FR2857222A1 - Microbicidal antiseptic, useful in cosmetics, pharmaceuticals and foods, is a synergistic mixture of 1,2-alkanediol and tea tree oil - Google Patents

Abstract

Microbicidal antiseptic (A) contains, as active agents, 5-10C 1,2-alkanediols (I) and tea tree oil (II). An independent claim is also included for a cosmetic, pharmaceutical or food containing (A). ACTIVITY : Antimicrobial-Gen.; Antibacterial. MECHANISM OF ACTION : None given.

Description

DESCRIPTION

  Antiseptic microbicide, and cosmetic, drug and food incorporating said antiseptic microbicide.

  FIELD OF THE INVENTION The invention relates to an antiseptic microbicide, as well as a cosmetic, a medicament and a food incorporating said antiseptic microbicide. Its goal is to provide an antiseptic microbicide that combines 1,2-alkanediols of 5 to 10 carbons and tea tree oil as active ingredients to enhance the natural antimicrobial potency of the plant. 1,2-alkanediols, as well as a cosmetic, a drug and a food incorporating said antiseptic microbicide.

  STATE OF THE ART In order to provide microbicidal and antiseptic properties to cosmetic (including parapharmaceutical), pharmaceutical or food products, compounds such as parabens, benzoates or salicylates are used. Only these compounds, irritating to the skin, are poorly tolerated by the body and must meet certain dosage limits, which are set for example at 1% for parabens and benzoates, at 0.2% for benzoic acid and salicylic acid. As they are also pH-sensitive compounds, their microbicidal and antiseptic efficacy lacks stability. It can also be damaged by the presence of other ingredients, starting with surfactants. Finally, the increase in recent years in cases of allergic reactions to these compounds has only increased the awareness of society about the safety of products, and increased the demand for cosmetics, medicines and foods that do not contain, or well at reduced doses, antiseptic microbicides.

  As advanced solutions for decreasing or eliminating antiseptic microbicides, for example, an antiseptic microbicide compound based on 1,2-alkanediols (Japanese Unexamined Patent Application H11-322591 [1999]), or a humectant has been proposed. and bacteriostatic for detergent or non-detergent cosmetics based on 1,2-octanediol (Japanese Unexamined Patent Application 200148720). The problem is that when 1,2-alkanediols (1,2-octanediol, etc.) are the only antiseptic microbicide used and are associated with nonionic surfactants, it is often necessary to force concentration. In addition, they have a very characteristic smell, which reflects on the cosmetic products that contain them.

  As advanced solutions in this field of antiseptic microbicides based on 1,2-alkanediols, there is for example proposed a composition for external use which combines 1,2-pentanediol and 2-phenoxyethanol (Japanese patent application). unexamined H10-53510 [1998]), or an antiseptic microbicide compound based on 1,2-alkanediols and parabens (Japanese Unexamined Patent Application H11-310506 [1999]).

  But the objective was in all cases to improve the effectiveness of the antiseptic by the fact of associating 1,2-alkane-diols (1,2pentane-diol, etc.), but in no way to suppress completely antiseptic or enhance the antimicrobial potency of 1,2-alkanediols.

  DISCLOSURE OF THE INVENTION In this context, the aim of the invention is to propose an antiseptic microbicide which combines 1,2-alkanediols and tea tree oil as active agents in order to amplify the power of natural antimicrobial 1,2-alkanediols, as well as a cosmetic, a drug and a food incorporating said antiseptic microbicide.

  Indeed, the invention according to claim 1 relates to an antiseptic microbicide, characterized in that it contains as active 1,2-alkanediols of 5 to 10 carbons and tea tree oil.

  The invention according to claim 2 relates to an antiseptic microbicide according to claim 1, characterized in that the 1,2-alkanediols are 1,2-hexane-diol and / or 1,2-octanediol.

  The invention according to claim 3 relates to an antiseptic microbicide according to claim 1, characterized in that the 1,2-alkanediols are 1,2-octanediol.

  The invention according to claim 4 relates to a cosmetic, a drug or a food, characterized in that it incorporates as an antiseptic microbicide an antiseptic microbicide according to any one of claims 1 to 3.

  The invention is capable of providing an antiseptic microbicide which enhances the natural antimicrobial potency of the 1,2-alkanediols, as well as a cosmetic, a drug and a food incorporating said antiseptic microbicide.

  The antiseptic microbicide according to the invention contains as active 1,2-alkanediols and tea tree oil.

  The first ingredient according to the invention consists of 1,2-alkanediols with a linear alkyl chain of 5 to 10 carbons. These are 1,2-pentanediol, 1,2-hexanediol, 1,2-heptane-diol, 1,2-octanediol, 1,2-nonanediol and 1,2 -décanediol. Among them, 1,2-hexane-diol and 1,2-octanediol are preferentially chosen, and more preferably 1,2-octanediol. In the invention, it is possible to use one or to combine several species.

  The second ingredient of the antiseptic microbicide according to the invention consists of tea tree oil. Tea tree oil is the essential oil that is extracted by steaming or using organic solvents from the leaf, bark or wood of the tea tree (Melaleuca alternifolia). , a plant native to Australia. You can also use commercial tea tree oil (tea tree oil).

  In the antiseptic microbicide according to the invention, the concentration of the 1,2-alkanediols constituting the first ingredient and the tea tree oil constituting the second ingredient is not subject to any particular exclusion, but is fixed in terms of weight ratio, between 0.1 / 1 and 10/1, and preferably between 0.2 / 1 and 5/1. Indeed, it is not recommended that the weight of 1,2-alkanediols be more than 10 times or less than 0.1 times the weight of tea tree oil, since can be expected, in either case, to increase the antimicrobial potency.

  Since it contains 1,2-alkanediols of 5 to 10 carbons as the first ingredient and tea tree oil as a second ingredient, the antiseptic microbicide according to the invention can be used as the first ingredient. support, as confirmed by the tests described below, on a synergistic effect of these first and second ingredients to develop a remarkable action of amplification of antimicrobial power. As a result, there is no need to incorporate, including low-dose, antiseptic microbicides of the prior art such as parabens, benzoates or salicylates, and therefore can be claimed to be very safe.

  The antiseptic microbicide according to the invention can be used in the formulation of cosmetics, medicines, foods, etc. Specifically, it can be used advantageously in skin cosmetics such as facial cleansers, lotions, milks, creams, foundations, mascaras, nail polishes, lipsticks, etc., in cosmetics for the hair such as shampoos, hair treatments, toning and stimulating hair growth, hair creams, hair mousse, permanent wave products, etc., in medicated cosmetics (parapharmacy) targeting a specific target such as stains or ephelides, in medications such as pimples, mouthwashes, lozenges, etc., and in foods such as chewing gums, sweets, beverages, etc. The cosmetic, medicament and food incorporating the antiseptic microbicide according to the invention may contain, appropriately and within limits which do not harm the effects of the invention, all the usual ingredients of cosmetics, drugs and foods. In the case of cosmetics (including parapharmacy) and drugs, mention may in particular be made of oils and fats, waxes, higher fatty acids, lower alcohols, higher alcohols, sterols, fatty acid esters, humectants, surfactants, macromolecular compounds, mineral pigments, dyes, antioxidants, UV filters, vitamins, astringents, brighteners, animal and plant extracts, sequestering agents, purified water, etc. On the other hand, in the case of foods, mention may in particular be made of animal and vegetable oils, polysaccharides, sweeteners, colorants, gum bases, etc. The concentration of the antiseptic microbicide according to the invention in said cosmetic, drug and food is not subject to any particular exclusion, but is attached to the composition, between 0.01 and 20% by weight, and preferably between 0.05 and 5% by weight. Indeed, less than 0.01% by weight, the antimicrobial effectiveness is affected, and more than 20% by weight, its effect no longer progresses.

  EXAMPLES OF EMBODIMENT EXAMPLE 1 Test microorganism The tests were carried out with Staphylococcus aureus IFO 13276.

  Preparation of the inoculum S. aureus was cultured at 35 ° C. on agar medium, then transferred to broth and again cultured at 35 ° C. The culture broth was then diluted to a concentration of approximately 108 cells / ml with broth medium.

  Preparation of dilution series of the substances of interest 1,2-octane diol was prepared in 5-fold dilutions; 4; 3; 2.5; 2.25; 2; 1.75; 1.5; 1.25; 1% (wlv) using ethylcellosolve at 20% (w / w) as dilution solvent. The tea tree oil (a product of V. MANE FILS JAPAN, LTD.) And an equimassic mixture of 1,2-octanediol and tea tree oil were prepared in serial dilutions of reason 2 starting from 5% solutions (wlv).

  Measurement of the Minimum Inhibitory Concentration (MIC) The test consisted in introducing into a culture dish an agar medium supplemented with each dilution of substance of interest and inoculating the inoculum into streaks of approximately 1 cm long. The reading (growth or not of the microorganism) was carried out after 2 days of culture at 35 C. The MIC was measured by the minimum concentration for which no cell growth was observed.

  The tests showed that the MIC was 2250 g / mL for 1,2-octanediol, 5,000 g / mL for tea tree oil, and 2,500 gg / mL for the equimassic 1,2-octane-diol and tea tree oil.

  The IJC assesses antimicrobial potency. If the substance of interest has no effect on the microorganism as long as it is present at a low dose, cell growth begins to slow down as its concentration increases, with a dose-dependent intensity until it stops. of development. The concentration corresponding to this stop of cellular development represents the MIC. In other words, there is extinction of the microorganism as soon as the concentration exceeds the MIC.

  Combined MIC The combined MIC chart was constructed by plotting the MICs of 1,2-octanediol, tea tree oil and equimassic 1,2-octanediol mixture and oil. tea tree based on the incorporated doses of 1,2-octanediol and tea tree oil. This diagram is presented Fig.l.

  The combined MIC makes it possible to characterize the effect of incorporating two substances with antimicrobial properties. In practice, this effect can be of three types: synergistic, additive or antagonist. By synergistic effect is meant the fact that the two substances have a multiplied action, that is to say that their natural antimicrobial power is amplified; by additive effect, the fact that the two substances simply unite their antimicrobial powers; by antagonistic effect, the fact that one of the substances annihilates the antimicrobial power of the other substance. The method of the combined MIC chart consists, as shown in Fig.2, in measuring the MIC for various proportions of two substances A and B and in characterizing the effect according to the diagram obtained. Specifically, it is a question of linking the representative points of the MIC of substance A alone (point A) and the MIC of substance B alone (point B), and to conclude that the two substances used together have a synergistic effect. (amplification of antimicrobial potency) if the MIC of their mixture is within the curve (point C), an additive effect if the MIC is on the curve (point D), an antagonistic effect (decreased antimicrobial potency) overall by annihilation of the antimicrobial potency of one or both substances) if the MIC is outside the curve (point E).

  Evaluation of antimicrobial efficacy From Fig. 1, it appears that the combination of 1,2-alkanediol and tea tree oil has a synergistic effect on antimicrobial potency.

  The following are examples of formulation of a cosmetic, a drug and a food incorporating the antiseptic microbicide according to the invention. In these examples, the concentrations are expressed in% by weight.

  Decaglyceryl monolaurate 1.0 POE (15) glyceryl monostearate 1.0 Hydrogenated soybean phospholipids 1.0 Stearic acid 4.0 Ketanol 2.0 Behenyl alcohol 2.0 Paraffin 3.0 Squalane 12.0 Example of formula 1: Moisturizing Cream 30 Jojoba Oil 4.0 Methylpolysiloxane 0.2 1,3-Butylene Glycol 3.0 L-Arginine 0.1 Xanthan Gum 0.001 1,2-Octanediol 0.25 Tea Tree Oil 0 , 1 Purified water qs 100.0 Total 100.0 Formula 2 example: hydrophilic ointment Ascorbic acid 0.5 POE cetyl ether 2.0 Hydrogenated soy phospholipids 1.0 Stearic acid 4.0 Glycerol monostearate 10.0 Liquid paraffin 10.0 Vaseline 4.0 Ketanol 5.0 Propylene Glycol 5.0 1,2-Hexanediol 0.5 Tea Tree Oil 0.2 Purified Water qs 100.0 Total 100.0 Example of Formula 3 : drink Ascorbic acid Glucose liquid sugar Grapefruit juice 1,2-Pentane-diol Tea tree oil Acidulant Thus, the antiseptic microbicide according to the invention boosts the antimicrobial potency. 1,2-alkanediols. In doing so, it makes it possible to overcome the necessity of 0.5 33.0 64.0 0.5 0.1 qs Total 100.0 to incorporate antiseptic microbicides of the prior art, which is the guarantee of high safety.

  The cosmetic, the drug and the food that incorporate the antiseptic microbicide according to the invention are not only no longer required to contain antiseptic microbicides of the prior art such as parabens, benzoic acid or salicylic acid, but allow to reduce the concentration of said antiseptic microbicide according to the invention since it has a magnified antimicrobial activity at a remarkable level. This guarantees them a very high level of safety.

  Fig. 1 is the combined MIC chart of Embodiment 1.

  Fig. 2 is a diagram illustrating the method that evaluates on the basis of the combined MIC the effect of combining two substances with antimicrobial properties.

Claims (4)

  1. Antiseptic microbicide, characterized in that it contains as active 1,2-alkanediols of 5 to 10 carbons and tea tree oil.   2. antiseptic microbicide according to claim 1, characterized in that the 1,2-alkanediols are 1,2-hexane-diol and / or 1,2-octanediol.   3. antiseptic microbicide according to claim 1, characterized in that the 1,2-10 alkanediols are 1,2-octanediol.   4. Cosmetic, drug or food, characterized in that it incorporates as an antiseptic microbicide an antiseptic microbicide according to any one of claims 1 to 3.