A traditional Chinese medicine external use spray for treating toothache and a composition thereof
Patent Information
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Filing Date
- 2026-06-12
- Publication Date
- 2026-08-11
AI Technical Summary
[0004]目前现有技术既未公开天蚕丝抗菌肽与本发明中药复方复配制备口腔喷剂的技术方案，也未披露二者的协同配比及在口腔局部外用喷雾中的应用形式
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Figure CN122537504A_ABST
Abstract
Description
Technical Field
[0001] This invention relates to the field of traditional Chinese medicine and biomedical preparations, specifically to a traditional Chinese medicine external spray for treating acute exacerbations of periodontitis, gingival swelling and toothache caused by stomach fire, wind-heat stagnation transforming into fire. Background Technology
[0002] Toothache is a common oral disease in clinical practice. Acute exacerbations of periodontitis, characterized by red, swollen, hot, and painful gums, are often caused by external wind-heat pathogens, accumulated heat in the stomach and intestines attacking upwards, and the fire evil obstructing the blood vessels of the mouth and teeth. Over time, the wind-heat pathogens penetrate deeper and transform into fire, forming a pathogenic pattern of wind-heat and stomach fire intertwined. Modern medical research has confirmed that this type of disease is mainly caused by the proliferation of pathogenic bacteria such as Streptococcus mutans and Porphyromonas gingivalis, which induce local inflammation, mucosal congestion, and edema.
[0003] Currently, clinical practice often employs modified formulas such as Qingwei San and Yinqiao San, as well as traditional Chinese medicine preparations like Huanglian Shangqing Wan. These traditional Chinese medicines possess the effects of clearing heat and detoxifying, cooling blood and reducing swelling, and can alleviate mild toothache and gum discomfort to some extent. However, pure Chinese medicine preparations have a relatively slow onset of action and limited ability to directly inhibit pathogenic bacteria, resulting in poor improvement for severe swelling and pain caused by acute flare-ups of periodontitis. Existing technologies include solutions for adding broad-spectrum antibacterial components to oral preparations, but using antibacterial components alone can only achieve antibacterial effects and cannot clear internal heat and relieve stagnation from the perspective of traditional Chinese medicine pathogenesis; the antibacterial performance of single Chinese medicine compound formulas is also insufficient. Combining traditional Chinese medicine compound formulas with biological antibacterial components can achieve complementary effects and synergistic effects, overcoming the shortcomings of existing products.
[0004] Currently, existing technologies do not disclose the technical solution for preparing an oral spray by combining silkworm silk antimicrobial peptides with the traditional Chinese medicine compound of this invention, nor do they disclose the synergistic ratio of the two and their application in topical oral sprays. Based on the above, this invention provides a scientifically formulated, rapidly effective compound oral spray that combines heat-clearing and fire-purging effects with targeted antibacterial activity. Summary of the Invention
[0005] The purpose of this invention is to overcome the deficiencies of existing technologies and provide a traditional Chinese medicine external spray and its composition for treating toothache. This product combines a traditional Chinese medicine compound with silkworm silk antimicrobial peptides. The two components have complementary effects and produce a synergistic effect. Compared to using the Chinese medicine compound or silkworm silk antimicrobial peptides alone, the product significantly enhances its antibacterial, anti-inflammatory, and analgesic effects. It is particularly suitable for gingival swelling and toothache induced by acute exacerbations of periodontitis. It is convenient to administer, highly targeted, and suitable for local oral application scenarios.
[0006] The mulberry branches used in this invention are Chinese medicinal materials listed in the Pharmacopoeia of the People's Republic of China. They are bitter and neutral in nature, enter the liver meridian, and can dispel wind and dampness, unblock the meridians, guide the medicine upward, and reach the gums, so as to guide the full medicinal power of the prescription directly to the oral lesions. The silkworm silk antimicrobial peptides used are commercially available pharmaceutical raw materials, with stable and readily available supply, no drug resistance, and high safety of use.
[0007] This invention provides two independent forms of traditional Chinese medicine compositions, both specifically designed for the preparation of oral topical spray formulations. One type is a raw material composition consisting of specific weight parts of Chinese medicinal materials, which can be extracted and refined to obtain an extract for use in the preparation of sprays; Another type is an extract composition obtained by extracting and refining the above-mentioned Chinese medicinal materials, which can be directly used to prepare oral sprays.
[0008] The traditional Chinese medicine composition (raw material form) of the present invention is made from the following raw materials in parts by weight: 5-14 parts of honeysuckle vine, 3-10 parts of scutellaria baicalensis, 5-12 parts of forsythia suspensa, 3-8 parts of chrysanthemum, 3-8 parts of lophatherum gracile, 3-10 parts of dandelion, 3-8 parts of gardenia, 2-6 parts of rehmannia glutinosa, 2-6 parts of peony root, 2-6 parts of angelica sinensis, 3-8 parts of imperata cylindrica root, 2-6 parts of mulberry twig, and 0.01-0.5 parts of silkworm silk antimicrobial peptide.
[0009] The traditional Chinese medicine composition (extract form) of the present invention is made from the following parts by weight of traditional Chinese medicine extracts and silkworm silk antimicrobial peptides: 5-14 parts of honeysuckle vine extract, 3-10 parts of scutellaria baicalensis extract, 5-12 parts of forsythia suspensa extract, 3-8 parts of chrysanthemum extract, 3-8 parts of lophatherum gracile extract, 3-10 parts of dandelion extract, 3-8 parts of gardenia extract, 2-6 parts of rehmannia glutinosa extract, 2-6 parts of peony root extract, 2-6 parts of angelica sinensis extract, 3-8 parts of imperata cylindrica root extract, 2-6 parts of mulberry twig extract, and 0.01-0.5 parts of silkworm silk antimicrobial peptides.
[0010] Preferably, both of the above compositions are made from the following components in parts by weight: 10 parts honeysuckle vine, 6 parts scutellaria baicalensis, 8 parts forsythia suspensa, 5 parts chrysanthemum, 5 parts lophatherum gracile, 6 parts dandelion, 5 parts gardenia, 4 parts rehmannia glutinosa, 4 parts peony root, 4 parts angelica sinensis, 5 parts imperata cylindrica root, 4 parts mulberry twig, and 0.1 parts silkworm silk antimicrobial peptide.
[0011] Further preferably, the weight parts of the silkworm silk antimicrobial peptide are 0.01 parts, 0.1 parts, or 0.5 parts.
[0012] The mechanisms of action of each component of this invention are described below: This invention strictly adheres to the principles of traditional Chinese medicine's monarch-minister-assistant-guide formula compatibility, combined with modern bioactive component synergistic mechanisms. The formula has a clear hierarchy and precise correspondence with the pathogenesis. The specific compatibility mechanism is as follows: The principal herbs are: Honeysuckle vine, Forsythia, Scutellaria baicalensis, Gardenia jasminoides, and Chrysanthemum morifolium. Honeysuckle vine and Forsythia jasminoides clear heat and detoxify, dispel wind-heat, and their light and clear properties allow them to directly reach the lesions in the head, face, mouth, and teeth. Scutellaria baicalensis clears and drains excess heat from the upper burner (lung and stomach), and removes accumulated heat in the oral cavity. Gardenia jasminoides clears and drains heat from the three burners, and guides heat downwards. Chrysanthemum morifolium is light and clear, dispersing stagnant wind-heat in the mouth and teeth, and clearing the head and eyes. The five principal herbs work together to directly target the core pathogenesis of wind-heat stagnation transforming into fire and stomach fire attacking upwards.
[0013] Assistant herb: Dandelion. Dandelion is cold in nature and sweet in taste, and it specifically enters the stomach and liver meridians. It has the effects of clearing heat and detoxifying, cooling blood and dispersing stagnation, reducing swelling and relieving pain. It assists the principal herb in enhancing the effects of clearing heat and detoxifying, dispersing blood stasis and reducing swelling.
[0014] The adjuvant herbs are: Rehmannia glutinosa, Paeonia lactiflora, and Angelica sinensis. Rehmannia glutinosa clears heat and cools the blood, nourishes yin and generates fluids, and moderates the bitter and cold nature of the other herbs in the formula; Paeonia lactiflora nourishes blood and astringes yin, softens the collaterals and relieves spasms; Angelica sinensis nourishes blood, invigorates blood circulation, and unblocks the collaterals and disperses blood stasis. The combination of these three adjuvant herbs nourishes yin and protects fluids, invigorates blood and relieves pain, thus eliminating pathogens without harming the body's vital energy.
[0015] The guiding herbs are: Lophatherum gracile, Imperata cylindrica root, and Morus alba twigs. Lophatherum gracile and Imperata cylindrica root clear heat, promote diuresis, and guide heat downwards; Morus alba twigs unblock meridians and guide the medicine upwards, directing the medicinal power of the entire formula directly to the gingival lesions. Silkworm silk antimicrobial peptides are bioactive synergistic components, not belonging to the traditional Chinese medicine system of principal, assistant, adjuvant, and guide herbs. They work synergistically with the above-mentioned herbs to achieve targeted antibacterial, anti-inflammatory, and mucosal repair-promoting effects.
[0016] The formula is meticulously formulated to achieve the effects of clearing heat and purging fire, cooling blood and detoxifying, reducing swelling and relieving pain, and promoting tissue regeneration. Experiments have confirmed that within the specified proportions of this invention, the antimicrobial peptides from silkworm silk and the traditional Chinese medicine compound can produce a non-linearly enhanced synergistic effect in antibacterial, anti-inflammatory, and analgesic properties. This spray is suitable for acute exacerbations of periodontitis, gingival redness and swelling, and toothache caused by stomach fire, wind-heat stagnation transforming into fire, etc.; it can also improve swelling and pain caused by secondary inflammation of caries, gingivitis, and pericoronitis of wisdom teeth. It should be noted that this invention can only relieve the inflammation and pain accompanying the above symptoms and cannot repair the hard tissue defects of teeth caused by caries.
[0017] Compared with the prior art, the present invention has the following significant advantages: 1. Significant synergistic effect: Pharmacological experiments show that when the silkworm silk antimicrobial peptide is combined with a specific ratio of traditional Chinese medicine compound, its minimum inhibitory concentration (MIC) is significantly reduced, and its anti-inflammatory and swelling inhibition rate and analgesic rate are significantly better than those of using traditional Chinese medicine compound or antimicrobial peptide alone (see Table 1-6). This non-linear synergistic effect of "1+1>2" effectively solves the shortcomings of existing technologies where traditional Chinese medicine alone has a slow onset of action and simple antimicrobial components cannot effectively clear heat and inflammation.
[0018] 2. Strong adaptability to pathogenesis: The formulation of this invention strictly follows the principle of "principal, assistant, adjuvant and guide" in traditional Chinese medicine, and is formulated to target the pathogenesis of stomach fire rising and wind-heat stagnation transforming into fire. At the same time, it utilizes silkworm silk antimicrobial peptides to target and inhibit pathogenic bacteria, achieving a perfect combination of traditional Chinese medicine syndrome differentiation and treatment and modern pharmacological antibacterial therapy, increasing the overall clinical efficacy rate to 91.67%.
[0019] 3. Outstanding dosage form advantages: It adopts an oral external spray formulation, which allows the drug to act directly on the gingival lesions, resulting in a high local drug concentration and rapid onset of action (effective within 0.5 hours after administration). It avoids the gastrointestinal irritation and first-pass effect of oral administration, making it convenient to use and suitable for home use and emergency backup.
[0020] 4. High safety: The formula does not contain nonsteroidal anti-inflammatory drugs or anesthetic drugs. All raw materials used are medicinal materials listed in the pharmacopoeia or mature biological products. There is no risk of drug resistance with long-term use, low toxicity and side effects, and good safety of medication. Attached Figure Description
[0021] Appendix Figure 1 This is a flowchart illustrating the compatibility mechanism of the traditional Chinese medicine composition of the present invention. The diagram shows that the principal, assistant, adjuvant, and guiding traditional Chinese medicine components are combined according to a specified weight ratio for the wind-heat and stomach fire syndrome, ultimately achieving antibacterial, anti-inflammatory, and analgesic therapeutic effects. Detailed Implementation
[0022] The present invention will be further described below with reference to specific embodiments. These embodiments are only used to explain the present invention and are not intended to limit the scope of protection of the present invention.
[0023] Example 1: Low-peptide formulation of traditional Chinese medicine spray for toothache Ingredients (parts by weight): 10 parts honeysuckle vine, 6 parts scutellaria baicalensis, 8 parts forsythia suspensa, 5 parts chrysanthemum, 5 parts lophatherum gracile, 6 parts dandelion, 5 parts gardenia, 4 parts rehmannia glutinosa, 4 parts peony root, 4 parts angelica sinensis, 5 parts imperata cylindrica root, 4 parts mulberry twig, 0.01 parts silkworm silk antimicrobial peptide.
[0024] Preparation method: The above-mentioned Chinese medicinal materials are extracted using conventional extraction processes (such as water extraction, alcohol precipitation, and refining) to obtain effective extracts. The filtrate is concentrated to a relative density of 1.05~1.10 (60℃). Silkworm silk antimicrobial peptides and conventional excipients for oral sprays (such as purified water, glycerin, sorbitol, and benzyl alcohol) are added. The mixture is stirred until completely dissolved, mixed, filtered for sterilization, and aseptically filled to obtain the finished product.
[0025] Example 2: Preferred formulation of traditional Chinese medicine spray for toothache Ingredients (parts by weight): 10 parts honeysuckle vine, 6 parts scutellaria baicalensis, 8 parts forsythia suspensa, 5 parts chrysanthemum, 5 parts lophatherum gracile, 6 parts dandelion, 5 parts gardenia, 4 parts rehmannia glutinosa, 4 parts peony root, 4 parts angelica sinensis, 5 parts imperata cylindrica root, 4 parts mulberry twig, 0.1 parts silkworm silk antimicrobial peptide.
[0026] The preparation method is the same as in Example 1.
[0027] Example 3: High-peptide-ratio traditional Chinese medicine spray for toothache Ingredients (parts by weight): 10 parts honeysuckle vine, 6 parts scutellaria baicalensis, 8 parts forsythia suspensa, 5 parts chrysanthemum, 5 parts lophatherum gracile, 6 parts dandelion, 5 parts gardenia, 4 parts rehmannia glutinosa, 4 parts peony root, 4 parts angelica sinensis, 5 parts imperata cylindrica root, 4 parts mulberry twig, 0.5 parts silkworm silk antimicrobial peptide.
[0028] The preparation method is the same as in Example 1.
[0029] Preparation instructions The composition of this invention is specifically designed for the preparation of oral sprays. The specific method involves: extracting and refining various Chinese medicinal herbs using conventional extraction processes to obtain herbal extracts; mixing the obtained extracts, silkworm silk antimicrobial peptides, and conventional pharmaceutical excipients for oral sprays; and then, after formulation, filtration, and aseptic filling, obtaining the oral spray of this invention. All oral sprays prepared using the herbal extracts specified in this invention, regardless of the extraction process employed, fall within the scope of protection of this invention.
[0030] Drug efficacy verification test All test samples, group controls, and detection procedures in the efficacy verification test of this invention comply with the relevant specifications for pharmaceutical trials. Huanglian Shangqing Pill was selected as the positive control, and a pure Chinese medicine compound group and a single silkworm silk antimicrobial peptide group were set up as parallel controls.
[0031] Statistical annotation: Compared with the model group, *P<0.05, **P<0.01; compared with the positive control group, #P<0.05; compared with the pure traditional Chinese medicine group and the single antimicrobial peptide group, △P<0.05; experimental data are uniformly expressed as mean ± standard deviation.
[0032] Table 1. Determination of minimum inhibitory concentration (MIC) for in vitro antibacterial activity (unit: mg / mL)
[0033] As shown in Table 1, both the pure Chinese medicine group and the single silkworm silk antimicrobial peptide group exhibited certain antibacterial effects against the three oral pathogens, but their antibacterial capabilities were limited. After compounding the formula of this invention, the minimum inhibitory concentration (MIC) of each dosage group was significantly reduced, with the medium and high dosage groups showing the best effects, significantly superior to the pure Chinese medicine group, the single antimicrobial peptide group, and the positive control group. This demonstrates that the combination of silkworm silk antimicrobial peptide and the Chinese medicine compound has an excellent synergistic antibacterial effect and can effectively inhibit the proliferation of oral pathogens.
[0034] Table 2. Data from the mouse ear swelling and anti-inflammatory experiment.
[0035] Table 2 shows the results of the mouse ear swelling experiment, indicating that all treatment groups could alleviate ear inflammation and swelling in mice. The pure Chinese medicine group and the single antimicrobial peptide group had similar anti-inflammatory effects, but lower swelling inhibition rates. The anti-inflammatory effect of the compound preparation of this invention increased in a dose-dependent manner at each dosage group, with the swelling inhibition rate of the medium and high dosage groups being significantly higher than that of the other control groups, demonstrating a significant synergistic effect in anti-inflammatory efficacy. This confirms that the combination of the two can synergistically enhance the body's local anti-inflammatory capacity.
[0036] Table 3. Data from the rat paw edema anti-inflammatory experiment (unit: mm) 3 )
[0037] As shown in Table 3, the rat paw edema test data revealed that the swelling volume in the model group rats continuously increased, indicating a significant inflammatory response. All treatment groups showed varying degrees of inhibition of inflammatory swelling. The swelling volumes in the medium- and high-dose groups at each time point were significantly lower than those in other groups, with a substantial increase in the average swelling inhibition rate. This indicates that the herbal compound antimicrobial peptide preparation of this invention has a rapid onset of action, a good sustained anti-inflammatory effect, and a prominent synergistic anti-inflammatory advantage.
[0038] Table 4. Analgesic Threshold Measurement by Hot Plate Method (Unit: s)
[0039] As shown in Table 4 of the hot plate analgesia experiment, the pain threshold in the blank group showed no significant change and no analgesic effect. All other treatment groups increased the pain threshold and produced analgesic effects in mice. The pure traditional Chinese medicine group and the single antimicrobial peptide group showed similar analgesic effects. However, the pain threshold in the medium and high dose groups of the compound preparation of this invention significantly increased at all time points after administration, with an analgesic rate far exceeding that of the control groups, demonstrating a significant synergistic analgesic effect, rapid onset, and long-lasting analgesic effect.
[0040] Table 5 Results of Acetic Acid Writhing Analgesia Test
[0041] Experiments have confirmed that the compound composition of the present invention has significant analgesic effects and clear synergistic effects.
[0042] Table 6 Comparison of Clinical Efficacy Observations
[0043] Clinical comparisons show that the clinical efficacy of the composition of the present invention is significantly better than that of the pure Chinese medicine group, the single antimicrobial peptide group, and existing Chinese patent medicines. The synergistic effect has also been verified in clinical trials.
[0044] The aforementioned silkworm silk antimicrobial peptide can be obtained commercially or prepared by referring to existing technical literature.
[0045] The above description is merely a preferred embodiment of the present invention and is not intended to limit the scope of protection of the present invention. Any modifications, equivalent substitutions, improvements, etc., made within the spirit and principles of the present invention should be included within the scope of protection of the present invention.
Claims
1. A traditional Chinese medicine composition for treating toothache, characterized in that, It is composed of the following raw materials in parts by weight: 5-14 parts of honeysuckle vine, 3-10 parts of scutellaria baicalensis, 5-12 parts of forsythia suspensa, 3-8 parts of chrysanthemum, 3-8 parts of lophatherum gracile, 3-10 parts of dandelion, 3-8 parts of gardenia, 2-6 parts of rehmannia glutinosa, 2-6 parts of peony root, 2-6 parts of angelica sinensis, 3-8 parts of imperata cylindrica root, 2-6 parts of mulberry twig, and 0.01-0.5 parts of silkworm silk antimicrobial peptide.
2. A traditional Chinese medicine extract composition for treating toothache, characterized in that, It is composed of the following extracts and functional components in parts by weight: 5-14 parts of honeysuckle vine extract, 3-10 parts of scutellaria baicalensis extract, 5-12 parts of forsythia suspensa extract, 3-8 parts of chrysanthemum extract, 3-8 parts of lophatherum gracile extract, 3-10 parts of dandelion extract, 3-8 parts of gardenia extract, 2-6 parts of rehmannia glutinosa extract, 2-6 parts of peony root extract, 2-6 parts of angelica sinensis extract, 3-8 parts of imperata cylindrica root extract, 2-6 parts of mulberry twig extract, and 0.01-0.5 parts of silkworm silk antimicrobial peptide.
3. The traditional Chinese medicine composition for treating toothache according to claim 1, characterized in that, It is composed of the following components in parts by weight: 10 parts honeysuckle vine, 6 parts scutellaria baicalensis, 8 parts forsythia suspensa, 5 parts chrysanthemum, 5 parts lophatherum gracile, 6 parts dandelion, 5 parts gardenia, 4 parts rehmannia glutinosa, 4 parts peony root, 4 parts angelica sinensis, 5 parts imperata cylindrica root, 4 parts mulberry twig, and 0.1 parts silkworm silk antimicrobial peptide.
4. The traditional Chinese medicine composition for treating toothache according to claim 1, characterized in that: The antimicrobial peptides from the silkworm silk are present in parts by weight of 0.01, 0.1, or 0.
5.
5. A traditional Chinese medicine external spray for treating toothache, characterized in that, It comprises the herbal extract composition of claim 2, and pharmaceutical excipients acceptable for oral sprays.
6. The traditional Chinese medicine external spray for treating toothache according to claim 5, characterized in that, The pharmaceutical excipients include at least one of purified water, glycerin, sorbitol, and benzyl alcohol.
7. The method for preparing the traditional Chinese medicine external spray for treating toothache according to claim 5, characterized in that, Includes the following steps: (1) Take the Chinese herbal extract composition according to claim 2, dissolve or disperse it, and then concentrate it to a concentrated solution with a relative density of 1.05~1.10 at 60°C; (2) Add the silkworm silk antimicrobial peptide and oral spray pharmaceutical excipients to the concentrate, stir until completely dissolved and mixed evenly; (3) The mixture is filtered, sterilized, and aseptically filled to obtain the finished product of the Chinese medicine external spray.
8. The use of the traditional Chinese medicine extract composition according to claim 2 and the traditional Chinese medicine external spray according to claim 5 in the preparation of an oral external spray medicine for treating acute exacerbations of periodontitis, gingival swelling and pain, and toothache caused by stomach fire, wind-heat stagnation and fire.