• 专利附录
  • 专利说明
  • 权利要求
  • 类似技术
  • 同族专利
  • 引用文献
  • 法律状态
  • 优先权
    • 专利摘要:
    The invention relates to compositions comprising the components calcium salt of L-5-methyl-tetrahydrofolate, N-acetylcysteine, L-selenomethionine, cholecalciferol, calcium D-panthothenate, methylcobalamin, pyridoxal-5'-phosphate, riboflavin, thiamine mononitrate , Zeaxanthin, lutein, D-α-tocopherol, calcium ascorbate, copper gluconate and zinc acetate.
    公开号:CH714164A2
    申请号:CH01057/18
    申请日:2018-09-05
    公开日:2019-03-15
    发明作者:Ulmann Martin；Wiesler Gerd
    申请人:Aprofol Ag；
    IPC主号:
    专利说明:

    Description The present invention is in the field of human nutrition and dietary supplementation and relates to compositions containing folic acid and 5-methyltetrahydrofolic acid and / or its polyglutamates.
    Folic acid is a widespread growth factor with vitamin character. Folic acid itself is absent in plant and animal foods.
    The naturally occurring forms of folic acid are reduced folates in the form of poly- and monoglutamates. The de novo synthesis of these folates is only possible for microorganisms and plants. Before absorption, the polyglutamates are degraded by the folate conjugase of the brush border cells of the small intestine to monoglutamates. Only the monoglutamates can be taken up by the intestinal mucosa in an active transport process. The biologically inactive folic acid is reduced by the enzyme dihydrofolate reductase to 7,8-dihydrofolic acid and by dihydrofolate reductase to 5,6,7,8-tetrahydrofolic acid (THF). THF is the actually physiologically active form of folic acid: THF is a transport metabolite for one-carbon bodies, their transfer via 5-methyl-tetrahydrofolate, 5,10-methylene-tetrahydrofolate, 5-formyl-tetrahydrofolate (folinic acid), 5 Formimino-tetrahydrofolate, 10-formyl-tetrahydrofolate or 5,10-methenyl-tetrahydrofolate proceeds. The C1 building blocks are u.a. for the biosynthesis of the purine nucleotides and deoxythymidine 5'-monophosphate, that is, as precursors of deoxyribonucleic acids (DNA) needed.
    Folate deficiency may be due to lack of nutritional intake, increased need (eg during pregnancy and lactation, alcohol abuse), lack of absorption from the diet (eg as a result of celiac disease or sprue), by simultaneous intake of antimetabolites (eg methotrexate or Aminopterin, which are used as competitive inhibitors of dihydrofolate reductase in the context of chemotherapy, or sulfonamides which inhibit folate biosynthesis as antimetabolites of 4-aminobenzoic acid) or by genetically induced dysfunction in one of the enzymes of folate metabolism, for example methylenetetrahydrofolate reductase. Other reasons for folate deficiency include age-related lower intestinal absorption, malabsorption syndrome, or microcirculation flow disturbances and associated lower uptake. The consequences of folate deficiency are disorders in amino acid and protein metabolism and in cell division (e.g., in nucleic acid metabolism). This manifests itself primarily in rapidly proliferating tissues, such as bone marrow cells, and can lead to megaloblastic anemia and death by thrombocytopenia. Folate deficiency is further associated with disorders in the growth and mental development of newborns. Epidemiological studies indicate that an increased incidence of neural tube defects (NTDs) in neonates, including spina bifida and adnexals, correlates with low folate status of the mothers. With supplements of pregnant women from 0.4 mg to 4 mg folic acid / day, the frequency of malformations in newborns could be significantly reduced.
    Also clinically proven is the effect of folic acid for lowering the homocysteine level (risk factor for cardiovascular diseases) in the blood. The intake of 400 pg folic acid per day is necessary to positively influence the level of homocysteine in the blood. The folates that are found in food, mainly in leafy vegetables and cereals, as well as in liver, are sensitive to heat and light, so even in healthy people adequate food supply can not always be guaranteed. A major cause of low folate status in humans is mainly seen in insufficient dietary intake.
    For these reasons, an increase in the dietary folate supply by means of the accumulation of food with folic acid or the oral intake of folic acid, for. recommended by the US Food and Drug Administration (FDA). The German Society for Nutrition (DGE) recommends a daily intake of 400 pg folic acid per day for healthy adults. For pregnant and lactating women (600 pg / day), correspondingly higher recommendations apply (reference values for nutrient intake, 1st edition, review Braus Verlag, Frankfurt am Main, 2000, published by the German Nutrition Society, p. 117). Folic acid is the oxidized form of folates in the form of monoglutamate.
    The body metabolizes only a small amount of folic acid (200 pg / day) while the excess enters the bloodstream as non-metabolized folic acid. Synthetic folic acid has a high affinity to the folate receptors but can not be absorbed into the cells. Due to the lower receptor affinity of the reduced folates, folic acid blocks the uptake of the active folates (Seihub et al., Biochimie, 126, (2016), 71).
    The object of the present invention is to provide compositions that ensure adequate folate supply in humans and animals. These compositions should ensure bioavailability of the folates in all parts of the population. These compositions should be chemically stable and usable independently of the formulation in foods, animal nutrition and dietary supplements for humans. It was of particular interest to provide preparations which guarantee sufficient folate supply in people with the most diverse disorders of folate metabolism (including genetic defects or resorption disorders). In addition, it would be desirable to obtain compositions which have a synergistic effect in terms of their efficacy (increasing blood folate status, preventing folate deficiency, etc.) as compared to the prior art compositions.
    权利要求:
    Claims (8)
    [1]
    claims
    A composition comprising calcium salt of L-5-methyl-tetrahydrofolate in an amount of 0.2 mg to 1.5 mg, N-acetylcysteine or its salt in an amount of 40 mg to 250 mg, L-selenomethionine in one Amount of 0.005 mg to 0.04 mg, cholecalciferol in an amount of 0.009 mg to 0.06 mg, calcium D-panthothenate in an amount of 1 mg to 8 mg, methylcobalamin in an amount of 0.003 mg to 0.8 mg , Pyridoxal-5'-phosphate in an amount of 1 mg to 4 mg, riboflavin in an amount of 2 mg to 14 mg, thiamine mononitrate in an amount of 0.2 mg to 2 mg, zeaxanthin in an amount of 1 mg to 3 mg, lutein in an amount of 4 mg to 15 mg, Da-to-copherol in an amount of 1 mg to 8 mg, calcium ascorbate in an amount of 20 mg to 65 mg, copper gluconate in an amount of 0.1 to 1 mg and zinc acetate in an amount of 7 mg to 33 mg.
    [2]
    2. The composition of claim 1 containing calcium salt of L-5-methyl-tetrahydrofolate in an amount of 0.5 mg to 1.1 mg, N-acetylcysteine in an amount of 90 mg to 190 mg, L-selenomethionine in one Amount of 0.01 mg to 0.03 mg, cholecalciferol in an amount of 0.015 mg to 0.045 mg, calcium D-panthothenate in an amount of 2 mg to 6 mg, methylcobalamin in an amount of 0.005 mg to 0.6 mg , Pyridoxal 5'-phosphate in an amount of 1.6 mg to 3.5 mg, riboflavin in an amount of 3.7 mg to 10.5 mg, thiamine mononitrate in an amount of 0.45 mg to 1, 6 mg, zeaxanthin in an amount of 1.9 mg to 2.1 mg, lutein in an amount of 9 mg to 11 mg, da-tocopherol in an amount of 2 mg to 6 mg, calcium ascorbate in an amount of 35 mg to 50 mg, copper gluconate in an amount of 0.2 mg to 0.8 mg and zinc acetate in an amount of 11 mg to 26 mg.
    [3]
    3. A composition according to claim 1 or 2 comprising calcium salt of L-5-methyl-tetrahydrofolate in an amount of 0.9 mg, N-acetylcysteine in an amount of 180 mg, L-selenomethionine in an amount of 0.02 mg , Cholecalciferol in an amount of 0.0375 mg, calcium D-panthothenate in an amount of 5 mg, methylcobalamin 0.5 mg, pyridoxal-5'-phosphate in an amount of 3 mg, riboflavin in an amount of 10 mg, Thiamine mononitrate in an amount of 1.5 mg, zeaxanthin in an amount of 2 mg, lutein in an amount of 10 mg, da-tocopherol in an amount of 5 mg, calcium ascorbate in an amount of 45 mg, copper Gluconate in an amount of 0.667 mg and zinc acetate in an amount of 25 mg.
    [4]
    4. The composition of claim 1 or 2 comprising calcium salt of L-5-methyl-tetrahydrofolate in an amount of 0.6 mg, N-acetylcysteine in an amount of 100 mg, L-selenomethionine in an amount of 0.02 mg , Cholecalciferol in an amount of 0.02 mg, calcium D-panthothenate in an amount of 3 mg, methylcobalamin 0.009 mg, pyridoxal 5'-phosphate in an amount of 2.1 mg, riboflavin in an amount of 4.2 mg, thiamine mononitrate in an amount of 0.55 mg, zeaxanthin in an amount of 2 mg, lutein in an amount of 10 mg, da-tocopherol in an amount of 3 mg, calcium ascorbate in an amount of 40 mg, Copper gluconate in an amount of 0.3 mg and zinc acetate in an amount of 12.5 mg.
    [5]
    5. Composition according to one of the preceding claims, characterized in that the composition one or more, preferably all adjuvants selected from the group consisting of soybean oil, refined, type NGM, soybean oil, partially hydrogenated 31 ° C-37 ° C, soybean oil, partially hydrogenated 36 ° C-42 ° C, soy lecithin and beeswax.
    [6]
    6. The composition according to any one of claims 1 to 4, characterized in that the composition one or more excipients selected from the group consisting of soybean oil, refined, type NGM, soybean oil, partially hydrogenated 31 ° C-37 ° C, soybean oil, partially hydrogenated 36 ° C-42 ° C, soy lecithin, beeswax, triglycerides of medium or longer chain length, phosphoglycerides containing at least one organic phosphoric ester, and ester compounds of alcohols having a chain length of C2o to C40 and fatty acids of medium or long chain length.
    [7]
    Composition according to any one of the preceding claims, characterized in that the composition is contained in a soft gelatin capsule.
    [8]
    Composition according to Claim 7, characterized in that the soft gelatine capsule contains gelatine, glycerol 98%, glycerol 86%, sorbitol 70%, titanium dioxide, sodium copper chlorophyllin and water.
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    同族专利:
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    引用文献:
    公开号 | 申请日 | 公开日 | 申请人 | 专利标题
    法律状态:
    优先权:
    申请号 | 申请日 | 专利标题
    DE202017105380.6U|DE202017105380U1|2017-09-06|2017-09-06|Folate compositions|
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