Dietary fiber inulin and medium-chain triglyceride composite capsule coating and preparation method thereof

Abstract

The present invention relates to the technical field of pharmaceutical excipients, and provides a composite capsule coating of dietary fiber inulin and medium-chain triglycerides, comprising the following raw materials in mass percentage: 60-80% dietary fiber inulin and 20-40% medium-chain triglycerides. The present invention also provides a method for preparing the above-mentioned capsule coating, comprising the following steps: mixing the raw materials, microemulsification treatment, and coating. The advantages of the present invention are: (1) it uses natural ingredients, has good biocompatibility, reduces side effects on the human body, and has high absorption efficiency; (2) it can effectively promote the balanced growth of intestinal flora and maintain intestinal health; (3) it can promote the colonization and reproduction of beneficial bacteria; (4) the process is simple and feasible, and has good application prospects.

Description

Technical Field

[0001] The present invention relates to the technical field of pharmaceutical excipients, and in particular to a dietary fiber inulin and medium-chain triglyceride composite capsule coating for promoting intestinal health and drug absorption, and a preparation method thereof. Background Art

[0002] In recent years, with increasing public awareness of health, research on intestinal health and the gut microbiome has become a hot topic. Currently, most capsule coatings on the market use synthetic chemical materials. While these materials can meet basic protection and release requirements, they have significant drawbacks, such as poor biocompatibility, significant toxic side effects, and low absorption efficiency. These synthetic chemical materials may induce immune responses or other adverse reactions after entering the human body, and long-term use may also burden organs such as the liver and kidneys.

[0003] Inulin, a natural polysaccharide with excellent water solubility and stability, can be fermented and utilized by intestinal bacteria to produce short-chain fatty acids, which lower intestinal pH and inhibit the growth of harmful bacteria, thereby promoting the proliferation of beneficial bacteria and improving the intestinal microecological environment. Inulin also promotes intestinal motility, increases stool bulk, and prevents constipation and diseases such as colon cancer.

[0004] Medium-chain triglycerides (MCTs) are a highly efficient energy source that is rapidly absorbed and metabolized by the body. Unlike long-chain triglycerides, MCTs do not require bile acids during digestion and can be metabolized directly into the liver through the portal vein. This rapid absorption and metabolism gives MCTs a unique advantage in promoting the colonization and growth of intestinal flora. MCTs also possess antibacterial and antiviral properties, helping to boost immunity and protect intestinal health.

[0005] In the prior art, there are few studies on combining dietary fiber inulin and medium-chain triglycerides for capsule coating, and no public reports have been found.

[0006] Based on this, we can try to develop a new composite capsule coating material of dietary fiber inulin and medium-chain triglycerides for promoting intestinal health and drug absorption. Summary of the Invention

[0007] The technical problem to be solved by the present invention is to provide a composite capsule coating of dietary fiber inulin and medium-chain triglycerides and a preparation method thereof, so as to solve the problems of poor biocompatibility, large toxic side effects, and low absorption efficiency of existing capsule coating materials, enhance the colonization and promotion effect on intestinal flora, and improve intestinal health.

[0008] The present invention adopts the following technical solutions to solve the above technical problems:

[0009] A dietary fiber inulin and medium-chain triglyceride composite capsule coating comprises the following raw materials in percentage by mass: 60-80% dietary fiber inulin and 20-40% medium-chain triglyceride.

[0010] As one of the preferred embodiments of the present invention, the raw materials are included in the following specific percentages by mass: 70% dietary fiber inulin and 30% medium chain triglycerides.

[0011] As one of the preferred embodiments of the present invention, the raw materials are included in the following specific percentages by mass: 65% dietary fiber inulin and 35% medium chain triglycerides.

[0012] As one of the preferred embodiments of the present invention, the raw materials are included in the following specific percentages by mass: 75% dietary fiber inulin and 25% medium chain triglycerides.

[0013] A method for preparing the dietary fiber inulin and medium-chain triglyceride composite capsule coating comprises the following steps:

[0014] S1. Raw material mixing: Dietary fiber inulin and medium-chain triglycerides are mixed uniformly according to a ratio to prepare a uniform raw material mixture;

[0015] S2. Microemulsification: The raw material mixture is treated by a microemulsification process to form stable tiny core-shell structure particles;

[0016] S3, coating: the tiny core-shell structure particles obtained in step S2 are evenly coated on the capsule shell to form a capsule coating.

[0017] As one of the preferred embodiments of the present invention, in step S1, the dietary fiber inulin and medium-chain triglycerides are placed in a mixing tank and stirred thoroughly to achieve uniform mixing of the raw materials; and wherein the stirring speed is 500-800 rpm and the stirring time is 10-15 min.

[0018] As one of the preferred embodiments of the present invention, in step S2, the specific process of microemulsification treatment is as follows:

[0019] Heat the raw material mixture to 30-40°C. This temperature range helps reduce viscosity and improve the effect of the subsequent emulsification process.

[0020] Add the emulsifier and co-surfactant to the raw material mixture and stir again at a stirring speed of 500-800 rpm for 5-10 minutes;

[0021] Use a high shear homogenizer for microemulsification treatment, maintain the temperature at 30-40°C, maintain the rotation speed at 8000-12000 rpm, and process for 20-40 minutes to ensure the formation of uniform micro core-shell structure particles.

[0022] As one of the preferred embodiments of the present invention, the emulsifier is 1-2% Tween-80, and the auxiliary surfactant is 1-2% lecithin.

[0023] As one of the preferred embodiments of the present invention, in step S2, the target size of the micro core-shell structured particles finally formed is usually less than 100 nanometers, with an average particle size of 50 to 100 nm.

[0024] As one of the preferred embodiments of the present invention, in step S3, the coating thickness is controlled to be 8-12 μm to ensure the solubility and release characteristics of the capsule.

[0025] Design principle:

[0026] The capsule coating of the present invention is composed of dietary fiber inulin and bioactive medium-chain triglycerides. These two ingredients are precisely proportioned and processed with scientific processes to form stable tiny core-shell structure particles, which are evenly coated on the capsule shell. Among them, dietary fiber inulin, as a prebiotic, can be fermented and utilized by intestinal bacteria to produce beneficial short-chain fatty acids and regulate the balance of intestinal flora; medium-chain triglycerides can be quickly absorbed and metabolized by the intestines, improving the colonization efficiency of beneficial flora. Through the scientific combination of dietary fiber inulin and medium-chain triglycerides, the capsule coating of the present invention can not only improve the microecological environment of intestinal flora and enhance intestinal health, but also improve the bioavailability of drugs and reduce side effects on the human body.

[0027] The advantages of the present invention over the prior art are:

[0028] (1) Good biocompatibility, low toxicity and side effects, and high absorption efficiency: The capsule coating of the present invention uses natural ingredients, has good biocompatibility, reduces side effects on the human body, and has high absorption efficiency;

[0029] (2) Promote the balanced growth of intestinal flora: Dietary fiber inulin, as a natural prebiotic, can be fermented and utilized by intestinal bacteria to produce short-chain fatty acids, lower the intestinal pH value, inhibit the growth of harmful bacteria, and thus promote the reproduction of beneficial bacteria; by improving the intestinal microecological environment, the present invention can effectively promote the balanced growth of intestinal flora and maintain intestinal health.

[0030] (3) Improve the colonization rate of bacterial flora: Medium-chain triglycerides (MCT) can be quickly absorbed and metabolized by the intestines, providing a direct energy source for beneficial intestinal flora and enhancing their colonization ability in the intestines; MCT also has antibacterial and antiviral functions, which can inhibit the growth of harmful bacteria and further promote the colonization and reproduction of beneficial bacteria;

[0031] (4) Simple and feasible process: The preparation process of the present invention is simple, easy to industrialize and has good application prospects. BRIEF DESCRIPTION OF THE DRAWINGS

[0032] Figure 1 This is a flow chart for preparing the coating of the composite capsule of dietary fiber inulin and medium-chain triglycerides in Example 1. DETAILED DESCRIPTION

[0033] The embodiments of the present invention are described in detail below. The embodiments are implemented under the premise of the technical solution of the present invention, and detailed implementation methods and specific operating procedures are given, but the protection scope of the present invention is not limited to the following embodiments. At the same time, the raw materials, reagents, equipment and methods used in the following examples are conventional raw materials, reagents, equipment and methods in the art unless otherwise specified, and are not repeated here.

[0034] Example 1

[0035] The dietary fiber inulin and medium-chain triglyceride composite capsule coating of this embodiment includes the following raw materials in percentage by mass: 70% dietary fiber inulin and 30% medium-chain triglycerides.

[0036] Preparation method (refer to Figure 1 ):

[0037] S1. Raw material mixing

[0038] Dietary fiber inulin and medium-chain triglycerides were placed in a mixing tank according to a proportion and stirred thoroughly at a stirring speed of 700 rpm for 12 minutes to prepare a uniform raw material mixture.

[0039] S2. Microemulsification treatment

[0040] ①Heat the raw material mixture to 37℃.

[0041] ② Add 1.5% Tween-80 and 1.5% lecithin to the raw material mixture and stir again at a stirring speed of 700 rpm for 8 minutes.

[0042] ③ Use a high shear homogenizer for microemulsification treatment, maintain the temperature at 37°C and the rotation speed at 10,000 rpm for 30 minutes to form uniform tiny core-shell structure particles with an average particle size of 50 to 100 nm.

[0043] S3, coating

[0044] The tiny core-shell structure particles obtained in step S2 are evenly coated on the capsule shell, and the coating thickness is controlled to be 10 μm to form a capsule coating.

[0045] Example 2

[0046] The dietary fiber inulin and medium-chain triglyceride composite capsule coating of this embodiment includes the following raw materials in percentage by weight: 65% dietary fiber inulin and 35% medium-chain triglycerides.

[0047] The preparation method is basically the same as that of Example 1, except that:

[0048] The microemulsification treatment time was 40 min;

[0049] The coating thickness was 12 μm.

[0050] Example 3

[0051] The dietary fiber inulin and medium-chain triglyceride composite capsule coating of this embodiment includes the following raw materials in percentage by mass: 75% dietary fiber inulin and 25% medium-chain triglycerides.

[0052] The preparation method is basically the same as that of Example 1, except that:

[0053] The microemulsification treatment time was 25 min;

[0054] The coating thickness was 8 μm.

[0055] Example 4

[0056] The dietary fiber inulin and medium-chain triglyceride composite capsule coating of this embodiment includes the following raw materials in percentage by mass: 60% dietary fiber inulin and 40% medium-chain triglycerides.

[0057] Preparation method:

[0058] S1. Raw material mixing

[0059] Dietary fiber inulin and medium-chain triglycerides were placed in a mixing tank according to the proportion and fully stirred at a stirring speed of 500 rpm for 15 minutes to prepare a uniform raw material mixture.

[0060] S2. Microemulsification treatment

[0061] ①Heat the raw material mixture to 30℃.

[0062] ② Add 1% Tween-80 and 1% lecithin to the raw material mixture and stir again at a stirring speed of 500 rpm for 10 minutes.

[0063] ③ Use a high shear homogenizer for microemulsification treatment, maintain the temperature at 30-40°C and the rotation speed at 8000 rpm for 40 minutes to form uniform tiny core-shell structure particles with an average particle size of 50-100 nm.

[0064] S3, coating

[0065] The tiny core-shell structure particles obtained in step S2 are evenly coated on the capsule shell, and the coating thickness is controlled to be 8 μm to form a capsule coating.

[0066] Example 5

[0067] The dietary fiber inulin and medium-chain triglyceride composite capsule coating of this embodiment includes the following raw materials in percentage by mass: 80% dietary fiber inulin and 20% medium-chain triglycerides.

[0068] Preparation method:

[0069] S1. Raw material mixing

[0070] Dietary fiber inulin and medium-chain triglycerides were placed in a mixing tank according to the proportion and stirred thoroughly at a stirring speed of 800 rpm for 10 minutes to prepare a uniform raw material mixture.

[0071] S2. Microemulsification treatment

[0072] ①Heat the raw material mixture to 40℃.

[0073] ② Add 2% Tween-80 and 2% lecithin to the raw material mixture and stir again at a stirring speed of 800 rpm for 5 minutes.

[0074] ③ Use a high shear homogenizer for microemulsification treatment, maintain the temperature at 40°C and the rotation speed at 12000 rpm for 20 minutes to form uniform tiny core-shell structure particles with an average particle size of 50 to 100 nm.

[0075] S3, coating

[0076] The tiny core-shell structure particles obtained in step S2 are evenly coated on the capsule shell, and the coating thickness is controlled to be 12 μm to form a capsule coating.

[0077] Experimental Example 1

[0078] This experimental example is used to verify the quality of the capsule coating material of the present invention (taking the capsule coating material of Example 1 as an example).

[0079] 1. Particle stability test:

[0080] 1. Experimental method: The stability (particle size) of tiny core-shell structure particles was tested at different temperatures (25°C, 37°C, 45°C) and pH conditions (pH 1.5, pH 6.8, pH 8.0) to ensure stable release of the particles in the intestinal environment.

[0081] 2. Experimental results:

[0082] The results are shown in Table 1.

[0083] Table 1 Particle stability test results

[0084]

[0085] The above results show that: under all test conditions, the tiny core-shell structure particles maintain a certain stability, and the particle size change is less than 5%, which proves that they have good stability in the simulated gastrointestinal environment.

[0086] 2. Solubility test:

[0087] 1. Experimental method: Test the solubility of the capsule coating in simulated gastric fluid (pH 1.2, 2.0) and intestinal fluid (pH 6.8, 7.4) to ensure effective release of the capsule in the gastrointestinal tract.

[0088] 2. Experimental results:

[0089] The results are shown in Table 2.

[0090] Table 2 Solubility test results

[0091]

[0092] From the above results we can see that:

[0093] In simulated gastric fluid (pH 1.2), the capsule coating completely dissolved within 45 minutes, and the drug release rate of the coating material within 20 minutes was less than 15%; in simulated gastric fluid (pH 1.2), the capsule coating completely dissolved within 30 minutes, and the drug release rate of the coating material within 20 minutes was less than 25%, ensuring that the drug is mainly released in the intestine.

[0094] In simulated intestinal fluid (pH 6.8), the capsule coating completely dissolved within 20 minutes, and the drug release rate of the coating material exceeded 85% within 30 minutes. In simulated intestinal fluid (pH 7.4), the capsule coating completely dissolved within 37 minutes, and the drug release rate of the coating material exceeded 90% within 40 minutes, ensuring effective drug release in the intestine.

[0095] 3. Biocompatibility and toxicity test

[0096] 1. Experimental methods: in vitro cell experiment method and animal experiment method.

[0097] The test subjects of the in vitro cell experiment method are intestinal epithelial cells and macrophages; the capsule coating material of the present invention is applied to the above cells at a dose of 1×10^8 CFU / mL, and the cell survival rate is observed.

[0098] The test subjects of the animal experiment method are mice; the mice are gavaged with the capsule coating material of the present invention at a dose of 1×10^9 CFU / kg, and their reactions are observed.

[0099] 2. Experimental results:

[0100] The results are shown in Table 3.

[0101] Table 3 Biocompatibility test results

[0102]

[0103] The above results demonstrate that in vitro cell experiments show that the cell survival rate of cells exposed to the coating material remained above 95%, demonstrating that the material exhibits no significant cellular toxicity. In animal studies, no significant toxic reactions were observed within 14 days of gavage administration of the capsule coating to mice; all mice survived and appeared normal. No histopathological damage was observed within 90 days. This demonstrates that the capsule coating of the present invention exhibits excellent biocompatibility and safety, without toxic side effects.

[0104] Experimental Example 2

[0105] This experimental example is used to verify the application effect of the capsule coating material of the present invention.

[0106] 1. Experimental methods:

[0107] Common drugs on the market were selected and compared with the capsule coatings of various embodiments of the present invention using traditional chemical synthetic material coatings (hydroxypropyl methylcellulose, HPMC). The application effects of the two coatings in promoting intestinal health, improving intestinal flora colonization and drug absorption efficiency were tested.

[0108] Among them, the drug selected a compound probiotic (7-combination), including the following species: Bifidobacterium spp. 2×10^9 CFU / g, Lactococcus lactis 1×10^9 CFU / g, Lactobacillus plantarum 1.5×10^9 CFU / g, Lactobacillus casei 1×10^9 CFU / g, Lactobacillus acidophilus 1×10^9 CFU / g, Lactobacillus rhamnosus 1.2×10^9 CFU / g, and Bifidobacterium longum 0.8×10^9 CFU / g.

[0109] The aforementioned "effects on promoting intestinal health, improving intestinal flora colonization, and enhancing drug absorption efficiency" are reflected in the form of flora growth rate and flora colonization rate. The flora growth rate is defined as the change in the number of intestinal flora after taking capsules containing the same number of flora. The flora colonization rate is defined as the change in the abundance of intestinal flora after taking capsules containing the same flora composition.

[0110] 2. Experimental results:

[0111] The results are shown in Table 4.

[0112] Table 4 Application effect results

[0113]

[0114]

[0115] From the above results, it can be seen that the application effect of the capsule coating of the present invention in promoting intestinal health, improving intestinal flora colonization and drug absorption efficiency is better than that of the control group; and in the examples of the present invention, the higher the content of dietary fiber inulin, the more significant the growth rate of the flora, which proves the key role of dietary fiber inulin in promoting the growth of beneficial bacteria; at the same time, the addition of medium-chain triglycerides significantly improves the colonization rate of beneficial bacteria in the intestine.

[0116] In summary, the capsule coating of the present invention can provide an energy source for intestinal bacteria and promote the growth and colonization of intestinal microflora by optimizing the ratio of the two components and the preparation process, and can also improve the health level of intestinal microflora and enhance the efficacy of the drug.

[0117] The above description is only a preferred embodiment of the present invention and is not intended to limit the present invention. Any modifications, equivalent substitutions and improvements made within the spirit and principles of the present invention should be included in the scope of protection of the present invention.

Claims

1. A dietary fiber inulin and medium chain triglyceride composite capsule coating, characterized in that: The preparation method is as follows: S1. Raw material mixing: Dietary fiber inulin and medium-chain triglycerides are uniformly mixed according to a ratio to prepare a uniform raw material mixture; the mass ratio of the dietary fiber inulin and medium-chain triglycerides is: 60-80% dietary fiber inulin, 20-40% medium-chain triglycerides; S2. Microemulsification: The raw material mixture is treated by a microemulsification process to form stable tiny core-shell structure particles. The specific process is as follows: the raw material mixture is heated to 30-40°C; an emulsifier and a co-surfactant are added to the raw material mixture and stirred again at a stirring speed of 500-800 rpm for 5-10 minutes; a high shear homogenizer is used for microemulsification, the temperature is maintained at 30-40°C, the speed is maintained at 8000-12000 rpm, and the treatment is carried out for 20-40 minutes; wherein, the emulsifier is 1-2% Tween-80 and the co-surfactant is 1-2% lecithin, and the particle size of the finally formed tiny core-shell structure particles is 50-100 nm; S3, coating: the tiny core-shell structure particles obtained in step S2 are evenly coated on the capsule shell, and the coating thickness is controlled to be 8-12 μm to form a capsule coating.

2. The dietary fiber inulin and medium chain triglyceride composite capsule coating according to claim 1, characterized in that: The specific mass ratio of the dietary fiber inulin and medium-chain triglycerides is: 70% dietary fiber inulin and 30% medium-chain triglycerides.

3. The dietary fiber inulin and medium chain triglyceride composite capsule coating according to claim 1, characterized in that The specific mass ratio of the dietary fiber inulin and medium-chain triglycerides is: 65% dietary fiber inulin and 35% medium-chain triglycerides.

4. The dietary fiber inulin and medium chain triglyceride composite capsule coating according to claim 1, characterized in that The specific mass ratio of the dietary fiber inulin and medium-chain triglycerides is: 75% dietary fiber inulin and 25% medium-chain triglycerides.

5. A method for preparing a composite capsule coating of dietary fiber inulin and medium-chain triglycerides according to any one of claims 1 to 4, characterized in that: The steps include: S1. Raw material mixing: Dietary fiber inulin and medium-chain triglycerides are uniformly mixed according to a ratio to prepare a uniform raw material mixture; the mass ratio of the dietary fiber inulin and medium-chain triglycerides is: 60-80% dietary fiber inulin, 20-40% medium-chain triglycerides; S2. Microemulsification: The raw material mixture is treated by a microemulsification process to form stable tiny core-shell structure particles. The specific process is as follows: the raw material mixture is heated to 30-40°C; an emulsifier and a co-surfactant are added to the raw material mixture and stirred again at a stirring speed of 500-800 rpm for 5-10 minutes; a high shear homogenizer is used for microemulsification, the temperature is maintained at 30-40°C, the speed is maintained at 8000-12000 rpm, and the treatment is carried out for 20-40 minutes; wherein, the emulsifier is 1-2% Tween-80 and the co-surfactant is 1-2% lecithin, and the particle size of the finally formed tiny core-shell structure particles is 50-100 nm; S3, coating: the tiny core-shell structure particles obtained in step S2 are evenly coated on the capsule shell, and the coating thickness is controlled to be 8-12 μm to form a capsule coating.

6. The method for preparing the dietary fiber inulin and medium-chain triglyceride composite capsule coating according to claim 5, characterized in that: In step S1, the dietary fiber inulin and medium-chain triglycerides are placed in a mixing tank and stirred thoroughly to achieve uniform mixing of the raw materials; and wherein the stirring speed is 500-800 rpm and the stirring time is 10-15 minutes.

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