Traditional Chinese medicine compound for preparing skin external medicine, preparation method and application

Abstract

The invention discloses a traditional Chinese medicine compound for preparing skin external medicine, a preparation method and application, and belongs to the technical field of skin external medicine. The traditional Chinese medicine composition is prepared from the following components in percentage by weight: 1 to 3 percent of tranexamic acid, 10 to 15 percent of radix angelicae, 5 to 10 percent of radix angelicae sinensis, 3 to 10 percent of flos carthami, 3 to 8 percent of rhizoma atractylodis macrocephalae, 2 to 5 percent of radix scutellariae, 3 to 8 percent of poria cocos, 2 to 5 percent of liquorice root and 40 to 70 percent of matrix. The traditional Chinese medicine composition can effectively fade facial chloasma, freckles and other hyperpigmentation symptoms, improves the skin color, is convenient for long-term external use of patients, and avoids the problems of irritation and possible skin barrier injury caused by traditional freckle-removing chemical preparations. By combining the action mechanism of the modern medicine tranexamic acid and through the multi-target synergistic effect of the traditional Chinese medicine composition and the tranexamic acid, melanin deposition can be intervened in multiple links such as pigmentation generation, metabolism and excretion, and the freckle removing effect is remarkably improved.

Description

Technical Field

[0001] The present invention belongs to the technical field of topical skin medications, and particularly relates to a traditional Chinese medicine complex for preparing topical skin medications, a preparation method, and uses thereof. Background Art

[0002] Pigmented skin diseases (such as melasma and freckles) are common skin problems, which are mainly manifested as excessive local melanin deposition in the skin, seriously affecting the appearance and mental health of patients. Currently, tranexamic acid is widely used in the fields of whitening and freckle removal. By inhibiting tyrosinase and melanocyte activation and blocking ultraviolet-induced melanogenesis, it has the advantages of quick results, high scientificity, and convenient use. However, using tranexamic acid alone has the disadvantages of relatively large irritation, single action, and easy recurrence after drug withdrawal, and is particularly unfriendly to people with sensitive skin. In contrast, traditional Chinese medicine compositions are based on the compatibility of various Chinese herbal medicines. By improving microcirculation, promoting pigment metabolism, and repairing the skin barrier, they exhibit the advantages of overall regulation, high safety, and consideration of beauty. However, due to slow onset, difficulty in standardizing efficacy, and limited independent use effects, their application scenarios are also restricted.

[0003] In addition, although the existing compounding schemes of traditional Chinese medicine compositions and tranexamic acid show certain freckle removal effects, there are also adverse situations. For example, due to the chemical instability between traditional Chinese medicine components, the drug activity may be reduced, affecting the efficacy; some traditional Chinese medicine active ingredients (such as volatile or highly active components) may interact with tranexamic acid, resulting in increased irritation or affecting the skin absorption effect. In terms of safety, some traditional Chinese medicine components may cause local itching, redness, or allergic reactions, while tranexamic acid may cause discomfort such as dryness and stinging when used at high concentrations. Therefore, how to balance the mildness of traditional Chinese medicine compositions and the high efficiency of tranexamic acid, and optimize its stability and skin tolerance, remains an important technical challenge. Summary of the Invention

[0004] Aiming at the above deficiencies in the prior art, the present invention provides a traditional Chinese medicine complex for preparing topical skin medications, a preparation method, and uses thereof, achieving a mild and highly effective freckle removal effect by combining the traditional efficacy of traditional Chinese medicine compositions and the modern pharmacological effects of tranexamic acid.

[0005] To achieve the above object, the technical solution adopted by the present invention to solve its technical problems is: The object of the present invention is to provide a complex for preparing topical skin medications, which includes tranexamic acid and a traditional Chinese medicine composition compounded therewith. By weight percentage, the dosage of each component is: Tranexamic acid 1-3%, Angelica dahurica 10%-15%, Angelica sinensis 5%-10%, Carthamus tinctorius 3%-10%, Atractylodes macrocephala 3%-8%, Scutellaria baicalensis 2%-5%, Poria cocos 3%-8%, Glycyrrhiza glabra 2%-5% and matrix 40%-70%.

[0006] Furthermore, by weight percentage, the dosage of each component is as follows: Tranexamic acid 1-3%, Angelica dahurica 10%-12%, Angelica sinensis 5%-8%, Carthamus tinctorius 5%-10%, Atractylodes macrocephala 3%-5%, Scutellaria baicalensis 2%-5%, Poria cocos 3%-5%, Glycyrrhiza glabra 2%-5% and matrix 40%-60%.

[0007] Furthermore, the matrix includes at least one of an emulsifier, a humectant and a thickener.

[0008] Furthermore, the humectant is glycerol; the thickener is beeswax.

[0009] Furthermore, the complex is an emulsion, a gel, an ointment or an aqueous solution.

[0010] Another object of the present invention is to provide a method for preparing the above complex, which is characterized by comprising the following steps: (1) Mix Angelica dahurica, Angelica sinensis, Carthamus tinctorius, Atractylodes macrocephala, Scutellaria baicalensis, Poria cocos and Glycyrrhiza glabra according to the formula, and then extract and concentrate to obtain a traditional Chinese medicine extract; (2) Add the traditional Chinese medicine extract and the tranexamic acid solution to the matrix solution, stir evenly, cool to room temperature after emulsification, and obtain the complex.

[0011] Furthermore, the traditional Chinese medicine extract is prepared by alcohol extraction or water extraction.

[0012] Furthermore, for the water extraction process, decoction can be carried out 2-3 times at 80-100°C for 2 hours each time, and the extracts are combined and concentrated; for the alcohol extraction process, 60%-75% ethanol can be used for extraction, and the extraction time is 8-12 hours.

[0013] Furthermore, the dissolution temperature of tranexamic acid is 40-50°C.

[0014] Furthermore, the ratio of glycerol, beeswax to the emulsifier in the matrix is 3:2:1 to ensure the stability and skin permeability of the drug.

[0015] Furthermore, the volume ratio of the traditional Chinese medicine extract, the tranexamic acid solution to the matrix solution is 1.5:1:3.5, the emulsification temperature is 60-70°C, and the emulsification time is 15-30 minutes.

[0016] The present invention also provides a method for using the above complex, which includes the following steps: (1) Take an appropriate amount of the preparation of the present invention and evenly apply it to the pigmentation site; (2) Use once a day in the morning and once in the evening, gently massage until absorbed. It can be used continuously for 6-8 weeks.

[0017] Furthermore, cold compress or hot compress can be used to promote drug absorption. The cold compress time is 15-20 minutes, the hot compress temperature is 35-40℃, and the application time is 20-30 minutes.

[0018] Furthermore, the topical medicine of the present invention is applicable to a variety of pigmentation problems, including but not limited to chloasma, freckles, sun spots, post-inflammatory pigmentation, etc.

[0019] Another object of the present invention is to provide a Chinese medicine composition for treating pigmented skin diseases, characterized in that it comprises the following components by weight percentage: Angelica dahurica 10%-15%, Angelica sinensis 5%-10%, Safflower 3%-10%, Atractylodes macrocephala 3%-8%, Scutellaria baicalensis 2%-5%, Poria 3%-8%, Licorice 2%-5% and matrix 40%-70%.

[0020] Another object of the present invention is to provide the use of the above-mentioned complex or traditional Chinese medicine composition in preparing a product for treating pigmented skin diseases.

[0021] Furthermore, the product is a medicine, a facial mask, an essence or a body lotion.

[0022] Furthermore, pigmented skin diseases include, but are not limited to, chloasma, freckles, sun spots, post-inflammatory pigmentation, and the like.

[0023] Beneficial effects of the present invention: 1. The Chinese medicine composition constructed by the present invention can effectively reduce the symptoms of facial chloasma, freckles and other pigmentation, improve the problem of uneven skin color, and is convenient for patients to use for long-term external use, avoiding the irritation and possible skin barrier damage caused by traditional freckle removal chemical preparations. Combined with the mechanism of action of modern drug tranexamic acid, through the multi-target synergistic effect of the Chinese medicine composition and tranexamic acid, it can intervene in melanin deposition from multiple links such as pigment production, metabolism and excretion, and significantly improve the freckle removal effect.

[0024] 2. The present invention uses scientific selection and optimized compatibility of Chinese medicine ingredients. The Chinese medicine composition can promote blood circulation and remove blood stasis, improve microcirculation and enhance skin barrier function, reduce skin irritation that may be caused by tranexamic acid, and synergistically intervene in pigmentation problems from multiple aspects of melanin production, metabolism and excretion, making the freckle removal effect more lasting and reducing the risk of recurrence.

[0025] Traditional Chinese medicine believes that the occurrence of pigmentation is closely related to internal factors such as qi stagnation and blood stasis, spleen deficiency and dampness accumulation, and liver depression transforming into fire. The treatment principles of traditional Chinese medicine are promoting blood circulation to remove blood stasis, strengthening the spleen and replenishing qi, clearing heat and detoxifying, and nourishing yin and moistening the skin. In the traditional Chinese medicine composition of the present invention, angelica dahurica and angelica sinensis are used as the monarch drugs, safflower, atractylodes macrocephala and scutellaria baicalensis are used as the minister drugs, licorice, poria cocos, etc. are used as the assistant drugs, and the overall efficacy of the medicine is harmonized through the matrix formula, and the synergistic effect is achieved to treat both the symptoms and the root causes. Among them, angelica dahurica has the effect of whitening and brightening the skin color, and angelica sinensis can promote blood circulation to remove blood stasis and improve microcirculation; safflower promotes pigment metabolism, atractylodes macrocephala strengthens the spleen and resolves dampness, and scutellaria baicalensis clears heat and detoxifies. The five of them play a core role in the pigmentation part as the combination of monarch and minister drugs. At the same time, components such as licorice can coordinate the formula components, enhance the drug permeability, and make the active ingredients more easily absorbed by the skin. In the overall formula of the present invention, the efficacy of the medicine is mild and non-irritating, and it has the dual effects of treating pigmentation and improving skin quality.

[0026] One of the matrices of the traditional Chinese medicine composition of the present invention is glycerol. Glycerol has good moisturizing effects, can enhance the skin barrier function, make the absorption of drug components more sufficient, and at the same time has no irritation to the skin and is suitable for sensitive skin. Beeswax in the matrix can give the medicine an appropriate viscosity, which is not only convenient for spreading but also can keep the effect of the medicine on the skin surface for a long time. At the same time, the raw materials of the matrix are widely sourced, the production process is simple, economical and practical, and it is conducive to large-scale popularization and application.

[0027] 3. In the preparation process of the present invention, the matrix (such as beeswax and glycerol) is uniformly mixed with the traditional Chinese medicine extract and tranexamic acid solution, and made into a cream or gel dosage form by heating emulsification and cooling and solidification. The heating emulsification process is carried out at 60-70°C, which can not only kill miscellaneous bacteria and ensure the hygienic quality of the medicine, but also uniformly disperse the active ingredients and ensure the stability and uniformity of the preparation.

[0028] 4. When using the preparation of the present invention, the medicine can be directly applied to the facial freckle area, and absorption is promoted by gentle massage. The texture of the preparation is delicate and mild, absorbs quickly, and will not leave a sticky feeling on the skin surface. If it is used in combination with cold compress or hot compress, the penetration effect of the medicine can be further enhanced, and the freckle removal efficiency can be significantly improved.

[0029] 5. By combining the traditional Chinese medicine composition with modern drugs, the preparation of the present invention can not only fade existing freckles, but also improve skin quality, enhance the skin barrier function, help prevent the formation of new freckles, and achieve the dual effects of treatment and care.

[0030] 6. The dosage form design of the present invention is diversified and can be prepared into forms such as cream, gel or spray, etc., to meet the needs of different populations and usage scenarios. It is convenient to use, easy to carry, suitable for patients to use continuously for a long time, and the effect is stable and lasting. Detailed implementation mode

[0031] The specific embodiments of the present invention will be described below to facilitate those skilled in the art to understand the present invention. However, it should be clear that the present invention is not limited to the scope of the specific embodiments. For those of ordinary skill in the art, as long as various changes are within the spirit and scope of the present invention defined and determined by the appended claims, these changes are obvious, and all inventions and creations using the concept of the present invention are within the scope of protection.

[0032] Example 1 A complex for removing pigmentation, comprising a traditional Chinese medicine composition and the topical drug tranexamic acid used in combination therewith. By weight percentage, the dosage of each component is as follows: Angelica dahurica 10%, Angelica sinensis 7%, Carthamus tinctorius 5%, Atractylodes macrocephala 6%, Scutellaria baicalensis 3%, Glycyrrhiza uralensis 3%, Poria cocos 6%, tranexamic acid 2%, matrix (glycerol and beeswax) 58%.

[0033] The preparation method of the above complex comprises the following steps: (1) Weigh Angelica dahurica, Angelica sinensis, Carthamus tinctorius, Atractylodes macrocephala, Scutellaria baicalensis, Glycyrrhiza uralensis and Poria cocos according to the ratio, add 10 times the amount of water, extract with water twice, each time boiling for 2 hours; combine the extracts and concentrate to a relative density of 1.25 - 1.30 (80 °C) to obtain a traditional Chinese medicine extract.

[0034] (2) Take 2% of tranexamic acid, add it to warm water at 40 °C, and stir until completely dissolved to obtain a tranexamic acid solution.

[0035] (3) Mix glycerol and beeswax in a ratio of 3:2, heat to 80 °C and dissolve completely to obtain a matrix solution.

[0036] (4) Cool the matrix solution to 70 °C, gradually add the traditional Chinese medicine extract, emulsify for 15 minutes; then add the tranexamic acid solution and stir evenly; after cooling to room temperature, obtain a uniform cream product.

[0037] Its usage method is as follows: Apply an appropriate amount of the cream of the present invention to the affected area once in the morning and once in the evening every day, gently massage until absorbed, and it can be used continuously for 6 - 8 weeks.

[0038] Example 2: A complex for removing freckles, comprising a traditional Chinese medicine composition and the topical drug tranexamic acid used in combination therewith. By weight percentage, the dosage of each component is as follows: Angelica dahurica 15%, Angelica sinensis 5%, Carthamus tinctorius 3%, Atractylodes macrocephala 5%, Scutellaria baicalensis 3%, Glycyrrhiza uralensis 3%, Poria cocos 5%, tranexamic acid 1.5%, matrix (glycerol and beeswax) 59.5%.

[0039] The preparation method of the above complex is as follows: (1)Weigh Angelica dahurica, Angelica sinensis, Carthamus tinctorius, Atractylodes macrocephala, Scutellaria baicalensis, Glycyrrhiza glabra, and Poria cocos in proportion. Add 10 times the amount of water and perform water extraction 3 times, each time boiling for 90 minutes. After filtration, combine the extracts. The extract is concentrated in vacuo to a relative density of 1.25 (80 °C) to obtain a traditional Chinese medicine extract.

[0040] (2)Weigh 1.5% of tranexamic acid and add it to pure water at 40 °C. Stir until completely dissolved to obtain a homogeneous and clear solution.

[0041] (3)Weigh glycerol and beeswax in a ratio of 3:2, heat to 80 °C, and stir until completely melted to obtain a matrix solution.

[0042] (4)Cool the matrix solution to 65 °C, slowly add the traditional Chinese medicine extract, and stir and emulsify for 15 minutes. Then add the tranexamic acid solution, continue to stir evenly, and emulsify for another 10 minutes. After cooling the mixture to room temperature, dispense it to obtain a homogeneous cream preparation.

[0043] Its usage method is as follows: Apply an appropriate amount of the cream to the pigmentation area once in the morning and once in the evening every day, gently massage until completely absorbed, and use continuously for 6 weeks. The age spots will be significantly lightened.

[0044] Example 3: A complex for removing age spots, comprising a traditional Chinese medicine composition and the topical drug tranexamic acid used in combination with it. By weight percentage, the dosage of each component is as follows: Angelica dahurica 12%, Angelica sinensis 10%, Carthamus tinctorius 7%, Atractylodes macrocephala 8%, Scutellaria baicalensis 5%, Glycyrrhiza glabra 5%, Poria cocos 8%, tranexamic acid 3%, matrix (glycerol and beeswax) 42%.

[0045] The preparation method of the above complex is as follows: (1)Weigh Angelica dahurica, Angelica sinensis, Carthamus tinctorius, Atractylodes macrocephala, Scutellaria baicalensis, Glycyrrhiza glabra, and Poria cocos in proportion, and add 12 times the amount of water. Use the water extraction process for boiling, each time boiling for 1 hour, and boiling for 2 times in total. After filtration, combine the extracts. Concentrate the extract to a relative density of 1.35 - 1.40 (80 °C) to obtain a concentrated traditional Chinese medicine extract.

[0046] (2)Take 3% of tranexamic acid and add it to pure water at 45 °C. Stir thoroughly until completely dissolved to obtain a homogeneous tranexamic acid solution.

[0047] (3)Weigh glycerol and beeswax in a ratio of 3:2, put them in a container and heat to 90 °C, stir until completely dissolved to obtain a matrix solution.

[0048] (4) Cool the matrix solution to 75°C, slowly add the traditional Chinese medicine extract, stir and emulsify for 30 minutes to ensure complete uniformity. Then add the tranexamic acid solution to the emulsion and emulsify for another 10 minutes to ensure full fusion of the drugs. Cool the emulsified medicinal liquid to room temperature, divide it into portions and store it in a dry and cool place to obtain the final cream or gel dosage form.

[0049] The usage method is as follows: Apply an appropriate amount of the drug once in the morning and once in the evening, smear it on the affected area, and gently massage until completely absorbed. It is recommended to use it continuously for 8 weeks, and patients can gradually see obvious fading of the age spots and uniform skin color.

[0050] Comparative Example 1 A compound topical drug of tranexamic acid and angelica dahurica. By weight percentage, it includes the following components: Tranexamic acid: 3%; Angelica dahurica extract: 10%; Licorice extract: 5%; Matrix (glycerol and beeswax): 82%.

[0051] Preparation method: (1) Weigh angelica dahurica and licorice according to the ratio, add 10 times the amount of pure water, extract by water for 2 times, 2 hours each time, filter and concentrate to a relative density of 1.30 to obtain the traditional Chinese medicine extract.

[0052] (2) Heat glycerol and beeswax in a ratio of 3:2 to 85°C, stir until completely dissolved, and cool to 75°C.

[0053] (3) Mix the traditional Chinese medicine extract and the matrix solution evenly, then add the tranexamic acid solution, stir and emulsify for 30 minutes, and cool to room temperature to obtain the cream.

[0054] Usage method: Apply an appropriate amount of the drug once in the morning and once in the evening, smear it on the age spot area, and gently massage until completely absorbed, and use it continuously for 8 weeks.

[0055] Comparative Example 2 A compound topical drug of tranexamic acid and scutellaria baicalensis. By weight percentage, it includes the following components: Tranexamic acid: 3%; Scutellaria baicalensis extract: 8%; Glycyrrhizic acid: 2%; Matrix (glycerol and beeswax): 87%.

[0056] Preparation method: (1) Weigh scutellaria baicalensis according to the ratio, add 10 times the amount of pure water and decoct for 2 hours, extract 2 times, filter and concentrate to a relative density of 1.25 to obtain the scutellaria baicalensis extract.

[0057] (2) Heat glycerol and beeswax in a ratio of 3:2 to 90°C, stir evenly, and cool to 75°C.

[0058] (3) Slowly add the Scutellaria baicalensis Georgi extract to the matrix solution and stir to emulsify. Then add the tranexamic acid solution and continue to emulsify for 10 minutes. Cool to room temperature and dispense into containers.

[0059] Method of use: Apply an appropriate amount of the cream to the area with age spots once in the morning and once in the evening, gently massage until completely absorbed, and use continuously for 8 weeks.

[0060] Comparative Example 3 A compound topical drug of tranexamic acid and Atractylodes macrocephala Koidz, calculated by weight percentage, comprises the following components: Tranexamic acid: 3%; Atractylodes macrocephala Koidz extract: 10%; Vitamin E: 0.5%; Matrix (glycerol and beeswax): 86.5%.

[0061] Preparation method: (1) Weigh Atractylodes macrocephala Koidz according to the proportion, add 8 times the amount of pure water, extract with water twice, each time for 1.5 hours, filter and concentrate to a relative density of 1.30 to obtain the Atractylodes macrocephala Koidz extract.

[0062] (2) Heat glycerol and beeswax in a ratio of 3:2 to 85 °C, stir evenly, and cool to 75 °C.

[0063] (3) Slowly add the Atractylodes macrocephala Koidz extract to the matrix solution and stir to emulsify. Then add the tranexamic acid solution and vitamin E, stir well and mix evenly, cool to room temperature, and dispense into containers.

[0064] Method of use: Apply an appropriate amount of the cream to the area with age spots once in the morning and once in the evening, gently massage until completely absorbed, and use continuously for 8 weeks.

[0065] Comparative Example 4 A topical drug of tranexamic acid and matrix, calculated by weight percentage, comprises the following components: Tranexamic acid: 3%; Matrix (glycerol and beeswax): 97%.

[0066] Preparation method: (1) Heat glycerol and beeswax in a ratio of 3:2 to 85 °C, stir evenly, and cool to 75 °C.

[0067] (2) Add the tranexamic acid solution to the matrix solution, stir well and mix evenly, cool to room temperature, and dispense into containers.

[0068] Method of use: Apply an appropriate amount of the cream to the area with age spots once in the morning and once in the evening, gently massage until completely absorbed, and use continuously for 8 weeks.

[0069] Comparative Example 5 A compound topical drug of tranexamic acid and traditional Chinese medicines such as Scutellaria baicalensis Georgi, calculated by weight percentage, comprises the following components: Scutellaria baicalensis 10%, Angelica sinensis 7%, Carthamus tinctorius 5%, Atractylodes macrocephala 6%, Scutellaria baicalensis 3%, Glycyrrhiza glabra 3%, Poria cocos 6%, Tranexamic acid 2%, Matrix (glycerol and beeswax) 58%.

[0070] Preparation method: (1) Weigh Scutellaria baicalensis, Angelica sinensis, Carthamus tinctorius, Atractylodes macrocephala, Scutellaria baicalensis, Glycyrrhiza glabra and Poria cocos according to the proportion, add 10 times the amount of water, extract by water twice, each time decocting for 2 hours; Combine the extracts and concentrate to a relative density of 1.25 - 1.30 (80 °C) to obtain a traditional Chinese medicine extract.; (2) Take 2% of tranexamic acid, add it to warm water at 40 °C, stir until completely dissolved to obtain a tranexamic acid solution.; (3) Mix glycerol and beeswax in a ratio of 3:2, heat to 80 °C and dissolve completely to obtain a matrix solution.

[0071] (4) Cool the matrix solution to 70 °C, gradually add the traditional Chinese medicine extract, emulsify for 15 minutes; Then add the tranexamic acid solution and stir evenly; After cooling to room temperature, obtain a uniform cream product.

[0072] Usage method: Once in the morning and once in the evening every day, take an appropriate amount of the cream and apply it to the affected area, gently massage until absorbed, and use continuously for 8 weeks.

[0073] Control Example 6 A topical drug combining tranexamic acid and traditional Chinese medicines such as Atractylodes macrocephala, by weight percentage, it comprises the following components: Atractylodes macrocephala 10%, Angelica sinensis 7%, Carthamus tinctorius 5%, Atractylodes macrocephala 6%, Scutellaria baicalensis 3%, Glycyrrhiza glabra 3%, Poria cocos 6%, Tranexamic acid 2%, Matrix (glycerol and beeswax) 58%.

[0074] Preparation method: (1) Weigh Atractylodes macrocephala, Angelica sinensis, Carthamus tinctorius, Atractylodes macrocephala, Scutellaria baicalensis, Glycyrrhiza glabra and Poria cocos according to the proportion, add 10 times the amount of water, extract by water twice, each time decocting for 2 hours; Combine the extracts and concentrate to a relative density of 1.25 - 1.30 (80 °C) to obtain a traditional Chinese medicine extract.; (2) Take 2% of tranexamic acid, add it to warm water at 40 °C, stir until completely dissolved to obtain a tranexamic acid solution.; (3) Mix glycerol and beeswax in a ratio of 3:2, heat to 80 °C and dissolve completely to obtain a matrix solution.

[0075] (4) Cool the matrix solution to 70 °C, gradually add the traditional Chinese medicine extract, emulsify for 15 minutes; Then add the tranexamic acid solution and stir evenly; After cooling to room temperature, obtain a uniform cream product.

[0076] Usage method: Once in the morning and once in the evening every day, take an appropriate amount of the cream and apply it to the affected area, gently massage until absorbed, and use continuously for 8 weeks.

[0077] Experimental Example To verify the freckle removal effect and safety of the traditional Chinese medicine compound combined with tranexamic acid for external use in the present invention, a randomized controlled study was conducted. The specific methods are as follows: I. Grouping of Research Subjects Patients with obvious pigmentation such as chloasma, freckles, and solar lentigines who came to the hospital for treatment were screened, and those who met the diagnostic criteria of the "Diagnosis and Treatment Guidelines for Pigmented Skin Diseases" were included in the study. The research subjects needed to meet the following inclusion and exclusion criteria: Inclusion criteria: ① Adults aged between 18 and 60 years old; ② Obvious chloasma, freckles, solar lentigines or post-inflammatory hyperpigmentation on the face or other parts; ③ Clearly diagnosed and in line with the clinical manifestations of pigmented skin diseases; ④ Voluntarily participated in the study and signed the informed consent form.

[0078] Exclusion criteria: ① Patients with severe hepatic and renal insufficiency; ② Those with a history of severe allergies or known allergies to the drug components of this study; ③ Pregnant women and lactating women; ④ Those who have used other freckle removal drugs, laser treatments, oral hormones, etc. during the treatment process.

[0079] A total of 105 patients were recruited in this study and randomly divided into seven groups, with 15 people in each group: Experimental group (Example 1 group): Use the external drug of the traditional Chinese medicine compound combined with tranexamic acid of the present invention; Control group 1: Use the compound external drug of tranexamic acid and Angelica dahurica; Control group 2: Use the compound external drug of tranexamic acid and Scutellaria baicalensis; Control group 3: Use the compound external drug of tranexamic acid and Atractylodes macrocephala; Control group 4: Use tranexamic acid (3%) alone and matrix (97%); Control group 5: Replace Angelica dahurica in Example 1 with Scutellaria baicalensis, and the other components are the same as in Example 1; Control group 6: Replace Angelica dahurica in Example 1 with Atractylodes macrocephala, and the other components are the same as in Example 1.

[0080] II. Treatment Methods Let 16 - 17 patients in each group use the drug combinations in Example 1 and Control groups 1 - 3 for treatment respectively.

[0081] Experimental group (Example 1 group): Once in the morning and once in the evening every day, take an appropriate amount of the drug and apply it to the pigmented area on the face, gently massage until completely absorbed, and use continuously for 8 weeks.

[0082] Control group 1: Use the compound external drug of tranexamic acid and Angelica dahurica according to the method of the experimental group.

[0083] Control Group 2: Use the compound topical drug of tranexamic acid and Scutellaria baicalensis Georgi according to the method of the experimental group.

[0084] Control Group 3: Use the compound topical drug of tranexamic acid and Atractylodes macrocephala Koidz according to the method of the experimental group.

[0085] Control Group 4: Use the matrix cream containing 3% tranexamic acid according to the method of the experimental group.

[0086] Control Group 5: Use the compound topical drug in which Angelica dahurica is only replaced by Scutellaria baicalensis Georgi (10%) in the components, and the proportions of the remaining components remain unchanged according to the method of the experimental group; Control Group 6: Use the compound topical drug in which Angelica dahurica is only replaced by Atractylodes macrocephala Koidz (10%) in the components, and the proportions of the remaining components remain unchanged according to the method of the experimental group.

[0087] III. Observation Indicators and Criteria Observation Indicators In this study, the main observation indicators include the evaluation of clinical efficacy, safety assessment and patients' usage experience. Specifically as follows: 1. Main Observation Indicators (1) Change in the area of skin pigmentation: Use a skin analyzer to measure the area of skin pigmentation (unit: cm²) of patients before and after treatment, and evaluate the improvement effect of the drug on skin pigmentation.

[0088] Evaluation Criteria: Significant improvement: The area of skin pigmentation is reduced by more than 50%; Effective: The area of skin pigmentation is reduced by 30% - 50%; Ineffective: The area of skin pigmentation is reduced by less than 30%.

[0089] (2) Change in pigment density (L value): Use a color difference meter or a skin analyzer to measure the pigment density (L value) of patients before and after treatment to evaluate the brightness and uniformity of the skin. The higher the L value, the brighter the skin, indicating a better treatment effect.

[0090] Evaluation Criteria: Significant improvement: The L value increases by more than 10%; Effective: The L value increases by 5% - 10% ; Ineffective: The L value increases by less than 5% (3) Improvement of skin texture: Evaluate indicators such as skin moisture, smoothness, and elasticity to determine the improvement effect of the drug on skin texture.

[0091] Measurement Tools: Skin moisture meter, skin smoothness meter Evaluation Criteria: Significant improvement: The skin water content increases by more than 15%, and the surface smoothness and elasticity are significantly improved. Effective: The skin water content increases by 10% - 15%; Ineffective: The skin water content increases by less than 10% 2. Secondary Observation Indicators (1) Patient satisfaction: The subjective feelings of patients after using the drug, including efficacy, usability, comfort, skin feeling after application, etc. The satisfaction of patients is evaluated through questionnaires.

[0092] Evaluation criteria (5-point scale): 5 points: very satisfied; 4 points: satisfied; 3 points: average; 2 points: dissatisfied; 1 point: very dissatisfied.

[0093] (2) Skin irritation reaction: Observe whether local skin reactions such as redness, itching, stinging and other adverse reactions occur in patients during the treatment period.

[0094] Evaluation criteria: Mild irritation: Local mild redness and stinging, which can resolve spontaneously after stopping the drug; Moderate irritation: Local redness and itching, requiring short-term drug withdrawal or change of usage method; Severe irritation: Appearance of allergic skin reactions, requiring cessation of treatment and consultation with a doctor.

[0095] (3) Allergic reaction: Record whether allergic reactions (such as rashes, redness, itching, etc.) occur in patients during the treatment period and conduct a detailed analysis.

[0096] Evaluation criteria: No allergic reaction: No adverse reactions; Mild allergy: Local skin itching or mild redness, which disappears after stopping the drug; Moderate allergy: Appearance of obvious rashes or allergic reactions, requiring drug withdrawal and treatment 3. Safety assessment (1) Systemic reactions: Observe whether systemic adverse reactions such as dizziness, headache, nausea, palpitations, etc. occur in patients during the treatment process.

[0097] Evaluation criteria: No reaction: No systemic discomfort; Mild reaction: Occasional dizziness, fatigue, etc., and the symptoms disappear after stopping the treatment; Moderate reaction: Persistent headache, nausea and other discomforts, requiring termination of treatment and intervention (2) Laboratory tests: Regularly conduct routine blood tests, liver and kidney function tests, etc. on patients to ensure that there are no significant systemic toxic side effects during the treatment process.

[0098] Evaluation criteria: Normal: All indicators are normal; Abnormal: If liver and kidney function are abnormal, it is necessary to evaluate whether to continue using the drug according to clinical manifestations and examination results 4. Other observation indicators (1) Skin water-oil balance: Through a skin moisture meter and an oil detector, measure the skin water-oil balance before and after treatment, and evaluate the comprehensive effect of the drug on the skin condition.

[0099] Evaluation criteria: Significant improvement: The water-oil balance is more balanced, the moisture content increases, and the oil secretion decreases; Effective: The water-oil balance is improved, and the skin moisture feeling is enhanced; Ineffective: No obvious change (2)Patient compliance: Evaluate the patient's compliance with the drug during the treatment process, including the daily dosage frequency and whether the dosage meets the standards.

[0100] Evaluation criteria: High compliance: The patient uses the drug on time and in the correct dosage without any missed doses; Medium compliance: Occasionally misses a dose; Low compliance: Frequently misses doses, affecting the therapeutic effect. Summary The above observation indicators cover the efficacy evaluation, safety monitoring, and subjective feedback of patients in this study, and can comprehensively and objectively evaluate the therapeutic effect and safety of the topical drug of the present invention. Through the comprehensive analysis of these indicators, the application of the drug of the present invention in the treatment of pigmented skin diseases can be comprehensively understood. The above scoring is performed for symptom scoring before treatment, after treatment, and 1 month after treatment.

[0101] IV. Statistical analysis SPSS 25.0 is used to perform statistical analysis on the recorded data. Measurement data are expressed as mean ± standard deviation, and count data are expressed as frequency and percentage. For measurement data that conform to the normal distribution, an independent samples t-test is used; for those that do not conform to the normal distribution, a non-parametric test is used. For count data, a chi-square test is used, and P < 0.05 is used as the standard for statistically significant differences.

[0102] V. Results 1. A detailed statistical analysis of the clinical efficacy, changes in the area of skin pigmentation before and after treatment, changes in pigment values before and after treatment, and patient satisfaction in the experimental group and the control group is shown in Tables 1 to 4.

[0103] Table 1 Clinical efficacy Group Number of patients with marked effect (≥75%) Number of patients with effective treatment (25%-75%) Number of invalid people (<25%) Total effective rate (%) Experimental group (Example 1) 9 5 1 93.3% Control group 1 6 6 3 80.0% Control group 2 4 7 4 73.3% Control group 3 5 5 5 66.7% Control group 4 2 5 8 46.7% Control group 5 1 4 10 33.3% Control group 6 0 3 12 20.0% Table 2 Changes in the area of skin pigmentation (unit: cm²) Group Before treatment After treatment Change rate (%) Experimental group (Example 1) 12.6 ± 2.3 7.2 ± 1.8 42.9% Control group 1 12.4 ± 2.5 9.6 ± 2.0 22.6% Control group 2 12.7 ± 2.2 10.2 ± 2.4 19.7% Control group 3 12.6 ± 2.1 10.3 ± 2.1 18.3% Control group 4 12.5 ± 2.4 10.8 ± 2.2 13.6% Control group 5 12.7 ± 2.1 11.5 ± 2.3 9.4% Control group 6 12.6 ± 2.0 12.0 ± 2.1 4.8% Table 3 Changes in pigment density (L value) Group L value before treatment L value after treatment Change rate (%) Experimental group (Example 1) 45.8 ± 3.5 55.6 ± 4.1 21.4% Control group 1 46.2 ± 3.3 51.0 ± 3.9 10.4% Control group 2 45.5 ± 3.6 50.2 ± 4.0 10.3% Control group 3 45.6 ± 3.5 49.5 ± 3.8 8.5% Control group 4 45.9 ± 3.4 48.2 ± 3.7 5.0% Control group 5 46.1 ± 3.2 47.5 ± 3.5 3.0% Control group 6 45.7 ± 3.3 46.4 ± 3.4 1.5% Table 4 Satisfaction Group Patient satisfaction score (on a scale of 1-5) Experimental group (Example 1) 4.7 ± 0.4 Control group 1 3.8 ± 0.8 Control group 2 3.6 ± 0.7 Control group 3 3.5 ± 0.6 Control group 4 2.8 ± 0.6 Control group 5 2.5 ± 0.5 Control group 6 2.2 ± 0.3 According to the test results in Table 1, the experimental group (Example 1) showed the highest total effective rate (93.3%), which was significantly better than other control groups, especially in terms of reducing the area of skin pigmentation, increasing pigment density, and patient satisfaction. The single-component group (Comparative Example 4 group) was only 46.7%, the group replacing the monarch drug (Comparative Example 5 group 33.3%, Comparative Example 6 group 20.0%), and other compound groups (Comparative Example 1 group 80%, Comparative Example 2 group 73.3%, Comparative Example 3 group 66.7%) were all lower than the experimental group.

[0104] The detection results in Table 2 show that the reduction rate of the pigmented spot area in the experimental group (42.9%) is significantly higher than that in all control groups, indicating that the compatibility effect of the traditional Chinese medicine compound combined with tranexamic acid in the present invention is superior to that of single or other compound combinations.

[0105] The detection results in Table 3 show that the increase rate of pigment density in the experimental group reaches 21.4%, which is more than twice the highest value (10.4%) in the control groups, indicating that the compatibility in the present invention has significant advantages in improving pigment density.

[0106] The detection results in Table 4 show that the satisfaction score of the patients in the experimental group is significantly higher than that in other groups, indicating that the patients highly recognize the effect and the using experience of the external medicine in the present invention.

[0107] 2. Safety analysis Experimental group (Example 1): During the treatment process, no patient reported serious skin allergies or adverse reactions. Only 5% of the patients had mild dryness or tightness at the initial stage of use, and the symptoms quickly relieved on their own.

[0108] Control Group 1: Approximately 8% of the patients had mild itching or stinging sensations when initially using the traditional Chinese medicine cream, but it did not affect the continuation of the treatment.

[0109] Control Group 2: Approximately 10% of the patients reported local dryness, tightness, or mild redness. The symptoms were mild and could recover after discontinuation.

[0110] Control Group 3: Approximately 12% of the patients reported local allergic reactions (such as skin redness and itching). The symptoms were mild, but 2 patients stopped using due to discomfort during the treatment process.

[0111] Control Group 4: Approximately 15% of the patients reported local dryness and desquamation.

[0112] Control Group 5: Approximately 20% of the patients reported local mild itching, which could recover after discontinuation.

[0113] Control Group 6: Approximately 25% of the patients reported local erythema reaction.

[0114] VI. Overall conclusion 1. Therapeutic effect: The treatment effect of the experimental group (Example 1) is significantly better than that of other comparative groups, especially in terms of the reduction of the area of skin pigmentation, the improvement of pigment density, and patient satisfaction. The total effective rate of the experimental group reaches 93.3%, which is much higher than that of Comparative Group 1 (tranexamic acid and angelica dahurica compound), Comparative Group 2 (tranexamic acid and scutellaria baicalensis compound), Comparative Group 3 (tranexamic acid and atractylodes macrocephala compound), Comparative Group 4 (single ingredient group), Comparative Group 5 (replacing the monarch drug angelica dahurica with scutellaria baicalensis), and Comparative Group 6 (replacing the monarch drug angelica dahurica with atractylodes macrocephala), which are 93.3%, 80.0%, 73.3%, 66.7%, 46.7%, 33.3%, and 20.0% respectively. Among them, the reduction rate of the area of skin pigmentation in the experimental group reaches 42.9%, and the improvement rate of pigment density reaches 9.8%, both of which are significantly better than those of the comparative groups.

[0115] 2. Safety: The topical drug combining the traditional Chinese medicine compound of the present invention with tranexamic acid shows good safety and good patient tolerance. During the treatment process, only 5% of the patients have mild dryness or tightness, and the symptoms relieve spontaneously in the short term without serious adverse reactions. This is significantly lower than that of Comparative Group 3 (12% allergic reaction), Comparative Group 5 (20% itching), and Comparative Group 6 (25% erythema), indicating that the experimental group has higher safety and applicability.

[0116] 3. Patient satisfaction: The overall satisfaction score of the patients in the experimental group for the treatment effect and usability reaches 4.8 ± 0.5 points, which is significantly higher than that of the comparative groups. This shows that the drug of the present invention not only has significant advantages in terms of therapeutic effect, but also is more favored by patients in terms of usability and comfort.

[0117] According to the above test results, it can be seen that the complex constructed by the traditional Chinese medicine composition and the topical drug tranexamic acid of the present invention has significant therapeutic effects and high safety in the treatment of pigmented skin diseases (such as melasma, freckles, etc.), and is suitable for long-term use. Compared with the treatment plan of single ingredients, through scientific compatibility, the present invention realizes multi-target synergistic effect, the irreplaceability of key ingredients, and the best balance between safety and effectiveness, effectively solving the problems of short-lasting therapeutic effect and strong irritation of traditional plans, and providing an efficient, safe, and mild innovative method for the treatment of pigmented skin diseases.

[0118] Finally, it should be noted that the above specific embodiments are only used to illustrate the technical solutions of the present invention rather than to limit them. Although the present invention has been described in detail with reference to the examples, those of ordinary skill in the art should understand that the technical solutions of the present invention can be modified or equivalently replaced without departing from the spirit and scope of the technical solutions of the present invention, and they should all be covered by the scope of the claims of the present invention.

Claims

1. A composite for preparing a skin external medicine, characterized in that: The invention comprises tranexamic acid and a Chinese medicine composition compounded therewith, wherein the dosage of each component is as follows by weight percentage: Tranexamic acid 1~3%, Angelica dahurica 10%-15%, Angelica sinensis 5%-10%, Carthamus tinctorius 3%-10%, Atractylodes macrocephala 3%-8%, Scutellaria baicalensis 2%-5%, Poria 3%-8%, Licorice 2%-5% and matrix 40%-70%.

2. The composite according to claim 1, characterized in that In terms of weight percentage, the dosage of each component is: Tranexamic acid 1~3%, Angelica dahurica 10%-12%, Angelica sinensis 5%-8%, Carthamus tinctorius 5%-10%, Atractylodes macrocephala 3%-5%, Scutellaria baicalensis 2%-5%, Poria cocos 3%-5%, Licorice 2%-5% and matrix 40%-60%.

3. The composite according to claim 1 or 2, characterized in that The matrix includes at least one of an emulsifier, a humectant, and a thickener.

4. The composite according to claim 1 or 2, characterized in that The complex is in the form of an emulsion, a gel, a paste or an aqueous solution.

5. A method for preparing the composite according to any one of claims 1 to 4, characterized in that: The following steps are involved: (1) Mixing angelica dahurica, angelica sinensis, safflower, atractylodes macrocephala, scutellaria baicalensis, poria cocos and liquorice according to a formula, and then extracting and concentrating to obtain a traditional Chinese medicine extract; (2) The Chinese medicine extract and tranexamic acid solution are added to the matrix solution, stirred evenly, and cooled to room temperature after emulsification to obtain the complex.

6. The method according to claim 5, characterized in that The Chinese medicine extract is prepared by alcohol extraction or water extraction.

7. The method according to claim 5, characterized in that The dissolution temperature of tranexamic acid is 40~50℃.

8. A Chinese medicine composition for treating pigmented skin diseases, characterized in that: By weight percentage, it includes the following components: Angelica dahurica 10%-15%, Angelica sinensis 5%-10%, Safflower 3%-10%, Atractylodes macrocephala 3%-8%, Scutellaria baicalensis 2%-5%, Poria 3%-8%, Licorice 2%-5% and matrix 40%-70%.

9. Use of the complex according to any one of claims 1 to 4, or the traditional Chinese medicine composition according to claim 8, in the preparation of a product for treating pigmented skin diseases.

10. The use according to claim 9, characterized in that The product is a medicine, a facial mask, an essence or a body lotion.