionally,
• ISA/EP at least one additive, excipient, carrier or a flavoring substance, synthetic or natural, of food or pharmaceutical grade, to give a composition CM or CM* or CM1 or CM2 or CM3 or CM4 or CM5 or CM6 or CM7 or CM8.
• said solid compositions are in the form of microgranules, granules, or powders.
• a maltodextrin preferably a maltodextrin having, for example, a CAS No. 9050-36-6;
• a silicon dioxide preferably a silicon dioxide having, for example, a CAS No. 112926-00-8;
• citric acid preferably citric acid having, for example, CAS No. 77-92-9.
• said compositions are useful in a preventive treatment in which said composition is preferably administered in a daily dose ranging from 10 g to 30 g, more preferably in a 20 g dose in a single-dose format as a granulate for oral use.
• said additive or excipient or carrier or flavor of food or pharmaceutical grade is selected from the group comprising or, alternatively, consisting of:
• a maltodextrin preferably a maltodextrin having, for example, a CAS No. 9050-36-6;
• vanilla flavor preferably a powder vanilla flavor
• sucralose preferably a sucralose having, for example, a CAS No. 56048-13-2;
• a silicon dioxide preferably a silicon dioxide having, for example, a CAS No. 112926-00-8;
• citric acid preferably citric acid having, for example, a CAS No. 77-92-9.
• the composition comprises said mixture in an amount by weight from 60% to 90%, preferably from 70% to 80%, and said additive or excipient or carrier in an amount by weight from 40% to 10%, preferably from 30% to 20%, with respect to the total weight of the composition.
• Both the mixture and the composition, that comprises said mixture are prepared using equipment and techniques known to the person skilled in the art belonging to the field of pharmaceutical, nutraceutical and dietary supplement preparations.
• the mixture may comprise:
• omega-3 DHA:EPA 4:1 of which 3.9 g of omega-3;
• the mixture comprises or, alternatively, consists of i) medium-chain triglycerides- MCT; ii) omega-3 powder, titrated in DHA-docosahexaenoic acid, from about 10% to 15%, and titrated in EPA-eicosapentaenoic acid, from about 1% to about 3%, microencapsulated from fish oil; and ill) a choline bitartrate.
• the study was set up to provide for the evaluation of the impact of the mixture and its components on cellular energy metabolism. It is, therefore, an in vitro study of evaluation of the synergistic effect among the mixture components by analyzing cellular energy metabolism in the presence of the individual components and the complete mixture.
• the formulations under study are: - control; - MTCs; - Omega-3 DHA:EPA; - choline (e.g. as choline bitartrate; - Mixture of: MTCs, Omega-3 DHA:EPA, choline (e.g. as choline bitartrate).
• the SH-SY5Y neuroblastoma cell model was used for the study.
• the activity includes:
• Dispersion/solubilization of samples in the most suitable medium to avoid precipitation or floating of substances during cells processing e.g. DMSO
• a dose-response at increasing concentrations of the components and mixture was performed in order to identify the maximum nontoxic concentration for each component and mixture. Based on the maximum nontoxic concentration value identified for each element, having to evaluate the synergistic effect, a common concentration was defined for all components and mixture that was used for the subsequent evaluation of the impact on cellular energy metabolism;

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