A composition for external use and its preparation method and application

Abstract

The invention discloses an external composition and a preparation method and application thereof. The external composition comprises a spearmint extract and ectoine. The spearmint extract has the effect of inhibiting the growth of Microsporum canis. The spearmint extract and ectoine are compounded in the invention to further enhance the effect of inhibiting the growth of Microsporum canis and has the effect of killing Microsporum canis. Therefore, the spearmint extract or a composition thereof with ectoine has an application prospect of preventing and / or treating ringworm in cats, tinea capitis, tinea corporis and / or tinea unguium.

Description

Technical Field

[0001] The present invention relates to an external composition and a preparation method and application thereof, and specifically to an external composition with easily available raw materials, high safety, and significant effect of inhibiting the growth and / or survival of Microsporum canis and a preparation method and application thereof, which can be used in the technical fields of medicine and personal care products. Background Art

[0002] Ringworm is the most common skin disease in cats. It often occurs on the face, trunk, limbs and tail. It is a round or oval ringworm spot. Cats infected with ringworm have severe itching and a long course of disease. After the scales fall off, bald spots are formed. In addition, ringworm is highly contagious. It is not only spread among animals, but also can be transmitted to humans.

[0003] Ringworm in cats is mainly caused by infection with Microsporum canis. It is usually treated by applying drugs containing ingredients such as terbinafine to the affected area. In severe cases, oral medication is also required. However, cats love to lick the lesions, and topical medications can easily cause serious adverse reactions. In addition, oral medications must also consider gastrointestinal irritation. Therefore, it is very valuable to study a drug that is easy to use, safe and effective for cats. Summary of the invention

[0004] In view of the above problems, the present invention finds that spearmint extract has the effect of inhibiting the growth of Microsporum canis. The combination of spearmint extract and tetrahydromethylpyrimidine carboxylic acid can further enhance the effect of inhibiting the growth of Microsporum canis and has the effect of killing Microsporum canis. Therefore, the spearmint extract or its composition with tetrahydromethylpyrimidine carboxylic acid can be used to prevent and / or treat ringworm, tinea capitis, tinea corporis and / or tinea unguium, and the ingredients are safe, and even licking the entrance will not cause adverse reactions. In addition, tetrahydromethylpyrimidine carboxylic acid can also repair the skin barrier, improve skin immunity, reduce the recurrence rate of ringworm, accelerate wound healing, and dilute the pigmentation caused by ringworm.

[0005] The specific technical solutions of the present invention are as follows:

[0006] The present application provides a topical composition, which includes an effective ingredient and may also include other ingredients in addition to the effective ingredient, wherein the effective ingredient is spearmint extract and tetrahydropyrimidine carboxylic acid, and the effective ingredient has a good inhibitory effect on Microsporum canis.

[0007] Further, in the above-mentioned external composition, the content of spearmint extract in the external composition is 20-99wt%, for example, 20wt%, 25wt%, 30wt%, 35wt%, 40wt%, 45wt%, 50wt%, 55wt%, 60wt%, 65wt%, 70wt%, 75wt%, 80wt%, 85wt%, 90wt%, 95wt%, 98wt%, 99wt%, preferably, the content of spearmint extract in the external composition is 30-98wt%, further preferably, the content of spearmint extract in the external composition is 70-98wt%.

[0008] Furthermore, in the above-mentioned topical composition, the content of tetrahydromethylpyrimidine carboxylic acid in the topical composition is 0.005-5wt%, for example, 0.005wt%, 0.01wt%, 0.05wt%, 0.1wt%, 0.5wt%, 0.8wt%, 1wt%, 1.2wt%, 1.5wt%, 1.8wt%, 2wt%, 3wt%, 4wt%, 5wt%, preferably, the content of tetrahydromethylpyrimidine carboxylic acid in the topical composition is 0.01-2wt%, further preferably, the content of tetrahydromethylpyrimidine carboxylic acid in the topical composition is 0.5-2wt%.

[0009] Further, in the above-mentioned topical composition, the spearmint extract is a spearmint water-soluble extract. The spearmint extract used in the present invention can be purchased directly from the market, or it can be prepared by the water extraction method commonly used in the prior art, such as placing the spearmint plant and water in an extraction device, and obtaining a condensed aqueous solution by distillation, heating, boiling, etc. Preferably, the spearmint plant is crushed, and water is placed in an extraction device, and a condensed aqueous solution is obtained by distillation, heating, boiling, etc., and the obtained condensed aqueous solution is purified. Further preferably, the spearmint plant is crushed, and water is placed in an extraction device, and a saturated condensed aqueous solution is obtained by multiple distillations, and the obtained condensed aqueous solution is purified, which can also be referred to as spearmint hydrosol. The spearmint extract generally exists in the form of an aqueous solution, and the content of the spearmint extract mentioned above in the topical composition is all based on the spearmint extract aqueous solution. For example, when the spearmint extract is spearmint hydrosol, the content of the spearmint hydrosol in the topical composition is 20-99wt%, and the content refers to the content of the spearmint hydrosol in the topical composition.

[0010] Furthermore, the above-mentioned external-use composition, in addition to the effective ingredients spearmint extract and ectoine, may also include one or more auxiliary materials, solvents, and other effective ingredients that do not affect the efficacy of the present invention.

[0011] Furthermore, the auxiliary materials include a thickener and a preservative, and the solvent includes water.

[0012] The present application provides a method for preparing the above-mentioned topical composition, which is not particularly limited in the present application, as long as the components can be mixed evenly, for example, spearmint extract and ectoine carboxylic acid can be directly mixed evenly to obtain the topical composition. Spearmint extract and ectoine carboxylic acid can also be mixed evenly in a solvent to obtain the topical composition. There is no special requirement for the mixing order of the components. Spearmint extract can be mixed with the solvent first, and then ectoine carboxylic acid can be added. Ectoine carboxylic acid can also be mixed with the solvent first, and then spearmint extract can be added. Spearmint extract and ectoine carboxylic acid can also be added to the solvent at the same time, and then fully stirred and mixed evenly.

[0013] The present application also provides the use of the above-mentioned external composition or the external composition prepared by the above-mentioned preparation method in the preparation of a product for inhibiting the growth and / or survival of Microsporum canis.

[0014] The present application also provides the use of the above-mentioned external composition or the external composition prepared by the above-mentioned preparation method in the preparation of products for preventing and / or treating ringworm in cats, tinea capitis, tinea corporis and / or tinea unguium.

[0015] The present application also provides the use of a spearmint extract in preparing a product for inhibiting the growth and / or survival of Microsporum canis.

[0016] The present application also provides the use of spearmint extract in preparing products for preventing and / or treating cat ringworm, tinea capitis, tinea corporis and / or onychomycosis.

[0017] The spearmint extract includes spearmint hydrosol.

[0018] The product is a medicine or a personal care product.

[0019] Furthermore, the medicine or personal care product can be prepared into various suitable dosage forms, including but not limited to spray, aqueous solution, gel, ointment, cream, and milk.

[0020] The present invention has the following beneficial effects:

[0021] 1. Spearmint extract has the effect of inhibiting the growth of Microsporum canis. Further, through the reasonable combination of spearmint extract and tetrahydromethylpyrimidine carboxylic acid, the growth and / or survival of Microsporum canis is effectively inhibited. Therefore, it has a preventive and therapeutic effect on cat ringworm, tinea capitis, tinea corporis and / or onychomycosis caused by Microsporum canis.

[0022] 2. The active ingredients of the present invention can penetrate the skin, accelerate wound healing, repair skin barrier, improve skin immunity, reduce the recurrence rate of tinea pedis, tinea capitis, tinea corporis and / or tinea onychomycosis, and dilute the pigmentation caused by tinea pedis, tinea capitis, tinea corporis and / or tinea onychomycosis.

[0023] 3. The ingredients of the present invention are safe, readily available, non-irritating, have no adverse reactions after licking the mouth after use, and will not produce drug resistance. DETAILED DESCRIPTION

[0024] The present invention is further described below in conjunction with examples. It should be understood that the examples are only used to further illustrate and explain the present invention, and are not intended to limit the present invention.

[0025] Unless otherwise defined, the technical and scientific terms in this specification have the same meaning as those commonly understood by those skilled in the art. Although similar or identical methods and materials as those described herein can be used in experiments or practical applications, the materials and methods are described below. In the event of a conflict, the definitions in this specification shall prevail. In addition, the materials, methods and examples are provided for illustration only and are not intended to be limiting.

[0026] The experimental methods used in the following examples and comparative examples are all conventional methods unless otherwise specified.

[0027] Unless otherwise specified, the materials and reagents used in the following examples and comparative examples can be obtained from commercial sources. Ectohydromethylpyrimidine carboxylic acid was obtained from Bloomage Biotechnology Co., Ltd., and spearmint extract was spearmint hydrosol purchased from Shandong Changlong Agricultural Technology Co., Ltd.

[0028] Example 1

[0029] 90 g of spearmint extract was mixed with 9 g of water, and stirred evenly until the mixture became clear and transparent. 1 g of tetrahydromethylpyrimidine carboxylic acid was added, and stirred evenly until the mixture was completely dissolved to obtain a composition for external use.

[0030] Example 2

[0031] 90 g of spearmint extract was mixed with 9.5 g of water, and stirred evenly until the mixture became clear and transparent. 0.5 g of tetrahydromethylpyrimidine carboxylic acid was added, and stirred evenly until the mixture was completely dissolved to obtain a composition for external use.

[0032] Example 3

[0033] 90 g of spearmint extract was mixed with 9.99 g of water, and stirred evenly until the mixture became clear and transparent. 0.01 g of tetrahydromethylpyrimidine carboxylic acid was added, and stirred evenly until the mixture was completely dissolved to obtain a composition for external use.

[0034] Example 4

[0035] 90 g of spearmint extract was mixed with 8 g of water, and stirred evenly until the mixture became clear and transparent. 2 g of tetrahydromethylpyrimidine carboxylic acid was added, and stirred evenly until the mixture was completely dissolved to obtain a composition for external use.

[0036] Example 5

[0037] 70 g of spearmint extract was mixed with 29 g of water, and stirred evenly until the mixture became clear and transparent. 1 g of tetrahydromethylpyrimidine carboxylic acid was added, and stirred evenly until the mixture was completely dissolved to obtain a composition for external use.

[0038] Example 6

[0039] 98 g of spearmint extract was mixed with 1 g of water, and stirred evenly until the mixture became clear and transparent. 1 g of tetrahydromethylpyrimidine carboxylic acid was added, and stirred evenly until the mixture was completely dissolved to obtain a composition for external use.

[0040] Example 7

[0041] 30 g of spearmint extract was mixed with 69 g of water, and stirred evenly until the mixture became clear and transparent. 1 g of tetrahydromethylpyrimidine carboxylic acid was added, and stirred evenly until the mixture was completely dissolved to obtain a composition for external use.

[0042] Example 8

[0043] 30 g of spearmint extract was mixed with 69.99 g of water, and stirred evenly until the mixture became clear and transparent. 0.01 g of tetrahydromethylpyrimidine carboxylic acid was added, and stirred evenly until the mixture was completely dissolved to obtain a composition for external use.

[0044] Example 9

[0045] 2 g of tetrahydromethylpyrimidine carboxylic acid was added to 98 g of spearmint extract, and the mixture was stirred evenly until completely dissolved to obtain a composition for external use.

[0046] Example 10

[0047] 90 g of spearmint extract and 1 g of tetrahydropyrimidine carboxylic acid were added into 9 g of water and stirred evenly until completely dissolved to obtain a composition for external use.

[0048] Embodiment 11

[0049] 98 g of spearmint extract was mixed with 2 g of water, and stirred evenly until the mixture became clear and transparent to obtain a composition for external use.

[0050] Comparative Example 1

[0051] 2 g of tetrahydromethylpyrimidine carboxylic acid was added to 98 g of water, and stirred evenly until the mixture became clear and transparent to obtain a composition for external use.

[0052] In the external-use compositions obtained in the above-mentioned embodiments and comparative examples, the contents of spearmint extract and ectoine are shown in Table 1 below:

[0053] Table 1

[0054]

[0055]

[0056] Test Example 1 In vitro antibacterial test

[0057] The standard strain used in this experiment was Microsporum canis.

[0058] (1) Test sample preparation

[0059] Take 110 sterile test tubes, add 2 mL of culture medium to the first tube as a growth control tube, add 2 mL of distilled water to the second tube as a blank control tube. Add 2 mL of the diluted external composition of Example 1 to the third to eleventh tubes, and the concentration dilution ratios are 1:2, 1:4, 1:8, 1:16, 1:32, 1:64, 1:128, 1:256, and 1:512, for a total of 9 tubes. The other examples and comparative examples are also diluted in the same ratio for standby use.

[0060] (2) Preparation of bacterial suspension

[0061] Pick one loopful of newly cultured Microsporum canis fungal colonies (seeded on Sabouraud agar medium), suspend them in 2 mL of normal saline, shake them for 15 min to mix them thoroughly, and adjust the turbidity to 10 5 -10 6 CFU / mL.

[0062] (3) Antibacterial performance test

[0063] Minimum inhibitory concentration (MIC) determination: Except for the second tube, add 50 μL of bacterial suspension to each sterile test tube using a micropipette, mix well, and culture in a 28°C incubator for 7 days. Observe and record the inhibition results.

[0064] Result determination: The NCCLS protocol recommends that the previous tube with no growth be determined as the endpoint. The growth control tube only contains culture medium and bacterial solution, without adding the external composition. The test is successful only when the growth control tube grows well and the bacterial growth gradient of other test tubes is inhibited as the sample concentration gradient increases.

[0065] Minimum bactericidal concentration (MBC) determination: Take 0.05 mL from the tube with antibacterial effect and transfer it into the culture medium, culture it for another 10 days, and observe the bactericidal results. The lowest dose without colony growth is the minimum bactericidal concentration.

[0066] The smaller the minimum inhibitory concentration and the minimum bactericidal concentration, the better the in vitro antibacterial effect of the topical composition, which further indicates that the therapeutic effect of the topical composition on ringworm in cats is better.

[0067] The results are shown in Table 2.

[0068] Table 2

[0069]

[0070] Note: —— indicates that no antibacterial or bactericidal activity was observed even at the highest concentration

[0071] It can be seen from the results in Table 2 that the spearmint extract alone has a certain antibacterial effect on Microsporum canis, while tetrahydromethylpyrimidine carboxylic acid alone has no effect on inhibiting and killing Microsporum canis. The present invention combines the spearmint extract and tetrahydromethylpyrimidine carboxylic acid, which significantly improves the effect of inhibiting the growth and / or survival of Microsporum canis, and the combination of the two shows a synergistic antibacterial and bactericidal effect on Microsporum canis.

Claims

1. A topical composition for inhibiting the growth and / or survival of Microsporum canis, characterized in that: The composition comprises spearmint hydrosol and ectoine carboxylic acid, wherein the content of the spearmint hydrosol in the external composition is 20-99wt%, and the content of the ectoine carboxylic acid in the external composition is 0.01-5wt%.

2. The composition for external use according to claim 1, characterized in that: The content of the spearmint hydrosol in the external composition is 30-98wt%, and the content of the tetrahydromethylpyrimidine carboxylic acid in the external composition is 0.01-2wt%.

3. The external-use composition according to claim 1 or 2, characterized in that: The content of the spearmint hydrosol in the external composition is 70-98wt%, and the content of the tetrahydromethylpyrimidine carboxylic acid in the external composition is 0.5-2wt%.

4. A method for preparing the external composition according to any one of claims 1 to 3, characterized in that: The spearmint hydrosol and ectoine are mixed evenly to obtain the external-use composition.

5. Use of the topical composition according to any one of claims 1 to 3 or the topical composition prepared by the preparation method according to claim 4 in preparing a product for inhibiting the growth and / or survival of Microsporum canis.

6. Use of the topical composition according to any one of claims 1 to 3 or the topical composition prepared by the preparation method according to claim 4 in preparing a product for preventing and / or treating tinea felis, tinea capitis, tinea corporis and / or tinea unguium caused by Microsporum canis.

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