JPS6333326A - Antibacterial composition - Google Patents

Abstract

PURPOSE:To provide an antibacterial composition containing bisabolol in combination with other antibacterial substance, thereby synergistically improving the antibacterial activity of each component and are markably reducing the skin irritation of the antiabacterial substance. CONSTITUTION:The objective antibacterial composition can be produced by compounding (A) bisabolol which is an active component of chamomile and (B) other antibacterial substance such as salicylic acid, hexachlorophene, sodium lauarylsufate, chloro-xylenol, etc., preferably at a ratio (A:B) of 1000:1-1:200, especially 1:(1-200) when the component B has high compatibility to the component A or (1000-100):1 when the compatiability is low. The obtained composition exhibits effective antibacterial activity against wide variety of micro- organisms such as Gram-positive bacteria, mold, etc., at a low concentration and is usable not only as a drug for cuticle but also as a hair treatment and a disinfectant for infectious diseases of oral cavity, etc, because of its low skin irritation.

Description

[Detailed Description of the Invention] [Industrial Field of Application] 0 Regarding the Antibacterial Agent Composition of the Present Inventor [Prior Art and its Problems] Conventionally, compounds having a bacterial growth inhibiting effect (hereinafter referred to as antibacterial active substances) It is widely used as a herbal medicine for parasitic skin diseases and disinfectants, and as a preservative.

However, these antibacterial active substances are often accompanied by irritation when applied to the skin, and these irritations cause side effects such as skin disorders. There are two possible reasons for this. One is that skin whose physiological functions are damaged by bacteria or their metabolites exhibits pathological phases such as papules and erosions, and is formulated as a treatment for parasitic skin diseases. An abnormally high sensitivity to things. Another reason is that when antibacterial active substances are incorporated as disinfectants or preservatives, the products are often baby products or cosmetics, and their use on sensitive skin cannot be avoided.

In this way, the concentration of antibacterial active substances in formulations is restricted in order to avoid the side effects of skin damage due to their irritation, and as a result, the number of parasitic skin diseases on the hands and feet and infections of the female genitals that have recently increased. At present, treatment for these symptoms is not sufficient.

On the other hand, antibacterial active substances often have selective specificity in their antibacterial properties. In other words, substances used as antifungal agents such as undecylenic acid and tolnaftate have an antibacterial effect only against filamentous fungi, and substances used as bactericidal agents such as hexachlorophene have an antibacterial effect against Staphylococcus aureus, Streptococcus, etc. Shows antibacterial activity against bacteria.

However, damaged areas of the skin always have the possibility of secondary infection, and there are cases where eczema worsens and causes impetigo (impetigo varicella), albinism and cansida infection, and eczema. There are many cases in which complex complications such as leukocytosis occur. Therefore, it is desirable to develop a hypoallergenic antibacterial agent that exhibits effective antibacterial activity against a wide range of bacteria at low concentrations. was.

[Means for solving problems]

In view of the current situation, the present inventors conducted intensive research to solve these problems, and found that if bisabolol, one of the active ingredients of chamomile, is combined with other antibacterial active substances, bisabolol and The present invention was completed based on the discovery that the antibacterial activity of other antibacterial active substances is synergistically enhanced and the irritation of the other antibacterial active substances is significantly attenuated.

That is, the present invention provides an antibacterial composition characterized by containing bisabolol and other antibacterial active substances.

Bisabolol blended into the composition of the present invention includes chamomile essential oil and ? It is one of the compounds discovered as a result of research into the potency-enhancing agent of azulene, which has long been known as an anti-inflammatory component of chamomile oil. Bisabolol is known not only to have excellent anti-inflammatory and anti-ulcer effects, but also to have antibacterial effects against fungi such as Bacillus alba and Candida, and against Durum-positive bacteria.

The composition of the present invention only needs to contain substantially bisabolol, and may be blended not only as isolated bisabolol but also as a bisabolol-containing plant extract.

Bisabolol-containing plant extract is chamomile,? Della, Myrocarpus x (Myrocarpus fromd.
osus Fr.

Allem), Lavender (L, official
is Chaix), /% Myopor
um Craasifolium) and other plants by extraction with organic solvents such as ethanol, ether, acetone, etc.
After recovering the essential oil from these extracts by steam distillation and separating it by chromatography using activated alumina as a carrier, it is obtained as an ethanol-eluted fraction.
Since it is obtained as α-bisabolol, it is preferable to use α-pisagoolol in the present invention.Other antibacterial active substances to be incorporated into the composition of the present invention include:
Those that mainly act externally, such as undecylenic acid, zinc undecylenate, salicylic acid, thianthol,
tolnaftate, clotrimazole, naphthiomate,
Zoropionic acid, caprylic acid, pentachlorophenol,
Salicylic acid 8-benzoxyquinoline, trichlorphenyl iododerono♀gyl ether, griseofulvin, variotin, pyrrolnidoline, moctal, sulfur, phenyl iodo undesinoate, halozolosin, trichomycin, variocin, virolnidoline, cytucanin,
Nystatin, exalamide, cyclovirox olamine, amphotericin B1 miconazole nitrate, econazole nitrate, inconazole nitrate, trimethylcetylammonium pentachlorophenate, bisdekarium acetate,
Antifungal agents such as dibenzthione: chlorxylenol, benzethonium chloride, inpropylmethylphenol, thymol, resorcinol, lysozyme chloride, chlorhexicine gluconate, orthophenylphenol, sorbic acid, dehydroacetic acid, sodium hypochlorite, iodine, iodotincture, iodoform ,? Bidon-iodine, IQ ethyl laoxybenzoate, no-Q propyl laoxybenzoate, boric acid, borax, oxidol, potassium permanganate,
Chloramine T, chlorcresol, chlorphenesin,
Formalin, phenol, hexachloro+272, creosote, chlorobutanol, thioxolone, thiram,
Examples include tribromusalan, methylrosalinine chloride, benzalkonium chloride, sodium lauryl sulfate, urea, alkyl-lyaminoethylglycine hydrochloride, ictamol, and the like.

To prepare the composition of the invention, it is necessary to dissolve other antibacterial active substances in bisabolol, since bisabolol is an oily substance at room temperature and has the property of dissolving most antibacterial active substances. can get.

The blending ratio of bisabolol and other antibacterial active substances is bisabolol:other antibacterial active substances=1000:l~1:200
It's amazing. In particular, other antimicrobial active substances include undecylenic acid, salicylic acid, moctal, phenyl iodo undedinoate, clotrimazole, virolnidoline, exalamide, halozolosin, cycloviroxolamine, chlorxylenol, isopropylmethylphenol, thymol, resorcinol, orthophenylphenol, /Q Propyl benzoate, chlorphenesin, sodium lauryl sulfate, NoQ ethyl benzoate, etc., which have high compatibility with bisabolol,
A blending ratio of 1:1-1:200 is desirable. In addition, when these substances are blended for the purpose of preventing microbiological contamination in the formulation, such as preservatives in cosmetics and shampoos, the l:l-1:10 ratio is particularly preferred; When used as a medicinal ingredient in products, etc., the ratio is 1:2.
0-1: 200 is particularly preferred.

In addition, other antibacterial active substances include zinc undecylenate, tolnaftate, sulfur, cytucanin, nystatin, miconazole nitrate, econazole nitrate, inconazole nitrate,
If the compatibility is low, such as trimethylcetylammonium pentachlorophenate, variotin, lysozyme chloride, chlorhexicine gluconate, iodine, iodine tincture, borax, benzalkonium chloride, etc., bisabolol: Antibacterial agent = loooo: l-100 : l
The blending ratio is desirable. In this case as well, for the purpose of preventing microbiological contamination,
A blending ratio of 200:
1 to 100:1 is preferred.

The composition of the present invention may optionally contain other anti-inflammatory agents, vitamins, antioxidants, humectants, astringents, antipruritics, adrenocortical hormones, analgesics, antibiotics other than the above-mentioned antibacterial active substances, sulfa drugs, and fragrances. , coloring materials, etc. can be blended.

The composition of the present invention can be used in emulsion forms such as liquids, oils, creams, and emulsions, powders such as knockers, liniments, nosters, oil-based ointments, aerosols, sprays, and no-Q tsude formulations, depending on the intended use. etc. Bases used in these formulations include lower alcohols such as ethanol and isoderono-Q-nol, olive oil, partially hydrogenated olive oil, almond oil, jojoba oil, peanut oil, coconut oil, gnome oil, Vegetable oils and hydrogenated oils such as safflower oil, sunflower oil, cottonseed oil, hydrogenated coconut oil, hydrogenated gnome oil, avocado oil, sesame oil; turdle oil, gazsen,
Animal oils such as mink oil, squalene, pristane, zaman, lauran, beef tallow, and egg yolk oil; Animal waxes such as spermaceti, shellac, beeswax, lanolin, liquid lanolin, reduced lanolin, and hard lanolin; Vegetable waxes such as carnauba wax and candelilla wax. Wax: Fluid No Q Rough In, Fluid Polyisobutylene, α-Olefin Oligo 1-, Squalane, Vaseline, No9 Rough In, Inno♀ Rough In, Fluid Inono 9
Hydrocarbons such as roughin, osikelite, shellac, toicrocrystalline wax, polyethylene powder: lauric acid, myristic acid, noqlumitic acid, stearic acid, isostearic acid, oleic acid, linoleic acid, ricinoleic acid, behenic acid, lanolin fatty acid Fatty acids such as nilauryl alcohol, cetanol, 2-hexyldodecanol, stearyl alcohol, isomeryl alcohol, oleyl alcohol, 2-octyldodecanol, behenyl alcohol, lanolin alcohol, cholesterol, higher alcohols such as phytosterols: ethylene glycol , ethylene glycol monoalkyl ether, diethylene glycol monoethyl ether, triethylene glycol, &lJ ethylene glycol, telopylene glycol, ? Riderobilene glycol, 1,3
-butylene glycol, glycerin, broken glycerin,
Polyhydric alcohols such as methyl alcohol and pentaerythritol: zoisoderovir azopic acid, hexyldecyl isostearate, cetyl isooctanoate, oleyl oleate, decyl oleate, lanolin acetate, hexyldecyl dimethyloctanoate, butyl stearate, zoiso f sebacate In addition to esters such as lovil, trioleyl phosphate, cetyl lactate, myristyl lactate, inzolovir rumitate, inpropyl myristate, zoethyl phthalate, myristin modified octyldodecyl, myristin & myristyl, and hexyl laurinate, propylene alginate Semi-synthetic polymer compounds such as glycol, ethyl cellulose, sodium carboxymethyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, methyl cellulose, etc.: Carboxyvinyl 1-1? Sodium lyacrylate? Rivinyl alcohol? Examples include synthetic polymer compounds such as lipinyl methyl ether and polyvinylpyrrolidone, and emulsifiers such as anionic surfactants, cationic surfactants, amphoteric surfactants, and nonionic surfactants.

〔Effect of the invention〕

The composition of the present invention is an excellent antibacterial agent composition in which the antibacterial activity of bisabolol and other antibacterial active substances is synergistically improved, and the skin irritation of other antibacterial active substances is significantly reduced.

Therefore, Durham-positive bacteria (5 taphyrococcus
aureua / Staphylococcus aureus s 5taphyr
ococcus epidermis/Staphylococcus epidermidis, Bacillus 5ubutilis/Bacillus subtilis,
Propionibacterium acnes /
Acne bacillus) filamentous 914 (Trichophyton)
mentagrophytos 7. Mentagrophytos, T.
ricophyton ruburum Candidaalbicans)
Various diseases caused by such diseases can be effectively treated and prevented at low concentrations. In addition, because the skin irritation is reduced, the range of applications is extremely wide, not only for external skin medicines such as parasitic skin diseases and disinfectants, but also for dandruff removers, hair tonics, shampoos, conditioners, etc. It can be used in hair preparations, sterilizing disinfectants for infectious diseases of the oral cavity, mucous membranes, ear, nose and throat, anus, genitals, etc., and various quasi-drugs or cosmetics for the purpose of preventing infection.

〔Example〕

Next, the present invention will be explained with reference to Examples.

Example 1 α-bisabolol and salicylic acid were mixed at various blending ratios,
The antibacterial activity against Staphylococcus aureus, Staphylococcus epidermidis, or Bacillus acnes was measured by the agar culture method. Note that α-bisabolol was prepared as a 30% ethanol solution, and salicylic acid was prepared as a 30% ethanol solution, and salicylic acid was prepared as a 30% ethanol solution.
:l) Used as a 10% solution.

method Plain Heart Infusion 22.2t.

Agar 9? 6007d of deionized water was added to the solution and dissolved in a 100°C hot bath. The four melted solutions were dispensed into 1001 nt Erlenmeyer flasks in 50 portions.

This was sterilized in an autoclave for 15 minutes and left for about 60 minutes. Thereafter, it was left in a hot bath at about 50°C.

The sample solution was added dropwise to the obtained agar medium, each flask was stirred using ultrasonic waves, and then gently poured into a sterilized Petri dish and left at room temperature for one day and night. Bacteria that had been seed cultured in advance were aseptically inoculated into each medium, and incubated at 37°C for 1 hour.
The culture was cultured for ~5 days and the presence or absence of bacterial growth was measured.
The same procedure as above was performed.

Results From the test results, the minimum inhibitory concentration (MIC) for each plot at each blending ratio of α-bisabolol and salicylic acid.
was determined and expressed as an MIC curve in FIG. 1K, with α-bisabolol concentration on the vertical axis and salicylic acid concentration on the horizontal axis. As a result, it is clear from FIG. 1 that the mixed system of α-bisabolol and salicylic acid showed a remarkable synergistic effect.

Example 2 α-Bisabolol and hexachlorophene.

Mix with each blending ratio to create a raccoon red and white color! The antibacterial properties against JI bacteria, P. albicans, and C. cansida were measured using the agar culture method in the same manner as in Example 1.

Note that hexachlorophene was used as a 30-mL ethanol solution.

As a result, as shown in FIG. 2, the mixed system of α-bisabolol and hexachlorophene showed a remarkable synergistic effect against all bacteria.

Example 3 White petrolatum 250 Stearyl alcohol 220 Zoropylene glycol 120 Sodium lauryl sulfate
15.0 α-Bisabolol 3.0 Purified water Total amount 100. Melt white petrolatum and stearyl alcohol and keep at 75°C. Heat sodium lauryl sulfate, add 10 pyrene glycol and mix. The melt was added thereto, stirred with a homomixer until it reached 50' cK, and then allowed to cool to obtain an ointment for pathogenic eczema containing α-bisabolol and sodium lauryl sulfate.

Example 4 Cholesterol 309 Stearyl alcohol 30? Beeswax
80? Chlorxylenol 0.2t Chamomile extract 2? White Vaseline total amount 1000? Stearyl alcohol, beeswax, white petrolatum, chlorxylenol and chamomile extract (approximately 10% as α-bisabolol)
119 (containing), stir well, add cholesterol to this, stir until completely dissolved, leave to cool,
- An athlete's foot ointment containing bisabolol and chlorxylenol was obtained.

[Brief explanation of drawings]

FIG. 1 shows the MIC curve for each fraction of the mixed system of α-bisabolol and salicylic acid multiplied by Example 1K, and FIG. 2 shows the MIC curve for each fraction of the mixed system of α-bisabolol and hexachloro-o7ene in Example 2. It is a drawing. Above is Figure 1. Add acid to fl.

Claims (1)

[Claims] 1. An antibacterial composition containing bisabolol and other antibacterial active substances.