Effective substance microcapsule composition with environmental response and preparation method thereof

Abstract

The invention relates to a drug microcapsule composition with environmental response, the drug microcapsule composition comprises a wall material and a core material, the wall material comprises the following components by mass: 3.0-30.0% of polyvinyl alcohol; 3.0 to 30.0 percent of starch; 40.0 to 90.0% of a cross-linking agent; 3.0 to 15.0% of an electrolyte; the cross-linking agent is selected from one or more of gellan gum, alginate, locust bean gum, carrageenan and gelatin; the mass ratio of the electrolyte to the cross-linking agent ranges from 1: 20 to 1: 5; the core material is prepared from the following components in percentage by mass: 0.5 to 30.0 percent of functional substance; 50.0 to 90.0% of a functional substance carrier; 0.5 to 30.0 percent of efficacy substance slow-release synergist; the mass ratio of the efficacy substance to the efficacy substance slow-release synergist is (1: 5)-(5: 1). The wall material in the product contains an environmental response component, so that the functional drug can respond in the oral environment according to the change of the oral environment and the acidity of saliva, the shell on the surface is damaged or dissolved, and the drug-loaded particles are slowly released, thereby realizing the lasting bacteriostasis and improving the bad breath.

Description

Technical Field

[0001] The invention belongs to the field of daily chemicals, and in particular relates to a microcapsule composition of functional substances applicable to the oral cavity and having environmental response, and a preparation method thereof. Background Art

[0002] Functional microcapsules are special functional core materials that have undergone microencapsulation treatment. Their color, shape, volume, quality, solubility and storage properties will change to a certain extent. Under certain conditions, the functional core materials will be slowly released to play a role. The sustained-release effect of functional microcapsules can allow the active ingredients in the functional substances to reach the human body's action site and then be slowly released. On the one hand, it can protect other body organs from drug stimulation, and on the other hand, it can prevent high concentrations of functional substances from strongly stimulating the action site, and the continuous and uniform action can achieve effective treatment of the targeted site.

[0003] Lips are functional organs for speech, swallowing, chewing, etc. They also have the image function of expressing emotions and are one of the important image organs of the face. With the rapid development of the economy, consumers are paying more and more attention to the health of the oral cavity and the aesthetics of the lips. The health and aesthetics of the lips are mainly reflected in the absence of bad smell in the mouth, clean teeth, no cavities, no pain, normal gum color, no bleeding, no inflammation, cracks, light red color and no pigmentation on the lips.

[0004] Modern medical research shows that dental plaque is the main factor that causes inflammatory reactions in teeth and surrounding tissues, which can easily lead to the two most common oral diseases: caries and periodontal disease. In the early stages of periodontitis, the gums swell and ache, which hinder chewing and affect eating. In severe cases, it can cause swelling of the cheek on the affected side. At present, most oral products on the market have added functional drug ingredients, such as natural honeysuckle extract, chemical preparations cetylpyridinium chloride, fluoride, etc., but in fact, their claimed efficacy is limited, mainly due to the low utilization rate of free drugs in the products, short contact time with the oral cavity and other limitations, resulting in poor drug efficacy. There have been decades of research and use experience in oral disease problems at home and abroad, and certain results have been achieved. However, the breakthrough point is to find more effective drugs to solve oral problems, to ensure that oral health problems can be alleviated to a certain extent during brushing and gargling, but it is more difficult to fundamentally solve the problems facing the oral cavity. For example, Baena-Santillán ES et al. studied the effects of hibiscus acid and chlorhexidine on pathogenic bacteria in the oral cavity. The results showed that both had excellent inhibitory effects on the activity of pathogenic bacteria and could effectively penetrate the bacterial membrane. In comparison, chlorhexidine had better effects, but long-term high-dose use of chlorhexidine can cause black tongue coating, taste changes, and staining of the oral mucosal surface and teeth. Patent CN202110426698.3 proposes the synergistic effect of dipotassium glycyrrhizinate and cetylpyridinium chloride, which can significantly improve the inhibition rate of Escherichia coli and Staphylococcus aureus in the oral cavity; however, the antibacterial effect of the product can only last about 3 minutes. Therefore, drug encapsulation and sustained-release technology is widely used in the pharmaceutical field due to its advantages such as high drug utilization, long-lasting efficacy, and small side effects, but it is currently less used in the daily chemical field. The phenomenon of uncontrollable speed of drug microcapsules in the human body often occurs. With the changes in the environment such as human saliva and gastric juice, the sustained-release effect will deviate from the ideal speed, which greatly reduces the efficacy of the drug. For example, the release speed is too fast to be fully absorbed by the human body, or it is excreted from the body before it can be fully released, or the contents are inactivated. In particular, some drugs that act on the oral cavity require a sustained-release effect in the oral cavity. Since the tongue in the oral cavity is the most sensitive taste organ, the detection threshold for the contents is extremely low, so a uniform, timely and effective sustained-release speed is very important. If the drug is used directly for a long time and in high doses, it will cause the tongue coating to turn black, the taste to change, and the oral mucosal surface and teeth to be discolored. Therefore, drug encapsulation and sustained-release technology is needed, and it also has the advantages of high drug utilization in the oral cavity, lasting efficacy, and small side effects. At present, there are few reports on related technologies.

[0005] Similarly, some active ingredients for teeth and lips also face corresponding demands. For example, peroxides for teeth cleaning and whitening are very easy to be inactivated when used directly in products, and high concentrations of peroxides will cause excessive stimulation to the mouth and gums; the anti-inflammatory and anti-pigmentation ingredients of the lips also have the same problem. Therefore, it is urgent to find a solution to achieve the ideal efficacy of functional microcapsules in the mouth and lips, which will not act on non-active sites, but also slowly release at the active sites, with uniform and continuous action time, to achieve long-term inhibition of pathogenic bacteria in the mouth, improve oral odor, and keep teeth continuously clean and lips beautified and healthy. Summary of the invention

[0006] In view of the above-mentioned defects, the present invention provides an environmentally responsive functional microcapsule composition suitable for the oral cavity, teeth and lips, and a related preparation method. The wall material of the product contains oral cavity, teeth and lip environmental responsive components, which can make the functional drug respond to the oral environment according to the changes in the environment and the pH value of saliva, and the surface shell is destroyed or dissolved, so that the drug-loaded particles are slowly released, achieving long-lasting antibacterial and improving oral odor.

[0007] An object of the present invention is to provide a functional microcapsule composition with environmental response, wherein the functional microcapsule composition with environmental response comprises a wall material and a core material, wherein:

[0008] The wall material comprises the following components by mass fraction:

[0009]

[0010] The mass ratio of the electrolyte to the cross-linking agent is in the range of 1:20-1:5;

[0011] The core material includes the following components by mass fraction:

[0012] Effective substance 0.5-30.0%;

[0013] Effective substance carrier 50.0-90.0%;

[0014] The sustained-release enhancer of the efficacy substance is 0.5-20.0%.

[0015] The mass ratio of the antibacterial drug to the drug sustained-release enhancer is in the range of 1:5-5:1.

[0016] The alcoholysis degree of the polyvinyl alcohol is 98-100%;

[0017] The polyvinyl alcohol is selected from one or more of PVA1499, PVA1799, PVA2099, PVA2299, PVA2499, PVA2699 and the like.

[0018] The selection and compounding of the wall material are based on the following considerations: first, the microcapsules in the present invention need to be disintegratable in the lips, and the main component of the saliva in the mouth is amylase, which has good solubility and digestion properties for starch, so starch needs to be added to the wall material to achieve sensitive response behavior (i.e., disintegration) when encountering saliva; however, the film-forming property of starch is poor. After compounding with PVA, coupled with the high bonding effect of the cross-linking agent, the film-forming property of its shell is improved, and the compatibility of PVA and starch is good. The wall material blended by the two has a uniform texture and a relatively ideal sustained-release effect. The release rate of the contents in the microcapsule will not be unstable, more or less, thereby causing intermittent irritation to the mouth, tongue and lips.

[0019] Furthermore, the starch is selected from one or more of corn, potato, sweet potato, rice, millet starch, etc.;

[0020] The cross-linking agent is selected from one or more of gellan gum, locust bean gum, carrageenan and gelatin.

[0021] Furthermore, the inorganic salt is selected from one or more of chlorides, sulfates, and citrates, such as sodium chloride, calcium chloride, magnesium sulfate, sodium citrate, potassium citrate, and the like.

[0022] Furthermore, the functional ingredient is suitable for the oral cavity, teeth and / or lips, and is selected from oral pathogenic bacteria antibacterial drugs, tooth cleaning active ingredients, lip care functional ingredients, etc.

[0023] The oral pathogenic bacteria antibacterial drug is selected from one or more of honeysuckle extract, white peony extract, bitter almond extract, dipotassium glycyrrhizinate, zinc lactate, eugenol, tannic acid, cymene, chlorhexidine, cetylpyridinium chloride, and triclosan;

[0024] The tooth cleaning active is selected from one or more of dihydroxyamide acid, tartaric acid, diglycolic acid esters, peroxides, sodium sulforicinoleate, trihydroxyamide acid, glycolic acid, and cactus slurry;

[0025] The lip care ingredients are selected from one or more of the anti-inflammatory and anti-pigmentation agents such as allantoin, vitamins, glycyrrhetinic acid, hydroquinone cream, kojic acid cream, azelaic acid cream, arbutin cream, etc.

[0026] Furthermore, the functional substance carrier is selected from one or more of cellulose, dextrin or polysaccharide materials.

[0027] Furthermore, the efficacy substance sustained-release enhancer is selected from one or more of fatty acids or fatty alcohols.

[0028] The sustained-release synergist of the functional substance in the core material of the present invention has a synergistic effect with the material of the wall material, can promote the disintegration of the cross-linking agent and the wall material, and improve the sustained-release rate.

[0029] Furthermore, the functional substance carrier is selected from one or more of methyl cellulose, ethyl cellulose, cellulose acetate, triacetyl-β-cyclodextrin, chitosan, and carboxymethyl chitosan.

[0030] Furthermore, the efficacy substance sustained-release enhancer is selected from one or more of stearic acid, isostearic acid, cetostearyl alcohol, and dodecanol.

[0031] Preferably, the size of the microcapsule composition of the environmentally responsive functional substance of the present invention is 1-100 um, preferably 1-50 um.

[0032] Another object of the present invention is to provide a method for preparing the above-mentioned environmentally responsive drug microcapsule composition, the method for preparing the environmentally responsive functional substance microcapsule composition comprising the following steps:

[0033] S1, placing the components in the core material in an organic phase solvent and mixing and stirring to form a homogeneous core material mother solution;

[0034] S2, placing the components of the wall material except the electrolyte in an aqueous solution, first heating to 80-95°C and stirring evenly, then cooling to 50-70°C, adding the electrolyte, and forming a wall material mother solution;

[0035] S3, performing three-fluid spray drying on the core material mother liquid with the wall material mother liquid to achieve wrapping of the core material by the wall material.

[0036] Furthermore, the organic phase solvent is immiscible with water, has a boiling point lower than 120° C., and is selected from one or more of ethyl acetate, n-butanol, cyclohexylcyclohexyl, and n-hexylcyclohexyl.

[0037] Furthermore, the mass ratio of the core material to the wall material is 1:4-4:1.

[0038] Furthermore, the size of the functional substance microcapsule is 1-100 um, preferably 1-50 um.

[0039] Furthermore, in step S3, the degree of wrapping, the wrapping rate is greater than 70%.

[0040] The present invention has the following beneficial effects:

[0041] 1. The functional substance microcapsules of the present invention have excellent responsiveness to the human oral environment. Under the action of saliva, the structure in the wall material will achieve uniform and stable disintegration at an ideal rate under the synergistic effect of various components, so that the contents overflow and fill the entire oral cavity. The ideal rate of sustained release will not cause any negative impact on the mucosa and tongue inside the oral cavity, and it also has the effect of high utilization rate of the functional substance and long-lasting efficacy.

[0042] 2. The traditional technology directly adds drugs and other functional substances into the product matrix, and the functional substances are easily inactivated by the matrix. In the present invention, drugs and other functional substances are encapsulated and released slowly by microencapsulation technology, which can effectively solve the problems of inactivation of functional substances in the product and instability due to environmental influences. At the same time, it can also effectively avoid the compatibility problem between drugs and other functional substances and the matrix.

[0043] 3. In the traditional spray drying method, the core material and the wall material are easily mixed together, the sustained release effect is poor, and the encapsulation rate is generally about 30%; while the present invention adopts three-fluid encapsulation technology, the core material and the wall material can be effectively separated, and the effective encapsulation of drugs and other functional substances can be achieved, and the encapsulation rate can reach more than 70%.

[0044] 4. The microcapsules of drugs and other functional substances in the present invention can only be slowly released in the presence of saliva, thus effectively realizing intelligent regulation. BRIEF DESCRIPTION OF THE DRAWINGS

[0045] Figure 1 (a) is a microscopic structural diagram of the drug microcapsules in Example 3; Figure 1 (b) is a microscopic structural diagram of the drug microcapsules in Comparative Example 1.

[0046] Figure 2 (a) is a particle size analysis diagram of Example 3; Figure 2 (b) is the particle size analysis diagram of Comparative Example 1.

[0047] Figure 3 This is the differential scanning calorimetry analysis diagram of Example 3. DETAILED DESCRIPTION

[0048] In order to more clearly illustrate the technical solution of the present invention, the following examples and comparative examples are listed. Unless otherwise stated, the raw materials, reactions and post-treatment methods in the examples and comparative examples are common raw materials on the market and technical methods well known to those skilled in the art.

[0049] Unless otherwise specified, all technical and scientific terms used herein have the same meaning as those commonly understood by those skilled in the art of the present invention. The terms used in the specification of the present invention are only for the purpose of describing specific embodiments and are not intended to limit the present invention.

[0050] Unless otherwise stated, all formulations and testing herein took place at room temperature.

[0051] Herein, "includes", "comprising", "including", "containing", "having" or other variations are intended to cover non-exclusive inclusions, and no distinction is made between these terms. The term "comprising" means that other steps and ingredients that do not affect the end result can be added. The term "comprising" also includes the terms "consisting of" and "consisting essentially of". The compositions and methods / processes of the present invention may include, consist of, and consist essentially of the essential elements and limitations described herein, as well as any additional or optional ingredients, components, steps, or limitations described herein.

[0052] Terms and Definitions:

[0053] Drug microcapsule embedding rate: refers to the ratio of the mass of the drug encapsulated by the wall material to the total mass of the drug, which is calculated by the following formula:

[0054]

[0055] Accurately weigh an appropriate amount of drug microcapsule product, recorded as M, extract with a certain volume of solvent for about 2 minutes, filter, and further extract with 2 times the volume of solvent, filter, collect the two filtrates, put them into a rotary evaporator for rotary evaporation until the solvent is completely removed, and record its mass as m. The embedding rate of drug microcapsules (%) = (1-m / M) × 100%. Generally, the higher the embedding rate of drugs, the better the sustained release effect; factors such as the ratio of wall material to core material, the ratio of electrolyte to cross-linking agent, etc. will affect the embedding rate of drug microcapsules.

[0056] Drug microcapsule particle size:

[0057] The size of drug microcapsules is an important factor affecting the antibacterial effect of drug microcapsules. The smaller the particle size of the microcapsule, the larger the specific surface area, the larger the contact surface with the site of action, and the better the effect; but if the size is too small, it is not easy to stay at the site of action, which reduces the effect. If the particle size is too large, the drug microcapsules will feel like foreign matter during use, which will deteriorate the experience. At the same time, it will also seriously affect the stability of the drug microcapsules in the matrix and their stay at the site of action. The particle size of the drug microcapsules in the present invention is analyzed and tested accordingly using a laser particle size analyzer, using D50, which is the particle size corresponding to when the cumulative particle size distribution percentage of the sample reaches 50%. The size of the drug microcapsule D50 in the present invention is 1-100um, preferably 1-50um.

[0058] Sustained release amount of drug microcapsules:

[0059] To simulate the oral environment, add amylase to the aqueous solution and adjust the pH value of the aqueous solution to control the response factor of the drug microcapsule. Use the UV spectrophotometer to scan the full UV band of drugs of different concentrations under different response conditions, and develop a standard curve. Then detect the absorbance of the drug in the release solution and calculate its concentration through the standard curve, and then calculate the cumulative release of the drug according to the following formula.

[0060]

[0061] in:

[0062] R n : The cumulative amount of drug released at the nth hour;

[0063] 100: volume of the solution (mL);

[0064] C n : At the nth hour, solution drug concentration (mg / mL);

[0065] 1000: conversion unit (μg / mg);

[0066] m: drug microcapsule powder mass (mg);

[0067] ω: encapsulation rate of drug microcapsules.

[0068] The embodiments of the present invention include three parts: a pharmaceutical microcapsule composition with environmental response, a preparation method and performance of amylase aqueous solution sustained release.

[0069] The mass fractions and mass fractions of the components described in the preparation method of the present invention can be converted: if the mass fraction of the core material is known to be 3g, then the mass fraction of cetylpyridinium chloride (mass fraction of 15%) is 0.45g, and so on.

[0070] Table 1 shows the components and related characteristics of the environmentally responsive pharmaceutical microcapsule compositions of Examples 1-4 and Comparative Examples 1-2.

[0071] Table 1 Composition of drug microcapsule compositions with environmental responses

[0072]

[0073]

[0074] Note: The drug microgels prepared by compositions A, B, C, D, E, and F were formulated into 1.0% microcapsule aqueous solutions, and the amylase concentrations in the aqueous solutions were 0.15 mg / ml, 0.15 mg / ml, 0.15 mg / ml, 0.15 mg / ml, 0.15 mg / L, and 0.5 mg / L, respectively.

[0075] Preparation method:

[0076] S1. According to the above mass fractions, the components in the core material are placed in 30-120 parts of ethyl acetate / n-butanol solution, sealed and mixed at 70-80 ° C for 30 minutes to form a core material mother solution;

[0077] S2. According to the above mass fractions, the components of the wall material except the electrolyte are placed in 100-400 parts of deionized water, mixed at 90 ° C for 1h, then cooled to 70 ° C, and then the electrolyte calcium chloride is added, stirred and dissolved to form a wall material mother liquor;

[0078] S3. Under the action of the three-fluid spray dryer, the core material mother liquid and the wall material mother liquid are sprayed out from the two nozzles of the three-fluid respectively to achieve spray drying of the core material and wrapping of the core material by the wall material, and the temperature at the nozzle of the three-fluid spray dryer is controlled to be 90 ° C;

[0079] Among them, the core materials corresponding to compositions A and C during the preparation process are dissolved in 30 parts of n-butanol, and the core material of composition E is dissolved in 30 parts of propylene glycol; the core material of composition B is dissolved in 90 parts of n-butanol, and the core materials of compositions D and F are dissolved in 60 parts of n-butanol.

[0080] The wall material of composition A was dispersed and dissolved in 400 parts of deionized water, the compositions B, C, and E were dispersed and dissolved in 100 parts of deionized water, and the compositions D and F were dispersed and dissolved in 200 parts of deionized water.

[0081] Table 2 Performance test results of environmentally responsive drug microcapsule compositions

[0082]

[0083] The compositions A, B, C, and D of Examples 1-4 have excellent embedding rates, and the particle size distribution D50 of the prepared functional microcapsules are 5.463 um, 28.775 um, 8.746 um, and 13.583 um, respectively, all below 30 um. Figure 1It can be observed under a microscope that the functional microcapsules prepared in Example 3 have excellent dispersibility; at the same time, its particle size distribution presents a relatively good normal distribution. Compared with Comparative Example 1 (particle size D50 is 214.318um) and Comparative Example 2 (particle size D50 is 15.214um), the functional microcapsules prepared in Examples 1-4 present excellent sustained release effects. This is mainly due to the lack of sustained release enhancer stearic acid in Comparative Example 1, which causes the system to release almost all the drug efficacy in about 2 hours, and does not have a sustained release effect; Comparative Example 2 has too high a starch content in the wall material, resulting in insufficient strength of the wall material, and rapid disintegration occurs under the action of amylase, resulting in poor sustained release effect. At the same time, since the boiling point of the solvent propylene glycol used in the core material of composition E in comparative example 1 is too high, and the core material solution and the wall material solution have relatively good compatibility, incomplete drying occurs during the spray drying process, resulting in large particle size of the obtained functional microcapsules, with D50 as high as 214.318um, and the encapsulation rate of the functional drug microcapsules is also low. The taste in the mouth can be clearly perceived, which is not conducive to practical application.

[0084] Figure 3 The differential scanning calorimetry analysis diagram of Example 3 is listed. It can be seen from the figure that the raw material ethyl cellulose of the core material has no obvious endothermic peak within the above temperature range, and the melting endothermic peaks of the raw materials cetylpyridinium chloride and stearic acid are about 85°C and 60°C respectively; the melting endothermic peaks of the raw materials gellan gum, polyvinyl alcohol and starch of the wall material are about 100°C, 220°C and 120°C respectively. The drug microcapsules prepared by the three-fluid spray drying method in the experiment disappeared at the above melting endothermic peaks of about 85°C, 60°C, 100°C, 220°C and 120°C, and a new melting endothermic peak was generated at about 130°C, that is, the prepared drug microcapsules changed the melting state of the original wall material components and the core material components, indicating that the drug microcapsules can effectively load the core material carrier components and drug efficacy components.

[0085] Table 3 shows the components and related characteristics of the environmentally responsive pharmaceutical microcapsule compositions of Examples 5-7 and Comparative Examples 3-6.

[0086] Table 3 Components of the environmentally responsive drug microcapsule compositions of Examples 5-7 and Comparative Examples 3-6

[0087]

[0088]

[0089] The preparation method is as follows:

[0090] S1. According to the above mass fractions, the components in the core material are placed in 60 parts of n-butanol solution, sealed and mixed at 85 ° C for 30 minutes to form a core material mother solution;

[0091] S2. According to the above mass fractions, the components of the wall material except the electrolyte are placed in 200 parts of deionized water, mixed at 95 ° C for 1h, then cooled to 60 ° C, and then the electrolyte sodium chloride is added, stirred and dissolved to form a wall material mother liquor;

[0092] S3. Under the action of the three-fluid spray dryer, the core material mother liquid and the wall material mother liquid are sprayed out from the two nozzles of the three-fluid respectively to achieve spray drying of the core material and wrapping of the core material by the wall material, and the temperature at the nozzle of the three-fluid spray dryer is controlled to be 90 ° C;

[0093] Table 4 Performance test components of the environmentally responsive microcapsule compositions of Examples 5-7 and Comparative Examples 3-6

[0094]

[0095] Note: The concentration of amylase in the aqueous solution in which the functional microcapsules prepared by the composition GM are placed for sustained release is 0.1 mg / ml.

[0096] As can be seen from the table, compositions G, H, and I have excellent embedding rates, and the particle size distribution D50 of the prepared functional microcapsules is 35.821um, 3.865um, and 4.236um, respectively. At the same time, compositions G, H, and I show uniform sustained-release effects, and the sustained-release rate can reach about 80% in 8h. In the comparative composition J, polyvinyl alcohol PVA1788 (alcoholysis degree is about 88%) is used to replace PVA1799 (alcoholysis degree is about 99%). The excellent water solubility of PVA1788 at room temperature makes the functional microcapsules very easy to collapse in the aqueous solution of amylase, resulting in the release of the functional substance in a short time, and there is no sustained-release effect. In addition, in comparative examples 4 and 5, protein powder and ethyl cellulose are used, and the phenomenon of decreased encapsulation rate of functional microcapsules or poor sustained-release effect occurs; and when xanthan gum of polysaccharides is used in composition M, it is impossible to cross-link gel with electrolytes for synergistic enhancement, and the problem of poor sustained-release effect of functional microcapsules also occurs.

[0097] It will be apparent to those skilled in the art that the present invention is not limited to the details of the exemplary embodiments described above and that the present invention can be implemented in other specific forms without departing from the spirit or essential features of the present invention. Therefore, the embodiments should be considered exemplary and non-restrictive in all respects, and the scope of the present invention is defined by the appended claims rather than the above description, and it is intended that all changes falling within the meaning and scope of the equivalent elements of the claims be included in the present invention.

[0098] In addition, it should be understood that although the present specification is described according to implementation modes, not every implementation mode contains only one independent technical solution. This description of the specification is only for the sake of clarity. Those skilled in the art should regard the specification as a whole. The technical solutions in each embodiment may also be appropriately combined to form other implementation modes that can be understood by those skilled in the art.

Claims

1. A microcapsule composition with environmental response, characterized in that: The environmentally responsive functional microcapsule composition comprises a wall material and a core material, wherein: The wall material comprises the following components by mass fraction: The mass ratio of the electrolyte to the cross-linking agent is in the range of 1:20-1:5; The core material includes the following components by mass fraction: Effective substance 0.5-30.0%; Effective substance carrier 50.0-90.0%; 0.5-30.0% of sustained-release enhancer of efficacy substance; The mass ratio of the functional substance to the functional substance sustained-release enhancer is in the range of 1:5-5:

1.

2. The environmentally responsive functional microcapsule composition according to claim 1, characterized in that: The alcoholysis degree of the polyvinyl alcohol is 98-100%; The polyvinyl alcohol is selected from one or more of PVA1499, PVA1799, PVA2099, PVA2299, PVA2499, PVA2699 and the like.

3. The microcapsule composition of environmentally responsive functional substance according to claim 1, characterized in that: The starch is selected from one or more of the starches in corn, potato, sweet potato, rice, millet, etc.; The cross-linking agent is selected from one or more of gellan gum, locust bean gum, carrageenan and gelatin.

4. The microcapsule composition of functional substance with environmental response according to claim 1, characterized in that: The electrolyte is an inorganic salt and / or an organic salt, selected from one or more of chlorides, sulfates, and citrates.

5. The microcapsule composition of functional substance with environmental response according to claim 1, characterized in that: The functional ingredient is suitable for the oral cavity, teeth and / or lips, and is selected from one or more of oral pathogenic bacteria antibacterial drugs, tooth cleaning active substances, and lip care functional substances; The oral pathogenic bacteria antibacterial drug is selected from one or more of honeysuckle extract, white peony extract, bitter almond extract, dipotassium glycyrrhizinate, zinc lactate, eugenol, tannic acid, cymene, chlorhexidine, cetylpyridinium chloride, and triclosan; The tooth cleaning active is selected from one or more of dihydroxyamide acid, tartaric acid, diglycolic acid esters, peroxides, sodium sulforicinoleate, trihydroxyamide acid, glycolic acid, and cactus slurry; The lip care ingredients are selected from one or more of the anti-inflammatory and anti-pigmentation agents such as allantoin, vitamins, glycyrrhetinic acid, hydroquinone cream, kojic acid cream, azelaic acid cream, arbutin cream, etc.

6. The microcapsule composition of environmentally responsive functional substance according to claim 1, characterized in that: The functional substance carrier is selected from one or more of cellulose, dextrin or polysaccharide materials.

7. The microcapsule composition of functional substance with environmental response according to claim 1, characterized in that: The sustained-release enhancer of the efficacy substance is selected from one or more of fatty acids or fatty alcohols.

8. The microcapsule composition of functional substance with environmental response according to claim 6, characterized in that: The functional substance carrier is selected from one or more of methyl cellulose, ethyl cellulose, cellulose acetate, triacetyl-β-cyclodextrin, chitosan, and carboxymethyl chitosan.

9. The microcapsule composition of environmentally responsive functional substance according to claim 7, characterized in that: The efficacy substance sustained-release enhancer is selected from one or more of lauryl alcohol, tetradecanol, hexadecanol, octadecyl alcohol, myristic acid, palmitic acid, and stearic acid.

10. The method for preparing the microcapsule composition of environmentally responsive functional substance according to any one of claims 1 to 9, characterized in that: The preparation method of the environmentally responsive microcapsule composition comprises the following steps: S1, placing the components in the core material in an organic phase solvent that is immiscible with water and mixing and stirring to form a core material mother solution; S2, placing the components of the wall material except the electrolyte in an aqueous solution, first heating to 80-95°C and stirring evenly, then cooling to 50-70°C, adding the electrolyte, and forming a wall material mother solution; S3, performing three-fluid spray drying on the core material mother liquid with the wall material mother liquid to achieve wrapping of the core material by the wall material.

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