A granule of an anti-gastric cancer composition based on a medicinal and edible material and a preparation method thereof

Abstract

This invention discloses an anti-gastric cancer granule composition based on medicinal and edible raw materials and its preparation method. The granules are formulated from four modules of raw materials: spleen-strengthening and body-supporting, detoxification and nodule-dispersing, immune regulation, and gut microbiota microenvironment regulation. All raw materials are from medicinal and edible sources and novel resource foods, ensuring safety and compliance. The formulation uses a multi-target synergistic effect to inhibit the proliferation of gastric cancer cells, induce apoptosis, and inhibit invasion and metastasis, while simultaneously regulating immunity, improving the gut microenvironment, and reducing the side effects of radiotherapy and chemotherapy. The preparation process employs compound hot reflux extraction, high-speed shear mixing, spray drying, and dry granulation, resulting in high retention of effective components, uniform and stable product, and convenient administration. In vitro and in vivo experiments have confirmed that this product can significantly inhibit gastric cancer growth, has low toxicity to normal cells, and good safety, making it suitable for preparing special medical purpose formula foods or health foods for adjuvant treatment of gastric cancer and improvement of patients' quality of life.

Description

Technical Field

[0001] This invention belongs to the field of functional food and traditional Chinese medicine preparation technology, and relates to an anti-gastric cancer composition granule based on food and medicine homologous raw materials and its preparation method. Background Technology

[0002] Gastric cancer is a highly prevalent malignant tumor worldwide with a poor prognosis. Current conventional treatments such as surgery, chemotherapy, and radiotherapy are often accompanied by significant toxic side effects and drug resistance. Therefore, developing adjuvant products derived from natural sources, with high safety profiles, and capable of multi-target intervention in gastric cancer is of significant clinical importance.

[0003] Traditional Chinese medicine and natural products have demonstrated unique advantages in the prevention and treatment of gastric cancer through synergistic effects involving multiple components, targets, and pathways. Studies have shown that natural polyphenolic compounds such as resveratrol, curcumin, and quercetin can combat gastric cancer through multiple mechanisms, including inducing apoptosis and inhibiting proliferation and migration. Meanwhile, some classic Chinese herbal formulas and their active ingredients have been shown to regulate key signaling pathways such as PI3K / AKT and MAPK, thereby inhibiting gastric cancer progression. Furthermore, edible fungal polysaccharides and "food and medicine homology" resources have also been found to possess significant immunomodulatory and direct antitumor activities.

[0004] However, there is currently a lack of mature solutions for systematically combining the aforementioned active ingredients and formulating them into granules that are easy to take, have good stability, and high bioavailability. Existing products either have limited efficacy, use ingredients that do not fall under the legal food category, or suffer from crude manufacturing processes that damage active ingredients and result in poor product uniformity, making it difficult to meet the market demand for a safe, effective, and convenient medical food for treating gastric cancer. Summary of the Invention

[0005] The purpose of this invention is to provide an anti-gastric cancer composition granule based on food-medicine homology raw materials and its preparation method. The composition is based on the traditional Chinese medicine treatment principles of "strengthening the spleen and supporting the body's resistance, clearing heat and detoxifying, regulating immunity and balancing the gut microbiota" and the design of modern oncology mechanisms. All raw materials comply with the national catalogs of food-medicine homology and new resource foods, and are safe and non-toxic.

[0006] According to the purpose of this invention, this invention provides an anti-gastric cancer composition granule based on food-medicine homologous raw materials, which is made from the following raw materials in parts by weight: Basic formula for strengthening the spleen and restoring vital energy: 15-25 parts of stir-fried yam, 10-20 parts of Poria cocos, 10-20 parts of stir-fried coix seed, and 5-15 parts of Polygonatum sibiricum; Detoxifying and dispersing active ingredients: 8-15 parts turmeric, 3-8 parts green tea extract (calculated as EGCG), 2-6 parts grape seed extract (calculated as resveratrol), and 5-10 parts dandelion. Immune-regulating and strengthening formula: 5-12 parts of maitake mushroom pollen or maitake mushroom extract, 5-10 parts of astragalus, and 3-8 parts of β-glucan; Microbial microenvironment regulation formula: 3-8 parts wheat oligopeptides, 5-15 parts resistant dextrin, and 5-10 parts prebiotics; Flavoring and carrier excipients: 10-30 parts maltitol, 5-15 parts microcrystalline cellulose, and 0.5-2 parts magnesium stearate.

[0007] Furthermore, the β-glucan is derived from oats or yeast; the prebiotic is fructooligosaccharide or galactooligosaccharide.

[0008] Further, the preferred formulation by weight is as follows: 20 parts stir-fried yam, 15 parts Poria cocos, 15 parts stir-fried coix seed, 10 parts Polygonatum sibiricum, 10 parts turmeric, 6 parts green tea extract, 5 parts grape seed extract, 8 parts dandelion, 10 parts maitake pollen, 8 parts Astragalus membranaceus, 5 parts β-glucan, 5 parts wheat oligopeptides, 10 parts resistant dextrin, 8 parts prebiotics, 20 parts maltitol, 10 parts microcrystalline cellulose, and 1 part magnesium stearate.

[0009] Furthermore, each gram of granules contains no less than 1.5 mg of curcumin, no less than 0.8 mg of resveratrol, and no less than 15% polysaccharides.

[0010] Furthermore, the particle size of the granules is 16-60 mesh, and the moisture content does not exceed 6.0%.

[0011] A method for preparing the above-mentioned anti-gastric cancer composition granules includes the following steps: S1 Raw material pretreatment and extraction: The stir-fried yam, poria cocos, stir-fried coix seed, polygonatum, astragalus, dandelion and turmeric were pulverized and passed through a 40-mesh sieve, and extracted by hot reflux. The filtrates were combined and concentrated under reduced pressure to obtain extract B. S2 Active ingredient integration and drying: Green tea extract, grape seed extract, maitake mushroom pollen or maitake mushroom extract, β-glucan, wheat oligopeptide, resistant dextrin, and prebiotics are added to extract B, mixed evenly, and then spray-dried to obtain composite powder D; S3 Granulation and Sizing: The composite powder D is mixed with maltitol and microcrystalline cellulose, dry granulation is performed, and after sizing, magnesium stearate is added and mixed to obtain the finished granules.

[0012] Further, in step S1, add 10-12 times the amount of purified water and extract twice by hot reflux at 90-95℃, each time for 1.5 hours; concentrate under reduced pressure at 60℃ and -0.09 MPa until the relative density at 60℃ is 1.10-1.15.

[0013] Furthermore, in step S2, the high-speed shear mixing temperature is 50-60℃ and the time is 30 minutes; the spray drying inlet air temperature is 160-180℃, the outlet air temperature is 80-90℃, and the atomization speed is 20000 rpm.

[0014] Furthermore, in step S3, the thickness of the dry granulation tablets is 1.0-1.5 mm, and the granules are sieved through a 16-60 mesh sieve.

[0015] The above-mentioned anti-gastric cancer composition granules are used in the preparation of special medical purpose formula foods or health foods that can help inhibit gastric cancer, regulate immunity, improve the tumor microenvironment, or reduce the side effects of radiotherapy and chemotherapy.

[0016] The beneficial effects of this invention are: This invention's granule formulation employs a scientific combination of four modules: strengthening the spleen and restoring vital energy, detoxifying and resolving lumps, regulating immunity, and regulating the gut microbiota microenvironment. All raw materials are of medicinal and edible origin, novel resource foods, and ordinary foods, ensuring safety, non-toxicity, and suitability for long-term use. The formulation achieves synergistic effects of direct tumor inhibition, immune enhancement, gut microbiota regulation, and nutritional support. It can inhibit the proliferation of gastric cancer cells at multiple targets, induce apoptosis, block invasion and metastasis, and regulate key PI3K / AKT and MAPK signaling pathways. Simultaneously, it improves the patient's spleen and stomach weakness, repairs the intestinal barrier, and reduces the toxic side effects of radiotherapy and chemotherapy. The process is highly adaptable, resulting in convenient granule administration, high stability, and good bioavailability. It combines significant adjuvant efficacy against gastric cancer with good patient compliance, making it suitable for industrial development. Attached Figure Description

[0017] Figure 1 This is a schematic diagram of the multi-module synergistic anti-gastric cancer mechanism of the present invention; Figure 2 This is a schematic diagram of the granule preparation process of the present invention. Detailed Implementation

[0018] The specific embodiments of the present invention will be further described below. It should be noted that these descriptions are for the purpose of aiding understanding the present invention, but do not constitute a limitation thereof. Furthermore, the technical features involved in the various embodiments of the present invention described below can be combined with each other as long as they do not conflict with each other.

[0019] Example 1 like Figure 1 As shown, an anti-gastric cancer composition granule based on food-grade medicinal materials is made from the following raw materials in parts by weight: Basic formula for strengthening the spleen and restoring vital energy: 15-25 parts of stir-fried yam, 10-20 parts of poria cocos, 10-20 parts of stir-fried coix seed, and 5-15 parts of polygonatum sibiricum; Detoxifying and dispersing active ingredients: 8-15 parts turmeric, 3-8 parts green tea extract (calculated as EGCG), 2-6 parts grape seed extract (calculated as resveratrol), and 5-10 parts dandelion. Immune-regulating and strengthening formula: 5-12 parts of maitake mushroom pollen or maitake mushroom extract, 5-10 parts of astragalus, and 3-8 parts of β-glucan; Microbial microenvironment regulation formula: 3-8 parts wheat oligopeptides, 5-15 parts resistant dextrin, and 5-10 parts prebiotics; Flavoring and carrier excipients: 10-30 parts maltitol, 5-15 parts microcrystalline cellulose, and 0.5-2 parts magnesium stearate.

[0020] Example 2 A gastric cancer-fighting granule composition based on food and medicine homologous raw materials, wherein, by weight, the yam (stir-fried with wheat bran) is 20 parts, the poria cocos is 15 parts, the coix seed (stir-fried) is 15 parts, and the polygonatum is 10 parts; The composition of the extract is as follows: 10 parts turmeric, 6 parts green tea extract (calculated as EGCG), 5 parts grape seed extract (calculated as resveratrol), and 8 parts dandelion. The composition of the ingredients was 10 parts of maitake mushroom pollen, 8 parts of astragalus, and 5 parts of β-glucan. The wheat oligopeptide is 5 parts, the resistant dextrin is 10 parts, and the prebiotic is 8 parts; The composition is 20 parts maltitol, 10 parts microcrystalline cellulose, and 1 part magnesium stearate.

[0021] Specifically, in the above embodiments, the β-glucan is derived from oats or yeast. The prebiotic is fructooligosaccharide or galactooligosaccharide.

[0022] In the above embodiments, each gram of granules contains not less than 1.5 mg of curcumin, not less than 0.8 mg of resveratrol, and not less than 15% polysaccharide.

[0023] The granules have a particle size of 16-60 mesh and a moisture content of no more than 6.0%.

[0024] Example 3 like Figure 2 As shown, a method for preparing the above-mentioned anti-gastric cancer composition granules includes the following steps: S1. Raw material pretreatment and extraction: Wash, dry, and pulverize yam, poria cocos, coix seed, polygonatum, astragalus, dandelion, and turmeric, and extract them through a 40-mesh sieve. Add purified water and extract under hot reflux. Combine the extracts, filter, and concentrate under reduced pressure to obtain extract B. S2. Integration and drying of active ingredients: Green tea extract, grape seed extract, maitake mushroom pollen or maitake mushroom extract, β-glucan, wheat oligopeptide, resistant dextrin, and prebiotics are added to extract B, and then spray-dried to obtain composite powder D. S3. Granulation and sizing: The composite powder D is mixed with maltitol and microcrystalline cellulose, dry granulated, sieved and then mixed with magnesium stearate to obtain the finished product. S4. Packaging and storage.

[0025] Specifically, in step S1, add 10-12 times the amount of purified water, and extract twice by hot reflux at 90-95℃, each time for 1.5 hours; concentrate under reduced pressure at 60℃ and -0.09MPa until the relative density is 1.10-1.15 (60℃).

[0026] In step S2, the mixing temperature is 50-60℃, and the high-speed shear mixing is carried out for 30 minutes; the spray drying inlet air temperature is 160-180℃, the outlet air temperature is 80-90℃, and the atomizer speed is 20000rpm.

[0027] In step S3, the dry granulation process is used to press the pellets into thin sheets with a thickness of 1.0-1.5 mm, which are then granulated through a 16-60 mesh sieve.

[0028] Example 4 A method for preparing the above-mentioned anti-gastric cancer composition granules includes the following steps: Raw material pretreatment and extraction: Wash, dry, and pulverize the yam, poria cocos, coix seed, polygonatum, astragalus, dandelion, and turmeric through a 40-mesh sieve; add 10-12 times the amount of purified water and extract twice by hot reflux at 90-95℃ for 1.5 hours each time. Combine the extracts and filter to obtain aqueous extract A; concentrate under reduced pressure at 60℃ and -0.09MPa to obtain extract B with a relative density of 1.10-1.15 (60℃). Active ingredient integration and drying: Green tea extract, grape seed extract, maitake mushroom pollen / extract, β-glucan, wheat oligopeptide, resistant dextrin, and prebiotics were added to extract B and mixed at high speed at 50-60℃ for 30 minutes to obtain mixture C; spray drying was carried out at an inlet air temperature of 160-180℃, an outlet air temperature of 80-90℃, and an atomizer speed of 20000rpm to obtain composite powder D; Granulation and sizing: The composite powder D is mixed with maltitol and microcrystalline cellulose in three dimensions for 20 minutes, dry granulation is performed and pressed into 1.0-1.5 mm thin sheets, crushed and passed through a 16-60 mesh sieve, and magnesium stearate is added and mixed for 5 minutes to obtain the finished product; Packaging and storage: Pack in aluminum-plastic composite film bags and store in a cool, dry place.

[0029] Example 5 This embodiment provides the application of the above-mentioned granules, including: The above-mentioned granules are used in the preparation of special medical purpose formula foods or health foods for adjuvant treatment of gastric cancer, improvement of the quality of life of gastric cancer patients, and reduction of the side effects of radiotherapy and chemotherapy.

[0030] Example 6 Quality Inspection Characteristics: Light yellowish-brown granules with a distinctive aroma and a slightly sweet taste; Particle size: Over 95% of the particles are between 16-60 mesh; Moisture: ≤6.0%; Solubility: Completely dissolved or slightly cloudy when stirred in 70℃ hot water for 5 minutes; Key ingredients: Curcumin ≥1.5mg, Resveratrol ≥0.8mg, Polysaccharides ≥15% per gram of granules.

[0031] Example 7 In vitro anti-gastric cancer experiment The granules showed dose-dependent inhibition of the proliferation of MKN-45 and MGC-803 gastric cancer cells, with inhibition rates of (65.4±3.2)% and (58.9±4.1)% respectively at a concentration of 2.0 mg / mL. They also significantly inhibited cell migration and invasion, induced apoptosis, and downregulated the expression of p-AKT and p-ERK.

[0032] Example 8 Animal in vivo experiments In a nude mouse xenograft model, the high-dose group showed a tumor inhibition rate of 42.8%, with no significant decrease in mouse body weight and no significant pathological damage to the heart, liver, spleen, lungs, or kidneys. It also increased the CD4+ / CD8+ ratio and NK cell activity.

[0033] Example 9 Gut microbiota regulation experiment It can improve intestinal flora imbalance caused by chemotherapy, increase the abundance of beneficial bacteria, reduce the abundance of opportunistic pathogens, and alleviate colon inflammation.

[0034] This invention features a scientifically formulated compound with four synergistic modules that target multiple points in gastric cancer intervention. It also has direct tumor suppression, immune regulation, intestinal microecological regulation, and nutritional support effects. All raw materials are food and medicine homologous, and are new resource foods, making them safe, legal, and suitable for long-term use. The preparation method of this invention is advanced, with a high retention rate of effective components, good particle stability, and excellent flowability, making it suitable for industrial production. In vitro and in vivo experiments have confirmed its clear anti-gastric cancer effect, high safety, and ability to reduce the side effects of radiotherapy and chemotherapy.

[0035] Although embodiments of the present invention have been shown and described, it will be understood by those skilled in the art that various changes, modifications, substitutions and alterations can be made to these embodiments without departing from the principles and spirit of the present invention, the scope of which is defined by the appended claims and their equivalents.

Claims

1. A granule formulation of an anti-gastric cancer composition based on food-medicine homologous ingredients, characterized in that, Made from the following raw materials in parts by weight: Basic formula for strengthening the spleen and restoring vital energy: 15-25 parts of stir-fried yam, 10-20 parts of Poria cocos, 10-20 parts of stir-fried coix seed, and 5-15 parts of Polygonatum sibiricum; Detoxifying and dispersing active ingredients: 8-15 parts turmeric, 3-8 parts green tea extract (calculated as EGCG), 2-6 parts grape seed extract (calculated as resveratrol), and 5-10 parts dandelion. Immune-regulating and strengthening formula: 5-12 parts of maitake mushroom pollen or maitake mushroom extract, 5-10 parts of astragalus, and 3-8 parts of β-glucan; Microbial microenvironment regulation formula: 3-8 parts wheat oligopeptides, 5-15 parts resistant dextrin, and 5-10 parts prebiotics; Flavoring and carrier excipients: 10-30 parts maltitol, 5-15 parts microcrystalline cellulose, and 0.5-2 parts magnesium stearate.

2. The anti-gastric cancer composition granules according to claim 1, characterized in that, The β-glucan is derived from oats or yeast; the prebiotic is fructooligosaccharide or galactooligosaccharide.

3. The anti-gastric cancer composition granules according to claim 1, characterized in that, The preferred formulation by weight is as follows: 20 parts stir-fried yam, 15 parts Poria cocos, 15 parts stir-fried coix seed, 10 parts Polygonatum sibiricum, 10 parts turmeric, 6 parts green tea extract, 5 parts grape seed extract, 8 parts dandelion, 10 parts maitake pollen, 8 parts Astragalus membranaceus, 5 parts β-glucan, 5 parts wheat oligopeptides, 10 parts resistant dextrin, 8 parts prebiotics, 20 parts maltitol, 10 parts microcrystalline cellulose, and 1 part magnesium stearate.

4. The anti-gastric cancer composition granules according to claim 1, characterized in that, Each gram of granules contains no less than 1.5 mg of curcumin, no less than 0.8 mg of resveratrol, and no less than 15% polysaccharides.

5. The anti-gastric cancer composition granules according to claim 1, characterized in that, The granules have a particle size of 16-60 mesh and a moisture content of no more than 6.0%.

6. A method for preparing the anti-gastric cancer composition granules according to any one of claims 1-5, characterized in that, Includes the following steps: S1 Raw material pretreatment and extraction: The stir-fried yam, poria cocos, stir-fried coix seed, polygonatum, astragalus, dandelion and turmeric were pulverized and passed through a 40-mesh sieve, and extracted by hot reflux. The filtrates were combined and concentrated under reduced pressure to obtain extract B. S2 Active ingredient integration and drying: Green tea extract, grape seed extract, maitake mushroom pollen or maitake mushroom extract, β-glucan, wheat oligopeptide, resistant dextrin, and prebiotics are added to extract B, mixed evenly, and then spray-dried to obtain composite powder D; S3 Granulation and Sizing: The composite powder D is mixed with maltitol and microcrystalline cellulose, dry granulation is performed, and after sizing, magnesium stearate is added and mixed to obtain the finished granules.

7. The preparation method according to claim 6, characterized in that, In step S1, add 10-12 times the amount of purified water and reflux extract twice at 90-95℃, each time for 1.5 hours; concentrate under reduced pressure at 60℃ and -0.09 MPa until the relative density at 60℃ is 1.10-1.

15.

8. The preparation method according to claim 6, characterized in that, In step S2, the high-speed shear mixing temperature is 50-60℃ and the time is 30 minutes; the spray drying inlet air temperature is 160-180℃, the outlet air temperature is 80-90℃, and the atomization speed is 20000 rpm.

9. The preparation method according to claim 6, characterized in that, In step S3, the dry granulation tablets are pressed to a thickness of 1.0-1.5 mm and then granulated through a 16-60 mesh sieve.

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