External traditional Chinese medicine formula for treating infantile asthma and preparation method thereof

Abstract

The invention discloses an external traditional Chinese medicine formula for treating infantile asthma and a preparation method thereof, and belongs to the technical field of traditional Chinese medicines. The formula consists of extracts of rhizoma pinellinae praeparata, euphorbia kansui, semen brassicae, corydalis tuber, agilawood, cinnamon, ginger, asarum and musk according to a specific proportion. The preparation method comprises the steps of raw material pretreatment, mixing homogenization, matrix preparation, preparation forming, sterilization packaging and the like, and ointment, patch or film coating agent can be prepared. The concentration of active ingredients is increased by adopting a water extraction, alcohol extraction or supercritical CO2 extraction process, and the drug transdermal absorption rate and stability are remarkably enhanced by combining the azone transdermal enhancer and the vitamin E antioxidant. Through a multi-target synergistic effect, the preparation has the characteristics of remarkable curative effect, low irritation, convenience in use and the like, and is suitable for being applied to the Danzhong acupoint, the Feishu acupoint and other acupoints.

Description

Technical Field

[0001] The present invention relates to the technical field of traditional Chinese medicine, in particular to an external-use traditional Chinese medicine formula for treating childhood asthma and a preparation method thereof. Background Art

[0002] Pediatric asthma is a common chronic respiratory disease in children, characterized by recurrent episodes of wheezing and coughing. Western medicine treatment often relies on glucocorticoids and bronchodilators, which can cause side effects (such as growth suppression and drug resistance) with long-term use. Traditional Chinese medicine offers unique advantages in the treatment of asthma, particularly topical transdermal administration, which avoids first-pass liver effects and gastrointestinal irritation, resulting in greater safety.

[0003] Traditional Chinese medicine believes that the pathogenesis of asthma is mostly related to "phlegm and fluid lurking in the lungs" and "lung, spleen and kidney deficiency", and the treatment principle requires warming the lungs and resolving phlegm, relieving cough and relieving asthma. Classic prescriptions such as the "Three-Fu Sticker" (containing white mustard seeds, kansui, etc.) recorded in "Zhang's Medical Encyclopedia" exert their therapeutic effects through acupoint stimulation, but have problems such as a single ingredient and poor transdermal absorption. In the existing technology, external use Chinese herbal compound prescriptions are mostly limited to a single dosage form (such as plasters), or lack standardized extraction processes (such as directly using crude drug powders), resulting in unstable efficacy and a high risk of skin irritation.

[0004] To address these issues, the present invention optimizes the formulation and employs modern extraction techniques (such as supercritical CO₂ extraction) to combine a transdermal penetration enhancer (azone) and an antioxidant (vitamin E) to provide a highly effective, low-irritation topical compound preparation. By modulating multiple targets (such as pinellia tuber to resolve phlegm, agarwood to promote qi absorption, and musk to stimulate the mind), the compound offers both rapid and long-lasting effects, filling a gap in the topical treatment of pediatric asthma. Summary of the Invention

[0005] The technical problem to be solved by the present invention is to provide a traditional Chinese medicine compound preparation for external use for treating pediatric asthma with stable efficacy, good transdermal absorption and low irritation, so as to overcome the defects of traditional therapies such as single ingredients, poor transdermal effect and large side effects.

[0006] The technical solution adopted by the present invention is: a traditional Chinese medicine formula for external use for treating childhood asthma, which is prepared from the following raw materials in the following weight ratios:

[0007] 1-20 grams of Pinellia ternata or its extract, 1-20 grams of Gelsemium elegans or its extract, 1-20 grams of White Mustard Seed or its extract, 1-20 grams of Corydalis yanhusuo or its extract, 1-20 grams of Aquilaria woodis or its extract, 1-20 grams of cinnamon bark or its extract, 1-20 grams of ginger or its extract, 1-20 grams of Asarum or its extract, 1-20 grams of Musk or its extract.

[0008] As a further solution of the present invention: it is composed of the following raw materials in parts by weight: 15 grams of French Pinellia extract, 10 grams of Kansui extract, 15 grams of white mustard extract, 10 grams of Corydalis extract, 7 grams of Aquilaria extract, 13 grams of cinnamon extract, 20 grams of ginger extract, 6 grams of Asarum extract, and 4 grams of musk extract.

[0009] As a further embodiment of the present invention: the extract is a water extract, an alcohol extract or a supercritical CO2 extract.

[0010] A method for preparing an external Chinese medicine formula for treating pediatric asthma comprises the following steps:

[0011] S1. Raw material pretreatment:

[0012] Grind Pinellia ternata, Ginseng sinensis, White mustard seeds, Corydalis yanhusuo, Aquilaria sinensis, Cinnamon bark, Ginger and Asarum into 80-100 meshes respectively, or use their extracts;

[0013] Grind musk to 120 mesh or use its extract;

[0014] S2. Mixing and homogenization:

[0015] Mix the raw materials according to the ratio and stir them in a three-dimensional mixer for 20-30 minutes to ensure uniform dispersion;

[0016] S3. Matrix preparation:

[0017] Choose vaseline, honey or hydrogel as the matrix and mix the powder to matrix in a ratio of 1:1-1:3;

[0018] Heat to 50-70°C to melt (vaseline) or reduce viscosity (honey);

[0019] S4. Preparation molding:

[0020] Ointment: Add the mixed powder to the molten matrix, stir for 20-30 minutes, and add 1-3% azone (transdermal enhancer) after cooling;

[0021] Patches: Mix the drug powder with pressure-sensitive adhesive, apply it to non-woven fabric, dry it at 60°C for 2 hours, cut and package.

[0022] Film coating: Disperse the drug powder in an ethanol-water solution, add film-forming material (polyvinyl alcohol), and dry to form a film;

[0023] S5. Sterilization and packaging:

[0024] Sterilize by ultraviolet irradiation for 30 minutes or cobalt-60 irradiation (≤10kGy);

[0025] Seal with aluminum-plastic composite film, store away from light, valid for 24 months.

[0026] As a further solution of the present invention: 0.1% vitamin E can be added to the S4 as an antioxidant.

[0027] The invention discloses an application of an external Chinese medicine formula for treating childhood asthma, wherein the formula is used to prepare a patch, ointment or film for treating childhood asthma.

[0028] As a further solution of the present invention: the patch, ointment or coating is applied via the Tanzhong point, Feishu point or Dingchuan point once a day for 2-4 hours each time.

[0029] Beneficial effects of the present invention:

[0030] 1. Significant therapeutic effect and synergistic effect of multiple targets

[0031] The formula combines Chinese herbs such as Pinellia (to resolve phlegm), Gelsemium elegans (to expel fluid), White Mustard Seed (to warm the lungs), Corydalis yanhusuo (to promote qi and relieve pain), Aquilaria sinensis (to absorb qi and relieve asthma), Cinnamon bark (to warm yang), Ginger (to dispel cold), Asarum (to open the orifices), Musk (to invigorate the mind), etc. Through the synergistic effect of multiple components, it achieves the comprehensive therapeutic effects of relieving cough and asthma, warming the lungs and resolving phlegm, promoting qi and unblocking the meridians, and significantly improving the symptoms of asthma in children.

[0032] 2. Good transdermal absorption and high bioavailability

[0033] Use extracts (water extraction, alcohol extraction or supercritical CO2 extraction) to replace traditional herbal powders to increase the concentration of active ingredients and reduce ineffective impurities;

[0034] Adding transdermal enhancers (such as azone) to enhance the drug's transdermal penetration ability and improve bioavailability;

[0035] Combined with acupoint application (Tanzhong point, Feishu point, etc.), the efficacy of the medicine is enhanced through meridian conduction.

[0036] 3. High safety and low irritation

[0037] Optimize the compatibility ratio, reduce the amount of irritating ingredients such as kansui, and reduce the risk of skin allergies;

[0038] Modern extraction technology is used to remove some allergenic ingredients, and vitamin E is added as an antioxidant to improve the stability of the preparation;

[0039] Topical administration avoids gastrointestinal and respiratory tract irritation caused by oral or inhalation therapy and is especially suitable for children.

[0040] 4. Various dosage forms and easy to use

[0041] It can be made into ointments, patches or coatings to meet the needs of different usage scenarios;

[0042] The patch uses pressure-sensitive adhesive and non-woven fabric as the base material, which has good adhesion and is not easy to fall off, making it suitable for use during children's activities;

[0043] The coating agent forms a film quickly and has good air permeability, reducing skin stuffiness and discomfort.

[0044] 5. Standardized preparation process and controllable quality

[0045] Use three-dimensional mixer for homogenization to ensure uniform drug dispersion;

[0046] Ultraviolet or cobalt-60 irradiation sterilization ensures the sterility and safety of the preparation;

[0047] The light-proof packaging made of aluminum-plastic composite film extends the shelf life to 24 months, making it easy to store and transport. BRIEF DESCRIPTION OF THE DRAWINGS

[0048] Figure 1 The present invention is a flow chart of a preparation method of a traditional Chinese medicine formula for external use for treating childhood asthma and its preparation method.

[0049] Figure 2 The present invention provides a comparative histogram of wheezing relief rates according to an embodiment of a Chinese medicine formula for external use for treating childhood asthma and a preparation method thereof. DETAILED DESCRIPTION

[0050] The present invention will be further described below.

[0051] Example 1 (basic formula, water extract + vaseline matrix)

[0052] Formula (parts by weight):

[0053] 15g of Pinellia ternata water extract, 10g of Gelsemium elegans water extract, 15g of White Mustard Seed water extract, 10g of Corydalis yanhusuo water extract, 7g of Aquilaria water extract, 13g of cinnamon bark water extract, 20g of ginger water extract, 6g of Asarum water extract, and 4g of musk alcohol extract.

[0054] Preparation method:

[0055] 1. Extraction: Each medicinal material (except musk) was extracted with water (decocted twice, the filtrate was combined and concentrated to an extract); musk was extracted with 70% ethanol.

[0056] 2. Mixing: Mix the extracts according to the proportion and stir in a three-dimensional mixer for 20 minutes.

[0057] 3. Matrix preparation: Mix the drug powder and vaseline in a ratio of 1:2, melt and stir at 60°C for 30 minutes.

[0058] 4. Molding: When cooled to 40℃, add 2% azone and fill into paste.

[0059] 5. Sterilization: UV irradiation for 30 minutes, aluminum-plastic packaging.

[0060] Effect analysis

[0061] Advantages: The water extraction process is simple and the cost is low; the vaseline matrix has good stability and is suitable for long-term storage.

[0062] Disadvantages: Transdermal absorption is slow, and the extraction rate of some fat-soluble components (such as cinnamon volatile oil) is low.

[0063] Example 2 (alcohol extract + hydrogel matrix)

[0064] Formula (parts by weight):

[0065] 15g of French Pinellia ternata ethanol extract, 10g of Gansui ethanol extract, 15g of white mustard seed ethanol extract, 10g of Corydalis yanhusuo ethanol extract, 7g of agarwood ethanol extract, 13g of cinnamon bark ethanol extract, 20g of ginger ethanol extract, 6g of asarum ethanol extract, 4g of musk supercritical CO2 extract.

[0066] Preparation method

[0067] 1. Extraction: All medicinal materials (except musk) were extracted with 70% ethanol reflux; musk was extracted with supercritical CO2.

[0068] 2. Mixing: After mixing, the extracts were homogenized for 30 minutes.

[0069] 3. Matrix preparation: Mix the drug powder and sodium carboxymethyl cellulose (CMC-Na) hydrogel at a ratio of 1:1.5.

[0070] 4. Molding: Add 1.5% azone and 0.1% vitamin E to make a coating agent.

[0071] 5. Sterilization: Cobalt-60 irradiation (8kGy).

[0072] Effect analysis

[0073] Advantages: The extraction rate of active ingredients in alcohol extracts (such as flavonoids and volatile oils) is high; the hydrogel has good air permeability and is suitable for sensitive skin.

[0074] Disadvantages: The cost of alcohol extraction is relatively high; the hydrogel is easy to lose water and dry out, and needs to be stored in a sealed container.

[0075] Example 3 (supercritical CO2 extract + pressure-sensitive adhesive patch)

[0076] Formula (parts by weight):

[0077] 15g of Pinellia ternata supercritical CO2 extract, 10g of Gelsemium elegans supercritical CO2 extract, 15g of Sinapis alba supercritical CO2 extract, 10g of Corydalis yanhusuo supercritical CO2 extract, 7g of Aquilaria wood supercritical CO2 extract, 13g of cinnamon bark supercritical CO2 extract, 20g of ginger supercritical CO2 extract, 6g of Asarum supercritical CO2 extract, and 4g of Musk supercritical CO2 extract.

[0078] Preparation method:

[0079] 1. Extraction: All medicinal materials were extracted by supercritical CO2 (pressure 25MPa, temperature 45℃).

[0080] 2. Mixing: Mix the extract with pressure-sensitive adhesive (acrylate) in a ratio of 1:1 and apply it on non-woven fabric.

[0081] 3. Drying: Dry at 60℃ for 2 hours and cut into patches.

[0082] 4. Sterilization: Cobalt-60 irradiation (10 kGy).

[0083] Effect analysis

[0084] Advantages: Supercritical extraction leaves no solvent residue and the ingredients are purer; the patch is easy to use and has a fast transdermal rate.

[0085] Disadvantages: High equipment cost; pressure-sensitive adhesive may cause skin allergies in a small number of children.

[0086] Comparative Analysis of Examples

[0087]

[0088]

[0089] Recommended optimal solution

[0090] Conventional treatment: Preferred embodiment 1 has low cost and high safety, and is suitable for long-term application in children with chronic asthma.

[0091] Acute attack: Example 3 is recommended. The supercritical extract has high activity and the patch takes effect quickly.

[0092] Sensitive skin: Use Example 2, the hydrogel matrix reduces the risk of irritation.

[0093] The present invention verifies the applicability of different processes and dosage forms through comparison of multiple examples, and the formulation and preparation method can be flexibly adjusted according to clinical needs.

[0094] The above embodiments are only used to illustrate the technical solutions of the present invention, rather than to limit the same. Although the present invention has been described in detail with reference to the aforementioned embodiments, those skilled in the art should understand that they can still modify the technical solutions described in the aforementioned embodiments, or make equivalent replacements for some of the technical features therein. However, these modifications or replacements do not deviate the essence of the corresponding technical solutions from the spirit and scope of the technical solutions of the embodiments of the present invention.

Claims

1. A Chinese medicine formula for external use for treating asthma in children, characterized by: Made from the following raw materials in the following weight ratios: 1-20 grams of Pinellia ternata or its extract, 1-20 grams of Gelsemium elegans or its extract, 1-20 grams of White Mustard Seed or its extract, 1-20 grams of Corydalis yanhusuo or its extract, 1-20 grams of Aquilaria woodis or its extract, 1-20 grams of cinnamon bark or its extract, 1-20 grams of ginger or its extract, 1-20 grams of Asarum or its extract, 1-20 grams of Musk or its extract.

2. The external-use Chinese medicine formula for treating childhood asthma according to claim 1, characterized in that: The drug is composed of the following raw materials in parts by weight: 15 grams of Pinellia ternata extract, 10 grams of Kansui extract, 15 grams of White Mustard Seed extract, 10 grams of Corydalis yanhusuo extract, 7 grams of Aquilaria sinensis extract, 13 grams of cinnamon bark extract, 20 grams of ginger extract, 6 grams of Asarum sieboldii extract, and 4 grams of musk extract.

3. The external-use Chinese medicine formula for treating childhood asthma according to claim 2, characterized in that: The extract is a water extract, an alcohol extract or a supercritical CO2 extract.

4. The method for preparing a traditional Chinese medicine formula for external use for treating childhood asthma according to claim 3, characterized in that: The following steps are involved: S1. Raw material pretreatment: Grind Pinellia ternata, Ginseng sinensis, White mustard seeds, Corydalis yanhusuo, Aquilaria sinensis, Cinnamon bark, Ginger and Asarum into 80-100 meshes respectively, or use their extracts; Grind musk to 120 mesh or use its extract; S2. Mixing and homogenization: Mix the raw materials according to the ratio and stir them in a three-dimensional mixer for 20-30 minutes to ensure uniform dispersion; S3. Matrix preparation: Choose vaseline, honey or hydrogel as the matrix and mix the powder to matrix in a ratio of 1:1-1:3; Heat to 50-70℃ to melt or reduce viscosity; S4. Preparation molding: Ointment: Add the mixed powder to the molten matrix, stir for 20-30 minutes, and add 1-3% azone after cooling; Patches: Mix the drug powder with pressure-sensitive adhesive, apply it to non-woven fabric, dry it at 60°C for 2 hours, cut and package. Film coating: Disperse the drug powder in an ethanol-water solution, add film-forming material, and dry to form a film; S5. Sterilization and packaging: Sterilize by ultraviolet irradiation for 30 minutes or cobalt-60 irradiation; Seal with aluminum-plastic composite film, store away from light, valid for 24 months.

5. The method for preparing a traditional Chinese medicine formula for external use for treating childhood asthma according to claim 4, characterized in that: 0.1% vitamin E may be added to the S4 as an antioxidant.

6. The use of a traditional Chinese medicine formula for external use for treating childhood asthma according to claim 5, characterized in that: The formula is used to prepare a patch, ointment or film for treating childhood asthma.

7. The use of a traditional Chinese medicine formula for external use for treating childhood asthma according to claim 6, characterized in that: The patch, ointment or coating is applied via the Tanzhong point, Feishu point or Dingchuan point once a day for 2-4 hours each time.

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