KR100467031B1 - Acne prevention and treatment composition - Google Patents

Abstract

The present invention strongly inhibits the activity of 5-alpha-reductase and at the same time significantly reduces the cotton wool to inhibit the excessive secretion of sebum, the main cause of acne, one of the extracts Or it relates to a composition for preventing and treating acne containing two or more kinds.

Description

Acne prevention and treatment composition

The present invention strongly inhibits the activity of 5 alpha-reductase to radically suppress the excessive secretion of sebum, which is the main cause of acne, and remarkably reduces the cotton wool induced in rabbit ears (Angelica koreana). ), Paeonia lactiflora, Gardenia jasminoides and Polygonum cuspidatum containing one or two or more of the extracts, and relates to a composition excellent in the prevention and treatment of acne.

[Technical Field to which the Invention belongs and Prior Art in the Field]

The cause of acne is still not clearly defined, but it has been recognized as the orthodox report in the past reports that three important causes are directly involved in acne, if genetic and environmental factors are excluded. . The three major causes of the acne outbreak briefly described as follows. The first cause may be due to excessive secretion of sebum. The formation of sebum is caused by the action of androgen hormones, and the abnormal increase in orrogen and various mechanisms associated with sebum causes the sebaceous glands to become more functional, resulting in excess sebum. The second is explained by the closure of the pores due to hyperkeratinization of the hair follicles. The generated sebum should be discharged smoothly out of the skin, but the pores are blocked due to the exaggeration of the hair follicles, thereby suppressing the smooth discharge of sebum, and consequently, the sebum is stagnated in the hair follicles to form microsurface. The third cause is due to acne bacteria (Propionibacterium acnes), which is explained as an important cause of acne lesion deterioration. Acne bacteria that reside in the hair follicles form pores wall irritants. The microvesicles gradually increase in size as the sebum continues to grow and develop into a scalp. As a result, the hair follicle wall becomes thin, and the irritant produced by the acne bacteria stimulates the thin wall of the hair follicles, which gradually deteriorates the scalp into inflammatory lesions. (Pain → pustules → nodule → scar).

Inhibiting the excessive production of sebum among the three causes is the most important factor for preventing or treating the onset of acne and the skin physiology and production mechanisms related to this are as follows. Within the skin are all the enzymes needed to convert inactive steroid precursors to active androgens. 5-alpha-reductase is one of them. Testosterone, one of the male hormones, enters the sebaceous gland and is converted to dihydrotestosterone by 5 alpha-reductases present in the cells. The path is followed, resulting in sebum.

In view of these problems, the present inventors strongly inhibit the activity of 5 alpha-reductase, an enzyme that promotes sebum production, to fundamentally inhibit sebum secretion, in order to suppress the excessive secretion of sebum, which is a fundamental cause of acne. As a result of systematic research experiments on various natural products in order to develop a substance, it was found that the active, red, peony, and gardenia extracts strongly inhibit sebum secretion against acne bacteria and have a strong antibacterial effect and complete the present invention. It became.

The present invention relates to a composition for the prevention and treatment of acne, characterized in that it contains one or two or more of the active, red peony, gardenia and ephedra root extract.

Hereinafter, the present invention will be described in detail.

General properties, applications, and confirmatory test methods for the activity, red peony, gardenia and ephedra root used in the present invention are as follows.

Kang-Bul is the scientific name Angelica koreana and the herbal name is Angelica Koreanae Radix, which uses the root and rhizome as the herbal medicine. Kang-Bul is a perennial, whose root stem is thick and columnar. Ingredients of the activity include Koreanin, Angelicoleanol, and iso-imperatorin. Invigoration is effective for menstruation, analgesic, neuralgia and sweating.

It is called Paeonia lactiflora because it is a perennial and it is called red peony because it is reddish when its root is cut. The root contains Paeoniflorin, Paeonol, Paeonin, Benzoic acid, essential oils, tannins, β-sistol and triterpenoides. It has been reported that the drug has an inhibitory effect on gastric and intestinal smooth muscle and uterine smooth muscle, gastric juice secretion, antiperspirant, diuretic, and antibacterial activity.

Gardenia is the scientific name Gardenia jasminoides, and its use is the fruit of gardenia. Usually six or more distinct lines protrude in the longitudinal direction of the fruit. Ingredients include alpha-crocin and αridoid glycosides, genipin and gardenenoside as pigments. Crosine-response reactions are immediately colored pale purple and purple after adding 1 drop of concentrated sulfuric acid to gardenia powder or debris. It is effective against jaundice, cholecystitis, bruises, hyperemia and hemorrhage.

Lastly, Ho Jang-geun is the scientific name of Polygonum cuspidatum, and it is a perennial that uses root stem as a herbal medicine, and root and root stem have free anthraquinone and anthraquinone glycosides (with root hydroxyanthraquinone 0.1). To 0.5%), and the main components are emodin, physcione and chrysophanol. Drug efficacy is excellent antibacterial action, there is relief, diuretic and analgesic action. It is also used to treat bruises and burns.

<Preparation of Root, Red Peony, Gardenia jasminoides and Kwonjang-Geun Extracts>

When explaining the extraction method of the active, red peony, Gardenia and K. koji extract used in the present invention. First, each crude drug was purified, powdered, and chilled for 5 days in about 10 times the amount of the extraction solvent, and the extract powder was dried by filtration, concentration, and lyophilization. The extraction solvent is selected from purified water and organic solvent (methanol, ethanol, propanol, butanol, glycerol, propylene glycol, 1,3-butylene glycol, methyl acetate, ethyl acetate, benzene, hexane, diethyl ether and dichloromethane) It is preferable to use one or two or more kinds of solvents for extraction.

<Evaluation of 5 Alpha-reductase Activity Inhibitory Activity of Root, Peony, Gardenia and Escherichia coli Extracts>

5-alpha-reductase used in 5-alpha-reductase inhibition experiments was obtained from rat liver (adult, Sprague-Dawley, male rat (8-10 weeks old), liver). A protein suspension was prepared. In addition, the enzyme reaction solution was prepared by a general method. Radiolabeled testosterone ( ³ H testosterone) was used as the reaction substrate of 5 alpha-reductase, and the enzyme reaction solution: protein suspension: extract = 70: 20: 10 for 2 minutes in a thermostat. After reacting in an incubator, the reaction solvent is blown out, the remaining material is dissolved in the developing solvent, and the thin layer chromatogram (TLC) is developed. The conversion from testosterone to dihydrotestosterone by 5 alpha-reductase was measured and the results were evaluated by comparing the results of the control with the control (conversion without addition of the extract). The inhibition rate calculation method is as follows.

% Inhibition = [(A-B) / A] X 100

A = conversion of testosterone to dihydrotestosterone (without extract)

B = conversion of testosterone to dihydrotestosterone (extract added)

Experimental results by the inhibition rate calculation method described above are as follows (Tables 1-1 and 1-2).

TABLE 1-1. Inhibition rate of 5 alpha-reductase activity when extract was used alone

TABLE 1-2. 5 Alpha-reductase activity inhibition rate when two or more extracts were mixed

As described above, it was evaluated that the activity of 5 alpha-riptase was significantly inhibited even at low concentrations when experimenting with one or more extracts of potent, potent, gardenia and ephedra root. When the mixture was mixed at the ratio, similar activity inhibitory effect was observed compared to the case of single use. This means that the activity inhibition rate for 5 alpha-riptase is excellent irrespective of the type and composition of the extract, and the excellent activity inhibitory power is not limited to the composition tested above.

<Experimental Effect of Cotton Root on Cotton Root Induced by Rabbit, Red Peony, Gardenia and K.

After drying the extract of the active, red, peony and gardenia root extract in ethanol to 1% by weight, respectively, a rabbit clinical test substance was prepared. The experimental animals were rabbits (New Zealand White) with a lot of pathological anatomical data to be compared, around 4 months of age, and used healthy males between 2.0 and 3.0 kg. In addition, after a period of one-week accrual period after the animals were obtained, the general state of health was observed, and only healthy animals were used for the test. The composition of the test group and the method of administration will be described as follows. 30 rabbits were inoculated with IPM (isopropyl myristate), a cotton-causing substance, on both ears of the rabbit every day for 50 days once a day for 10 days. Twenty-four observed animals were selected and classified into four groups such that six animals per group (A, B, C, D, E, F) were considered in consideration of the degree of progression of the cotton cloth.

The effect of reducing cotton cloth was tested once daily by applying 0.7 ml of the extract test substance of the active, red, medicinal and gardenia root and K. roots in the right ear of the rabbit which produced the induced cotton cloth, and then 10 to 15 times with a cotton swab. To the left ear, 0.7 ml of ethanol used as a base was administered to the left ear, and then applied 10 to 15 times with a cotton swab to compare with the right ear. The healing period lasted for three weeks. When the test drug was administered, the extent of the lesion progress was visually evaluated every day, and the effect of reducing the test cloth was evaluated according to a certain evaluation scale (see Table 2-1).

Three weeks after application of the test substance, each experimental group was euthanized, the ears of each animal were cut out, and the base of the right and left ears (outer part of the ear canal) was cut out about 2.5 cm x 1.5 cm. The cut tissue was soaked in water at 60 ° C. for 1 minute, taken out, and only the epidermis was peeled off. Then, each of the whole hole-mounted tissues, which had been well spread on the slide glass, was raised, and then dried under a stereoscopic microscope. Observed by belly. Thereafter, the number and the area of the scrim of the hole-mounted tissue were calculated (see Tables 2-2, 2-3, and 2-4).

TABLE 2-1. Gross Findings Results of Earthenware Vessel Condition During the Treatment Period (3 Weeks).

TABLE 2-2. Three weeks after the extract application, the hole mount of the rabbit scrim was observed.

TABLE 2-3. The area / number ratio of the cotton cloth after 3 weeks of extract application.

TABLE 2-4. Relative reduction of cotton area / number after 3 weeks of extract application.

According to the above rabbit clinical test results (Tables 2-1, 2-2, 2-3 and 2-4), the composition containing the active, red, peony, gardenia and K. koji extracts was evaluated to have a remarkable reduction effect.

When explaining the present invention in more detail, the present invention is a composition for preventing and treating acne containing active extracts, potions, gardenia and ephedra root extract obtained by the above method

To facial cleansers, soaps and creams. The composition for preventing and treating acne of the present invention is based on the base of each product of a general cleanser, soap, and cream, which does not contain excessive fat, and the dry powder of active, red peony, gardenia and K. koji extract is 0.01% for each composition. It is preferable to contain -10% by weight.

In the present invention, the cleansing agent and the soap contain one or two or more kinds of active, red peony, gardenia and kojang-geun extracts in a conventional cleansing agent and soap base, and various additives may be used to increase the clinical effect. In addition, the cream may contain one or more active, red peony, Gardenia and K. koji extracts in the base of the general oil-in-water type (O / W), and synthetic or natural materials may be added to enhance the clinical effect.

The face wash, soap and cream according to the present invention can be easily prepared by conventional manufacturing methods. The properties of the composition for preventing and treating acne according to the present invention can be easily applied to any of different dosage forms, such as liquid, cream, paste or solid, and are not limited to the following examples.

Hereinafter, although an Example and a comparative example demonstrate this invention, the technical scope of this invention is not limited to these Examples.

Example 1 Preparation and Efficacy Test of Facial Cleanser Composition Containing One or More Types of Extracts

A face wash composition was prepared such that 99.99 wt% of the face wash base (including water) and 0.01 wt% of the dry powder of the active extract were mixed in a homo mixer through stirring, heating, degassing, and cooling. In the following Examples and Comparative Examples, workability and stability mean ease of use (solubility in the extract product) and phase stability (presence or absence of phase separation) when preparing the face wash by mixing the extract.

TABLE 3-1. Facial wash, Example 1 (with active extract). (Unit: weight%)

Examples 2-11

A facial cleanser composition according to the present invention was prepared according to the same method as in Example 1 except for changing the proportion of each component as shown in the following table.

TABLE 3-2. Facial wash, Example 2 (containing peony extract). (Unit: weight%)

TABLE 3-3. Facial wash, Example 3 (containing gardenia extract). (Unit: weight%)

TABLE 3-4. Facial wash, Example 4 (containing Rhodon root extract). (Unit: weight%)

TABLE 3-5. Facial wash, Example 5 (containing active and red peony extract). (Unit: weight%)

TABLE 3-6. Facial wash, Example 6 (containing active and gardenia extract). (Unit: weight%)

TABLE 3-7. Facial wash, Example 7 (containing active and ephedra root extract). (Unit: weight%)

TABLE 3-8. Facial wash, Example 8 (containing peony and gardenia extract). (Unit: weight%)

TABLE 3-9. Facial cleanser, Example 9 (containing peony and ephedra root extract). (Unit: weight%)

TABLE 3-10. Facial wash, Example 10 (containing Gardenia and K. root extract). (Unit: weight%)

TABLE 3-11. Facial wash, Example 11 (containing active, red peony, gardenia and knotweed extract). (Unit: weight%)

5α-reductase activity inhibitory experiment

In order to confirm the effect of preventing and treating acne for the compositions prepared in Examples and Comparative Examples, each composition was diluted to a specific concentration using purified water to evaluate the inhibition rate of 5α-reductase activity by the method described above in detail. It was. The inhibition rate of 5α-reductase activity is shown in Tables 4-1, 4-2 and 4-3.

TABLE 4-1. Inhibition rate of 5-alpha-reductase activity of face wash composition.

TABLE 4-2. Inhibition rate of 5-alpha-reductase activity of face wash composition.

TABLE 4-3. Inhibition rate of 5-alpha-reductase activity of face wash composition.

Clinical Trials on the Prevention and Treatment of Acne in Rabbits

Examples 1-3, 2-3, 3-3, 4-3, 5-3, 6-3, 7-3, 8- in which the total content of the single or mixed extract in the examples of the composition was 1% by weight, respectively. Six healthy rabbits in each group to determine the clinical effects of acne prevention and treatment using the cleansers (administration group) and the extracts (control group) of 3, 9-3, 10-3 and 11-3. Induce the cotton wool in rabbit ears, as described in detail above, and then apply the cleansing agent containing the extract to the right ear, the cleansing agent not containing the extract evenly applied 0.5 grams once daily to the left ear and thoroughly washed with water for 3 weeks. Experiment After that, the rabbits were euthanized, the ears were cut out, the outer skin of the ears was detached, and the reduction rate of the cotton cloth was evaluated by the hole-mount method in which the condition of the cotton cloth was evaluated under a microscope. The results are shown in Tables 5-1, 5-2, 5-3, and 5-4 is shown.

TABLE 5-1. Three weeks after application of the face wash containing the herbal extracts, the whole ears of rabbit ears were observed.

TABLE 5-2. Three weeks after application of the face wash containing the herbal extracts, the whole ears of rabbit ears were observed.

TABLE 5-3. The area / number ratio of the cotton cloth 3 weeks after application of the extract-containing cleanser.

TABLE 5-4. Relative decrease in cotton area / number 3 weeks after application of extract-containing cleanser

As shown in the above experimental results (Tables 4-1, 4-2, and 4-3), a facial cleanser containing at least one extract of potent, red peony, Gardenia vulgaris and Escherichia coli extracts did not contain 5 alpha-reductase. It was evaluated as a strong and remarkably inhibiting activity, even in the case of rabbit clinical trials containing face wash with 1% by weight of each extract (Tables 5-1, 5-2, 5-3 and 5-4) Compared to (the left ear with the cleanser which does not contain the extract), all showed excellent cotton reducing effect. According to the above results, in the case of the face wash containing one or more kinds of potent extract, gardenia jasminoides and gardenia root extract, all of the extracts in the face wash were less than 0.01% by weight to inhibit the activity of 5 alpha-reductase. It was evaluated to be somewhat low, and in the case of more than 10% by weight, the activity inhibition rate was excellent, but the workability and stability were more difficult. Therefore, the facial cleansing agent according to the present invention containing at least one of active, red peony, Gardenia jasminoides and ephedra root extracts inhibits the activity of 5-alpha-reductase, the workability and stability of the product in the range of 0.01 to 10% by weight of the extract. This appeared to be very excellent.

Example 12 Preparation and Efficacy Test of Soap Compositions Containing One or More Types of Root, Red Peony, Gardenia and K.

A soap composition in the form of a solid soap was prepared by mixing 99.99% by weight of the face wash base (including water and various additives) and 0.01% by weight of the dry powder of the active extract in a mixer, and then extruding, cutting and molding in a soap manufacturing machine. The active extract can be prepared by including not only general soap but also synthetic soap and mixed soap according to a conventional soap manufacturing method. Workability and stability in Examples and Comparative Examples means ease of operation (solubility in the product of the extract) when the soap is prepared by mixing the extract.

TABLE 6-1. Soap, Example 12 (containing active extract).

                          (Unit: weight%)

Examples 13-15

A soap composition according to the present invention was prepared according to the same method as in Example 12 except for changing the proportion of each component as shown in the following table.

TABLE 6-2. Soap, Example 13 (containing active and red peony extract).

                 (Unit: weight%)

TABLE 6-3. Soap, Example 14 (containing actives, peony and gardenia extract).

        (Unit: weight%)

TABLE 6-4. Soap, Example 15 (includes active, red peony, gardenia and knotweed extract).

   (Unit: weight%)

5α-reductase activity inhibitory experiment

In order to confirm the effect of preventing and treating acne for the soap compositions prepared in Examples and Comparative Examples, each composition was diluted to a specific concentration using purified water, and thus the activity inhibition rate of 5α-reductase was previously described in detail. Evaluated. The inhibition rate of 5α-reductase activity is shown in Table 7-1.

TABLE 7-1. Inhibition Rate of 5-alpha-Reductase Activity of Soap Compositions

Clinical Trials on the Prevention and Treatment of Acne in Rabbits

The soap (control group) and the soap (control group) of Examples 12-3, 13-3, 14-3, and 15-3, each containing 1 wt% of the total or single extract of the composition, were added Use 6 healthy rabbits in each group to identify clinical effects on acne prevention and treatment, using cotton rabbits in rabbit ears as described in detail above, and then soap containing extracts in the right ear and no extracts. Soap is a three-week experiment by applying an even coat of 0.5 grams daily to the left ear and rinsing with plenty of water. After that, the rabbits were euthanized, the ears were cut out, the outer skin of the ears was removed, and the reduction rate of the cotton was evaluated by a hole mount method of measuring the condition of the cotton with a microscope. The results are shown in Tables 8-1, 8-2, and 8-3. It was.

TABLE 8-1. Whole mount of rabbit ear scrim was observed after 3 weeks of soap containing herbal extract.

TABLE 8-2. The area / number ratio of the cotton cloth 3 weeks after application of the extract-containing soap.

TABLE 8-3. Relative decrease in area / number of cotton cloth 3 weeks after application of extract-containing soap

As shown in the above experimental results (Table 7-1), soaps containing at least one extract of potent, red peony, Gardenia jasminoides and K. koji muscles strongly and significantly inhibited the activity of 5-alpha-reductase than those containing no extract thereof. In rabbit trials containing 1% by weight of each extract (Tables 8-1, 8-2 and 8-3), compared to the control (left ear with soap without extract) All showed excellent cotton reducing effect. According to the above results, in the case of the soap containing one or more kinds of extracts of potent, peony, gardenia and kojang-geun, if the total extract content of the face wash was less than 0.01% by weight, the degree of inhibiting the activity of 5 alpha-reductase was all high. It was evaluated to be somewhat low, and in the case of exceeding 10% by weight, the activity inhibition rate was excellent, but the workability was difficult in manufacturing. Therefore, the soap according to the present invention containing at least one of active, red peony, gardenia and K. koji extracts has very good activity inhibition rate and workability of 5 alpha-reductase in the range of 0.01 to 10% by weight of the extract. appear.

Example 16 Preparation and Efficacy Test of a Cream Composition Containing One or More Types of Root, Red Peony, Gardenia and K.

To 99.99% by weight (including water) of a combination of an oily component, an aqueous component, and a surfactant, which is a cream base, 0.01% by weight of the dry powder of the peony extract was well emulsified in a mixer, degassed, filtered, and cooled to prepare a cream composition. In addition, it was prepared in the oil-in-water type (O / W) so that a small amount of oily components are present, this red peony extract can be conveniently added to basic cosmetics such as foam cleansing, lotion, essence, etc. can be used as a preventive and therapeutic agent of acne. Workability and stability in Examples and Comparative Examples means workability (solubility in the product of the extract) when preparing the cream by mixing the extract and phase stability (with or without phase separation) after preparation.

TABLE 9-1. Cream, Example 16 (with Peony extract).

                            (Unit: weight%)

Examples 17-19

A facial cleanser composition according to the present invention was prepared according to the same method as in Example 16, except for changing the proportion of each component as shown in the following table.

TABLE 9-2. Cream, Example 17, containing Peony and Gardenia extract.

            (Unit: weight%)

TABLE 9-3. Cream, Example 18, containing Peony, Gardenia and K. Root Extract.

         (Unit: weight%)

TABLE 9-4. Cream, Example 19 (includes active, red peony, gardenia and ephedra extract).

       (Unit: weight%)

5α-reductase activity inhibitory experiment

In order to confirm the effect of preventing and treating acne for the cream compositions prepared in Examples and Comparative Examples, each composition was diluted to a specific concentration using purified water, and thus the activity inhibition rate of 5α-reductase was previously described in detail. Evaluated. The inhibition rate of 5α-reductase activity is shown in Table 10-1.

TABLE 10-1. Inhibition rate of 5-alpha-reductase activity of cream composition

Clinical Trials on the Prevention and Treatment of Acne in Rabbits

The cream (control group) and the extract (control group) of Examples 16-3, 17-3, 18-3 and 19-3, wherein the total content of the single or mixed extract in the examples of the composition was 1% by weight, respectively. Using 6 healthy rabbits in each group to identify clinical effects on acne prevention and treatment, using a rabbit to induce cotton wool in rabbit ears, as described in detail above, the soap containing the extract in the right ear, the extract containing Soaps that are not used are tested for 3 weeks by applying 0.5 grams daily to the left ear and rinsing with plenty of water. After that, the rabbits were euthanized, the ears were cut out, the outer skin of the ears was removed, and the reduction rate of the cotton was evaluated by a hole mount method for evaluating the condition of the cotton with a microscope. The results are shown in Tables 11-1, 11-2, and 11-3. Indicated.

TABLE 11-1. Three weeks after application of the cream containing the herbal extracts, the whole hole was observed in the rabbit's ears.

TABLE 11-2. Area / number ratio of the cotton cloth 3 weeks after application of the cream containing extract.

TABLE 11-3. Relative reduction in cotton area / number 3 weeks after application of extract-containing cream (unit%)

As shown in the above experimental results (Table 10-1), the cream containing one or more kinds of extracts of potent, peony, Gardenia and K. koji extract strongly and remarkably inhibits the activity of 5 alpha-reductase than the other one. For rabbit clinical trials containing creams with 1% by weight of each extract (Tables 11-1, 11-2 and 11-3), compared to the control (left ear with cream without extract) All showed excellent cotton reducing effect. According to the above results, in the case of the cream containing one or more kinds of extracts of active, red, and gardenia and jangjang-geun, if the total extract content of the face wash is less than 0.01% by weight, the degree of inhibiting the activity of 5 alpha-reductase is all It was evaluated to be somewhat low, and in the case of more than 10% by weight, the activity inhibition rate was excellent, but the workability and stability were more difficult. Therefore, the cream according to the present invention containing at least one activity, red pepper, gardenia and ephedra root extract has an activity inhibition rate of 5 alpha-reductase, a workability and stability of the product in the total content of the extract ranges from 0.01 to 10% by weight. This appeared to be very excellent

Therefore, according to the present invention, facial cleansers, soaps, and creams containing one or two or more extracts of potent, red peony, gardenia and K. koji are evaluated to be excellent in preventing and treating acne.

Claims (2)

Cleansing, soap or cream composition for acne prevention and treatment, characterized in that it contains 0.01 to 10% by weight of one or two or more dry powders selected from the group consisting of active, gardenia and ephedra root extract. The composition of claim 1, further comprising 0.01 to 10% by weight of a dry powder of the red peony.