Traditional Chinese medicine external preparation for treating scalp inflammation

Abstract

The invention relates to a traditional Chinese medicine external preparation for treating scalp inflammation. The traditional Chinese medicine external preparation is prepared from honeysuckle, radix sophorae flavescentis, fructus kochiae, cortex dictamni, dandelion, radix salviae miltiorrhizae, menthol, borneol and a transdermal enhancer. The preparation plays anti-inflammatory, bacteriostatic and barrier repairing roles through a multi-target synergistic mechanism, and is suitable for scalp inflammatory diseases such as seborrheic dermatitis and contact dermatitis. The preparation maximally retains active ingredients by adopting a specific extraction process, and the transdermal efficiency is improved by combining a triple permeation enhancing technology. The active ingredients reach the treatment concentration in the deep hair follicle. The pH value (5.5-6.0) of the preparation is matched with the weak acid environment of scalp, malassezia is selectively inhibited without damaging effective microbial communities, and the recurrence risk is reduced from the source. A spray, a lotion and a gel are proved to be capable of remarkably relieving erythema pruritus, inhibiting pathogenic bacteria colonization and accelerating cuticle repair, and have no skin irritation.

Description

Technical Field

[0001] This invention relates to the field of traditional Chinese medicine preparations, specifically to a topical traditional Chinese medicine preparation for treating scalp inflammation. Background Technology

[0002] Inflammatory scalp diseases such as seborrheic dermatitis and contact dermatitis clinically manifest as erythema, itching, and desquamation. Their pathogenesis is closely related to the excessive release of inflammatory factors, microbial dysbiosis, and damage to the skin barrier. Current mainstream treatments rely on corticosteroids and antifungal drugs, which can relieve symptoms in the short term, but long-term use can easily lead to side effects such as skin atrophy and microecological imbalance, and the relapse rate is high after discontinuation of the drugs.

[0003] Traditional Chinese medicine preparations have significant limitations in treating scalp inflammation. On the one hand, the active ingredients in ordinary decoctions or tinctures have low transdermal absorption rates, making it difficult to achieve effective therapeutic concentrations. On the other hand, existing compound preparations mostly focus on single anti-inflammatory or antibacterial effects, lacking multi-target synergistic conditioning strategies, and cannot simultaneously address core issues such as inflammatory responses, dysbiosis, and barrier repair. Summary of the Invention

[0004] The purpose of this section is to outline some aspects of embodiments of the present invention and to briefly describe some preferred embodiments. Simplifications or omissions may be made in this section, as well as in the abstract and title of this application, to avoid obscuring the purpose of these documents; however, such simplifications or omissions should not be construed as limiting the scope of the invention.

[0005] In view of the problems existing in the prior art, the inventors have proposed the present invention.

[0006] Therefore, the purpose of this invention is to overcome the shortcomings of the prior art and provide a traditional Chinese medicine external preparation for treating scalp inflammation.

[0007] To solve the above-mentioned technical problems, the present invention provides the following technical solution: a traditional Chinese medicine external preparation for treating scalp inflammation, made from the following raw materials in parts by weight: honeysuckle 15-30 parts, sophora flavescens 10-25 parts, kochia scoparia 8-20 parts, dictamnus dasycarpus 5-18 parts, dandelion 12-28 parts, salvia miltiorrhiza 5-15 parts, menthol 0.5-3 parts, borneol 0.3-2 parts, and azone 1-4 parts.

[0008] As a preferred embodiment of the traditional Chinese medicine external preparation for treating scalp inflammation according to the present invention, the ingredients are as follows: 20 parts honeysuckle, 18 parts sophora flavescens, 12 parts kochia scoparia, 10 parts dictamnus dasycarpus, 22 parts dandelion, 8 parts salvia miltiorrhiza, 1.5 parts menthol, 1 part borneol, and 2.5 parts azone.

[0009] As a preferred embodiment of the traditional Chinese medicine external preparation for treating scalp inflammation according to the present invention, the preparation is a spray, lotion, or gel.

[0010] A method for preparing a topical traditional Chinese medicine preparation for treating scalp inflammation includes the following steps: (a) Extracting volatile oils from honeysuckle and dandelion by water distillation; (b) The residue was extracted with ethanol by reflux with Sophora flavescens, Kochia scoparia, Dictamnus dasycarpus, and Salvia miltiorrhiza, and the extracts were combined. (c) After concentration, precipitate with alcohol and filter to obtain the supernatant; (d) Add menthol, borneol, azone and the volatile oil obtained in step (a), and mix well; (e) Add excipients according to dosage form requirements to form the product.

[0011] As a preferred embodiment of the preparation method of the traditional Chinese medicine external preparation for treating scalp inflammation according to the present invention, in step (b), 60% ethanol is used, and the mixture is refluxed and extracted twice. The first extraction is carried out with 8 times the amount of ethanol for 1.5 hours, and the second extraction is carried out with 6 times the amount of ethanol for 1 hour.

[0012] In a preferred embodiment of the preparation method of the traditional Chinese medicine external preparation for treating scalp inflammation as described in this invention, in step (c), the concentration is increased to a relative density of 1.15-1.20 (60°C), ethanol is added to adjust the alcohol content to 70%, and the mixture is refrigerated for 24 hours to allow precipitation.

[0013] A spray consisting of a traditional Chinese medicine external preparation for treating scalp inflammation and a propellant, characterized in that the mass ratio of the medicine liquid to the propellant is 1:3, and the propellant is HFC-134a.

[0014] A lotion composed of a traditional Chinese medicine external preparation for treating scalp inflammation and a surfactant, characterized in that each 100ml contains 4-6g of sodium lauryl ether sulfate and 2-4g of cocamidopropyl betaine, with a pH value of 5.5-6.0.

[0015] A gel composed of a traditional Chinese medicine external preparation for treating scalp inflammation and a gel matrix, characterized in that each 100g contains 1.0-1.5g of carbomer 940, 0.8-1.2g of triethanolamine, and 3-6g of propylene glycol.

[0016] The application of a traditional Chinese medicine external preparation for treating scalp inflammation in the preparation of drugs for treating scalp inflammation, wherein the scalp inflammation includes seborrheic dermatitis and contact dermatitis.

[0017] The beneficial effects of this invention are as follows: This formulation, through the core combination of honeysuckle, sophora flavescens, and kochia scoparia, synergistically inhibits the TLR4 / NF-κB inflammatory pathway, reducing the expression of key factors such as TNF-α and IL-6, thus blocking the inflammatory cascade response at its source. Simultaneously, the combination of dandelion and dictamnus dasycarpus can clear oxidized lipids, while salvia miltiorrhiza promotes microcirculation in hair follicles, forming a triple mechanism of action: anti-inflammatory, antioxidant, and repair. The triple penetration-enhancing system composed of menthol, borneol, and azone significantly improves the transdermal efficiency of the drug, allowing the active ingredients to reach therapeutic concentrations deep within the hair follicles. The formulation's pH value (5.5-6.0) matches the slightly acidic environment of the scalp, selectively inhibiting Malassezia without disrupting beneficial flora, thereby reducing the risk of recurrence from the root cause. Detailed Implementation

[0018] To make the above-mentioned objects, features and advantages of the present invention more apparent and understandable, the specific embodiments of the present invention will be described in detail below with reference to the examples in the specification.

[0019] Many specific details are set forth in the following description in order to provide a full understanding of the invention. However, the invention may also be practiced in other ways different from those described herein, and those skilled in the art can make similar extensions without departing from the spirit of the invention. Therefore, the invention is not limited to the specific embodiments disclosed below.

[0020] Secondly, the term "an embodiment" or "embodiment" as used herein refers to a specific feature, structure, or characteristic that may be included in at least one implementation of the present invention. The phrase "in one embodiment" appearing in different places throughout this specification does not necessarily refer to the same embodiment, nor is it a single embodiment or an embodiment selectively excluded from other embodiments.

[0021] Example 1 This embodiment provides a traditional Chinese medicine external application preparation for treating scalp inflammation, specifically, the preparation of a spray.

[0022] Raw material ratio: Specifically, this embodiment provides a traditional Chinese medicine spray for treating scalp inflammation, which is made from the following raw materials in parts by weight: honeysuckle 20 parts, sophora flavescens 18 parts, kochia scoparia 12 parts, dictamnus dasycarpus 10 parts, dandelion 22 parts, salvia miltiorrhiza 8 parts, menthol 1.5 parts, borneol 1 part, and azone 2.5 parts. Preferably, the raw materials include: honeysuckle and dandelion harvested during the flowering period, with chlorogenic acid content ≥5.0% (HPLC determination); Sophora flavescens root diameter 0.8~1.2cm, with oxymatrine content ≥2.2%; Kochia scoparia and Dictamnus dasycarpus pretreated by supercritical CO2 extraction to remove fat-soluble irritants; Furthermore, the preparation of the spray includes the following steps: Volatile oil extraction: Add 10 times the amount of purified water to honeysuckle and dandelion, and distill at 100℃ for 3 hours in a multi-functional extraction tank. Collect the volatile oil (yield 0.85%±0.05%), and filter out the residue for later use. Ethanol gradient extraction: Mix the residue with Sophora flavescens, Kochia scoparia, Dictamnus dasycarpus, and Salvia miltiorrhiza, add 8 times the amount of 60% ethanol (v / v), reflux at 80℃±2℃ for 1.5 hours, and filter out the first extract; Add 6 times the amount of 60% ethanol to the residue, reflux twice at 70℃±2℃ for 1 hour, and combine the two extracts. Concentration and purification: The combined solution was concentrated under reduced pressure to a relative density of 1.18 at 60℃ (allowable deviation ±0.02); 95% ethanol was added to adjust the alcohol content to 70% (v / v), and the precipitate was refrigerated at 4℃ for 24 hours; Formulation: Take the supernatant and recover the ethanol until there is no alcohol odor. Add menthol, borneol, azone and the volatile oil obtained in step 1, and stir until completely dissolved. Add purified water to make up to 1000 ml, filter through a 0.22 μm microporous membrane, fill into aluminum cans, and pressurize and seal according to the ratio of drug solution to propellant HFC-134a = 1:3 (w / w).

[0023] Example 2 This embodiment provides a traditional Chinese medicine external preparation for treating scalp inflammation, specifically, the preparation of a wash.

[0024] As one implementation method, the preferred ratio is: 18 parts honeysuckle, 15 parts sophora flavescens, 10 parts kochia scoparia, 8 parts dictamnus dasycarpus, 20 parts dandelion, and 6 parts salvia miltiorrhiza (based on a concentrated solution with a density of 1.20). Specifically, the detergent also contains the following excipients: Surfactant system: Sodium lauryl ether sulfate (SLES) 4.5g / 100ml, cocamidopropyl betaine (CAPB) 3.2g / 100ml; Stabilizers: EDTA-2Na 0.1g / 100ml, glycerol 4.0g / 100ml; pH adjuster: citrate buffer (maintain pH 5.8 ± 0.2); Furthermore, industrial production methods for detergents include: Preparation of drug solution: Prepare concentrated drug solution (relative density 1.20±0.01, 60℃) according to steps 1-4 of Example 1. Construction of emulsion system: Mix SLES and CAPB in a 65°C water bath, add glycerin and stir until homogeneous; slowly add concentrated drug solution and shear emulsify at 800 rpm for 15 minutes; Volume adjustment: Add purified water to a total volume of 1000 ml, add EDTA-2Na; adjust the pH to 5.8 ± 0.2 with citric acid solution; Post-treatment: Let stand for 24 hours to defoam, then fill into HDPE bottles.

[0025] Example 3 This embodiment provides a topical Chinese medicine preparation for treating scalp inflammation, specifically, the preparation of a gel.

[0026] Preferably, this embodiment provides a repair gel for severe scalp barrier damage, the active components of which are in the following weight parts: honeysuckle 25 parts, sophora flavescens 20 parts, kochia scoparia 15 parts, dictamnus dasycarpus 12 parts, dandelion 25 parts, and salvia miltiorrhiza 10 parts (enhanced antioxidant components). Furthermore, the gel matrix contains: gel forming agent: carbomer 940 1.2g / 100g; neutralizing agent: triethanolamine 1.0g / 100g; moisturizing and penetration enhancing agent: propylene glycol 5.0g / 100g; synergist: azone 3.0g / 100g; Specifically, the preparation steps of the gel are as follows: Preparation of medicinal solution: Prepare the medicinal solution according to steps 1-4 of Example 1, and make up to 500ml (equivalent to a crude drug concentration of 2.0g / ml); Gel matrix pretreatment: Carbomer 940 was dispersed in 300 ml of purified water, swollen for 24 hours, and then homogenized. Drug-loaded gel formation: Add the drug solution to the carbomer matrix with stirring, then add propylene glycol; Add triethanolamine dropwise until the pH reaches 6.8 ± 0.1 (peak gel viscosity). Addition of active ingredients: 1.8g of menthol and 1.2g of borneol were pre-dissolved in 3.0g of azone and then added to the gel system; Homogenize and fill into aluminum tubes, and store away from light.

[0027] The core formula of this preparation follows the traditional Chinese medicine treatment principles of "clearing heat and drying dampness, dispelling wind and relieving itching, and promoting blood circulation and tissue regeneration," forming a three-layer dynamic regulatory system: honeysuckle is the principal ingredient, which is sweet and cold in nature and enters the lung and stomach meridians, effectively clearing heat and toxins from the upper burner; sophora flavescens is bitter, cold, and descending, specifically targeting damp-heat in the lower burner, and the two herbs work together to eliminate heat accumulation on the scalp. Dandelion assists honeysuckle in detoxifying and dispersing nodules, and modern pharmacology has confirmed that its chicoric acid can neutralize sebum oxidation products and block the pathological cycle of "damp-heat turning into toxins."

[0028] The wind-dispelling and itch-relieving effects of Kochia scoparia fruit stem from the regulation of TRPV1 ion channels by saponins, directly reducing the transmission of itch nerve signals. The combination with Dictamnus dasycarpus root bark enhances antihistamine efficacy and inhibits erythema exudation caused by mast cell degranulation. Menthol, as a guiding herb, uses its pungent and cooling properties to open the pores and promote the penetration of the medicine to the affected area.

[0029] Danshen invigorates blood circulation and unblocks collaterals. Its tanshinone component activates perifollicular capillary endothelial growth factor (VEGF) to improve local microcirculation disorders. Borneol "opens up all orifices and disperses stagnant heat," accelerating barrier structure reconstruction by increasing the expression of the tight junction protein occludin.

[0030] Furthermore, volatile oil components (such as linalool from honeysuckle) are volatile, and steam distillation is used to avoid high-temperature damage; while alkaloids such as matrine and fat-soluble components such as tanshinone require a moderately polar solvent (60% ethanol) for full dissolution. Alcohol precipitation purification removes large molecular impurities such as tannins, reducing the irritation of the preparation, which aligns with the ancient adage that "the key to external application of traditional Chinese medicine lies in its purity."

[0031] Transient penetration (menthol): Activates transient receptor potential M8 (TRPM8), transiently opens keratinocyte calcium channels, and forms a short-term drug delivery window; Long-lasting penetration (azone): Disrupts the orderly arrangement of the lipid bilayer of the stratum corneum, continuously expanding molecular diffusion channels; Targeted delivery (borneol): Increases the surface tension of the hair follicle opening, guiding the medication to penetrate deeply along the hair follicle-sebaceous gland unit. The three elements form a cascade effect of "opening the door-expanding the path-guiding," solving the problem of "superficial retention" in traditional tinctures.

[0032] Furthermore, the spray utilizes propellant power to atomize the medication into 30μm particles, uniformly covering the irregular scalp surface, making it suitable for acute exudative inflammation; The shampoo maintains the normal microecology of the scalp in a weakly acidic environment (pH 5.8), and the surfactant SLES / CAPB compound system avoids excessive degreasing while effectively cleaning; The carbomer matrix of the gel forms a bioadhesive hydrogel film at scalp temperature, continuously releasing the drug and reducing moisture evaporation, specifically targeting chronic barrier damage.

[0033] The dynamic link between dosage form, pathology, and TCM syndrome reflects the TCM concept of "treating the same disease differently".

[0034] This formulation inhibits abnormal immune responses through a three-tiered pathway: Upstream signal blocking: Matrine downregulates Toll-like receptor 4 (TLR4) expression, cutting off the pathogen recognition initiation signal; Core pathway inhibition: Chlorogenic acid blocks IκBα phosphorylation, inhibits NF-κB nuclear translocation, and reduces the synthesis of pro-inflammatory factors such as TNF-α and IL-6; End-effect regulation: Dictamnus dasycarpus inhibits cyclooxygenase-2 (COX-2) and reduces the analgesic and pruritus-inducing effects of prostaglandin E2 (PGE2).

[0035] Based on the holistic view of traditional Chinese medicine, this invention achieves precise regulation of "clearing heat without damaging yin and drying dampness without promoting fire" through the core combination of honeysuckle, sophora flavescens, and kochia scoparia. It solves the problem of transdermal absorption of traditional Chinese medicine with modern formulation technology, and the triple penetration-enhancing system makes a qualitative leap in the delivery efficiency of active ingredients. Furthermore, it realizes personalized treatment of "treatment according to the stage" through multi-dosage form design.

[0036] It should be noted that the above embodiments are only used to illustrate the technical solutions of the present invention and are not intended to limit it. Although the present invention has been described in detail with reference to preferred embodiments, those skilled in the art should understand that modifications or equivalent substitutions can be made to the technical solutions of the present invention without departing from the spirit and scope of the technical solutions of the present invention, and all such modifications or substitutions should be covered within the scope of the claims of the present invention.

Claims

1. A traditional Chinese medicine external application preparation for treating scalp inflammation, characterized in that: It is made from the following ingredients in parts by weight: honeysuckle 15-30 parts, sophora flavescens 10-25 parts, kochia scoparia 8-20 parts, dictamnus dasycarpus 5-18 parts, dandelion 12-28 parts, salvia miltiorrhiza 5-15 parts, menthol 0.5-3 parts, borneol 0.3-2 parts, and azone 1-4 parts.

2. The topical Chinese medicine preparation for treating scalp inflammation as described in claim 1, characterized in that: The weight parts of each ingredient are as follows: honeysuckle 20 parts, sophora flavescens 18 parts, kochia scoparia 12 parts, dictamnus dasycarpus 10 parts, dandelion 22 parts, salvia miltiorrhiza 8 parts, menthol 1.5 parts, borneol 1 part, and azone 2.5 parts.

3. A topical traditional Chinese medicine preparation for treating scalp inflammation as described in claim 1 or 2, characterized in that: The formulation is a spray, lotion, or gel.

4. The method for preparing a topical traditional Chinese medicine preparation for treating scalp inflammation as described in claim 1, characterized in that: Includes the following steps: (a) Extracting volatile oils from honeysuckle and dandelion by water distillation; (b) The residue was extracted with ethanol by reflux with Sophora flavescens, Kochia scoparia, Dictamnus dasycarpus, and Salvia miltiorrhiza, and the extracts were combined. (c) After concentration, precipitate with alcohol and filter to obtain the supernatant; (d) Add menthol, borneol, azone and the volatile oil obtained in step (a), and mix well; (e) Add excipients according to dosage form requirements to form the product.

5. The method for preparing a topical traditional Chinese medicine preparation for treating scalp inflammation as described in claim 4, characterized in that: In step (b), 60% ethanol was used for reflux extraction twice. The first extraction was performed with 8 times the amount of ethanol for 1.5 hours, and the second extraction was performed with 6 times the amount of ethanol for 1 hour.

6. A topical traditional Chinese medicine preparation for treating scalp inflammation as described in claim 4, characterized in that: In step (c), concentrate to a relative density of 1.15-1.20 (60℃), add ethanol to adjust to an alcohol content of 70%, and refrigerate for 24 hours to precipitate.

7. A spray formulation comprising a traditional Chinese medicine external preparation for treating scalp inflammation as described in any one of claims 1-2 and a propellant, characterized in that... The mass ratio of the drug solution to the propellant is 1:3, and the propellant is HFC-134a.

8. A wash comprising a traditional Chinese medicine external preparation for treating scalp inflammation as described in any one of claims 1-2 and a surfactant, characterized in that... Each 100ml contains 4-6g of sodium lauryl ether sulfate and 2-4g of cocamidopropyl betaine, with a pH value of 5.5-6.

0.

9. A gel formulation comprising a traditional Chinese medicine external preparation for treating scalp inflammation as described in any one of claims 1-2 and a gel matrix, characterized in that... Each 100g contains 1.0-1.5g of carbomer 940, 0.8-1.2g of triethanolamine, and 3-6g of propylene glycol.

10. The application of the traditional Chinese medicine external preparation for treating scalp inflammation as described in claim 1 in the preparation of a drug for treating scalp inflammation, wherein the scalp inflammation includes seborrheic dermatitis and contact dermatitis.