Oral lozenge with anti-inflammatory and bacteriostatic effects

Abstract

The invention provides an oral lozenge with anti-inflammatory and bacteriostatic effects. The oral lozenge comprises the following components in parts by weight: 50-80 parts of a dandelion extract, 20-40 parts of catechin, 20-60 parts of a hydrogen source disintegrating agent, 1-10 parts of a surfactant, 1-5 parts of a flavoring agent and 0.5-3 parts of a preservative. The prepared oral lozenge has a high bacteriostasis rate on staphylococcus aureus, candida albicans, porphyromonas gingivalis and streptococcus mutans, is low in swelling value and good in anti-inflammatory effect, and can effectively inhibit bacteria and treat inflammation when being applied to the oral cavity.

Description

Technical Field

[0001] The present invention belongs to the field of oral technologies, and particularly relates to an oral buccal tablet with anti-inflammatory and antibacterial effects. Background Art

[0002] The oral cavity is a complex microbial environment that contains various bacteria, especially bacteria related to periodontal diseases. These bacteria can enter the blood circulation through tiny gum wounds and trigger a systemic inflammatory response. These bacteria and the inflammatory factors they trigger can promote the development of atherosclerosis, thereby increasing the risk of heart disease and stroke. Therefore, developing substances with anti-inflammatory and antibacterial effects is crucial for maintaining oral health.

[0003] With the in-depth research on natural ingredients and plant extracts, more and more ingredients with anti-inflammatory and antibacterial effects have been applied to oral care products. For example, dipotassium glycyrrhizinate, arginine, asiatic pennywort extract, etc. have been widely studied and applied due to their anti-inflammatory and antibacterial properties. However, the disadvantages of these traditional anti-inflammatory and antibacterial substances are that the therapeutic effect is slow, the effect is limited, and it takes a relatively long time to sense their effects on inflammation and antibacterial.

[0004] As a new therapeutic gas with anti-inflammatory and antibacterial effects, hydrogen shows broad application prospects in the biomedical field. Its anti-inflammatory effect is mainly achieved by selective antioxidant, regulating cell signaling pathways and gene expression, etc., and can effectively reduce or inhibit the inflammatory response, and has significant prevention and treatment effects on various inflammation-related diseases. However, the research on the anti-inflammatory effect of hydrogen still faces some challenges, such as the need to improve bioavailability, preparation and storage problems, relatively high cost when used alone, and limited antibacterial and anti-inflammatory effects.

[0005] Aiming at the problems existing in the prior art, how to provide an oral buccal tablet that can be applied to the oral field and has a high antibacterial rate, good anti-inflammatory effect, and is convenient to use is an urgent problem to be solved by the present invention. Summary of the Invention

[0006] The purpose of the present invention is to provide an oral buccal tablet with anti-inflammatory and antibacterial effects to solve the problems raised in the above background art.

[0007] To achieve the above purpose, the present invention provides an oral buccal tablet with anti-inflammatory and antibacterial effects, which is characterized in that the oral buccal tablet contains the following components in parts by weight: 50 - 80 parts of dandelion extract, 20 - 40 parts of catechins, 20 - 60 parts of hydrogen source disintegrant, 1 - 10 parts of surfactant, 1 - 5 parts of flavoring agent, 0.5 - 3 parts of preservative;

[0008] The surfactant is modified sodium alginate.

[0009] As a further improvement, the raw materials for preparing the modified sodium alginate include alginic acid and cholesterol.

[0010] As a further improvement, the synthesis of the modified sodium alginate comprises the following steps:

[0011] (1) Place an organic solvent in a flask, add alginic acid, stir at 40 - 60 °C for 6 - 12 h, and then cool to room temperature;

[0012] (2) Dissolve cholesterol and a catalyst in the organic solvent respectively, and then slowly drop them into the mixture in step (1). Then stir and react at room temperature for 12 - 24 h. After the reaction ends, perform post-treatment to obtain a solid substance;

[0013] (3) Dissolve the dried solid substance in distilled water, adjust the pH to 6 - 7 with a sodium-containing alkaline solution, let it stand for 2 - 5 h, then centrifuge to separate and remove insoluble substances. Rotate and evaporate the supernatant to concentrate it, and perform post-treatment to obtain the modified sodium alginate.

[0014] As a further improvement, the catalyst is N,N'-dicyclohexylcarbodiimide and 4-dimethylaminopyridine.

[0015] As a further improvement, the addition amount of the hydrogen source disintegrant is 30 - 50% of the total addition amount of dandelion extract and catechin.

[0016] As a further improvement, the preparation of the hydrogen source disintegrant comprises the following steps:

[0017] (1) Mix the hydrogen production matrix and the disintegrant according to mass percentages;

[0018] (2) Mix and dry the binder and the filler, and then add them to step (1). Sieve to obtain the hydrogen source disintegrant.

[0019] As a further improvement, the hydrogen production matrix is magnesium powder.

[0020] As a further improvement, the acid source is a mixture of malic acid, tartaric acid, and adipic acid.

[0021] As a further improvement, the binder is a composition of microcrystalline cellulose and modified microcrystalline cellulose.

[0022] As a further improvement, the filler is glucose.

[0023] As a further improvement, the flavoring agent is at least one of apple essence, blackberry powder, stevioside, sucrose, and sorbitol.

[0024] Preferably, the flavoring agent is apple essence.

[0025] As a further improvement, the preservative is at least one of methyl paraben, ethyl paraben, sorbic acid, sodium benzoate, and benzyl alcohol.

[0026] Preferably, the preservative is ethyl paraben.

[0027] The present invention also provides a method for preparing an oral buccal tablet with anti-inflammatory and antibacterial effects, which is characterized by comprising the following steps:

[0028] By weight, first mix the dandelion extract, catechin, and hydrogen source disintegrant, and then add the surfactant, flavoring agent, and preservative and continue to mix. After sieving and molding with a mold, an oral buccal tablet with anti-inflammatory and antibacterial effects is obtained.

[0029] Compared with the prior art, the beneficial effects of the present invention are:

[0030] The present invention provides an oral buccal tablet with anti-inflammatory and antibacterial effects, so that the prepared oral buccal tablet has a high antibacterial rate against Staphylococcus aureus, Candida albicans, Porphyromonas gingivalis, and Streptococcus mutans, and has a low swelling value and good anti-inflammatory effect. When applied to the oral cavity, it can effectively inhibit bacteria and treat inflammation. Specific Embodiments

[0031] The following will describe the present invention in combination with specific embodiments. It should be noted that the following examples are examples of the present invention and are only used to illustrate the present invention, rather than to limit the present invention. Other combinations and various improvements within the concept of the present invention can be made without departing from the gist or scope of the present invention.

[0032] In the following examples, except for modified sodium alginate, modified microcrystalline cellulose, and hydrogen source disintegrant, the other compound monomers and related reagents used can be purchased from the market. Among them, the dandelion extract is purchased from Xinyang Mufan Biotechnology Co., Ltd., model number MF-010973, catechin is purchased from Hubei Guangao Biotechnology Co., Ltd., product number GA1704, alginic acid is purchased from Shanghai Aladdin Biochemical Technology Co., Ltd., product number A110570, sodium alginate is purchased from Shanghai Aladdin Biochemical Technology Co., Ltd., product number S100128, cholesterol is purchased from Shanghai Aladdin Biochemical Technology Co., Ltd., product number C104028, apple essence is purchased from Hangzhou Tairen Biotechnology Co., Ltd., microcrystalline cellulose is purchased from Shanghai Linchen Pharmaceutical Technology Co., Ltd., model number KG-802, and glucose is purchased from Guangzhou Tianheng Technology New Materials Co., Ltd., model number 225.

[0033] The synthesis of modified sodium alginate comprises the following steps:

[0034] (1) Place 100 mL of dimethyl sulfoxide in a dry flask, add 3 g of alginic acid, stir at 50 °C for 12 h, and then cool to room temperature;

[0035] (2) Dissolve 1.5 g of cholesterol in 10 mL of chloroform, and slowly drop it into the mixture in step (1). Dissolve 0.96 g of N,N'-dicyclohexylcarbodiimide and 0.28 g of 4-dimethylaminopyridine in 15 mL of dimethyl sulfoxide, and then drop it into the mixture in step (1). Stir and react at room temperature for 24 h. After the reaction is completed, add 400 mL of absolute ethanol, centrifuge, remove the supernatant, retain the solid and dry it under vacuum;

[0036] (3) Dissolve the dried solid in 50 mL of distilled water, adjust the pH to 7 with a 4% sodium bicarbonate solution, let it stand for 3 h and then centrifuge to remove insoluble substances. Rotate and evaporate the supernatant to concentrate it to 20 mL, and then dialyze it in a dialysis bag with a molecular weight of 1400 for 5 days. After taking it out, add it to 80 mL of absolute ethanol, centrifuge, retain the solid and dry it to obtain modified sodium alginate.

[0037] The synthesis of modified microcrystalline cellulose comprises the following steps:

[0038] (1) Add 4 g of microcrystalline cellulose and 40 mL of distilled water to a flask and stir to mix to obtain a suspension, and then add 60 mL of absolute ethanol thereto and perform ultrasonic treatment for 30 min;

[0039] (2) Add 4 g of stearic acid to step (1), continue ultrasonic treatment for 30 min, and then stir and mix at 80 °C for 4 h. After the reaction is completed, centrifuge the solution with a refrigerated high-speed centrifuge, wash the precipitate with absolute ethanol, and finally dry it with hot air at 50 °C for 12 hours to obtain modified microcrystalline cellulose.

[0040] The preparation of the hydrogen source disintegrant comprises the following steps:

[0041] (1) Mix 8.5 g of magnesium powder, 26.8 g of malic acid, 14.4 g of tartaric acid, and 5.9 g of adipic acid;

[0042] (2) Mix 0.6 g of microcrystalline cellulose, 0.2 g of modified microcrystalline cellulose, and 43.6 g of glucose and dry at 50 °C, and then add it to step (1) and pass through a 100-mesh sieve to obtain the hydrogen source disintegrant.

[0043] The preparation methods of Examples 1-3 and Comparative Examples 1-3 include the following steps:

[0044] By weight parts, first mix dandelion extract, catechin, and hydrogen source disintegrant, and then add surfactant, flavoring agent, and preservative and continue mixing. Sieve through a 30-mesh sieve and press into tablets with a mold (each tablet is about 0.8 g) to obtain an oral buccal tablet with anti-inflammatory and antibacterial effects.

[0045] The components and contents used in Examples 1-3 and Comparative Examples 1-3 are shown in Table 1 below:

[0046] Table 1

[0047]

[0048] Perform antibacterial rate and anti-inflammatory effect tests on the oral buccal tablets with anti-inflammatory and antibacterial effects prepared in Examples 1-3 and Comparative Examples 1-3. The test methods are as follows:

[0049] Antibacterial rate: Test according to the 7.3 standard of QB / T 2738-2012. Take 0.1 g of the oral buccal tablet and add it to a sterilized test tube containing the test bacteria, add 5 mL of sterile water, mix well for 10 min, and perform the antibacterial rate test. The test bacteria are Staphylococcus aureus, Candida albicans, Porphyromonas gingivalis, and Streptococcus mutans, which are common in oral diseases;

[0050] Anti-inflammatory effect: Divide 60 healthy white mice with a body weight of about 20-25 g into 6 groups, 10 mice per group, with half males and half females. Apply xylene evenly on both sides of the right auricle of each mouse to cause inflammation, with a dose of 100 μL / mouse (50 μL / mouse on one side), and do not treat the left ear as a blank control group; 10 min after xylene-induced inflammation, use the oral buccal tablets of Examples 1-3 and Comparative Group 1-3 for the first time according to the grouping for the mice. The usage method is as follows: Quickly mix 5 g of the oral buccal tablet and 20 mL of distilled water in a container, immerse the right ear of the anesthetized mouse for 5 min, and after soaking, dry it; 20 min after inflammation induction, use the oral buccal tablets of Examples 1-3 and Comparative Group 1-3 for the second time according to the grouping for the mice. The usage method is the same as the first time. At the end of the experiment, anesthetize the mice, decapitate them by cervical dislocation, cut off both auricles, wash them with physiological saline, dry them, weigh them, and calculate the swelling value;

[0051] Swelling value = weight of the right ear auricle - weight of the left ear auricle; the smaller the swelling value, the better the anti-inflammatory effect.

[0052] The test results are shown in Table 2, as follows:

[0053] Table 2

[0054]

[0055] As can be seen from Example 2 and Comparative Example 1 in Table 2, compared with the buccal tablets prepared using unmodified sodium alginate, the buccal tablets prepared using modified sodium alginate have a higher antibacterial rate against Staphylococcus aureus, Candida albicans, Porphyromonas gingivalis, and Streptococcus mutans, and a lower swelling value, indicating a better anti-inflammatory effect.

[0056] As can be seen from Example 2 and Comparative Examples 2-3, compared with the buccal tablets prepared without using a hydrogen source disintegrant or with the ratio of the addition amount of the hydrogen source disintegrant to the total addition amount of dandelion extract and catechin not within the appropriate range, the buccal tablets prepared using a hydrogen source disintegrant and with the addition amount ratio within the appropriate range have a higher antibacterial rate and can, to a certain extent, reduce the swelling value, making the anti-inflammatory effect more excellent.

[0057] As can be seen from the test results of Examples 1-3, the buccal tablets prepared by the preparation method provided by the present invention have a higher antibacterial rate against Staphylococcus aureus, Candida albicans, Porphyromonas gingivalis, and Streptococcus mutans, a lower swelling value, and a better anti-inflammatory effect, indicating that a good antibacterial rate and anti-inflammatory effect can be achieved when applied to the oral cavity.

[0058] The above embodiments are only for illustrating the technical concept and features of the present invention, and their purpose is to enable those familiar with this technology to understand the content of the present invention and implement it. However, the protection scope of the present invention cannot be limited thereby. Any equivalent changes or modifications made according to the spirit and essence of the present invention should be covered within the protection scope of the present invention.

Claims

1. An oral buccal tablet with anti-inflammatory and antibacterial effects, characterized in that, The oral buccal tablets contain the following components in parts by weight: 50 - 80 parts of dandelion extract, 20 - 40 parts of catechin, 20 - 60 parts of hydrogen source disintegrant, 1 - 10 parts of surfactant, 1 - 5 parts of flavoring agent, 0.5 - 3 parts of preservative; The surfactant is modified sodium alginate.

2. The buccal tablet with anti-inflammatory and antibacterial effects according to claim 1, wherein, The raw materials for preparing the modified sodium alginate include sodium alginate and cholesterol.

3. The buccal tablets with anti-inflammatory and antibacterial effects according to claim 1 are characterized in that, The synthesis of the modified sodium alginate comprises the following steps: (1) Place an organic solvent in a flask, add sodium alginate, stir at 40 - 60 °C for 6 - 12 h, and then cool to room temperature; (2) Dissolve cholesterol and a catalyst in the organic solvent respectively, slowly drop them into the mixture in step (1), then stir and react at room temperature for 12 - 24 h, after the reaction ends, perform post-treatment to obtain a solid substance; (3) Dissolve the dried solid substance in distilled water, adjust the pH to 6 - 7 with a sodium-containing alkaline solution, let it stand for 2 - 5 h, then centrifuge to separate, remove the insoluble substances, rotary evaporate and concentrate the supernatant, and perform post-treatment to obtain the modified sodium alginate.

4. An oral buccal tablet with anti-inflammatory and antibacterial effects according to claim 1, characterized in that, The addition amount of the hydrogen source disintegrant is 30 - 50% of the total addition amount of the dandelion extract and catechin.

5. The oral buccal tablet with anti-inflammatory and antibacterial effects according to claim 1, characterized in that, The preparation of the hydrogen source disintegrant comprises the following steps: (1) Mix the hydrogen production matrix and the disintegrant according to mass percentage; (2) Mix and dry the binder and the filler, then add them to step (1), and sieve to obtain the hydrogen source disintegrant.

6. The buccal tablets with anti-inflammatory and antibacterial effects according to claim 1, characterized in that, The flavoring agent is at least one of apple essence, blackberry powder, stevioside, sucrose, and sorbitol.

7. An oral buccal tablet with anti-inflammatory and antibacterial effects according to claim 1, characterized in that, The preservative is at least one of methyl paraben, ethyl paraben, sorbic acid, sodium benzoate, and benzyl alcohol.

8. A preparation method of an oral buccal tablet with anti-inflammatory and antibacterial effects according to any one of claims 1-7, characterized in that, Comprises the following steps: By weight, first mix the dandelion extract, catechin, and hydrogen source disintegrant, then add the surfactant, flavoring agent, and preservative and continue to mix, sieve, and press into shape with a mold to obtain an oral buccal tablet with anti-inflammatory and antibacterial effects.

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