Malassezia globosa growth inhibitor

Hinokitiol, minoxidil, and pyridoxine, or their salts, are used to inhibit Malassezia globosa growth, addressing the need for effective treatments and prevention of associated skin diseases.

JP7723340B2Active Publication Date: 2025-08-14TAISHO PHARMACEUTICAL CO LTD
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Patent Information

Application Number
JP2021021470
Authority / Receiving Office
JP · JP
Patent Type
Patents
Current Assignee / Owner
Priority Date
2020-03-04
Filing Date
2021-02-15
Publication Date
2025-08-14
Estimated Expiration
2041-02-15

AI Technical Summary

Technical Problem

There is a lack of effective drugs that directly inhibit the growth of Malassezia globosa, a yeast-like fungus associated with skin diseases, necessitating the development of agents that can treat, ameliorate, and prevent conditions caused by this organism.

Method used

The use of hinokitiol, minoxidil, pyridoxine, and/or their medically acceptable salts as active ingredients to inhibit the growth of Malassezia globosa, formulated in cosmetics, quasi-drugs, or pharmaceuticals for application on skin and hair.

Benefits of technology

The identified compounds effectively inhibit the growth of Malassezia globosa, reducing its population and associated skin diseases such as tinea versicolor, seborrheic dermatitis, Malassezia folliculitis, atopic dermatitis, psoriasis, and acne.

✦ Generated by Eureka AI based on patent content.

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Abstract

To provide a growth inhibitor for Malassezia globosa.SOLUTION: A growth inhibitor for Malassezia globosa comprises at least one kind selected from the group of a hinokitiol, a minoxidil, a pyridoxine and / or its medically acceptable salt as an active ingredient. The growth inhibitor for Malassezia globosa can be utilized in the fields of cosmetic, quasi-drug, and drug medicine to cure, improve, and prevent diseases involving Malassezia globosa like dermatosis such as tinea versicolor, seborrheic dermatitis, malassezia folliculitis, atopic dermatitis, psoriasis, and acne.SELECTED DRAWING: None
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Description

[Technical Field]

[0001] The present invention relates to growth inhibitors against Malassezia globosa. [Background technology]

[0002] The genus Malassezia is a yeast-like fungus normally present on human skin. It is a lipophilic fungus that requires lipids for growth. Depending on the condition of the host, it is known to cause or exacerbate skin diseases such as tinea versicolor, seborrheic dermatitis, Malassezia folliculitis, atopic dermatitis, psoriasis, and acne. Currently, the genus Malassezia is classified into 18 species, and Malassezia globosa is a species that is always detected from the skin of patients with skin diseases and healthy individuals (Non-Patent Documents 1 and 2). Of the above diseases, for example, known therapeutic agents for seborrheic dermatitis include topical steroids, nonsteroidal anti-inflammatory agents for topical use, and antifungal agents such as ketoconazole (Non-Patent Document 3). [Prior art documents] [Non-patent literature]

[0003] [Non-Patent Document 1] Persononia Vol.41,56-70,2018 [Non-patent document 2] Med.Mycol.J.Vol.54(No.1),39-44,2013 [Non-patent document 3] Jpn.J.Med.Mycol.Vol.46(No.3),163-167,2005 Summary of the Invention [Problem to be solved by the invention]

[0004] However, there have been few reports of drugs that have a direct growth inhibitory effect on Malassezia fungi, especially Malassezia globosa, which is detected on human skin. Therefore, there is a need for drugs that can treat, ameliorate, and prevent diseases and symptoms associated with Malassezia globosa. An object of the present invention is to provide a growth inhibitor for Malassezia globosa in order to solve the above-mentioned problems in the prior art. [Means for solving the problem]

[0005] As a result of extensive research aimed at solving the above problems, the present inventors have found that at least one member selected from the group consisting of hinokitiol, minoxidil, pyridoxine and / or medically acceptable salts thereof is suitable for a novel use in inhibiting the growth of Malassezia globosa, and have thus completed the present invention.

[0006] That is, the present invention provides: (1) A growth inhibitor for Malassezia globosa, characterized by containing at least one active ingredient selected from the group consisting of hinokitiol, minoxidil, pyridoxine and / or medically acceptable salts thereof; (2) A growth inhibitor against Malassezia globosa according to (1), which is for use on skin and / or hair. [Effects of the Invention]

[0007] According to the present invention, it is possible to provide an inhibitor of growth of Malassezia globosa. DETAILED DESCRIPTION OF THE INVENTION

[0008] The growth inhibitor for Malassezia globosa of the present invention contains at least one selected from the group consisting of hinokitiol, minoxidil, pyridoxine, and / or medically acceptable salts thereof, and is used for skin and / or hair. Each of the above-mentioned agents can be of the same quality as that used in ordinary pharmaceuticals, quasi-drugs, or cosmetics.

[0009] Hinokitiol is a crystalline acidic substance with an aromatic seven-membered ring structure found in cypress oil, hiba oil, etc., and has a bactericidal effect on pathogenic bacteria in the oral cavity. Hinokitiol may be either natural or synthetic. When provided as a pharmaceutical, quasi-drug, cosmetic or reagent, the amount of hinokitiol in the growth inhibitor for Malassezia globosa of the present invention is preferably 0.0001% by mass or more, preferably 0.0005% by mass or more, more preferably 0.001% by mass or more, relative to the total composition, with the upper limit being preferably 5% by mass, more preferably 1% by mass.

[0010] Minoxidil, whose chemical name is 6-(1-piperidinyl)-2,4-pyrimidinediamine-3-oxide, is known for its application as a hair growth agent, and there have been many reports of it being a drug that exhibits excellent hair growth and hair loss prevention effects. When provided as a drug, quasi-drug, cosmetic, or reagent, the amount of minoxidil in the growth inhibitor for Malassezia globosa of the present invention is preferably 0.001% by mass or more, preferably 0.005% by mass or more, and more preferably 0.01% by mass or more, relative to the total mass of the composition, with the upper limit being preferably 15% by mass, and more preferably 10% by mass.

[0011] Pyridoxine has been reported to improve contact dermatitis and eczema, and to have the effect of inhibiting lipid synthesis, and is used in many hair growth products. When provided as a drug, quasi-drug, cosmetic, or reagent, the amount of pyridoxine and / or a medically acceptable salt thereof in the growth inhibitor for Malassezia globosa of the present invention is 0.001% by mass or more, preferably 0.005% by mass or more, and more preferably 0.01% by mass or more, based on the total mass of the composition, with the upper limit being preferably 5% by mass, and more preferably 1% by mass.

[0012] In the present invention, "inhibiting the growth of Malassezia globosa" refers to inhibiting the growth of Malassezia globosa, and also includes preventing an increase or reducing the number of live bacteria of Malassezia globosa, and sterilizing Malassezia globosa.

[0013] The growth inhibitor for Malassezia globosa of the present invention can be used for applications such as cosmetics, quasi-drugs, and pharmaceuticals. Furthermore, the form of the growth inhibitor for Malassezia globosa of the present invention is not particularly limited as long as it is a dosage form that can be applied to the skin (including the scalp) or hair. Specific dosage forms include lotions, creams, emulsions, gels, emulsions, and ointments. Other examples include shampoos, treatments, and conditioners. [Example]

[0014] EXAMPLES The present invention will be explained in more detail below with reference to examples and test examples, but the present invention is not limited to these examples in any way.

[0015] (Test Example 1: Growth inhibition test against Malassezia globosa) To evaluate the inhibitory effect on Malassezia globosa, the minimum inhibitory concentration (MIC) of Malassezia globosa was measured by the following method. (Test medium preparation) The test medium was prepared according to the broth microdilution method for lipophilic bacteria in accordance with CLSI M27-A3. RPMI 1640 supplemented with MOPS was mixed with 1.8% glucose, 1% peptone, 0.5% ox bile, 0.5% malt extract, 1% glycerol, 0.5% Tween 40, 0.05% Tween 80, and 250 mg / L chloramphenicol and sterilized. (Preparation of inoculum solution) Malassezia globosa was pre-cultured in modified LNA medium (32°C, 3 days, and left stationary). The obtained test bacteria were collected with a sterile loop, suspended in PBS, and washed. The washed bacterial suspension was diluted to a bacterial count of approximately 10 5 The bacterial solution was diluted with the test medium to give a concentration of CFU / mL and used as the inoculation solution. (Test substance preparation) Hinokitiol, minoxidil, and pyridoxine hydrochloride were dissolved in 50% ethanol to prepare concentrations of 12%, 3%, and 12%, respectively. The test substances were serially diluted two-fold with 50% ethanol and then diluted with test medium to the desired concentrations. The final concentration of ethanol was 1%. (Antibacterial test) 100 μL of the prepared inoculum and test substance were added to each well of a 96-well sterile U-bottom plate, and after incubation at 32°C for 4 days, the bacterial growth in each well was visually compared with that in the solvent control. The point at which bacterial growth was suppressed by approximately half was determined as the minimum inhibitory concentration (MIC) of each test substance. 100 μL of test medium was added instead of the test substance as a positive control. 100 μL of ethanol-added test medium (final ethanol concentration 1%) was added instead of the test substance as a solvent control. 100 μL of test medium was added instead of the inoculum as a negative control, and these were incubated in the same manner.

[0016] (Test results) Table 1 shows the MICs obtained for each drug.

[0017] [Table 1]

[0018] As is clear from Table 1, the MICs of hinokitiol, minoxidil, and pyridoxine hydrochloride against Malassezia globosa were confirmed, demonstrating that at least one selected from the group consisting of hinokitiol, minoxidil, pyridoxine, and / or medically acceptable salts thereof has an inhibitory effect on the growth of Malassezia globosa. [Industrial Applicability]

[0019] The growth inhibitor for Malassezia globosa of the present invention can be used in the fields of cosmetics, quasi-drugs, and pharmaceuticals for treating, improving, and preventing diseases associated with Malassezia globosa, such as tinea versicolor, seborrheic dermatitis, Malassezia folliculitis, atopic dermatitis, psoriasis, and acne, as well as other skin diseases and symptoms.

Claims

1. A growth inhibitor for Malassezia globosa, characterized by containing at least one active ingredient selected from the group consisting of hinokitiol, minoxidil, pyridoxine and / or medically acceptable salts thereof (however, when minoxidil is contained as an active ingredient, those containing piroctone olamine are excluded).

2. The growth inhibitor against Malassezia globosa according to claim 1, which is for use on skin and / or hair.

Citation Information

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