阅读说明：本技术 一种抑菌和/或脱敏的口腔用糊剂 (Antibacterial and/or desensitizing paste for oral cavity ) 是由 张文娟 王东隶 于 2021-07-16 设计创作，主要内容包括：本发明属于药物制剂技术领域,具体涉及一种抑菌和/或脱敏的口腔用糊剂。本发明公开的口腔用糊剂包括脱敏活性成分、抑菌活性成分、粘合剂、固体基质、抗氧剂、溶剂。通过优选脱敏活性成分的种类及比例、优化脱敏活性成分和抑菌活性成分的配比及其他辅料的种类和用量,共同提高本品的脱敏和抑菌效果,通过筛选抗氧剂的种类及用量,解决了活性成分易被氧化的问题,提高产品的稳定性。(The invention belongs to the technical field of pharmaceutical preparations, and particularly relates to antibacterial and/or desensitizing paste for oral cavity. The paste for oral cavity disclosed by the invention comprises desensitization active ingredients, antibacterial active ingredients, an adhesive, a solid matrix, an antioxidant and a solvent. The desensitization and bacteriostasis effects of the product are improved together by optimizing the type and proportion of the desensitization active ingredients, optimizing the proportion of the desensitization active ingredients and the bacteriostasis active ingredients and the type and dosage of other auxiliary materials, the problem that the active ingredients are easy to oxidize is solved by screening the type and dosage of the antioxidant, and the stability of the product is improved.)

1. An oral paste, which is characterized by comprising a desensitizing active ingredient, a bacteriostatic active ingredient, a binder, a solid matrix, an antioxidant and a solvent.

2. The paste for oral cavity according to claim 1, wherein the desensitizing active ingredient is 4-12 parts, the bacteriostatic active ingredient is 0.5-3 parts, the adhesive is 10-25 parts, the solid matrix is 50-80 parts, the antioxidant is 0.5-3 parts, and the solvent is 10-20 parts by weight.

3. The oral paste of claim 2, wherein the desensitizing active ingredient is 8 parts, the bacteriostatic active ingredient is 2 parts, the binder is 15 parts, the solid matrix is 60 parts, the antioxidant is 1 part, and the solvent is 14 parts by weight.

4. The oral paste of claim 1 wherein the desensitizing active ingredient is selected from one or more of sodium fluoride, ammonium fluoride, silver oxide, stannous fluoride, silver nitrate, potassium nitrate, preferably silver nitrate and stannous fluoride.

5. An oral paste according to claim 4, wherein the ratio of silver nitrate to stannous fluoride is 1:1 to 4 parts by weight, preferably 1: 3.

6. The oral paste of claim 1, wherein the bacteriostatic active ingredient is selected from one or more of chlorhexidine, ammonium bicarbonate, glutaraldehyde, and preferably chlorhexidine.

7. An oral paste according to claim 2 wherein the weight ratio of desensitizing and bacteriostatic active ingredients is from 1:0.1 to 0.3, preferably 1: 0.25.

8. The oral paste of claim 1, wherein the solid matrix is selected from one or more of kaolin, talc, calcium carbonate, magnesium carbonate, preferably kaolin; the adhesive is selected from one or more of tragacanth, carbomer, cyclodextrin and sodium alginate, and is preferably tragacanth; the solvent is selected from a hydroxyethyl methacrylate solution or/and an orthophosphoric acid solution, and is preferably a 5% hydroxyethyl methacrylate solution in mass fraction.

9. The oral paste of claim 1, wherein the antioxidant is selected from one or more of butyl hydroxy cumarin ether, dibutyl hydroxy toluene, gallocatechin gallate, and tert-butyl hydroquinone, preferably gallocatechin gallate.

10. Use of an oral paste according to any of claims 1 to 9 for alleviating tooth sensitivity and/or inhibiting oral bacteria.

Technical Field

The invention belongs to the technical field of pharmaceutical preparations, and particularly relates to antibacterial and/or desensitizing paste for oral cavity.

Background

Dentine hypersensitivity is defined as transient pain produced by exposed dentine, usually in response to chemical, temperature, tactile or osmotic stimuli, which cannot be explained by any other tooth defect or pathology. Erosion of the outer surface of the tooth (enamel) and/or gingival atrophy often results in exposure of the dentinal tubules, creating a pathway between the nerve fibers in the oral cavity and pulp. In vivo it has been shown that there is a pressure gradient across the dentin, which results in outward flow of fluid. This fluid flow is disturbed or increased in response to tactile, temperature (hot or cold), and osmotic stimuli (high concentrations of sugar, etc.), which are believed to result in a mechanoreceptor response of the nerve fibers within the pulp (detected as pain). Dentin hypersensitivity is a subjective symptom caused by external stimulation of exposed dentin, has the symptoms of tooth soreness and pain, and seriously influences the food intake and physical and psychological health of patients. Dentin hypersensitivity in stomatological diseases belongs to a common disease with high morbidity, and is clinically treated by laser desensitization treatment or medicaments such as fluoride, strontium chloride, silver ammonium fluoride, silver iodide and the like, but the single medicaments have the advantages and the disadvantages, the treatment effect is not ideal, the treatment effective rate is low, the effective maintaining time is short, and the recurrence rate is high.

Chinese patent CN106581078A discloses an oral desensitizing paste taking calcium powder, silicon dioxide, carboxymethyl cellulose, strontium chloride, potassium nitrate, fluoride, gel, sodium dodecyl sulfate, essence and/or honeycomb extract as main and auxiliary materials and a preparation method thereof, but the effective components of the paste are easy to oxidize, difficult to store and low in long-term stability.

With the increase of patients with tooth sensitivity, there is an urgent need to develop a therapeutic agent having more excellent effects than existing tooth sensitivity therapeutic agents, and to increase the bacteriostatic effect of the therapeutic agent to prevent tooth decay, slow down erosion of tooth enamel on the outer surface of teeth, and reduce the degree of tooth sensitivity.

Disclosure of Invention

The oral paste overcomes the defects of the prior art, solves the problem that active ingredients are easy to oxidize by optimizing and screening main and auxiliary materials and improving the prescription of the preparation, and has high long-term stability and can effectively relieve tooth sensitivity and/or oral bacteriostasis.

In order to achieve the purpose, the following technical scheme is adopted in the application:

the invention provides an oral paste which comprises a desensitizing active ingredient, a bacteriostatic active ingredient, an adhesive, a solid matrix, an antioxidant and a solvent.

Furthermore, the desensitizing active ingredient is 4 to 12 parts, the bacteriostatic active ingredient is 0.5 to 3 parts, the adhesive is 10 to 25 parts, the solid matrix is 50 to 80 parts, the antioxidant is 0.5 to 3 parts and the solvent is 10 to 20 parts by weight.

Preferably, 8 parts of desensitization active ingredient, 2 parts of bacteriostatic active ingredient, 15 parts of adhesive, 60 parts of solid matrix, 1 part of antioxidant and 14 parts of solvent.

Further, the desensitizing active ingredients are selected from one or more of sodium fluoride, ammonium fluoride, silver oxide, stannous fluoride, silver nitrate and potassium nitrate, preferably silver nitrate and stannous fluoride.

Specifically, the weight ratio of the silver nitrate to the stannous fluoride is 1:1-4, and preferably 1: 3.

Further, the bacteriostatic active ingredient is selected from one or more of chlorhexidine, ammonium bicarbonate and glutaraldehyde, and preferably chlorhexidine.

Specifically, the weight ratio of the desensitizing active ingredient to the bacterial ingredient is 1:0.1-0.3, preferably 1: 0.25.

Further, the solid matrix is selected from one or more of kaolin, talcum powder, calcium carbonate and magnesium carbonate, and is preferably kaolin; the adhesive is selected from one or more of tragacanth, carbomer, cyclodextrin and sodium alginate, and is preferably tragacanth; the solvent is selected from a hydroxyethyl methacrylate solution or/and an orthophosphoric acid solution, and is preferably a 5% hydroxyethyl methacrylate solution in mass fraction; the antioxidant is selected from one or more of butyl hydroxy miaquilon, dibutyl hydroxy toluene, gallocatechin gallate and tert-butyl hydroquinone, preferably gallocatechin gallate.

A second object of the present invention is to provide the use of said oral paste for alleviating tooth sensitivity and/or inhibiting oral bacteria.

Compared with the prior art, the invention has the beneficial effects that:

(1) the type and the proportion of desensitization active ingredients are optimized, and the desensitization effect of the product is improved;

(2) the proportion of the desensitization active ingredients and the bacteriostatic active ingredients and the types and the dosage of other auxiliary materials are optimized, and the desensitization and bacteriostatic effects and various physical properties of the product are improved together;

(3) by screening the types of the antioxidants, the problem that the active ingredients are easy to oxidize is solved, and the stability is improved.

Detailed Description

In order to make the purpose and technical solution of the present invention more clear, the present invention is further described with reference to the following examples, but the scope of the present invention is not limited to these examples, and the examples are only used for explaining the present invention. It will be understood by those skilled in the art that various changes may be made and equivalents may be substituted without departing from the true scope of the invention. The present invention will be further described with reference to the following examples, but the present invention is not limited to these examples.

Example 1:

the preparation method comprises the following steps:

mixing the above raw materials and adjuvants, stirring, and mixing.

Example 2:

the preparation method comprises the following steps: the same as in example 1.

Example 3:

the preparation method comprises the following steps: the same as in example 1. Comparative example 1:

the preparation method comprises the following steps: the same as in example 1. Comparative example 2:

the preparation method comprises the following steps: the same as in example 1. Comparative example 3:

the preparation method comprises the following steps: the same as in example 1. Comparative example 4:

the preparation method comprises the following steps: the same as in example 1.

Verification examples

First, stability detection

The oral pastes prepared in examples 1 to 3 of the present invention and comparative examples 1 to 4 were tested for their properties, mildew and hardening after 6 months storage in an oven at 42 ℃ and 75% humidity for 6 months at room temperature.

TABLE 1 Properties, cases of mildew and hardening of the products of examples

The paste for oral cavity prepared by the protection scheme of the invention has excellent stability and long-term stability, and no hardening condition, mildew condition and the like are found, while the paste stability of the comparative example is not as good as that of the invention, especially, the paste of the comparative example 3 has precipitation, yellowing color, mildew, peculiar smell, hardening and the like after 6 months at 42 ℃, and is not easy to store.

Secondly, the sterilization performance is tested

The product performs experiments on the sterilization performance of escherichia coli, staphylococcus aureus and candida albicans, the results are shown in the following table, the experimental data in the table is the average value of three results,mean sterilization rate (%). It should be noted that, the sterilization effect in 5 minutes is only listed here, and sterilization experimental data of 10, 15, and 30 minutes may be provided.

TABLE 2 Sterilization Performance for the examples

The paste for oral cavity prepared by the protection scheme of the invention has an effect on staphylococcus aureus, escherichia coli and candida albicans for 5 minutes, has a sterilization rate of more than or equal to 99.6 percent, and has a remarkable sterilization effect. The paste prepared by the scheme of the comparative example has obviously inferior bactericidal effect to that of the example of the invention.

Third, summary of clinical cases

1. Clinical statistical case

1.1 case selection

45 out-patient cases were all dental hypersensitivity cases.

1.2 methods of treatment

Closely isolating the affected teeth, probing dentin hypersensitive region with a sharp probe, taking 10 as the most sensitive and 0 as no sensitivity, recording the hypersensitive degree of the patient as a pre-test baseline. Sterilizing and degreasing the sensitive area of the affected tooth with 75% alcohol, drying, coating the sensitive area with product paste with length of about 1cm, applying to the affected part for about 5 min, washing the residual paste with distilled water, probing the sensitive area of the tooth with sharp probe, and recording the degree of sensitivity of the patient. Tooth sensitivity was 0-2, as marked as significant, 3-8 as significant, and 9-10 as not significant.

1.3 assay of therapeutic efficacy

Table 3 example 1 overall efficacy analysis

TABLE 4 analysis of the overall efficacy of the comparative examples

As can be seen from the statistical data in tables 3-4, the invention has significant overall treatment effect on the tooth allergy patients, the total number of cases is 45, and the total effective rate reaches 95.5%. As can be seen from Table 4, the treatment effect of the comparative example on tooth sensitivity is poor, the total effective rate of the comparative example 1 is 28.8%, and the total effective rate of the comparative example 4 is 46.6%.

2. Typical cases

The treatment method is the same as 1.2.

Typical case 1: zhangqi, male, age 40. The degree of allergy was 9, and the affected part was coated with the paste of example 1 of the present invention for about 5 minutes, and after rinsing, the degree of sensitivity was significantly reduced to 1.

Typical case 2: hu-shi, woman, 45 years old. The degree of allergy was 8, and the affected part was coated with the paste of example 1 of the present invention for about 5 minutes, and after rinsing, the degree of sensitivity was significantly reduced, and the degree of allergy was 2.

It should be noted that the inventor also performed clinical trials on other examples and comparative examples, but these examples are not listed here, and supplementary data may be provided if necessary.