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

Abstract

The invention relates to the technical field of pharmaceutic adjuvants, and provides a dietary fiber inulin and medium chain triglyceride composite capsule coating which comprises the following raw materials in percentage by mass: 60-80% of dietary fiber inulin and 20-40% of medium chain triglyceride. The invention also provides a preparation method of the capsule coating. The preparation method comprises the following steps: raw material mixing, micro-emulsification treatment and coating. The invention has the advantages that: (1) natural components are adopted, so that good biocompatibility is achieved, side effects on a human body are reduced, and the absorption efficiency is high; (2) balanced growth of intestinal flora can be effectively promoted, and intestinal health is maintained; (3) field planting and reproduction of effective microbial communities can be promoted; and (4) the process is simple and feasible, and has a good application prospect.

Description

Technical Field

[0001] The 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, as people pay more and more attention to health, the research on intestinal health and intestinal flora has become a hot topic. Most of the capsule coatings on the market currently use chemical synthetic materials. Although these materials can meet the basic protection and release requirements, they have some significant defects, such as poor biocompatibility, large toxic side effects, and low absorption efficiency. These chemical synthetic materials may cause immune reactions or other adverse reactions after entering the human body, and long-term use may also cause burdens on organs such as the liver and kidneys.

[0003] Dietary fiber inulin is a natural polysaccharide with good water solubility and stability. It 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, thereby promoting the reproduction of beneficial bacteria and improving the intestinal microecological environment. In addition, dietary fiber inulin can also promote intestinal peristalsis, increase stool volume, and prevent constipation and diseases such as colon cancer.

[0004] Medium-chain triglycerides (MCT) are an efficient energy source that can be quickly absorbed and metabolized by the body. Unlike long-chain triglycerides, MCT does not require the participation of bile acid during digestion and can directly enter the liver through the portal vein for metabolism. This rapid absorption and metabolic characteristic gives MCT a unique advantage in improving the colonization and growth of intestinal flora. MCT also has antibacterial and antiviral functions, which helps to improve 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 dietary fiber inulin and medium-chain triglyceride composite capsule coating and a preparation method thereof, so as to solve the problems of poor biocompatibility, large toxic and side effects, low absorption efficiency, etc. of existing capsule coating materials, improve 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 mass percentages: 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 mass percentages: 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 mass percentages: 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 treatment: 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 raw materials are uniformly mixed by placing dietary fiber inulin and medium-chain triglycerides in a mixing tank and stirring them fully; and wherein the stirring speed is 500 to 800 rpm and the stirring time is 10 to 15 minutes.

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

[0019] Heat the raw material mixture to 30-40°C, which helps reduce viscosity and improve the effect of the subsequent emulsification process;

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

[0021] A high shear homogenizer is used for microemulsification treatment, the temperature is maintained at 30-40°C, the rotation speed is maintained at 8000-12000rpm, and the treatment is performed for 20-40min 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 structure particles finally formed is usually less than 100 nanometers, and the average particle size is 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 biologically active medium-chain triglycerides. These two components are processed through precise proportions and 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 to improve 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 compared to 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 of the preparation of the dietary fiber inulin and medium-chain triglyceride composite capsule coating in Example 1. DETAILED DESCRIPTION

[0033] The embodiments of the present invention are described in detail below. The embodiments are implemented on the premise of the technical solution of the present invention, and detailed implementation methods and specific operation processes 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 embodiments are conventional raw materials, reagents, equipment and methods in the art unless otherwise specified, and will not be repeated.

[0034] Example 1

[0035] The dietary fiber inulin and medium-chain triglyceride composite capsule coating of the present embodiment comprises 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 the proportion and fully stirred at a stirring speed of 700 rpm for 12 minutes to prepare a uniform raw material mixture.

[0039] S2. Microemulsification

[0040] ① Heat 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, keep the temperature at 37°C and the rotation speed at 10,000 rpm for 30 minutes to form uniform micro 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 the present embodiment comprises 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 in 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 the present embodiment comprises the following raw materials in percentage by weight: 75% dietary fiber inulin and 25% medium-chain triglycerides.

[0052] The preparation method is basically the same as that in 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 the present embodiment comprises the following raw materials in percentage by weight: 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

[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 min.

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

[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 the present embodiment comprises the following raw materials in percentage by weight: 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 a proportion and fully stirred at a stirring speed of 800 rpm for 10 minutes to prepare a uniform raw material mixture.

[0071] S2. Microemulsification

[0072] ① Heat 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, keep the temperature at 40°C and the rotation speed at 12000 rpm for 20 minutes to form uniform micro 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 the 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] From the above results, it can be seen that: under all test conditions, the tiny core-shell structure particles maintain a certain stability, and the particle size changes by less than 5%, proving 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 the 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 know that:

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

[0094] In simulated intestinal fluid (pH 6.8), the capsule coating was 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 was completely dissolved within 37 minutes, and the drug release rate of the coating material exceeded 90% within 40 minutes, ensuring the effective release of the drug 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 objects 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 1×10^9 CFU / kg of the capsule coating material of the present invention, 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] From the above results, it can be seen that in the in vitro cell experiment, the survival rate of cells in contact with the coating material remained above 95%, proving that the material had no obvious toxicity to the cells. In the animal experiment, no obvious toxic reaction was observed within 14 days after mice were gavaged with the capsule coating of the present invention, and all mice survived and behaved normally; within 90 days, there was no tissue pathological damage. This shows that the capsule coating of the present invention has good biocompatibility and safety, and has no 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 traditional chemical synthetic material coatings (hydroxypropyl methylcellulose, HPMC) and capsule coatings of various embodiments of the present invention, and the application effects of the two coatings in promoting intestinal health, improving intestinal flora colonization and drug absorption efficiency were tested respectively.

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

[0109] The above-mentioned "application effects in promoting intestinal health, improving intestinal flora colonization and 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 of the user after taking capsules containing the same amount of flora. The flora colonization rate is defined as the change in the abundance of intestinal flora of the user after taking capsules containing the same flora components.

[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 embodiments 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 flora 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 protection scope of the present invention.

Claims

1. A dietary fiber inulin and medium chain triglyceride composite capsule coating, characterized in that: The invention comprises the following raw materials in percentage by weight: 60-80% of dietary fiber inulin and 20-40% of medium chain triglyceride.

2. The dietary fiber inulin and medium chain triglyceride composite capsule coating according to claim 1, characterized in that: The invention comprises the following raw materials in specific percentage by weight: 70% of dietary fiber inulin and 30% of medium chain triglyceride.

3. The dietary fiber inulin and medium chain triglyceride composite capsule coating according to claim 1, characterized in that: The invention comprises the following raw materials in specific percentages by weight: 65% of dietary fiber inulin and 35% of medium chain triglyceride.

4. The dietary fiber inulin and medium chain triglyceride composite capsule coating according to claim 1, characterized in that: The invention comprises the following raw materials in specific percentages by weight: 75% of dietary fiber inulin and 25% of medium chain triglyceride.

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 mixed uniformly according to a ratio to prepare a uniform raw material mixture; S2. Microemulsification treatment: The raw material mixture is treated by a microemulsification process to form stable tiny core-shell structure particles; S3, coating: the tiny core-shell structure particles obtained in step S2 are evenly coated on the capsule shell 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 the step S1, the dietary fiber inulin and medium-chain triglycerides are placed in a mixing tank and stirred sufficiently to achieve uniform mixing of the raw materials; wherein the stirring speed is 500 to 800 rpm and the stirring time is 10 to 15 minutes.

7. The method for preparing the dietary fiber inulin and medium chain triglyceride composite capsule coating according to claim 5, characterized in that: In step S2, the specific process of microemulsification treatment is as follows: Heat the raw material mixture to 30-40°C; Add the emulsifier and auxiliary surfactant to the raw material mixture and stir again at a stirring speed of 500-800 rpm for 5-10 min; Use a high shear homogenizer for microemulsification treatment, keep the temperature at 30-40°C, keep the rotation speed at 8000-12000rpm, and process for 20-40min.

8. The method for preparing the dietary fiber inulin and medium chain triglyceride composite capsule coating according to claim 7, characterized in that: The emulsifier is 1-2% Tween-80, and the auxiliary surfactant is 1-2% lecithin.

9. The method for preparing the dietary fiber inulin and medium chain triglyceride composite capsule coating according to claim 5, characterized in that: In the step S2, the particle size of the finally formed tiny core-shell structure particles is 50-100 nm.

10. The method for preparing the dietary fiber inulin and medium chain triglyceride composite capsule coating according to claim 5, characterized in that: In the step S3, the coating thickness is controlled to be 8-12 μm.

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