Gastrodia elata effervescent tablet and preparation method thereof

Abstract

The invention relates to the technical field of health care products, in particular to gastrodia elata effervescent tablets and a preparation method thereof. Comprising the following components in parts by weight: 120 to 150 parts of rhizoma gastrodiae extract dry powder, 20 to 30 parts of curcumin, 50 to 80 parts of Omega-3 fatty acid microcapsules, 0.2 to 0.4 part of vitamin D3 (micronized), 0.5 to 1.0 part of mecobalamin, 80 to 100 parts of citric acid, 90 to 110 parts of sodium bicarbonate, 60 to 80 parts of lactose, 40 to 60 parts of microcrystalline cellulose, 10 to 15 parts of povidone K30, 2 to 3 parts of magnesium stearate and 5 to 10 parts of vitamin C. Compared with a single-component preparation, the pharmaceutical composition is more suitable for treatment of rheumatism complicated with nerve injury, and multi-target synergistic interaction is realized.

Description

Technical Field

[0001] The present invention relates to the technical field of health care products, in particular to a gastrodia elata effervescent tablet and a preparation method thereof. Background Art

[0002] As a traditional precious Chinese medicinal material, Gastrodia elata contains a variety of effective ingredients such as ginseng, glycosides and trace alkaloids, and has the effects of calming the liver and relieving wind, dispelling wind and unblocking the meridians.

[0003] Making Gastrodia elata into effervescent tablets can not only improve its convenience of taking, but also promote the rapid release and absorption of active ingredients by leveraging its effervescent and disintegrating properties.

[0004] Traditional Gastrodia elata effervescent tablets usually use Gastrodia elata extract as the main active ingredient, or are only combined with simple excipients, relying solely on the single ingredient of Gastrodia elata. They are difficult to play a role in multiple dimensions such as neuroprotection, anti-inflammation, anti-oxidation, and nutritional supplementation, and their effects on improving neurasthenia, cardiovascular and cerebrovascular health are relatively limited.

[0005] At the same time, most existing Gastrodia elata effervescent tablets only focus on the sedative and anticonvulsant effects of Gastrodia elata, and are mainly used to relieve symptoms such as dizziness and headaches, and lack coverage of comprehensive health needs (such as antioxidants, cardiovascular and cerebrovascular care, nutrient supplementation, etc.).

[0006] This article describes in detail a Gastrodia elata effervescent tablet and its preparation method, aiming to retain the key ingredients in Gastrodia elata to the greatest extent and optimize product performance. Summary of the Invention

[0007] (1) Technical issues

[0008] The present invention aims to at least solve the problems of single ingredients, extensive process and limited functions in the prior art.

[0009] (2) Technical content

[0010] The present invention provides a Gastrodia elata effervescent tablet comprising the following components in parts by weight: 120-150 parts of Gastrodia elata extract dry powder, 20-30 parts of curcumin, 50-80 parts of omega-3 fatty acid microcapsules, 0.2-0.4 parts of vitamin D3 (micronized), 0.5-1.0 parts of methylcobalamin, 80-100 parts of citric acid, 90-110 parts of sodium bicarbonate, 60-80 parts of lactose, 40-60 parts of microcrystalline cellulose, 10-15 parts of povidone K30, 2-3 parts of magnesium stearate, and 5-10 parts of vitamin C.

[0011] This solution also provides a method for preparing a Gastrodia elata effervescent tablet, comprising the following steps:

[0012] S1, mixing and granulation:

[0013] 1.1 Stepwise mixing: Add the dry powder of Gastrodia elata extract, the prepared curcumin inclusion complex, Omega-3 fatty acid microcapsules, vitamin D3 (micronized), methylcobalamin, lactose, and microcrystalline cellulose into a three-dimensional mixer and mix at 20 rpm for 20 minutes to ensure that the ingredients are fully and evenly dispersed;

[0014] 1.2 Granulation: Prepare a 5%-8% ethanol solution of povidone K30 and slowly add it to the above mixed powder while stirring to prepare a soft material; the soft material should be able to form a ball when held in the hand and fall apart when pressed lightly; granulate the soft material through a 16-mesh sieve to obtain wet granules;

[0015] 1.3 Drying: Place the wet granules in a hot air drying oven and dry them at 40-50°C to control the moisture content of the granules to ≤3%;

[0016] S2, secondary mixing

[0017] 2.1 Pass citric acid, sodium bicarbonate and vitamin C through 80 mesh sieve respectively;

[0018] 2.2 Mix the magnesium stearate with the sieved citric acid, sodium bicarbonate, and vitamin C, and then place them in a two-dimensional mixer with the dried granules. Mix at 10 rpm for 10 minutes to ensure that the ingredients are evenly mixed and that no premature effervescence occurs.

[0019] S3, tableting

[0020] A rotary tablet press was used and a shallow concave die with a diameter of 8 mm was selected for tableting;

[0021] Set the tablet press pressure parameters, control the hardness of the effervescent tablets at 2-3kg, and control the tablet weight difference within ±5%, to ensure that the effervescent tablets have a smooth appearance and are free of cracks and loose tablets.

[0022] Furthermore, the curcumin inclusion compound is prepared by:

[0023] Curcumin was slowly added to a saturated aqueous solution of β-cyclodextrin at a weight ratio of 1:3, and ultrasonic inclusion was performed at 50°C for 30 minutes with an ultrasonic power of 200 W.

[0024] After the inclusion is completed, the solution is cooled to room temperature, freeze-dried, and crushed through a 100-mesh sieve to obtain the curcumin inclusion compound for use.

[0025] Furthermore, the Omega-3 fatty acid microcapsules are prepared by:

[0026] Using the complex coacervation method, gelatin and gum arabic were prepared into a 2% aqueous solution at a weight ratio of 1:1 and heated to 50°C to completely dissolve;

[0027] Slowly add Omega-3 fatty acids to the above mixed solution and stir at high speed (2000r / min) to form colostrum;

[0028] The pH of the system was adjusted to 4.0-4.5, glutaraldehyde was added to carry out cross-linking and curing reaction for 2 hours, and then spray-dried (inlet air temperature 180°C, outlet air temperature 80°C) to obtain microcapsules, which were passed through an 80-mesh sieve for later use.

[0029] Furthermore, the dry powder of Gastrodia elata extract, vitamin D3 (micronized), and methylcobalamin were respectively passed through a 100-mesh sieve to remove lumps and impurities and ensure the uniformity of the powder.

[0030] (3) Technical effects

[0031] The above structure enables this solution to have the following beneficial effects:

[0032] 1. It can effectively retain the active ingredients in Gastrodia elata, such as galangin, glycosides, and trace alkaloids, thereby enhancing the product's efficacy. It can be used in areas such as daily health care, fatigue relief, and sleep improvement. It can also be used as a supplement to functional foods or medicines to meet the needs of different consumers.

[0033] 2. Most existing effervescent tablets do not contain oily ingredients such as Omega-3. This formula achieves solidification through microencapsulation, expanding the applicability of effervescent tablet dosage forms;

[0034] 3. Gastrodia elata (for clearing meridians) + curcumin (for anti-inflammatory) + Omega-3 (for immune regulation) + methylcobalamin (for nerve repair) + vitamin D (for regulation of bone metabolism) is more suitable for the treatment of rheumatism combined with nerve damage than single-ingredient preparations, achieving multi-target synergistic enhancement. DETAILED DESCRIPTION

[0035] The technical solutions in the embodiments of the present invention will be clearly and completely described below in conjunction with the embodiments of the present invention. Obviously, the described embodiments are only part of the embodiments of the present invention, rather than all the embodiments; based on the embodiments of the present invention, all other embodiments obtained by ordinary technicians in this field without making creative work are within the scope of protection of the present invention.

[0036] A Gastrodia elata effervescent tablet comprising the following components in parts by weight: 120-150 parts of Gastrodia elata extract dry powder, 20-30 parts of curcumin, 50-80 parts of omega-3 fatty acid microcapsules, 0.2-0.4 parts of vitamin D3 (micronized), 0.5-1.0 parts of methylcobalamin, 80-100 parts of citric acid, 90-110 parts of sodium bicarbonate, 60-80 parts of lactose, 40-60 parts of microcrystalline cellulose, 10-15 parts of povidone K30, 2-3 parts of magnesium stearate, and 5-10 parts of vitamin C;

[0037] The added curcumin (anti-inflammatory and antioxidant), omega-3 fatty acids (nerve cell protection), vitamin D (regulates calcium and phosphorus metabolism and assists nerve signal transmission), and methylcobalamin (nourishes peripheral nerves) can synergize with Gastrodia elata to enhance nerve repair and anti-fatigue effects, making up for the "weak efficacy of a single ingredient" defect of existing products.

[0038] Through the use of complex ingredients (such as vitamin D + methylcobalamin to assist calcium absorption and nerve repair, vitamin C + curcumin to enhance antioxidant capacity), the applicable population can be expanded to cover a wider range of health needs;

[0039] The addition of vitamin D3, methylcobalamin, and vitamin C can not only maximize the efficacy of Gastrodia elata but also supplement essential nutrients for the human body. It is especially suitable for people who need to balance neurological health and nutritional balance (such as menopausal women and those recovering from surgery).

[0040] Lactose (sweetener) and vitamin C (acidity regulator) can neutralize the bitter taste of Gastrodia elata and curcumin. At the same time, magnesium stearate as a lubricant can improve tablet formability, avoid granularity during disintegration, and enhance the taking experience.

[0041] Curcumin: The main active ingredient in turmeric, it has powerful anti-inflammatory and antioxidant properties. It can inhibit the release of inflammatory factors (such as TNF-α and IL-6) and reduce joint inflammation in rheumatic diseases. When used in conjunction with Gastrodia elata, curcumin can enhance the analgesic effect of Gastrodia elata, and the two show a good synergistic effect in improving joint pain and swelling.

[0042] Omega-3 fatty acids: Commonly found in deep-sea fish oil, they have immune-regulating and anti-inflammatory properties, can reduce C-reactive protein levels in rheumatic patients, and alleviate systemic inflammation. Gastrodia elata regulates nerve function, and omega-3 fatty acids improve the body's inflammatory microenvironment. The combination of the two helps alleviate limb numbness and pain symptoms caused by rheumatism. The particle size of the omega-3 fatty acid microcapsules is controlled at 50-100 μm to prevent oil precipitation after contact with water, which would affect the formation of effervescent tablets. Omega-3 microencapsulation and vitamin D3 micronization can increase the surface area of ​​the ingredients and promote intestinal absorption.

[0043] Vitamin D: It not only participates in calcium and phosphorus metabolism but also has immune-regulating effects. Studies have found that rheumatoid arthritis patients often suffer from vitamin D deficiency. Vitamin D supplementation can reduce inflammation and enhance immunity. Gastrodia elata extract, synergistically combined with vitamin D, can improve rheumatic symptoms and limb numbness from two perspectives: neuromodulation and immune improvement.

[0044] Methylcobalamin: It is the active coenzyme form of vitamin B12, which can promote the synthesis of nucleic acids and proteins in neurons and repair damaged peripheral nerves; it is used in conjunction with Gastrodia elata to treat dull numbness in the limbs. Methylcobalamin focuses on nerve repair, while Gastrodia elata focuses on nerve function regulation. The two complement each other and accelerate the recovery process of nerve function.

[0045] In one embodiment, a Gastrodia elata effervescent tablet comprises the following components in parts by weight: 135 parts of Gastrodia elata extract dry powder, 25 parts of curcumin, 65 parts of Omega-3 fatty acid microcapsules, 0.3 parts of vitamin D3 (micronized), 0.75 parts of methylcobalamin, 90 parts of citric acid, 100 parts of sodium bicarbonate, 70 parts of lactose, 50 parts of microcrystalline cellulose, 12.5 parts of povidone K30, 2.5 parts of magnesium stearate, and 7.5 parts of vitamin C.

[0046] In one embodiment, a Gastrodia elata effervescent tablet comprises the following components in parts by weight: 120 parts of Gastrodia elata extract dry powder, 20 parts of curcumin, 50 parts of Omega-3 fatty acid microcapsules, 0.2 parts of vitamin D3 (micronized), 0.5 parts of methylcobalamin, 80 parts of citric acid, 90 parts of sodium bicarbonate, 60 parts of lactose, 40 parts of microcrystalline cellulose, 30-15 parts of povidone K, 2 parts of magnesium stearate, and 5 parts of vitamin C.

[0047] In one embodiment, a Gastrodia elata effervescent tablet comprises the following components in parts by weight: 150 parts of Gastrodia elata extract dry powder, 30 parts of curcumin, 80 parts of Omega-3 fatty acid microcapsules, 0.4 parts of vitamin D3 (micronized), 1.0 part of methylcobalamin, 100 parts of citric acid, 110 parts of sodium bicarbonate, 80 parts of lactose, 60 parts of microcrystalline cellulose, 15 parts of povidone K30, 3 parts of magnesium stearate, and 10 parts of vitamin C.

[0048] This solution also provides a method for preparing a Gastrodia elata effervescent tablet, comprising the following steps:

[0049] S1, raw material preparation

[0050] 1.1 Preparation of curcumin inclusion compound:

[0051] Curcumin was slowly added to a saturated aqueous solution of β-cyclodextrin at a weight ratio of 1:3, and ultrasonic inclusion was performed at 50°C for 30 minutes with an ultrasonic power of 200 W.

[0052] After the inclusion is completed, the solution is cooled to room temperature, freeze-dried, and crushed through a 100-mesh sieve to obtain the curcumin inclusion compound for use.

[0053] 1.2 Preparation of Omega-3 fatty acid microcapsules:

[0054] Using the complex coacervation method, gelatin and gum arabic were prepared into a 2% aqueous solution at a weight ratio of 1:1 and heated to 50°C to completely dissolve;

[0055] Slowly add Omega-3 fatty acids to the above mixed solution and stir at high speed (2000r / min) to form colostrum;

[0056] Adjust the pH of the system to 4.0-4.5, add glutaraldehyde to carry out cross-linking and curing reaction for 2 hours, and then spray dry (inlet air temperature 180°C, outlet air temperature 80°C) to obtain microcapsules, and pass through an 80-mesh sieve for later use;

[0057] 1.3 Gastrodia elata extract powder, vitamin D3 (micronized), and methylcobalamin were sieved separately with 100 mesh to remove lumps and impurities to ensure powder uniformity;

[0058] 1.4 Preparation of Gastrodia elata extract dry powder:

[0059] 1.4.1 Gastrodia elata pretreatment

[0060] Cleaning and slicing: Select fresh, mold-free Gastrodia elata, rinse with running water to remove impurities such as mud and sand on the surface, and cut into slices about 2-3mm thick for subsequent extraction;

[0061] Removing numbness and bitterness: Soak the Gastrodia elata slices in a 0.5% sodium chloride solution for 40-60 minutes, with the mass ratio of Gastrodia elata to sodium chloride solution being 1:6, to remove the numbness of the Gastrodia elata.

[0062] Then, the Gastrodia elata slices were soaked in a 2.5% β-cyclodextrin solution at 45°C for 50 minutes, with the mass ratio of Gastrodia elata to β-cyclodextrin solution being 1:8, to remove the bitterness and improve the taste.

[0063] After soaking, rinse with clean water and dry for later use;

[0064] 1.4.2 Extraction of active ingredients

[0065] Enzyme-assisted extraction: Grind the dried Gastrodia elata slices, pass through a 40-mesh sieve, mix the Gastrodia elata powder with water at a material-liquid ratio of 1g:15ml, add 2.5% cellulase based on the weight of Gastrodia elata, and perform enzymatic hydrolysis at 50°C for 30 minutes to destroy the Gastrodia elata cell walls and promote the dissolution of the active ingredients;

[0066] Ultrasonic-extraction combined extraction: The mixed solution after enzymatic hydrolysis was transferred to an ultrasonic extraction device, and an appropriate amount of ethanol-water mixed solvent (ethanol volume fraction of 60%) was added. The extraction was carried out at an ultrasonic power of 200 W and a temperature of 40°C for 40 minutes, and then filtered to collect the filtrate;

[0067] Repeat the extraction of the residue 1-2 times and combine the filtrates;

[0068] 1.4.3 Concentration and drying

[0069] Concentration under reduced pressure: Place the filtrate in a vacuum concentration device and concentrate it to an extract with a relative density of 1.2-1.3 (measured at 60°C) at 60°C and a vacuum degree of 0.08MPa to reduce the loss of active ingredients at high temperatures;

[0070] Spray drying: spray drying the concentrated extract at an air inlet temperature of 180°C and an air outlet temperature of 80°C to obtain dry powder of Gastrodia elata extract for later use;

[0071] S2, mixing and granulation:

[0072] 2.1 Stepwise mixing: Add the dry powder of Gastrodia elata extract, the prepared curcumin inclusion complex, omega-3 fatty acid microcapsules, vitamin D3 (micronized), methylcobalamin, lactose, and microcrystalline cellulose into a three-dimensional mixer and mix at 20 rpm for 20 minutes to ensure that the ingredients are fully and evenly dispersed;

[0073] 2.2 Granulation: Prepare a 5%-8% ethanol solution of povidone K30 and slowly add it to the above mixed powder while stirring to prepare a soft material; the soft material should be able to form a ball when held in the hand and fall apart when pressed lightly; granulate the soft material through a 16-mesh sieve to obtain wet granules;

[0074] 2.3 Drying: Place the wet granules in a hot air drying oven and dry them at 40-50°C to control the moisture content of the granules to ≤3%;

[0075] The dried granules are sieved through a 16-mesh sieve to remove large particles and fine powder;

[0076] S3, secondary mixing

[0077] 3.1 Pass citric acid, sodium bicarbonate and vitamin C through 80 mesh sieve respectively;

[0078] 3.2 Mix the magnesium stearate with the sieved citric acid, sodium bicarbonate, and vitamin C, and then place them in a two-dimensional mixer with the dried granules. Mix at 10 rpm for 10 minutes to ensure that the ingredients are evenly mixed and that no premature effervescence occurs.

[0079] S4, tableting

[0080] A rotary tablet press was used and a shallow concave die with a diameter of 8 mm was selected for tableting;

[0081] Set the tablet press pressure parameters, control the hardness of the effervescent tablets at 2-3kg, and control the tablet weight difference within ±5%, to ensure that the effervescent tablets have a smooth appearance and are free of cracks and loose tablets.

[0082] The contents of cymene, glycosides and trace alkaloids in the effervescent tablets were determined by high performance liquid chromatography. The detection results showed that the cymene content was not less than 0.5 mg / g and the total glycoside content was not less than 2 mg / g.

[0083] Unless otherwise expressly specified or limited, the terms "disposed," "installed," "connected," and "connected" should be understood broadly. For example, they may refer to fixed, detachable, or integral connections; mechanical or electrical connections; direct or indirect connections through an intermediary; and internal communication between two components. Those skilled in the art will understand the specific meanings of these terms in this application.

[0084] While embodiments of the present invention have been shown and described, it will be appreciated by those skilled in the art that various changes, modifications, substitutions, and variations may be made to these embodiments without departing from the principles and spirit of the invention, and that the scope of the invention is defined by the appended claims and their equivalents.

Claims

1. A Gastrodia elata effervescent tablet, characterized in that: The invention comprises the following components in parts by weight: 120-150 parts of dry powder of Gastrodia elata extract, 20-30 parts of curcumin, 50-80 parts of omega-3 fatty acid microcapsules, 0.2-0.4 parts of vitamin D3, 0.5-1.0 parts of methylcobalamin, 80-100 parts of citric acid, 90-110 parts of sodium bicarbonate, 60-80 parts of lactose, 40-60 parts of microcrystalline cellulose, 10-15 parts of povidone K30, 2-3 parts of magnesium stearate and 5-10 parts of vitamin C.

2. A Gastrodia elata effervescent tablet according to claim 1, characterized in that The vitamin D3 is micronized vitamin D3.

3. A Gastrodia elata effervescent tablet according to claim 1, characterized in that The particle size of the Omega-3 fatty acid microcapsules is 50-100 μm.

4. A method for preparing a Gastrodia elata effervescent tablet according to claims 1-3, characterized in that ,, including the following steps: S1, mixing and granulation: 1.1 Stepwise mixing: Add the dry powder of Gastrodia elata extract, the prepared curcumin inclusion complex, Omega-3 fatty acid microcapsules, vitamin D3, methylcobalamin, lactose, and microcrystalline cellulose into a three-dimensional mixer and mix at 20 rpm for 20 minutes to ensure that all ingredients are fully and evenly dispersed; 1.2 Granulation: Prepare a 5%-8% ethanol solution of povidone K30 and slowly add it to the above mixed powder while stirring to form a soft material; granulate the soft material through a 16-mesh sieve to obtain wet granules; 1.3 Drying: Place the wet granules in a hot air drying oven and dry them at 40-50°C to control the moisture content of the granules to ≤3%; S2, secondary mixing 2.1 Pass citric acid, sodium bicarbonate and vitamin C through 80 mesh sieve respectively; 2.2 Mix the magnesium stearate with the sieved citric acid, sodium bicarbonate, and vitamin C, and then place them in a two-dimensional mixer with the dried granules. Mix at 10 rpm for 10 minutes to ensure that the ingredients are evenly mixed and that no premature effervescence occurs. S3, tableting A rotary tablet press was used and a shallow concave die with a diameter of 8 mm was selected for tableting.

5. The preparation method according to claim 4, characterized in that In step 1.3, the dried granules are sieved through a 16-mesh sieve to remove adhered large particles and fine powder.

6. The preparation method according to claim 4, characterized in that Preparation of the curcumin inclusion compound: Curcumin was slowly added to a saturated aqueous solution of β-cyclodextrin at a weight ratio of 1:3, and ultrasonic inclusion was performed at 50°C for 30 minutes with an ultrasonic power of 200 W. After the inclusion is completed, the solution is cooled to room temperature, freeze-dried, and crushed through a 100-mesh sieve to obtain the curcumin inclusion compound for use.

7. The preparation method according to claim 4, characterized in that Preparation of the Omega-3 fatty acid microcapsules: Using the complex coacervation method, gelatin and gum arabic were prepared into a 2% aqueous solution at a weight ratio of 1:1 and heated to 50°C to completely dissolve; Slowly add Omega-3 fatty acids to the above mixed solution and stir at high speed to form colostrum; The pH of the system was adjusted to 4.0-4.5, and glutaraldehyde was added to carry out cross-linking and curing reaction for 2 hours, and then spray-dried to obtain microcapsules, which were passed through an 80-mesh sieve for later use.

8. The preparation method according to claim 4, characterized in that The dry powder of Gastrodia elata extract, vitamin D3 and methylcobalamin are respectively passed through a 100-mesh sieve before use to remove lumps and impurities.