FR2884691A1 - Oral composition, useful to prepare food complement to aid fertility and to prevent abortion and embryonic malformations, comprises mixture of antioxidizing agents and mixture of energizing elements - Google Patents

Abstract

Oral composition comprises: a mixture of antioxidant made up of vitamin C, vitamin E, dismutase superoxide, zinc in salt or complex form and selenium; and a mixture of energizing elements made up of magnesium in salt or complex form, arginine and taurine. ACTIVITY : Antiinfertility. MECHANISM OF ACTION : None given.

Description

2884691 1

  The present invention relates to novel dietary supplements that are useful as aids to fertility in men and women.

  The causes of infertility are sought at four levels: sperm quality, ovulation, female and male genital tract, and incompatibility between sperm and female genital environment.

  Numerous studies have demonstrated the decline in sperm quality of fertile men over the last twenty years, which would lead to an alteration of fertility in the years to come.

  The issue of marital infertility must raise awareness of the impact on male and female fertility of environmental factors and nutritional factors.

  In industrialized countries, 15% of couples are infertile whose causes are identified but a large proportion show no anomaly at the level of each of the two spouses and yet they fail to conceive a child: it is infertility unexplained.

  Infertility can be caused by the action of toxic agents, pesticides (dioxin with estrogenic effect by blocking androgen receptors), heavy metals, tobacco (through free radicals), alcohol, pharmacological agents , X and gamma rays, hormones (absorbed by livestock and then consumed by humans), infection or inflammation. These factors are likely to lead to the onset of oxidative stress. Oxidative stress is, in this context, the intermediary in infertility.

  Oxidative stress explanation: 98% of inspired oxygen is reduced to water molecules by capture of four electrons and is accompanied by ATP formation, which is responsible for the production of energy by the cell for his defense, his mobility, his reproduction. But in 2% of cases, there is a leak of electrons, which are directly related to oxygen. This oxygen will be assigned to a single electron, which will result in the formation of toxic reactive oxygen species. Thus are born: - the superoxide anion; hydrogen peroxide; peroxynitric acid; and singlet oxygen.

  Oxidative stress can worsen in certain situations: pollution, xenobiotics, overexposure to the sun, irradiation, infectious, inflammatory or degenerative conditions. On the other hand, the aging is accompanied by an alteration of the electron transport and thus an increase of reactive oxygen species.

  In response to the formation of oxygenated species, our organism has developed defense lines protecting us from the harmful effects of reactive oxygen species by combining antioxidants with free radicals to form neutral oxidized derivatives.

  Oxidative stress results from the imbalance between destructive oxygen species and protective antioxidants (destructive oxygen species> protective antioxidants).

  The possible consequences of oxidative stress on fertility are as follows: (1) Chromosome breaks in the genetic message (measured by sperm DNA fragmentation index (DFI)); 2) Peroxidation of the polyunsaturated fatty acids of the cellular membranes causing a deficiency of the permeability and disorders in the exchanges up to the cell death.

  In humans, oxidative stress will affect: - sperm concentration (oligospermia> azoospermia) sperm motility (asthenospermia, less than 40% motile spermatozoa) - sperm morphology (teratospermia, less than 30% of spermatozoa) normal sperm) In women, oxidative stress can cause the same problems for the oocyte as for the spermatozoon (attack of DNA and polyunsaturated fatty acids of the membrane). In addition, the woman is exposed to specific risks, depending on the deficit in certain antioxidants. For example, selenium deficiency (which is associated with a decrease in glutathione peroxidase) could lead to miscarriage as a result of direct oxidative damage to membranes and fetal DNA. Vitamin deficiency B6, B9 and B12 can also lead to miscarriage, this time through the elevation of homocysteine (early vascular damage to implantation). The risk of miscarriage can be further amplified when there is a zinc deficiency (repercussion on oogenesis). Finally, deficiency of vitamins B6 and B9 and zinc can cause fetal neural tube defects (spina bifida) as well as vesical and heart malformations.

  The subject of the invention is a dietary supplement which makes it possible to combat oxidative stress and thus to help male or female fertility, and to reduce the risks of miscarriage and malformation.

  The invention therefore relates to a dietary supplement, intended for oral administration, comprising a combination of: (a) a mixture of antioxidant agents consisting of vitamin C, vitamin E, superoxide dismutase, zinc, in the form of salts or complexes, and selenium; and (b) a mixture of energizing elements consisting of magnesium, salts or complexes, arginine and taurine.

  Vitamin C protects the DNA from free radicals and protects the essential hydroxylases for energy production. In a particular embodiment of the present invention, the source of vitamin C is a natural extract, in particular an acerola extract. According to one particular characteristic of the present invention, the dietary supplement comprises 30 to 120 mg of vitamin C, advantageously 30 mg of vitamin C. Vitamin E makes it possible to protect the lipid membrane against lipoperoxidation and thus makes it possible to provide membrane stabilization. According to one particular characteristic of the present invention, the dietary supplement comprises 3 to 7 mg of vitamin E. Superoxide dismutase (SOD) is an enzyme which eliminates hydroxyl radicals and thus blocks the free radical formation process from its very beginning. . SOD can be of animal (bovine for example) or vegetable origin. In particular, SOD is present in melon (cucumis melo).

  In the dietary supplement according to the invention, a melon extract, more particularly 5 to 20 mg of melon extract, advantageously 5 mg of melon extract, is advantageously introduced as a source of superoxide dismutase.

  Zinc plays a role in testicular development, especially in the transformation of testosterone into DHT (dihydrotestosterone, active form of testosterone). Zinc is advantageously in the form of a zinc salt, such as zinc citrate, or in the form of a complex. In an advantageous variant of the invention, the dietary supplement comprises 12 to 25 mg, advantageously 25 mg, of zinc citrate.

  Selenium plays a role in the biosynthesis of testosterone and therefore spermatogenesis. It preserves the integrity of the flagellum. It is advantageously introduced into the dietary supplement in the form of extracts of yeasts fed selenium or sodium selenite. According to a variant of the invention, it is introduced into the dietary supplement in the form of sodium selenite, advantageously in an amount ranging from 0.042 to 0.084 mg. According to another variant of the invention, it is introduced into the dietary supplement in the form of selenium-fed yeast extracts (between 15 and 20 mg, advantageously 18.75 mg of yeast extracts).

  Magnesium is an energizing element. It helps to fight against the asthenia of spermatozoa. It is advantageously introduced into the dietary supplement in the form of magnesium oxide (exogenous supply). The food supplement according to the invention then advantageously comprises 80 to 300 mg, more advantageously 249 mg, of magnesium oxide.

  Taurine and arginine help retain magnesium, which is rapidly eliminated in the body. Thus, magnesium remains available longer in the human body. According to an advantageous variant of the invention, the source of taurine and / or arginine is at least one natural extract, still more advantageously a plant extract. In particular, the source of taurine and arginine is an extract of prickly pear. In this variant, the dietary supplement advantageously comprises 50 to 200 mg of prickly pear extract, and still more advantageously 50 mg of prickly pear extract.

  According to a preferred variant of the invention, the dietary supplement comprises: - 30 mg of vitamin C; - 5 mg of vitamin E; 18.75 mg of selenium on yeasts; - 25 mg of zinc citrate; - 5 mg of melon extract (SOD) - 249 mg of magnesium oxide; - 50 mg of prickly pear extract.

  In the context of the present invention, the food supplement also comprises (c) at least one other antioxidant agent selected from the group consisting of a green tea extract, an olive extract, a citrus extract, beta-carotene, lycopene, vitamin B6 (which in the context of the invention acts as an antioxidant and reinforces the antioxidant action of group (a)), vitamin B9 (which in the context of the invention prevents malformation), grape extract, brewer's yeast (which allows glutathione intake in small amounts, in the order of traces), and their mixtures.

  The invention also relates to the use of the food supplement according to the invention in the treatment of infertility (male or female), in particular marital infertility. The dietary supplement according to the invention is effective for the support of fertility, particularly because of its preventive role against oxidative stress.

  The invention also relates to the use of the food supplement according to the invention in the prevention of miscarriages, in particular early miscarriages, and embryonic malformations.

  The dietary supplement according to the invention makes it possible to ensure the protection of spermatozoa and oocytes. In addition, it prevents oxidative damage (on membranes, DNA) on the embryo and thus reduces the risk of miscarriage.

  The complement according to the invention also makes it possible to prevent the risk of early vascular damage at the level of implantation (to prevent a rise in homocysteine) and thus it also makes it possible, by means of this second mechanism, to reduce the risk miscarriages, including early miscarriages.

  Thus, the said supplement advantageously makes it possible to reduce the risks of early miscarriages and the risks of embryonic malformations, in particular the 5 malformations: of the neural tube; -vésicales; - heart.

  The different compounds of the dietary supplement can be administered simultaneously (in the same tablet for example) or as combination products for separate use or spread over time.

  The dietary supplement is formulated to be administered orally. It can thus be in the form of capsule, capsule, tablet, granule, advantageously in the form of tablet. When the food supplement is in the form of soft capsule or capsule, the envelope of these soft capsules or capsules may contain in particular animal gelatin such as fish gelatin, glycerin, or a source material plant such as a cellulose or starch derivative, or a vegetable protein. When the dietary supplement is in capsule, tablet, or granule form, the active mixture can be attached to a powdery carrier such as silica, cellulose, and maltodextrin.

  According to a variant of the invention, the instructions for use are two doses per day (for the father and / or the mother). According to this variant, the dietary supplement is titrated to allow the administration of a daily dose of about 250 mg of magnesium per day, about 60 mg of vitamin C per day, about 10 mg of vitamin E per day, about 15 mg of zinc per day and about 75 g of selenium per day.

  Advantageously according to the present invention, the dietary supplement may comprise any suitable vehicle or excipient, acceptable from a nutraceutical point of view, as well as conventional additives, known to those skilled in the art.

  The following examples are intended to illustrate the invention without in any way limiting its scope.

  2884691 7 Example 1: Dietary supplement according to the invention INGREDIENTS Amount (mg) Magnesium oxide '249 Acerola natural2 120 Beer yeast 80 Prickly pear extract 50 Grape extract 35 Green tea extract 35 Olive fruit extract 35 Zinc citrate 25 Citrus extract (bioflavonoids) Beta-carotene natural (7.5%) Selenium on yeast 18.75 Natural vitamin E (y tocopherol) 3.5 Natural vitamin E (33 tocopherol) 1.5 Melon extract SOD4 5 Lycopene 5% 5 1 Vitamin B6 1 Vitamin B9 0.1 Microcrystalline cellulose QS Dextrose QS Magnesium stearate QS QS = sufficient quantity 160.3% Mg2 + ion 230 mg element (vitamin C) 375 g element selenium 4 SOD = super oxide dismutase 550 g of lycopene element This composition is formulated in the form of breakable tablets.

  In the treatment of conjugal infertility, the usage tips are two tablets a day for the father and two tablets a day for the mother.

  Example 2: Dietary supplement according to the invention 685.65 mg tablet having the following composition by weight: Natural vitamin C Magnesium oxide Prickly pear Zinc citrate Alpha tocopherol Pyridoxine hydrochloride Folic acid Sodium selenite Brewer's yeast Marc de grain OPC Green tea extract Olive fruit extract Citrus extract Beta carotene natural Melon extract Tomato extract 30-120 mg 80-250 mg 50-200 mg 12-25 mg 3-7mg 0.5-lmg 0.05- l mg 0, 042-0,085mg 80mg 160mg 3 Omg-100mg 3 Omg-100mg 3 Omg-100mg 25mg-75mg 20mg-60mg 5mg-20mg 1mg-3mg

Claims (1)

9 CLAIMS   1. Association for oral administration comprising: (a) a mixture of antioxidant agents consisting of vitamin C, vitamin E, superoxide dismutase, zinc, in the form of salts or complexes, and selenium; and (b) a mixture of energizing elements consisting of magnesium, salts or complexes, arginine and taurine.   2. Association according to claim 1, characterized in that the zinc is in the form of zinc citrate and / or the magnesium is in the form of magnesium oxide.   3. Combination according to any one of the preceding claims, characterized in that the selenium is introduced in the form of extracts of yeasts fed selenium or sodium selenite.   4. Association according to any one of the preceding claims, characterized in that the source of superoxide dismutase is a melon extract.   5. Association according to any one of the preceding claims, characterized in that the source of taurine and / or arginine is at least one natural extract, preferably a plant extract.   6. Association according to claim 5, characterized in that the source of taurine and arginine is an extract of fig of barbarism.   7. Association according to any one of the preceding claims, characterized in that it comprises: - 30 mg of vitamin C; -5 mg vitamin E; - 18.75 mg of selenium on yeasts; 28 - 25 mg of zinc citrate; - 5 mg of melon extract -249 mg of magnesium oxide; 50 mg of prickly pear extract.   8. Combination according to any one of the preceding claims, characterized in that it also comprises (c) at least one other antioxidant agent selected from the group consisting of a green tea extract, an olive extract, an extract of citrus, beta-carotene, lycopene, vitamin B6, vitamin B9, grape extract, yeast, and mixtures thereof.   9. Association according to any one of the preceding claims for its use in the fertility aid.   10. Association according to any one of the preceding claims, for its use in the prevention of miscarriages, in particular early miscarriages.   11. Association according to any one of the preceding claims, for its use in the prevention of embryonic malformations.   12. Use of an association according to any one of claims 1 to 8, for the manufacture of a dietary supplement.