JP2001097890A - Antiseptic mildewproofing agent - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a new antiseptic and mildewproofing agent by using crotamiton which is a colorless to pale yellow, transparent and liquid antipruritic agent to be coated on a diseased part as an agent for external use for relieving itching of eczema, urticaria, or the like, and diphenhydramine which is a pale yellow to yellow liquid having antihistamic activities and widely used for urticaria, eczema, or the like, as an agent for external use. SOLUTION: This antiseptic mildewproofing agent contains the crotamiton and/or the diphenhydramine as an active ingredient. The antiseptic and mildewproofing method with the agent for external use comprises using the agent added with the crotamiton and/or the diphenhydramine.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

The present invention relates to a new antiseptic / antifungal agent.

[0002]

2. Description of the Related Art External preparations such as ointments and lotions are easily contaminated with bacteria because the contents in the container are directly touched and used repeatedly after opening. Generally, existing preservatives and fungicides such as parabens are often used to prevent bacterial contamination.

[0003]

The existing preservatives and fungicides are:
It may interact with the medicinal components in the ointment and may cause skin irritation. Therefore, it is desirable not to use it if possible.
Some commercially available ointments do not contain an existing antiseptic and fungicide because the active ingredient has an antiseptic and fungicidal action. The present inventors have studied the ointment and found that some of the active ingredients surprisingly have an antiseptic and fungicidal action, and completed the present invention.

[0004]

The present invention is an antiseptic / antifungal agent containing crotamiton and / or diphenhydramine as an active ingredient. The present invention is also a method for preserving and preventing an external preparation by adding crotamiton and / or diphenhydramine.

[0005] The crotamiton in the present invention is colorless to
It is a pale yellow, transparent liquid antipruritic that is applied to the affected area as an external preparation to prevent itching of eczema, hives and the like, and is also compounded with anti-athlete's foot drugs, skin moisturizers, and the like. Diphenhydramine is a pale yellow to yellow clear liquid and has an antihistamine action. It is widely used as an external preparation for urticaria, eczema, etc., and is also used as an external preparation for rough skin and softening of keratin.

The concentration of crotamiton having an antiseptic and antifungal effect (minimum inhibitory concentration, MIC) is 1% or less for yeast and many bacteria (provided that P. aeruginosa IAM1095, Pa
eruginosaIFO13275, E.coliATCC8739, S.marcescensIFO
MIC against 12648 is more than 5%), MIC against mold
Is 1% or less. In the case of diphenhydramine, the MIC against bacteria and yeast is 0.2% or less,
In addition, it is 0.2% or less for mold.

[0007] In order to use crotamiton and / or diphenhydramine as an antiseptic / antifungal agent, the effect can be exerted by mixing an ointment, lotion or the like with the above-mentioned minimum growth inhibitory concentration (MIC) or more. The production can be carried out according to the usual production methods of ointments and lotions. Crotamiton and diphenhydramine can be used alone or in combination as an antiseptic / antifungal agent, but these compounds are compounds having excellent antipruritic and antihistamine functions themselves, and are often used as external preparations. . Therefore, external preparations containing these substances are contaminated by microorganisms such as bacteria, yeasts and molds without using the conventionally known antiseptic and antifungal agents of parabens as long as they are at least the minimum inhibitory concentration. Never.

A lotion containing crotamiton can be produced, for example, as follows. Liquid paraffin 50 g, medium-chain fatty acid triglyceride 50 g, polyoxyethylene polyoxypropylene cetyl ether 60
g, and after sufficiently stirring and mixing, 50 g of crotamiton is dissolved. Separately, purified water is added to 100 g of urea, 60 g of glycerin, and an appropriate amount of citric acid to make 1000 g, and the mixture is stirred and dissolved. Next, the two liquids are mixed, and coarse emulsification and phase inversion emulsification are sequentially performed, whereby a lotion agent containing crotamiton can be produced.

[0009]

EFFECT OF THE INVENTION As a medium for the examination of MIC of crotamiton and diphenhydramine, SCDA (soybean casein digest agar medium (BBL)) for bacteria and GPA (glucose peptone agar medium (Nissui Pharmaceutical) for fungi) were used for bacteria. . The concentration of crotamiton in the medium is 0%,
0.2%, 0.5%, and 1%. As a medium for the test of antiseptic and fungi, in the case of bacteria, SCDA or SCDLPA,
For fungi, GPA or GPLPA was used. Here, the antiseptic / antifungal test is a test for examining a change in the number of bacteria over time in a lotion preparation containing diphenhydramine.

The test strains shown in Table 1 were used as test strains for examining the MIC of various microorganisms such as diphenhydramine and crotamiton. The strains shown in Table 2 were used as test strains for the preservative and fungicide tests.

[0011]

[Table 1]

[0012]

[Table 2]

[0013] The method of measuring the MIC is as follows.
Cultured at 48 ° C. for 48 hours and for molds at 25 ° C. for 1 week or more were used. For these test bacteria and yeast, 1
A bacterial solution was prepared to be about 0 ⁵ cfu / ml, and this prepared solution was inoculated on a plate medium. For mold, a bacterial solution was prepared for a preservative / antifungal test and smeared on a plate medium. The plate medium inoculated with the bacteria was stored under the same temperature conditions as the pre-culture conditions for 3 days for bacteria, 7 days for yeast, and 14 days for mold, and the growth of each microorganism on the plate medium was visually confirmed. The results are shown in Tables 3 and 4.

[0014]

[Table 3]

[0015]

[Table 4]

The antiseptic and antifungal test was carried out according to the company's general test method. However, as the test strain, a microorganism known to exist in a general environment was used. The sample used in the preservative / mold test was prepared according to the formulation shown in Table 5 in Example 1.
It was manufactured in the same manner as described above. The results are shown in Table 6.

[0017]

[Table 5]

[0018]

[Table 6]

The MIC of diphenhydramine against bacteria and yeast was 0.2% or less. In addition, MI against mold
C was 0.2% or less. The MIC of crotamiton against bacteria is P. aeruginosa IFO13275, E. coli ATCC8739.
MIC for other bacteria was 5% or more, and MIC for other bacteria was 1% or less. On the other hand, the MIC for yeast was 1% or less, and the MIC for mold was 1% or less.

[0020]

EXAMPLES Hereinafter, specific embodiments of the present invention will be described with reference to examples, but the present invention is not limited thereto.

Example 1 In a dissolution tank A, 50 g of liquid paraffin, 50 g of medium-chain fatty acid triglyceride (ODO), and polyoxyethylene (2
0) Polyoxypropylene (8) cetyl ether (PB
C-44) 60 g was added thereto, sufficiently stirred and mixed at 80 ° C., and 50 g of crotamiton and 10 g of diphenhydramine were dissolved. Separately, 565 g of purified water, 60 g of glycerin, 1.25 g of citric acid, and 10 g of glycine were put into dissolution tank B, and stirred and mixed. Then, 5 g of dipotassium glycyrrhizinate was added, and the mixture was stirred and dissolved at 87 ° C. To dissolve. Next, at 75 ° C., in an emulsifying tank C,
The solution in dissolving tank A was subjected to suction filtration, and the solution in dissolving tank B was further subjected to suction filtration, and then subjected to coarse emulsification (W / O) for 30 minutes. Next, the mixture was cooled to 65 ° C. and subjected to phase inversion emulsification (O / W) for 20 minutes. Finally, secondary cooling was performed to 30 ° C. to obtain a lotion containing crotamiton and diphenhydramine.

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Claims (2)

[Claims] 1. An antiseptic and fungicide containing crotamiton and / or diphenhydramine as an active ingredient. 2. An antiseptic and fungicidal method for an external preparation by adding crotamiton and / or diphenhydramine.