DE202013003675U1 - Mouthwash oil with tocotrienol for the care of gums, teeth and oral cavity - Google Patents

Abstract

Agent consisting of a lipophilic substance containing or releasing medium-chain fatty acids with 0.1% to 70% tocotrienols, derivatives of tocotrienols, tocotrienol-rich fractions of natural products or mixtures thereof for introduction into the oral cavity for the purpose of care of the mouth and pharyngeal, gum and tooth health and for the treatment of inflammatory and other diseases of the oral cavity.

Description

• • zur Entzündungshemmung und Wachstumsförderung im Zahnfleisch
• • und als antibakterielles Mittel zur Gesunderhaltung von Zahn und Zahnfleisch
• • zur Reinigung der Mundhöhle

The present invention relates to an oil composition of oils with medium-chain fatty acids and tocotrienols. This is equally suitable

• • for anti-inflammatory and growth promotion in the gums
• • and as an antibacterial agent for the health of teeth and gums
• • for cleaning the oral cavity

Idea of the invention

Tocotrienols are isomers of the vitamin E family, which have a markedly anti-inflammatory effect when applied topically to the skin. Medium chain fatty acids such as caprylic acid (C8: 0) are present in some natural triglycerides (eg coconut oil) and in neutral oil (MCT oil) (obtained by transesterification). They have a marked inhibiting effect on bacteria and fungi.

Both elements are oil soluble (lipophilic). Oils are necessary for the solution and dilution of tocotrienol extracts and at the same time improve penetration of the active ingredients into the skin as a penetration enhancer (or permeation enhancer).

Combining these two elements in an oil (or emulsion) for use in the oral cavity gives a product which has the following advantages:

Advantages of the invention

• 1. Tocotrienols are very good anti-inflammatory, by influencing the factors NF-kB, iNOS, COX-2 and other metabolic pathways that have not yet been definitively explored. The anti-inflammatory effect is well documented by scientific studies and practical experience. Inflammatory processes in the gums (periodontitis) are common problems in oral hygiene. These inflammations can be effectively counteracted by tocotrienols.
• 2. Medium chain fatty acids have a markedly antibacterial (and fungicidal) effect. This effect serves the health of gums and teeth.
• 3. Mild taste: both agents are characterized by skin friendliness and mild taste. Thus, they are also recommended for sensitive skin in the oral cavity or with appropriate personal preference.
• 4. By "gargling" the oil can reach the complete mouth and pharynx and thus unfold the positive effects of tocotrienols and fatty acids to the throat. This oil is also effective for throat infections.
• 5. When cleaning the tooth space when "brushing your teeth" almost exclusively water-soluble agents and cleaners are used. As far as deposits, dental plaque, tongue coatings and food residues are oil-soluble, they can be achieved much better with an oil and eliminated.
• 6. Preservation and improvement of the voice. Singing voices are recommended as "home remedies" the use of sunflower oil. I explain this by the high vitamin E content of sunflower oil. Firstly, the use of tocotrienol allows the use of a higher concentration of vitamin E solution, while secondly, a much better antioxidant effect is achieved by tocotrienols.
• 7. The product can be used for traditional oral rinse ("oil pulling"), which is known from traditional Indian medicine (Ayurveda) and is widely recommended by naturopaths. Here, an amount of oil, for example, 10 g is moved in the mouth and sucked through the interdental spaces and rinsed. After several minutes, this produces a milky liquid, which should be spit out.
• 8. Alternatively, the mouthwash oil described may simply be used in smaller quantities to wet the teeth and oral cavity with the oil. The oil residues can be left in the oral cavity. Ingestion does not represent any danger or inconvenience.

State of the art

Care products for the oral cavity are so far mainly water-soluble and contain more or less aggressive bactericidal agents such as essential oils, herbal extracts, fluorine compounds and cleaning bodies. This care product is not intended to replace the mouthwash oil described, but to complement.

Naturopaths and traditional Indian medicine recommend "oil pulling". The oils to be used are not specified. It is usually used a "high quality" vegetable oil, for example sesame oil or olive oil. Of course, some of these vegetable oils contain weak anti-inflammatory substances such as sesamin. These natural oils used so far are substantially improved by the mouthwash oil described, since this is less viscous, has a higher vitamin E content and has a separate anti-inflammatory component with the tocotrienols.

A dental treatment of periodontitis consists in the mechanical cleaning of the periodontal pockets on the necks and the subsequent introduction of bactericidal substances (example Betaisodona ^® ). Anti-inflammatory agents are usually not used, or are available only with significant side effects (corticosteroids). By using the tocotrienols, an anti-inflammatory component comes into play, which in contrast to corticosteroids does not slow down the growth of the skin (collagen degradation) but promotes and is free from side effects.

An Irish research group at the University of Warwick described coconut oil in 2012, which has been treated with certain enzymes as a "natural antibiotic" suitable for dental care and caries protection. This became known through an article in the magazine Der Spiegel to a larger audience. In addition, mouthwashes with coconut oil are recommended as a home remedy. I explain the antibiotic effect of coconut oil mainly by the lipolysis released medium chain fatty acids contained in coconut oil to about 8%. Lipolysis is promoted by the enzymes of the Irish Research Unit.

So far, oral care oils are known neither with tocotrienols nor on the basis of medium-chain fatty acids.

tocotrienols

Tocotrienols are naturally occurring isomers of vitamin E. They are characterized by many properties that are not found in tocopherols. Tocotrienol-rich vitamin extracts have been produced from various vegetable oils for several decades. Such extracts are also called TRF (tocotrienol rich fraction). They are manufactured and marketed on a large scale for nutritional supplements and food, and are thus available at relatively low prices.

Tocotrienols are characterized by the fact that they penetrate and spread much better into skin and other tissues than conventional vitamin E. In vivo, tocotrienols are characterized by a 40- to 60-fold higher antioxidant activity on the cell membranes. Tocotrienols have a lower residence time than tocopherols in tissues with a half-life of 3-5 hours. Studies and practical experience confirm the anti-inflammatory effects of tocotrienol rich oils. Tocotrienols occur in nature predominantly as alpha-tocotrienol, beta-tocotrienol, gamma-tocotrienol and delta-tocotrienol. The strongest anti-inflammatory effect is evidenced for gamma-tocotrienol and delta-tocotrienol. These are also referred to as DMT3 (desmethyl tocotrienols).

• • Varianten (Isomere) der verbreiteten Tocopherole (Vitamin E), die sich dadurch auszeichnen, dass sie anstelle des gesättigten Radikals der Tocopherole andere Radikale mit ungesättigten Doppelbindungen aufweisen
• • die natürlichen in der Ölpalme Elaeis Guineensis vorkommenden Tocotrienole, insbesondere mit dreifach ungesättigter Seitenkette
• • die in der Annatto-Pflanze natürlich vorkommenden Tocotrienole aus gamma- und delta-Tocotrienol
• • die in Getreiden natürlich vorkommenden Vitamin E ähnlichen Substanzen
• • Fraktionen natürlicher vorkommender Tocotrienol-Gemische, insbesondere solche, die reich an delta- und gamma-Tocotrienol sind
• • Tocomonoenole, MDT
• • chemisch, synthetisch oder biotechnologisch erzeugte ähnliche Varianten

With tocotrienols for the purposes of this invention are referred to

• Variations (isomers) of the widespread tocopherols (vitamin E), which are characterized by the presence of other radicals with unsaturated double bonds instead of the saturated radical of the tocopherols
• • the natural tocotrienols found in the oil palm Elaeis Guineensis, especially with triple unsaturated side chain
• • the tocotrienols of gamma and delta tocotrienol found naturally in the Annatto plant
• • the naturally occurring in cereals vitamin E similar substances
• Fractions of naturally occurring tocotrienol mixtures, especially those that are rich in delta and gamma tocotrienol
• Tocomonoenols, MDT
• • chemically, synthetically or biotechnologically produced similar variants

The oil base with medium chain fatty acids

• 1. die direkte Hemmwirkung durch die freien Fettsäuren
• 2. da Mikroorganismen ihre Zellwände aus den vorliegenden Fetten aufbauen würde deren Struktur geschwächt, wenn sie die kürzeren Fettsäuren dazu verwenden.
• 3. Öle sind lipophil und können die wasserlöslichen Nährstoffe, die zum Wachstum von Pathogenen notwendig sind, nicht lösen. Werden Oberflächen mit Ölen benetzt, verdrängen sie Wasser und wasserlösliche Substanzen und entziehen Bakterien und Pilzen so die Lebensgrundlage. Unter Öl wird auch der Zutritt von Sauerstoff verhindert, dieser Umstand wird bei der Konservierung von Lebensmitteln in Öl genutzt.

The antibiotic effect of coconut oil can be explained by elimination of medium-chain fatty acids, for example caprylic acid (C8: 0), capric or lauric acid. Fats and oils consist of triglycerides in which three fatty acids are linked to one glycerine molecule. Coconut oil contains about 8% caprylic acid. In lipolysis, ie the disintegration or decomposition of fats, the fatty acids are released as "free fatty acids". This lipolysis is carried out by microorganisms or by special enzymes or spontaneously. The antibiotic effect against bacteria and fungi is explained by

• 1. the direct inhibitory effect of the free fatty acids
• 2. Because microorganisms build up their cell walls from the fats present, their structure will be weakened if they use the shorter fatty acids to do so.
• 3. Oils are lipophilic and can not dissolve the water-soluble nutrients necessary to grow pathogens. If surfaces are wetted with oils, they displace water and water-soluble substances, thus depriving bacteria and fungi of their livelihood. Under oil, the access of oxygen is prevented, this circumstance is used in the preservation of food in oil.

For many technical purposes, as well as for nutrition and for special diets medium chain fatty acids are converted by transesterification in low viscosity oils. In this process, triglycerides are produced with predominantly or exclusively medium-chain fatty acids, for example with 60% caprylic acid and 40% capric acid or even 98 Percent caprylic acid. Such oils are called MCT oil (Middle Chain Triglyceride) or neutral oil.

By using such a MCT oil, lipolysis naturally releases not only a small proportion but only medium-chain fatty acids.

Other ingredients in the mouthwash oil

Further ingredients in the mouthwash oil described here are essential oils, lipolytic enzymes and other oil-soluble active ingredients.

Essential oils:

Essential oils are often included in mouth and dentifrice oils. They dissolve well in fatty oils and can be added to the mouthwash oil described here to improve the effect. For example: sage oil, tea tree oil, camphor, and myrrhene extracts. Essential oils are often characterized by a pleasant taste, they are self-bacterial inhibiting and improve the penetration of other active ingredients, especially the tocotrienols, into the skin as a permeation enhancer.

Lipolytic enzymes:

These can be used to promote the desired slow cleavage of the fatty acids. Since the agent described here generally contains an increased proportion of medium-chain fatty acids, the dosage of the necessary enzymes can be reduced.

Dosage of tocotrienols

The dosage of tocotrienols is calculated so that the desired concentration can be achieved for the volume of tissue to be treated. A clear anti-inflammatory effect was described for tocotrienols at concentrations from 5 μmol.

The effective concentrations are between about 0.1 and 100% tocotrienol, whereby the optimum penetration behavior is achieved in mixtures with an oil. The tocotrienols should be dosed to achieve a concentration of 0.5 to 20 microg / mL in the range of application with typical application (this dosage may be significantly increased in the case of increased inflammation, single treatment or illness).

Example calculation:

We estimate about 10 cubic centimeters of gum and pharyngeal tissue. At 5 microg / mL, this requires 0.05 mg tocotrienols.

Using, for example, 3-5 grams of the mouthwash oil, we are assuming 0.5 grams of the mouthwash oil that comes to rest on the surface of the gum and oral cavity.

If we use the described mouthwash oil with 1% tocotrienols, you will have 5 mg of tocotrienols on the skin. Applied to the dermis, according to studies, 40% reach the stratum corneum. In the mouth and throat, this rate of immigration would be reduced by the higher water content, but improved by the absence of the cornea. If we calculate with only 1% continuously available T3 in the first millimeter, the desired concentration is achieved.

Basically, a plentiful dosage should be sought, as an overdose is naturally hardly possible with vitamin E. For anti-inflammatory applications, the use of delta-tocotrienol and gamma-tocotrienol is particularly recommended, as this has been the most effective in studies.

Used biological materials of plant origin and their countries of origin

For the purposes of this patent application Tocotrienole of natural origin can be used. Commonly used are so-called TRF extracts from red palm oil from Malaysia, and tocotrienol oils from the USA. Tocotrienols are also produced in Europe from cereals (barley) and in other countries from rice.

Summary

1. Designation

• Local NF-κB modulation by topical tocotrienol

2nd short version

2.1. Technical problem of the invention = technical task and objective

• Care of the oral cavity, especially the gums and teeth, as well as reduction of inflammation in the gums, jaws and throat.

2.2. Solution of the problem or the technical task

Tocotrienols provide an anti-inflammatory, oil-soluble substance that can be applied with an oil to the surfaces of the oral cavity, from where it penetrates into the other tissue. At the same time, the use of an oil containing medium-chain fatty acids has an antibacterial effect.

2.3. field of use

• 1. Mundspülöl für den täglichen oder gelegentlichen Gebrauch nach der Zahnreinigung.
• 2. Mundspülöl zur besseren Durchführung der traditionellen Zahnreinigung „Ölziehen”
• 3. Behandlung verschiedener entzündlicher Krankheiten oder Entzündungen in der Mundhöhle, insbesondere Paradontitis und Halsentzündungen.

The present invention has the following main fields of application:

• 1. Mouthwash oil for daily or occasional use after cleansing the teeth.
• 2. Mouthwash oil to better carry out the traditional "oil pulling" tooth cleaning
• 3. Treatment of various inflammatory diseases or inflammation in the oral cavity, especially periodontitis and throat infections.

3. drawing

• no drawing

Claims (9)

Agent consisting of a lipophilic substance containing or releasing medium-chain fatty acids with 0.1% to 70% tocotrienols, derivatives of tocotrienols, tocotrienol-rich fractions of natural products or mixtures thereof for introduction into the oral cavity for the purpose of care of the mouth and pharyngeal, gum and tooth health and for the treatment of inflammatory and other diseases of the oral cavity. The composition of claim 1, wherein tocotrienols are a composition selected from the group consisting of alpha-tocotrienol, beta-tocotrienol, gamma-tocotrienol, delta-tocotrienol, desmethyltocotrienol, didesmethyltocotrienol, or mixtures thereof; or tocotrienol-rich fractions of natural products, in particular of the palm species Elaeis guineensis, Annato seeds or cereals; or from other synthetically or biotechnologically produced variants of vitamin E. A composition as claimed in any one of the preceding claims using MCT oil containing 30 to 100% caprylic acid (C8: 0) with 2% of a tocotrienol-rich extract of natural products. Composition according to one of the preceding claims with addition of a substance, in particular one or more enzymes which promotes or causes the release of the fatty acids. A composition as claimed in any one of the preceding claims with the addition of essential oils for the purpose of penetration enhancement into the skin of the oral cavity, for the purpose of providing additional bacterial inhibiting or killing effect or for improving the taste. Composition according to one of the preceding claims, wherein the administration consists of a liquid to be introduced into the oral cavity, a spray or a gel-like thickened substance. Agent according to one of the preceding claims with additional use of vitamin A in the form of retinol or carotenes. Composition according to one of the preceding claims, wherein with the aid of an emulsifier an emulsion with water content of 70% to 10% is produced. Composition according to claim 7 wherein additional active ingredients are introduced into the water content, in particular vitamins C and B12.