Glucosamine sulfate effervescent tablet composition and preparation method thereof

Abstract

The invention discloses a glucosamine sulfate effervescent tablet composition and a preparation method thereof, and belongs to the technical field of biological medicines. The effervescent tablet contains glucosamine sulfate, and the effective drug content is high and is 1000mg / tablet; the soft capsule contains glucosamine sulfate, chondroitin sulfate and collagen which jointly maintain the stable state of cartilage, delay the development of osteoarthritis and relieve symptoms; glucosamine sulfate and vitamin C are reasonably matched, so that the joint discomfort recovery period is shortened; and moreover, the prescription contains sodium salt, is low in calorie, helps to maintain moisture balance, and is suitable for people with high-intensity metabolic movement. According to the method, the effervescent tablets obtained through step-by-step granulation and total pressure are high in dissolution speed during use, quick in active ingredient release, quick in effect taking, high in bioavailability and convenient to carry, and are particularly suitable for the old, children and users who cannot swallow solid preparations.

Description

Technical Field

[0001] The invention belongs to the technical field of biomedicine, and particularly relates to a glucosamine sulfate effervescent tablet composition and a preparation method thereof. Background Art

[0002] Osteoarthritis, the most common synovial joint disease in middle-aged and elderly people, is characterized primarily by focal or complete loss of articular cartilage, bone changes, and dysregulation of inflammatory and noninflammatory pathways, including the hydrolysis of aggrecan and collagen and aberrations in their synthesis by chondrocytes.

[0003] Glucosamine sulfate is an amino monosaccharide found throughout the body, particularly in articular cartilage. It is a crucial component of proteoglycan synthesis within the human articular cartilage matrix. It selectively targets bony joints, blocking the pathological process of osteoarthritis and stimulating chondrocytes to produce glycoproteins with a normal polysaccharide polymer structure. It also inhibits the activity of cartilage-damaging enzymes such as collagenase and phospholipase A2. It also inhibits the production of superoxide free radicals in damaged cells, preventing damage to chondrocytes by corticosteroids and certain nonsteroidal anti-inflammatory drugs, and reduces the release of endotoxins from damaged cells. This has a direct anti-inflammatory effect, alleviating the pain symptoms of osteoarthritis, improving joint function, and preventing the progression of the disease. Therefore, glucosamine sulfate is recognized by the international medical community as the only specific drug currently available for the treatment of osteoarthritis.

[0004] Currently, the glucosamine sulfate products on the market are mainly capsules and tablets, and the specifications are relatively small (mostly 0.25g). They need to be taken three times a day, two tablets each time. The high frequency of administration leads to low patient compliance. Summary of the Invention

[0005] The first purpose of the present invention is to provide a glucosamine sulfate effervescent tablet, which contains glucosamine sulfate and has a high effective drug content of 1000 mg / tablet. One tablet is taken daily, which is convenient to take and improves patient compliance; contains glucosamine sulfate, chondroitin sulfate, and collagen, which together maintain cartilage homeostasis, have a synergistic effect, can delay the development of osteoarthritis and alleviate symptoms; contains vitamin C (100 mg / tablet), meets daily needs, has antioxidant effect, and can promote collagen synthesis and accelerate osteoarthritis recovery. Glucosamine sulfate and vitamin C are reasonably matched to help shorten the recovery period of joint discomfort; does not contain sucrose, and the prescription contains sodium salt, is low in calories and helps maintain water balance, and is suitable for people with high-intensity metabolic exercise.

[0006] The second object of the present invention is to provide a method for preparing glucosamine sulfate effervescent tablets. The effervescent tablets obtained by step-by-step granulation and total compression have a fast dissolution rate during use, rapid release of active ingredients, rapid onset of action, high bioavailability, and are easy to carry. They are particularly suitable for the elderly, children, and users who cannot swallow solid preparations.

[0007] The present invention is achieved through the following technical solutions:

[0008] A glucosamine sulfate effervescent tablet composition, comprising the following prescription components in the following proportions:

[0009] Glucosamine sulfate 0.5-1.5g, chondroitin sulfate 0.05-0.15g, anhydrous citric acid 0.5-1.5g, anhydrous sodium carbonate 0.475-1.425g, mannitol 0.24-0.72g, sorbitol 0.03-0.09g, orange flavor 0.035-0.105g, sucralose 0.005-0.015g, polyethylene glycol 6000 0.085-0.255g, vitamin C 0.05-0.15g, collagen 0.02-0.06g, beta-carotene 0.01-0.03g;

[0010] The total tablet weight is 2 to 6 g.

[0011] Preferably, the effervescent tablet composition is composed of the following prescription components:

[0012] Glucosamine sulfate 1g, chondroitin sulfate 0.1g, anhydrous citric acid 1g, anhydrous sodium carbonate 0.95g, mannitol 0.48g, sorbitol 0.06g, orange flavor 0.07g, sucralose 0.01g, polyethylene glycol 60000 0.17g, vitamin C 0.1g, collagen 0.04g, beta-carotene 0.02g;

[0013] The total tablet weight is 4g.

[0014] A glucosamine sulfate effervescent tablet is prepared from the glucosamine sulfate effervescent tablet composition.

[0015] A method for preparing glucosamine sulfate effervescent tablets comprises the following steps:

[0016] S1. Anhydrous citric acid granulation:

[0017] Anhydrous citric acid and mannitol are selected, crushed and sieved to remove lumps, weighed and mixed according to the prescribed amount, and then added with a sorbitol aqueous solution and β-carotene. The mixture is wet-granulated on a sieve, dried to a moisture content of no more than 1.0%, and dry-granulated on a sieve to obtain anhydrous citric acid granules.

[0018] S2. Anhydrous sodium carbonate granulation:

[0019] Anhydrous sodium carbonate and mannitol are selected, crushed and sieved to remove lumps, weighed and mixed according to the prescribed amount, and then added with a sorbitol aqueous solution and β-carotene. The mixture is wet-granulated on a sieve, dried to a moisture content of no more than 1.0%, and dry-granulated on a sieve to obtain anhydrous sodium carbonate granules.

[0020] S3. Glucosamine sulfate granulation:

[0021] Glucosamine sulfate and mannitol are selected, crushed and sieved to remove lumps, and then glucosamine sulfate, chondroitin sulfate, and mannitol are weighed according to the prescribed amount and mixed evenly. A sorbitol aqueous solution and β-carotene are added to the mixture, and the mixture is wet-granulated on a sieve, dried to a moisture content of no more than 1.0%, and dry-granulated on a sieve to obtain glucosamine sulfate granules.

[0022] S4. Total mixing and tableting:

[0023] The anhydrous citric acid granules, anhydrous calcium carbonate granules and glucosamine sulfate granules are selected, orange flavor, sucralose, powdered polyethylene glycol 6000, vitamin C and collagen are added according to the prescribed amount, mixed evenly, and tableted to obtain effervescent tablets.

[0024] Preferably, in S1, anhydrous citric acid and mannitol are selected and crushed and passed through a 50-60 mesh sieve to remove lumps;

[0025] The prescription amount of anhydrous citric acid: mannitol: β-carotene is 1.0g / tablet: 0.14g / tablet: 0.0075g / tablet;

[0026] The mass concentration of the sorbitol aqueous solution is 40%;

[0027] The amount of the sorbitol aqueous solution added is 2 to 8% of the total weight of the anhydrous citric acid and mannitol.

[0028] The mixture is wet granulated through a 20-24 mesh sieve, dried in an oven at 70-75° C. until the moisture content is no more than 1.0%, and dry granulated through a 20-24 mesh sieve to obtain the product.

[0029] Preferably, in S2, anhydrous sodium carbonate and mannitol are selected and crushed and passed through a 50-60 mesh sieve to remove lumps;

[0030] The prescription amount of anhydrous sodium carbonate: mannitol: β-carotene is 0.95g / tablet: 0.09g / tablet: 0.005g / tablet;

[0031] The mass concentration of the sorbitol aqueous solution is 40%;

[0032] The amount of the sorbitol aqueous solution added is 2 to 8% of the total weight of the anhydrous citric acid and mannitol.

[0033] The product is wet granulated through a 20-24 mesh sieve, dried in an oven at 45-50° C. until the moisture content is no more than 1.0%, and dry granulated through a 20-24 mesh sieve to obtain the product.

[0034] Preferably, in S3, glucosamine sulfate and mannitol are selected and crushed and passed through a 50-60 mesh sieve to remove lumps;

[0035] The prescription amount of glucosamine sulfate: chondroitin sulfate: mannitol: β-carotene is 1.0g / tablet: 0.1g / tablet: 0.25g / tablet: 0.0075g / tablet;

[0036] The mass concentration of the sorbitol aqueous solution is 40%;

[0037] The amount of the sorbitol aqueous solution added is 2 to 8% of the total weight of the anhydrous citric acid and mannitol.

[0038] The product is wet granulated through a 20-24 mesh sieve, dried in an oven at 45-50° C. until the moisture content is no more than 1.0%, and dry granulated through a 20-24 mesh sieve to obtain the product.

[0039] Preferably, in S4, the vitamin C is sieved through a 50-60 mesh sieve when used.

[0040] Preferably, the hardness of the effervescent tablet is 20-50N.

[0041] Preparation of the 40% sorbitol aqueous solution: If preparing samples in batches of 1000 tablets, weigh 90g of purified water into a beaker, place in a 40°C water bath, stir continuously, slowly add 60g of sorbitol, stir until completely dissolved, and cool to room temperature.

[0042] Compared with the prior art, the present invention has at least the following technical effects:

[0043] (1) The present invention provides a glucosamine sulfate effervescent tablet, which contains glucosamine sulfate and has a high effective drug content of 1000 mg / tablet. One tablet is taken daily, which is convenient to take and improves patient compliance; it contains glucosamine sulfate, chondroitin sulfate, and collagen, which together maintain cartilage homeostasis and have a synergistic effect, can delay the development of osteoarthritis and alleviate symptoms; it contains vitamin C (100 mg / tablet), which meets daily needs, has antioxidant effects, and can promote collagen synthesis and accelerate osteoarthritis recovery. Glucosamine sulfate and vitamin C are reasonably matched to help shorten the recovery period of joint discomfort; it does not contain sucrose, and the prescription contains sodium salt, which is low in calories and helps maintain water balance, and is suitable for people who do high-intensity metabolic exercises.

[0044] (2) A method for preparing the glucosamine sulfate effervescent tablets. The effervescent tablets obtained by step-by-step granulation followed by total compression have a fast dissolution rate during use, rapid release of active ingredients, rapid onset of action, high bioavailability, and are easy to carry. They are particularly suitable for the elderly, children, and users who cannot swallow solid preparations.

[0045] (3) The glucosamine sulfate effervescent tablets, through reasonable prescription and dosage form design, have the advantages of high dosage, rapid onset of effect, high bioavailability, and easy portability, while solving the problem of poor medication compliance of marketed drugs.

[0046] (IV) In this preparation method, anhydrous citric acid granules, anhydrous calcium carbonate granules and glucosamine sulfate granules are carried out in separate steps. Based on the wet granulation process adopted, if anhydrous citric acid and anhydrous sodium carbonate are granulated together, a neutralization reaction will occur and they must be granulated separately; glucosamine sulfate is granulated separately to avoid contact with acid and alkali during the wet granulation process, which affects stability. BRIEF DESCRIPTION OF THE DRAWINGS

[0047] Figure 1 This is a schematic diagram of the actual product produced in Example 1. DETAILED DESCRIPTION

[0048] The embodiments of the present invention will be described in detail below with reference to the examples. However, those skilled in the art will understand that the following examples are only used to illustrate the present invention and should not be construed as limiting the scope of the present invention. Specific conditions not specified in the examples are carried out according to conventional conditions or conditions recommended by the manufacturer. Reagents or instruments used without indicating the manufacturer are all conventional products that can be purchased commercially.

[0049] Example 1:

[0050] A prescription composition of glucosamine sulfate effervescent tablets: specific products such as Figure 1 As shown:

[0051]

[0052]

[0053] A preparation method of glucosamine sulfate effervescent tablets comprises:

[0054] (1) Anhydrous citric acid granulation:

[0055]

[0056] Anhydrous citric acid is crushed, and mannitol is passed through a 60-mesh sieve to remove lumps. Anhydrous citric acid and mannitol are weighed according to the prescribed amount, mixed evenly, and 40% sorbitol aqueous solution is added for granulation (addition amount: approximately 4.8% of the weight of the material in the pot, and 0.0075g / tablet β-carotene is added to the sorbitol solution). The granules are wet-sieved through a 24-mesh sieve and then dried in an oven at 75°C until the moisture content is less than 1.0% (rapid moisture meter, 105°C automatic mode). After drying, the granules are dried through a 24-mesh sieve to obtain anhydrous citric acid granules.

[0057] (2) Anhydrous sodium carbonate granulation:

[0058]

[0059] Anhydrous sodium carbonate was crushed, and mannitol was passed through a 60-mesh sieve to remove lumps. Anhydrous sodium carbonate and mannitol were weighed according to the prescribed amount, mixed evenly, and 40% sorbitol aqueous solution was added for granulation (the amount added was about 4.2% of the weight of the material in the pot, and 0.005g / tablet of β-carotene was added to the sorbitol solution). The granules were wet-sieved through a 24-mesh sieve and then dried in an oven at 50°C until the moisture content was less than 1.0% (rapid moisture meter, 105°C automatic mode). After drying, the granules were dried through a 24-mesh sieve to obtain anhydrous sodium carbonate granules.

[0060] (3) Glucosamine sulfate granulation:

[0061]

[0062] Glucosamine sulfate was passed through a 60-mesh sieve to remove lumps, and mannitol was passed through a 60-mesh sieve to remove lumps. Glucosamine sulfate, chondroitin sulfate, and mannitol were weighed according to the prescribed amount and mixed uniformly. A 40% concentration of sorbitol aqueous solution was added to granulate the granules (the amount added was approximately 4.4% of the weight of the material in the pot, and 0.0075g / tablet of β-carotene was added to the sorbitol solution). The granules were wet-sieved through a 24-mesh sieve and then dried in an oven at 50°C until the moisture content was less than 1.0% (rapid moisture meter, 105°C automatic mode). After drying, the granules were dried through a 24-mesh sieve to obtain glucosamine sulfate granules.

[0063] (4) Total mixing and tableting:

[0064] The granules prepared above were added with orange flavor, sucralose, polyethylene glycol 6000 (powdered), vitamin C (passed through a 60-mesh sieve), and collagen according to the prescribed amount, mixed evenly, and compressed into tablets after the total mixing. The tablet weight was controlled to be about 4.0 g and the hardness was controlled to be about 30-40 N.

[0065] Finally, it should be noted that the above description is only 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 shall be included in the scope of protection of the present invention.

Claims

1. A glucosamine sulfate effervescent tablet composition, characterized in that: The effervescent tablet composition is composed of the following prescription components in the following proportions: composition: Glucosamine sulfate 0.5-1.5g, chondroitin sulfate 0.05-0.15g, anhydrous citric acid 0.5-1.5g, anhydrous sodium carbonate 0.475-1.425g, mannitol 0.24-0.72g, sorbitol 0.03-0.09g, orange flavor 0.035-0.105g, sucralose 0.005-0.015g, polyethylene glycol 6000 0.085-0.255g, vitamin C 0.05-0.15g, collagen 0.02-0.06g, beta-carotene 0.01-0.03g; The total tablet weight is 2 to 6 g.

2. A glucosamine sulfate effervescent tablet composition according to claim 1, characterized in that, The effervescent tablet composition is composed of the following prescription components: Glucosamine sulfate 1g, chondroitin sulfate 0.1g, anhydrous citric acid 1g, anhydrous sodium carbonate 0.95g, mannitol 0.48g, sorbitol 0.06g, orange flavor 0.07g, sucralose 0.01g, polyethylene glycol 6000 0.17g, vitamin C 0.1g, collagen 0.04g, beta-carotene 0.02g; The total tablet weight is 4g.

3. A glucosamine sulfate effervescent tablet, characterized in that: The effervescent tablet is prepared from the glucosamine sulfate effervescent tablet composition according to claim 1 or 2.

4. A method for preparing the glucosamine sulfate effervescent tablets according to claim 3, characterized in that: The steps include: S1. Anhydrous citric acid granulation: Anhydrous citric acid and mannitol are selected, crushed and sieved to remove lumps, weighed and mixed according to the prescribed amount, and then added with a sorbitol aqueous solution and β-carotene. The mixture is wet-granulated on a sieve, dried to a moisture content of no more than 1.0%, and dry-granulated on a sieve to obtain anhydrous citric acid granules. S2. Anhydrous sodium carbonate granulation: Anhydrous sodium carbonate and mannitol are selected, crushed and sieved to remove lumps, weighed and mixed according to the prescribed amount, and then added with a sorbitol aqueous solution and β-carotene. The mixture is wet-granulated on a sieve, dried to a moisture content of no more than 1.0%, and dry-granulated on a sieve to obtain anhydrous sodium carbonate granules. S3. Glucosamine sulfate granulation: Glucosamine sulfate and mannitol are selected, crushed and sieved to remove lumps, and then glucosamine sulfate, chondroitin sulfate, and mannitol are weighed according to the prescribed amount and mixed evenly. A sorbitol aqueous solution and β-carotene are added to the mixture, and the mixture is wet-granulated on a sieve, dried to a moisture content of no more than 1.0%, and dry-granulated on a sieve to obtain glucosamine sulfate granules. S4. Total mixing and tableting: The anhydrous citric acid granules, anhydrous calcium carbonate granules and glucosamine sulfate granules are selected, orange flavor, sucralose, powdered polyethylene glycol 6000, vitamin C and collagen are added according to the prescribed amount, mixed evenly, and tableted to obtain effervescent tablets.

5. The method for preparing a glucosamine sulfate effervescent tablet according to claim 4, wherein: In S1, anhydrous citric acid and mannitol are selected and crushed and passed through a 50-60 mesh sieve to remove lumps; The prescription amount of anhydrous citric acid: mannitol: β-carotene is 1.0g / tablet: 0.14g / tablet: 0.0075g / tablet; The mass concentration of the sorbitol aqueous solution is 40%; The amount of the sorbitol aqueous solution added is 2 to 8% of the total weight of the anhydrous citric acid and mannitol. The mixture is wet granulated through a 20-24 mesh sieve, dried in an oven at 70-75° C. until the moisture content is no more than 1.0%, and dry granulated through a 20-24 mesh sieve to obtain the product.

6. The method for preparing a glucosamine sulfate effervescent tablet according to claim 4, wherein: In S2, anhydrous sodium carbonate and mannitol are selected and crushed and passed through a 50-60 mesh sieve to remove lumps; The prescription amount of the anhydrous sodium carbonate: mannitol: β-carotene is 0.95g / tablet: 0.09g / tablet: 0.005g / tablet; The mass concentration of the sorbitol aqueous solution is 40%; The amount of the sorbitol aqueous solution added is 2 to 8% of the total weight of the anhydrous citric acid and mannitol. The product is wet granulated through a 20-24 mesh sieve, dried in an oven at 45-50° C. until the moisture content is no more than 1.0%, and dry granulated through a 20-24 mesh sieve to obtain the product.

7. The method for preparing a glucosamine sulfate effervescent tablet according to claim 4, wherein: In S3, glucosamine sulfate and mannitol are selected and crushed and passed through a 50-60 mesh sieve to remove lumps; The prescription amount of glucosamine sulfate: chondroitin sulfate: mannitol: β-carotene is 1.0g / tablet: 0.1g / tablet: 0.25g / tablet: 0.0075g / tablet; The mass concentration of the sorbitol aqueous solution is 40%; The amount of the sorbitol aqueous solution added is 2 to 8% of the total weight of the anhydrous citric acid and mannitol. The product is wet granulated through a 20-24 mesh sieve, dried in an oven at 45-50° C. until the moisture content is no more than 1.0%, and dry granulated through a 20-24 mesh sieve to obtain the product.

8. The method for preparing a glucosamine sulfate effervescent tablet according to claim 4, wherein: In the S4, the vitamin C is passed through a 50-60 mesh sieve when used.

9. The method for preparing a glucosamine sulfate effervescent tablet according to claim 4, wherein: The hardness of the effervescent tablet is 20-50N.

Images