Silybum angustifolium curcuma schisandra capsule for assisting in protecting chemical liver injury and preparation method thereof

Abstract

The application discloses a capsule for assisting in protecting chemical liver injury and a preparation method thereof, and belongs to the technical field of health-care food. The capsule is composed of curcuma longa extract 100g, silybum marianum extract 70g, schisandra chinensis extract 60g, microcrystalline cellulose 109.5g, silicon dioxide 7g and magnesium stearate 3.5g, and 1000 capsules are taken as a unit. The curcuma longa extract contains curcumin, the content of which is greater than or equal to 10% (10:1), the silybum marianum extract contains silybin, the content of which is greater than or equal to 20% (25:1), and the schisandra chinensis extract contains schisandrin, the content of which is greater than or equal to 1.5% (12.5:1). The three kinds of plant extracts are scientifically compounded, and the effects of antioxidation, anti-inflammation, liver cell membrane protection and bile secretion regulation are synergistically exerted. Through systematic screening of the types and dosages of the filling agent, the flow agent and the lubricant, the technical problems of poor flowability of the mixed plant extract powder, large filling difference and easy jamming are solved.

Description

Technical Field

[0001] This invention belongs to the field of health food technology, specifically relating to a milk thistle, turmeric, and schisandra capsule for the adjuvant protection against chemically induced liver damage and its preparation method. Background Technology

[0002] Chemical liver injury is liver damage caused by hepatotoxic substances such as alcohol, drugs, and environmental pollutants. Long-term and repeated damage can lead to hepatocyte necrosis, fibrosis, and even cirrhosis and liver cancer. With the accelerated pace of modern life, the increase in alcohol consumption, and the prevalence of drug abuse, the incidence of chemical liver injury is rising year by year, becoming a significant public health problem threatening human health.

[0003] Currently, most health supplements on the market that are used to assist in the protection against chemically induced liver damage use milk thistle extract as the main ingredient, which suffers from limited efficacy and poor synergistic effects. Curcumin in turmeric has antioxidant, anti-inflammatory, and hepatic stellate cell activation-inhibiting effects; schisandrol A in schisandra can promote liver glycogen production, protect hepatocytes, and enhance liver detoxification function; the combination of these two with silybin can exert a synergistic liver-protective effect from multiple targets.

[0004] However, plant extracts generally have the characteristics of strong hygroscopicity, high viscosity, and poor flowability. In the capsule production process, the types and amounts of fillers, flow aids, and lubricants have not been systematically optimized, resulting in poor flowability of the mixed powder. The angle of repose is usually greater than 45°. During filling, powder clumping and bridging are prone to occur, resulting in large differences in filling volume and even jamming problems, which affect production efficiency and product quality.

[0005] Therefore, developing a compound capsule with a scientifically formulated, stable, and quality-controllable formula that has significant auxiliary protective effects against chemically induced liver damage, and its preparation method, has important market value and social significance. Summary of the Invention

[0006] The purpose of this invention is to overcome the shortcomings of the prior art and provide a milk thistle, turmeric, and schisandra capsule for the adjuvant protection against chemically induced liver damage and its preparation method, thereby solving the technical problems of poor efficacy of single components, poor fluidity of plant extract capsules, uneven mixing, and easy moisture absorption in the prior art.

[0007] To achieve the above objectives, the present invention adopts the following technical solution: A milk thistle, turmeric, and schisandra capsule for adjuvant protection against chemically induced liver injury, per 1000 capsules, is composed of the following raw and excipient materials: 90-100g turmeric extract, 60-70g milk thistle extract, 60-65g schisandra extract, 100-109.5g microcrystalline cellulose, 5-7g silicon dioxide, and 3-3.5g magnesium stearate; wherein the turmeric extract contains ≥10% curcumin at an extraction ratio of 10:1; the milk thistle extract contains ≥20% silybin at an extraction ratio of 25:1; and the schisandra extract contains ≥1.5% schisandrol A at an extraction ratio of 12.5:1.

[0008] As an improvement, based on 1000 capsules, it is composed of the following raw and auxiliary materials: 100g turmeric extract, 70g milk thistle extract, 60g schisandra extract, 109.5g microcrystalline cellulose, 7g silicon dioxide, and 3.5g magnesium stearate; the turmeric extract contains ≥10% curcumin, with an extraction ratio of 10:1; the milk thistle extract contains ≥20% silybin, with an extraction ratio of 25:1; and the schisandra extract contains ≥1.5% schisandrol A, with an extraction ratio of 12.5:1.

[0009] As an improvement, the capsules are 0.35g-0.50g / capsule, the contents are yellow to brownish-yellow powder, the disintegration time is ≤15 minutes, and the content difference is controlled within ±7.5%.

[0010] Furthermore, the capsules are 0.35g / capsule, contain yellow to brownish-yellow powder, have a disintegration time of ≤15 minutes, and have a content variation controlled within ±7.5%.

[0011] This invention also provides a method for preparing the above-mentioned milk thistle, turmeric, and schisandra capsules, comprising the following steps: S1 Raw and auxiliary material pretreatment: Turmeric extract, milk thistle extract, schisandra extract, microcrystalline cellulose, silicon dioxide, and magnesium stearate are sieved through a mesh screen and used after passing the inspection. S2 Weighing and Mixing: Weigh the pretreated raw and auxiliary materials according to the formula, place them in a high-speed mixer and mix to obtain a uniformly mixed powder; S3 Capsule Filling: The mixed powder is filled into capsules; S4 Post-processing: Polish the filled capsules, then perform inner packaging and outer packaging in sequence. After passing inspection, they are put into storage.

[0012] As an improvement, in S1, all raw and auxiliary materials are passed through an 80-mesh sieve.

[0013] As an improvement, in S2, the temperature of the Class 100,000 clean area is 22°C and the relative humidity is 55%.

[0014] As an improvement, in S2, the mixture is fed into a high-speed mixer and mixed at a speed of 22 r / min for 30 minutes.

[0015] As an improvement, in S3, 0# gelatin hollow capsules are used for filling, the filling parameters are adjusted, and the content of each capsule is controlled to be 0.35g, with a content difference of ±7.5%.

[0016] As an improvement, in S4, oral solid medication high-density polyethylene bottles are used for inner packaging, with 60 tablets per bottle.

[0017] Beneficial effects Compared with the prior art, the present invention has the following beneficial effects: (1) This invention determined the optimal compound ratio of turmeric extract, milk thistle extract, and schisandra extract to be 10:7:6. Among them, silybin can stabilize hepatocyte membranes, scavenge free radicals, and promote hepatocyte repair; curcumin has antioxidant, anti-inflammatory, and liver fibrosis-inhibiting effects; schisandrol A can enhance liver detoxification function and promote bile secretion. The three work synergistically to exert auxiliary protective effects against chemical liver damage from multiple dimensions such as hepatocyte membrane protection, antioxidant, anti-inflammatory, and detoxification, with significantly better effects than single-component products.

[0018] (2) Through systematic investigation of the types and amounts of fillers, flow aids, and lubricants, this invention ultimately determined that microcrystalline cellulose is used as the filler, silica as the flow aid, and magnesium stearate as the lubricant, with amounts of 109.5 g / 1000 capsules, 7 g / 1000 capsules, and 3.5 g / 1000 capsules, respectively. This excipient formulation reduced the angle of repose of the mixed powder to 38.94°, ensuring that the flowability met the requirements for capsule filling. It completely solved problems such as powder clumping, bridging, large differences in filling weight, and jamming during the production process, and the difference in filling weight was stably controlled within ±7.5%.

[0019] (3) Through experiments on mixing time, this invention determined that the optimal mixing time is 30 minutes, at which the RSD value of schisandrol A is 4.69%. This ensures that the active ingredients are mixed evenly and avoids the increase in material moisture absorption and energy consumption caused by excessive mixing time. At the same time, through hygroscopicity studies, the critical relative humidity of the product was determined to be 73%. Based on this, humidity control standards for production and storage environments were formulated, which effectively improved the stability of the product.

[0020] (4) The capsules prepared by this invention have a disintegration time of ≤7 minutes, which is far better than the 60 minutes specified in the pharmacopoeia. The active ingredients can be released quickly, which improves bioavailability.

[0021] (5) The preparation process of the present invention does not require complex equipment, is easy to operate, has a short production cycle, controllable cost, and stable product quality, making it suitable for large-scale industrial production. Detailed Implementation

[0022] The present invention will be further described in detail below with reference to specific embodiments and comparative examples.

[0023] Example 1 This embodiment provides a milk thistle, turmeric, and schisandra capsule for adjuvant protection against chemically induced liver injury. The formula for 1000 capsules is as follows: 100g of turmeric extract (curcumin 10.2%, 10:1), 70g of milk thistle extract (silymarin 21.5%, 25:1), 60g of schisandra extract (schisandrin A 1.6%, 12.5:1), 109.5g of microcrystalline cellulose, 7g of silicon dioxide, and 3.5g of magnesium stearate.

[0024] The preparation method is as follows: S1 Raw and auxiliary material pretreatment: The above raw and auxiliary materials are passed through an 80-mesh sieve and tested in accordance with the 2025 edition of the Pharmacopoeia of the People's Republic of China and the company's internal control standards before being put into use; S2 Weighing and Mixing: In a Class 100,000 clean area (temperature 22℃, relative humidity 55%), accurately weigh each raw and auxiliary material according to the formula, put them into a high-speed mixer, mix at a speed of 22r / min for 30 minutes, take a sample to test the uniformity of schisandrol A content, the RSD value is 4.69%, which meets the requirements, and the mixed powder is obtained. S3 Capsule Filling: The mixed powder is fed to a fully automatic capsule filling machine, and 0# gelatin hollow capsules are used for filling. The filling parameters are adjusted to control the filling weight of each capsule to be 0.35g, with a filling weight difference of ±7.5%. S4 Post-processing: The filled capsules are sent to a capsule polishing machine for polishing to remove surface dust; then they are inner-packaged in high-density polyethylene bottles for oral solid pharmaceuticals, with 60 capsules per bottle; finally, they are outer-packaged in corrugated cardboard boxes, and stored after passing the finished product inspection.

[0025] Comparative Example 1 Dextrin was used as a filler, with a dosage of 109.5g. The rest of the formulation and preparation method were the same as in Example 1.

[0026] Comparative Example 2 Corn starch was used as a filler, with a dosage of 109.5g. The rest of the formula and preparation method were the same as in Example 1.

[0027] Comparative Example 3 The amount of silica used is 3.5g / 1000 particles, and the rest of the formula and preparation method are the same as in Example 1.

[0028] Comparative Example 4 The mixing time was 20 minutes, and the rest of the formulation and preparation method were the same as in Example 1.

[0029] Example 2: Comparison Test of Filler Types The flowability of the mixed powders prepared in Example 1, Comparative Example 1, and Comparative Example 2 was tested, and the results are shown in the table below: The experimental results show that when microcrystalline cellulose is used as a filler, the mixed powder has the best flowability, which is significantly better than that of dextrin and corn starch.

[0030] Example 3: Comparison Test of Gliding Agent Dosage The flowability and production conditions of the mixed powders prepared in Example 1 and Comparative Example 3 were tested, and the results are shown in the table below: The test results show that when the amount of silica is 7g / 1000 particles, the mixed powder has better flowability, smaller difference in filling amount, and no jamming phenomenon.

[0031] Example 4: Comparison of Mixing Time Seven samples were randomly selected from the mixed powders of Example 1 and Comparative Example 4, respectively. The content of schisandrol A was determined, and the RSD value was calculated. The results are shown in the table below: The experimental results show that the uniformity of the active ingredients is significantly better when mixed for 30 minutes than when mixed for 20 minutes.

[0032] Example 5: Three batches of pilot-scale testing Following the formula and process of Example 1, three batches of pilot production were conducted, with each batch containing 100,000 capsules. The production results are shown in the table below: All three batches of pilot products met the standard requirements, with a yield of ≥98.2%, indicating that the process of this invention is stable and reliable and suitable for large-scale industrial production.

[0033] Example 6 Accelerated Stability Test The product prepared in Example 1 was subjected to an accelerated stability test for 6 months at a temperature of 40℃±2℃ and a relative humidity of 75%±5%. Samples were taken and tested at 0, 1, 2, 3, and 6 months, and the results are shown in the table below: Accelerated testing results show that the product of this invention, after being placed under accelerated conditions for 6 months, meets all standard requirements and exhibits stable quality.

[0034] The above description is merely a preferred embodiment of the present invention and is not intended to limit the scope of protection of the present invention. Any modifications, equivalent substitutions, improvements, etc., made within the spirit and principles of the present invention should be included within the scope of protection of the present invention.

Claims

1. A milk thistle, turmeric, and schisandra capsule for adjuvant protection against chemically induced liver injury, characterized in that... Based on 1000 capsules, the product is composed of the following raw and auxiliary materials: 90-100g of turmeric extract, 60-70g of milk thistle extract, 60-65g of schisandra extract, 100-109.5g of microcrystalline cellulose, 5-7g of silicon dioxide, and 3-3.5g of magnesium stearate; the turmeric extract contains ≥10% curcumin, with an extraction ratio of 10:1; the milk thistle extract contains ≥20% silybin, with an extraction ratio of 25:1; and the schisandrin A content in the schisandra extract is ≥1.5%, with an extraction ratio of 12.5:

1.

2. The milk thistle, turmeric, and schisandra capsule according to claim 1, characterized in that, The capsules are 0.35g-0.50g / capsule, containing a yellow to brownish-yellow powder, with a disintegration time of ≤15 minutes and a content variation controlled within ±7.5%.

3. A method for preparing milk thistle, turmeric, and schisandra capsules as described in claim 1 or 2, characterized in that, Includes the following steps: S1 Raw and auxiliary material pretreatment: Turmeric extract, milk thistle extract, schisandra extract, microcrystalline cellulose, silicon dioxide, and magnesium stearate are sieved through a mesh screen and used after passing the inspection. S2 Weighing and Mixing: Weigh the pretreated raw and auxiliary materials according to the formula, place them in a high-speed mixer and mix to obtain a uniformly mixed powder; S3 Capsule Filling: The mixed powder is filled into capsules; S4 Post-processing: Polish the filled capsules, then perform inner packaging and outer packaging in sequence. After passing inspection, they are put into storage.

4. The preparation method according to claim 3, characterized in that, In step S2, the mixing process is carried out in a Class 100,000 clean area, with the ambient temperature controlled at 18-26℃ and the relative humidity controlled below 73%.

5. The preparation method according to claim 3, characterized in that, In step S2, the speed of the high-speed mixer is 20-25 r / min.

6. The preparation method according to claim 3, characterized in that, In step S3, the relative humidity of the environment is controlled at 45%-65% during filling.

7. The preparation method according to claim 3, characterized in that, In step S4, the inner packaging uses a high-density polyethylene bottle for oral solid medicine, with 60 tablets per bottle.

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