EP3393471A1 - Kombinationsprodukt, das dabei hilft, zu entspannen und einzuschlafen - Google Patents
Kombinationsprodukt, das dabei hilft, zu entspannen und einzuschlafenInfo
- Publication number
- EP3393471A1 EP3393471A1 EP15837133.6A EP15837133A EP3393471A1 EP 3393471 A1 EP3393471 A1 EP 3393471A1 EP 15837133 A EP15837133 A EP 15837133A EP 3393471 A1 EP3393471 A1 EP 3393471A1
- Authority
- EP
- European Patent Office
- Prior art keywords
- sleep
- melatonin
- chamomile
- combination product
- passionflower
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Withdrawn
Links
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Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/28—Asteraceae or Compositae (Aster or Sunflower family), e.g. chamomile, feverfew, yarrow or echinacea
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- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
- A61K31/4045—Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/53—Lamiaceae or Labiatae (Mint family), e.g. thyme, rosemary or lavender
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
- A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
- A61K8/9783—Angiosperms [Magnoliophyta]
- A61K8/9789—Magnoliopsida [dicotyledons]
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- 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
- A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
- A61K9/145—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic compounds
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- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4808—Preparations in capsules, e.g. of gelatin, of chocolate characterised by the form of the capsule or the structure of the filling; Capsules containing small tablets; Capsules with outer layer for immediate drug release
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- 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
- A61P25/20—Hypnotics; Sedatives
Definitions
- the present invention relates to a combination product comprising as active substances, at least melatonin, passionflower, chamomile and melissa or a bioequivalent compound thereof to help relaxation and / or sleep.
- the invention finally relates to the use of a combination product as previously defined for the treatment of somnipathies.
- a sleep disorder is a disorder related to an individual's sleep habits. Some sleep disorders are serious enough to interfere with physical, mental and emotional functioning. A test commonly used for sleep disorders is polysomnography.
- Sleep dysfunction can be caused by a variety of problems, from grinding of teeth (bruxism) to night terrors. When an individual has difficulty falling asleep without apparent cause, it is insomnia. In addition, sleep disorders can lead the individual to sleep enormously, a situation known as hypersomnia. Other conditions of the sleep disorder may be related to substantial abuse.
- Sleep disorders include:
- hypopnoea respiratory or cardiac abnormality during sleep
- -narcolepsy sudden sleep often spontaneous at any time of the day; cataplexy, sudden weakness of the motor muscles that may result in a fall on the ground; - nocturnal terror, pavor nocturnus, nocturnal disorder characterized by strong fear and anxiety; sleepwalking, an activity that is physically and unconsciously engaged during sleep; Somniphobia, afraid to sleep; sleep apnea
- Sleep medicine is now adapted in internal medicine, family medicine, pediatrics, otolaryngology, psychiatry and neurology.
- the present invention relates to a composition for assisting relaxation and sleep in adults and children.
- the duration and organization of sleep are subject to changes during development. Basic knowledge helps distinguish true sleep disorders from variations in the norm. As an indication the approximate values of sleep duration in 24 hours are: 16 hours for the newborn term, 13 hours for the child of 2 years, 11 hours to 5 years, 10 hours to 9 years and about 9 hours for a 14 year old. Young adults still need about 8 hours, a fact often forgotten. The variability of these values is quite important and corresponds to the distribution of genetic traits in the population. Individual sleep needs are more easily established during weekends and holidays when the body is allowed to sleep for as long as needed.
- a sleep cycle includes a passage through the three states.
- deep sleep may originate different parasomnias (non-REM parasomnias): for example the night terrors of small children, which are replaced by sleepwalking in the larger child. Since sleep cycles with deep phases occur in the first half of the night, it is usual to observe these parasomnias during the first hours after falling asleep.
- Valdispert such as Nuit Paisible, which contains melatonin, magnesium, zinc and vitamin B6, or Bonne Nuit, which contains melatonin alone.
- SomniPhyt of Green Health contains melatonin associated with Griffonia Simplicifolia, Magnolia officinalis, Valeriana Offcinalis, Eschscholzia calfornica, L-tryptophan, L-glutamine, Hypericum perforatum and Vitamin B6.
- Nova Night Sleep product from Sanofi is based on passionflower, melatonin, California poppy, lemon balm and vitamin B6.
- Nutreov's OptiNuit Flash product contains melatonin and vitamin B6.
- Somdor + Melatonin Granionin contains melatonin, lemon balm extract, hawthorn, passionflower, hops and valerian. None of the products proposed contains the association object of the present invention.
- the combination product of the present invention provides a soothing effect to facilitate falling asleep, especially for children, and help them to naturally recover a restful sleep, without nocturnal awakening.
- the product according to the present invention has no side effects or addiction.
- the combination product of the present invention helps to help you fall asleep, soothes, relaxes and helps maintain a healthy sleep. It also contributes to the proper functioning of the nervous system.
- the product according to the present invention also has the advantage of preferably containing no artificial dyes, allergens and preferably being lactose or gluten-free.
- the product of the present invention has a galenic adapted to the child and the adult, preferably in the form of a capsule.
- the present invention also relates to a combination product comprising as active substances at least: (i) melatonin, (ii) passionflower, (iii) chamomile, and
- the combination product according to the invention comprises, in addition to melatonin, passionflower, chamomile and / or lemon balm, as active substances:
- Plants or extracts of plants such as, for example, orange blossom, lavender, hawthorn, marjoram, hops, gentian, valerian and / or rhodiola,
- Vitamins and minerals such as for example vitamin D, vitamins of group B, such as vitamin B6, magnesium and / or calcium
- the combination product of the invention is characterized in that passionflower, chamomile and lemon balm are in the form of plant extracts and are administered at a daily dose of 50 to 500 mg / day. preferably 50 to 200 mg / day of passionflower extracts of 5 to 200 mg / day, preferably 10 to 80 mg / day of chamomile extracts of 5 to 50 mg / day, preferably 10 to 30 mg / day of lemon balm extracts
- the combination product of the invention is characterized in that melatonin is administered at a daily dose of 0.5 to 2.0 mg / day, preferably 1.0 to 1.5 mg / day. .
- the combination product according to the invention may be in the form of a single (or combined) composition containing at least as active substances:
- the combination product is characterized in that the active ingredients (i), (ii), (iii), (iv) or a bioequivalent compound thereof are in a medium adapted to oral administration.
- the suitable medium is a liquid medium.
- the combination product is in the form of powder or a capsule containing said powder.
- the combination product according to the present invention is especially intended for adults or children.
- Passionflower, chamomile and melissa may be present as ingredients (ii), (iii) or (iv) in a combination product of the invention in more or less purified form, especially in the form of a plant extract .
- the Applicant has demonstrated that the combination of at least (i) melatonin, (ii) passionflower, (iii) chamomile and (iv) lemon balm, has a synergistic effect to help relaxation and / or falling asleep
- the combination of at least (i) melatonin, (ii) passionflower, (iii) chamomile and (iv) lemon balm has an effect on helping relaxation and / or asleep during treatment which is superior to the cumulative effects of a treatment (a) comprising the administration of melatonin, not associated with passionflower, chamomile and lemon balm, and conversely a treatment (b) comprising the administration of passionflower, not associated with melatonin, lemon balm and chamomile or a treatment (c) comprising the administration of chamomile, not associated with melatonin with lemon balm and passionflower or treatment (d) comprising the administration of lemon balm, not associated with melatonin, passionflower and chamomile.
- Melatonin (or N-acetyl-5-methoxytryptamine), often referred to as sleep hormone, is best known as the central hormone regulating chronobiological rhythms by being synthesized especially at night. It regulates many hormonal secretions, in humans and in all mammals. This neurohormone is synthesized from a neurotransmitter, serotonin, which itself derives from tryptophan. It is secreted by the pineal gland (in the brain) in response to the absence of light.
- Melatonin is also synthesized by the retina but also by bone marrow cells, lymphocytes and epithelial cells. Normally, the concentration of melatonin in these cells is greater than that found in the blood, but it does not appear to be regulated by photoperiod.
- Nuts and hazelnuts are an important source of melatonin easily absorbed by the body. Melatonin is also found in corn, tomatoes and potatoes, but in much smaller amounts. The melatonin content of many foods is still poorly known. The body can also extract it from vegetable sources (rice, bananas, pineapples, etc.).
- melatonin is secreted at night only (peak secretion at 5 am in humans, and on average because its production is inhibited by light) and it (partially) manages circadian rhythms.
- Passiflora is a genus of plants, the passiflora, of more than 530 species of the family Passifloraceae. They are spectacular flowering climbers, but their abundance is only guaranteed in areas with mild climate.
- the aerial parts of the officinal passionflower (Passiflora incarnata) are known in herbal medicine for their anxiolytic and sedative action.
- Passiflora incarnata has several alkaloids including inhibitors of monoamine oxidase (MAOI) and light sedatives.
- MAOI monoamine oxidase
- Matricaria recutita differs from the other two medicinal chamomiles in that it is an annual plant, consisting of a single upright erect stem.
- -Spasmolytic the hydro-alcoholic extract of flowers is spasmolytic. This activity could be due to apigenol which is more active than papaverine on isolated guinea pig ileum -Antibacterial, antifungal: the essential oil of feverfew Chamomile is weakly antibacterial and antifungal. It stimulates biliary secretion in cats and dogs.
- -Sedative observations in humans have reported a sedative action of Chamomile chamomile.
- the chamomile feverfew is used as the Roman chamomile: it is known as tonic, stomachic, antispasmodic and analgesic.
- Melissa or Melissa officinalis is a perennial herb of the Lamiaceae family. Its name comes from the Greek melissophullon which means “bee leaf”. It is also known as lemon balm or simply lemongrass, not to be confused with lemongrass (Cymbopogon citratus) used in Asian cooking. It is a plant native to the eastern Mediterranean basin, which has spread throughout Europe since ancient times. Lemon balm, or lemongrass balm, has been cultivated in gardens since ancient times. Originally from Europe, it was introduced in North America. The stems and leaves are still used as a tonic and mild stimulant. The taste is astringent and the aroma is light. The alcohol is obtained by distillation of its fresh leaves: melissa water has antispasmodic properties. Lemon balm can also be consumed as herbal teas.
- Melissa is most often used for its soothing and relaxing virtues. In fact, it regulates nerve impulses, which has a beneficial effect on tachycardia, but also reduces spasms of the stomach and colon (it also has antifungal properties). In infusion, lemon balm has a slightly sedative effect, and further promotes sweating, so it is recommended in cases of insomnia, or hot weather in infants and the elderly.
- a physiologically acceptable medium is a medium having no toxic or detrimental effect under the conditions of use and inert with respect to the active ingredients of the combination product.
- a medium may for example comprise different adjuvants according to its therapeutic or cosmetic purpose, such as, but not limited to, flavors, dyes, fillers, preservatives, diluents, wetting or suspending agents, etc.
- the media may also allow immediate, modified or delayed release of any of the active ingredients.
- Physiologically acceptable medium may be water, mash and / or fruit juice, texturizers, emulsifiers, colorants, preservatives, flavors, sugar or sugars.
- mash and / or fruit juice is meant a more or less liquid preparation, in particular according to the nature of the fruit and / or the fineness of the grinding, prepared by grinding, pressing or other extraction process of one or several fruits and optionally the concentration of the ground material obtained and / or separation (in particular filtration) of the seeds, achenes and / or all or part of the pulp, and / or flash pasteurisation.
- the fruits can be chosen from: apple, banana, strawberry, peach, raspberry, blackberry, mango, kiwi, blueberry, blackcurrant, currant, orange, cherry, fig, pear, apricot, coconut, passion fruit, guava, papaya, melon, lychee, pineapple, lemon, mandarin, mirabelle plum, grapefruit, grape, rhubarb and their mixtures, without this list being exhaustive.
- Textturizers means compounds that modify the texture of the products in which they are incorporated.
- texturants are: guar and carob flour; gum arabic, xanthan and gellan; carrageenans; starches (native or modified); microcrystalline cellulose; gelatin; pectin; alginates (E400 to E405); agar-agar; and their mixtures.
- emulsifiers amphiphilic compounds characterized by their HLB (Hydrophilic Lipophilic Balance) value, in particular capable of stabilizing oil-in-water emulsions (particularly advantageous if it is desired to add, for example, liposo-rich active ingredients).
- HLB Hydrophilic Lipophilic Balance
- examples of dietary emulsifiers are lecithin and its derivatives present especially in egg yolk, mono- and diglycerides of fatty acids, and polysorbate 80.
- dye is meant compounds of natural or synthetic origin capable of conferring on their own a coloration to the composition.
- Examples of food colorants are known in Europe under the codes El 00 to El 80.
- Preservatives means compounds which inhibit the proliferation of microorganisms, in particular yeasts and / or molds and / or bacteria, in particular Staphylococcus aureus, in the composition.
- Examples of food preservatives are sorbic acid and its salts (E200 to E203: benzoic acid and its salts (E210 to E219), sulfites and derivatives (E220 to E228), natamycin, nisin, and mixtures thereof
- the composition according to the invention does not comprise any preservative.
- “Aromas” means compounds of natural or synthetic origin which alone are capable of modifying the taste of the composition.
- sugar or sugar is understood to mean any sweetening carbohydrate, preferably glucose syrup, sucrose, glucose, fructose, invert sugar, honey, maltose, polyol or mixtures thereof.
- sugar used is a polyol, preferably sorbitol.
- the combination product may include, by way of example, vitamins, mineral salts, essential amino acids, essential fatty acids, trace elements, various plant extracts, fibers, antioxidants, flavonoids.
- such additional asset may be intended to enhance the desired effect as described above.
- those skilled in the art will take care to choose the additional assets and their amount so that the advantageous properties of the composition according to the invention are not, or not substantially impaired by the addition envisaged.
- water-soluble vitamins As additional assets that can be used, mention may be made of: - water-soluble vitamins and fat-soluble vitamins.
- water-soluble vitamins present in the syrupy product prepared according to the invention are in particular: vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid) also called vitamin PP (preventive pellagra), vitamin B5 (pantothenic acid), vitamin B6 (pyridoxine), vitamin B8 or H (biotin), vitamin B9 (folic acid), vitamin B12 (cobalamin) and vitamin C (ascorbic acid).
- liposoluble vitamins present in the syrupy product prepared according to the invention are in particular: vitamin A (retinol), vitamin D3 (cholecalciferol), vitamin E (mixture of tocopherols and tocotrienols) and vitamin K (phylloquinone) .
- antioxidants such as curcuminoids; carotenoids, especially chosen from beta.
- -carotene astaxanthin, zeaxanthin, lutein or compounds containing it such as goji berries; polyphenol compounds, flavonoids such as catechins; proanthocyanidins, anthocyanins, OPCs (procyanidolic oligomers); ubiquinones; coffee extracts containing polyphenols and / or diterpenes; chicory extracts; ginkgo biloba extracts; grape extracts rich in proanthocyanidins; chili extracts; soy extracts; Cocoa ; the grenade ; the Emblica; CoenzymeQ10; selenium,
- amino acids especially sulfur-containing amino acids, such as glutathione precursors, the amino acids of selenium, citrulline,
- phytosterols resveratrol, hesperidin, neohesperidin, orthosilicic acid, monomethylsilanetriol, and mixtures thereof.
- the combination of active agents comprises, as additional active ingredient, a liposo-fucous vitamin, in particular vitamin D3, minerals such as potassium or magnesium.
- a combination product according to the invention is administered orally.
- suitable forms for the oral route are, for example, tablets, capsules, lozenges, powders, granules, lyophilisates, oral solutes and syrups. Tablets, powders, granules, lyophilisates, oral solutes and syrups constitute the pharmaceutical or cosmetic form suitable for the currently preferred oral route.
- a solid composition in the form of tablets it is possible, for example, to mix the main active ingredients (i), (ii), (iii) or (iv) with a physiologically acceptable carrier such as gelatin, starch, magnesium stearate, talc, gum arabic or analogies.
- the tablets may be varied in nature, immediate release, controlled or delayed and optionally in effervescent or orodispersible form.
- a capsule preparation is obtained by mixing the active ingredient (i), (ii), (iii) or (iv) in powder form and pouring the resulting mixture into soft or hard gelatin capsules.
- composition is obtained by mixing the various compounds according to the methods conventionally used for this type of preparation.
- the composition is then preferably injected into capsules.
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Applications Claiming Priority (1)
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PCT/FR2015/053731 WO2017109300A1 (fr) | 2015-12-22 | 2015-12-22 | Produit de combinaison pour aider à la relaxation et à l'endormissement |
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EP15837133.6A Withdrawn EP3393471A1 (de) | 2015-12-22 | 2015-12-22 | Kombinationsprodukt, das dabei hilft, zu entspannen und einzuschlafen |
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IT202000032345A1 (it) * | 2020-12-23 | 2022-06-23 | Uriach Consumer Healthcare Sl | Composition comprising melatonin, piperine and vitamin d, controlled-release formulation and use thereof for the treatment of sleep disorders |
BE1030549B1 (fr) * | 2022-05-23 | 2023-12-18 | Laboratoire Puressentiel S A | Complément alimentaire |
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US20030012824A1 (en) * | 2001-07-03 | 2003-01-16 | Ott Dana Beth | Orally administered anti-stress composition |
US6998112B2 (en) * | 2003-03-18 | 2006-02-14 | Arthur Zuckerman | Sleep inducing toothpaste made with natural herbs and a natural hormone |
US7476405B2 (en) * | 2006-02-23 | 2009-01-13 | Iomedix Sleep International Srl | Compositions and methods for the induction and maintenance of quality sleep |
WO2013119605A1 (en) * | 2012-02-07 | 2013-08-15 | University Of Pittsburgh - Of The Commonwealth System Of Higher Education | Promoting sleep using at1 receptor blockers |
US20140017337A1 (en) * | 2012-07-11 | 2014-01-16 | Paul Amoruso | Therapeutic methods |
ITMI20132194A1 (it) * | 2013-12-23 | 2015-06-24 | Velleja Res Srl | Formulazioni a base di astragaloside iv o di estratti che lo contengono per la prevenzione e il trattamento dell'insonnia e dei distrubi da jet-lag |
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