Active Ginseng Orally Disintegrating Tablets, Their Preparation Methods and Applications
Active ginseng orally disintegrating tablets were prepared by low-temperature culture and freeze-drying technology, which solved the problems of loss of active ingredients and difficulty in swallowing, and achieved rapid disintegration and efficient absorption, making them suitable for the rehabilitation treatment of the elderly and patients with throat cancer.
Patent Information
- Authority / Receiving Office
- CN · China
- Patent Type
- Patents(China)
- Current Assignee / Owner
- TONGHUA XINYE BIOTECHNOLOGY R & D CO LTD
- Filing Date
- 2024-05-14
- Publication Date
- 2026-07-17
AI Technical Summary
Existing ginseng deep-processed products suffer significant loss of active ingredients during high-temperature processing, and the ginseng products on the market are difficult to meet the swallowing difficulties of the elderly, especially orally disintegrating tablets, which are not easy to dissolve in the mouth, affecting drug absorption and compliance.
Active ginseng orally disintegrating tablets were prepared using low-temperature culture and freeze-drying technology. Low-temperature culture reduced the starch content of ginseng while retaining active polysaccharides. Ginseng isomaltooligosaccharide was used as a disintegrant to ensure that enzyme activity was not destroyed, thus producing rapidly disintegrating orally disintegrating tablets.
It improves the utilization value of ginseng, making it suitable for the elderly, enhances the bioavailability of the drug, promotes postoperative recovery for patients with throat cancer, reduces swallowing difficulties, and improves patient compliance.
Smart Images
Figure BDA0004839093310000061 
Figure BDA0004839093310000081
Abstract
Description
Technical Field
[0001] This invention belongs to the field of ginseng deep processing, and in particular relates to active ginseng orally disintegrating tablets, their preparation methods, and their applications. Background Technology
[0002] Ginseng (Latin name: *Panax ginseng* CAMey.) is the dried root of a perennial herbaceous plant belonging to the Araliaceae family and the *Panax* genus. Ginseng is a plant in the *Panax* genus of the Araliaceae family, with a sweet and slightly bitter taste and warm properties. It has the effects of tonifying qi and nourishing yin, clearing heat and promoting body fluids, and enters the heart, lung, and kidney meridians. Currently, most deep-processed ginseng products use dried ginseng as raw material, and are made into food, medicine, or health products through high-temperature extraction, concentration, and drying processes. During the above processing, some volatile components, active enzymes, and other heat-sensitive components in fresh ginseng are lost or destroyed, which greatly reduces the activity of deep-processed ginseng products.
[0003] Fresh ginseng contains a wealth of active enzymes, including peroxidase (POD), catalase (CAT), malate dehydrogenase (MDH), superoxide dismutase (SOD), esterase (EST), acid phosphatase (ACP), amylase (AMY), and lactate dehydrogenase (LDH). These active enzymes exhibit significant antioxidant activity, attracting widespread attention.
[0004] Orally disintegrating tablets are a relatively new dosage form that disintegrates or dissolves rapidly in the mouth. The typical disintegration time is several seconds to over ten seconds, generally not exceeding one minute. No water or chewing is required in the mouth; the tablets quickly disintegrate upon contact with saliva to form a suspension, which is then swallowed and takes effect in the stomach. Compared to regular tablets, this rapid disintegration allows the drug to be absorbed through the mucous membranes. This dosage form is particularly suitable for the elderly, children, patients with swallowing difficulties, or people traveling in conditions of dehydration, and it features rapid onset of action and high bioavailability.
[0005] The current marketed disintegrating tablets have the drawback that disintegrants need to be added during the preparation of orally disintegrating tablets. These disintegrants are mostly poorly soluble high molecular weight compounds. After disintegration in the oral cavity, they cannot dissolve and will form a suspension, which will hinder the full absorption of the active ingredients in the oral cavity. For elderly patients, if saliva secretion is insufficient, the orally disintegrating tablets may form a thick paste in the oral cavity, which may cause choking in severe cases.
[0006] With the increase in average human lifespan and the decline in swallowing ability with age, oral tablet administration has become a concern. According to statistics, the incidence of difficulty swallowing tablets and capsules is relatively high in clinical drug use. Among the elderly, up to 35% of patients may have difficulty swallowing, and the proportion increases with age, affecting drug treatment compliance. The development of orally disintegrating tablets can improve the compliance of some populations. Its significance is: (1) reducing swallowing difficulties in some patients and improving compliance; (2) medication use in special populations and for the elderly, children and other patients with swallowing disorders; (3) medication can be used in emergency or water-free environments; for some patients who are not used to or have difficulty drinking water; (4) it can reduce the movement of some hospitalized patients and home patients with mobility difficulties and reduce the workload of nursing staff; (5) some drugs have improved bioavailability due to rapid absorption in the oral cavity or reduced enterohepatic metabolism.
[0007] Currently, ginseng and its products sold on the market are generally inconvenient to consume, especially for the elderly who often experience difficulty swallowing. Therefore, developing an active ginseng orally disintegrating tablet product can improve the utilization value of ginseng while meeting the needs of the elderly, which is of great practical significance. Summary of the Invention
[0008] To address the shortcomings of existing technologies, the purpose of this invention is to develop an orally disintegrating active ginseng tablet to enhance the utilization value of ginseng while providing convenience for consumption, thus meeting the needs of specific populations. This orally disintegrating active ginseng tablet is used for the rehabilitation treatment of patients with pharyngeal cancer after surgery and radiotherapy / chemotherapy.
[0009] To achieve the above objectives, the technical solution adopted by the present invention is as follows:
[0010] In a first aspect, the present invention provides a method for preparing orally disintegrating ginseng tablets, comprising the following steps:
[0011] S1. Fresh ginseng is cultured at low temperature for 20 to 40 days at 0 to 5°C and 70 to 90% relative humidity, preferably at 3°C and 80% relative humidity for 30 days.
[0012] S2, the ginseng cultured at low temperature in step S1 is washed with deionized water, crushed into granules, and extracted using ultrasound at 1-35℃ (preferably 5-10℃). The extract is filtered, centrifuged, and then centrifuged to obtain centrifuged liquid and crude starch. The centrifuged liquid is concentrated in a reverse osmosis device until the liquid density reaches 1.2-1.7 g / ml to obtain the first concentrate and reverse osmosis water. The density of the first concentrate is preferably 1.55 g / ml.
[0013] S3, add 1 to 10 times (preferably 5 times) of distilled water by weight of the crude starch obtained in step S2 to form a suspension, heat to 55 to 60°C, add 20 U / g α-glucosidase, and stir. React for 20 to 60 hours (preferably 40 hours). After the reaction is completed, heat to boiling, inactivate the enzyme, and filter to obtain ginseng isomaltooligosaccharide filtrate. The filtrate is concentrated by reverse osmosis concentrator to a liquid density of 1.2 to 1.7 g / ml to obtain a second concentrate. Preferably, the density of the second concentrate is 1.55 g / ml. The second concentrate is freeze-dried to obtain ginseng isomaltooligosaccharide freeze-dried powder.
[0014] S4, add 1-5% (preferably 2%) of ginseng isomaltooligosaccharide freeze-dried powder by weight of the first concentrate to the first concentrate, mix evenly to form a solution, add the solution quantitatively to a cold aluminum blister pack, freeze-dry after quick freezing in a liquid nitrogen tunnel, and obtain active ginseng orally disintegrating tablets.
[0015] In step S1, fresh ginseng is cultured at low temperature, which reduces the starch content of the ginseng to below 7% of the dry weight of the ginseng, while increasing the content of active polysaccharides in the ginseng to above 5% of the dry weight of the ginseng.
[0016] The ginseng isomaltooligosaccharide obtained in step S3 has excellent hygroscopicity and solubility, and can be used as a disintegrant for ginseng orally disintegrating tablets.
[0017] The active ginseng orally disintegrating tablets prepared by the above-mentioned preparation method of the present invention have a ginsenoside Rg1 content of up to 3%.
[0018] Optionally, the ginseng in step S1 can be fresh forest ginseng, garden ginseng, or American ginseng, preferably fresh forest ginseng aged 15 to 18 years.
[0019] Optionally, in step S2, distilled water or reverse osmosis water is used as the extraction solvent during ultrasonic extraction. Reverse osmosis water is recycled as the extraction solvent, achieving green production.
[0020] Optionally, in step S2, the particles are crushed into 60-100 mesh; the extract is filtered through a 100-mesh sieve; and the centrifugation speed is 5000-25000 r / min, preferably 20000 r / min.
[0021] Optionally, in step S3, the stirring speed is 120 r / min.
[0022] Optionally, in step S3, the freeze-drying conditions are as follows: Pre-freezing stage: The product is placed in the freeze-drying chamber and cooled to -50°C, and maintained at -50°C for 3–5 hours, at which point the pre-freezing stage ends; Sublimation stage: The plate temperature is controlled at 10–15°C, and the product temperature is maintained at -20–-25°C until the frozen ice in the product has completely sublimated; Desorption stage: The product temperature is heated to 20–33°C and maintained until the freeze-drying is complete. Preferably, to ensure that the active ginseng isomaltooligosaccharide does not absorb moisture, after the freeze-drying process is completed, the freeze-drying chamber is filled with dry, high-purity nitrogen.
[0023] Optionally, in step S4, the freeze-drying conditions are as follows: Pre-freezing stage: The product is placed in the freeze-drying chamber and cooled to -50°C, and maintained at -50°C for 3-5 hours, at which point the pre-freezing stage ends; Sublimation stage: The plate temperature is controlled at 10-15°C, and the product temperature is maintained at -20--25°C until the frozen ice in the product has completely sublimated; Desorption stage: The product temperature is heated to 20-33°C and maintained until the freeze-drying is completed. Preferably, to ensure that the orally disintegrating active ginseng slices are not oxidized or absorb moisture from the air, after the freeze-drying process is completed, the freeze-drying chamber is filled with dry, high-purity nitrogen.
[0024] Secondly, this aspect provides an active ginseng orally disintegrating tablet, which is prepared using the preparation method described in the first aspect.
[0025] The average disintegration time of the active ginseng orally disintegrating tablets is 1-30 seconds.
[0026] Thirdly, the present invention provides the application of the active ginseng orally disintegrating tablets described in the second aspect in the preparation of rehabilitation drugs for patients with pharyngeal cancer after surgery and radiotherapy and chemotherapy.
[0027] Fourthly, this invention provides a low-temperature culture method for increasing the content of active polysaccharides in ginseng, comprising the following steps: culturing fresh ginseng at 0–5°C and 70–90% relative humidity for 20–40 days, preferably at 3°C and 80% relative humidity for 30 days. After low-temperature culture, the starch content in the fresh ginseng decreases to below 7% of the ginseng's dry weight, while the content of active polysaccharides reaches above 5% of the ginseng's dry weight. Optionally, in the low-temperature culture method for increasing the content of active polysaccharides in ginseng, the ginseng can be fresh forest-grown ginseng, cultivated ginseng, or American ginseng, preferably fresh forest-grown ginseng aged 15–18 years.
[0028] More specifically, the low-temperature cultivation method includes the following steps: freshly harvested ginseng is spread on a breathable tray with a thickness of 10-15cm, the tray is placed on a shelf with a 10cm gap between two trays of ginseng, and the shelf is placed in a ventilated cold storage, with the indoor relative humidity controlled at 70%-90%, preferably 80%, and the indoor temperature controlled at 0-5℃, preferably 3℃; the cold storage is ventilated once a day from 5 am to 8 am, preferably at 6 am, for 10-30 minutes each time, preferably 15 minutes.
[0029] Fifthly, the present invention provides a method for preparing a ginseng isomaltooligosaccharide disintegrant, comprising the following steps:
[0030] (1) Fresh ginseng is cultured at low temperature for 20 to 40 days at 0 to 5℃ and 70 to 90% relative humidity, preferably at 3℃ and 80% relative humidity for 30 days;
[0031] (2) The ginseng after low-temperature culture is washed with deionized water, crushed into granules, and extracted by ultrasound at 1-35℃ (preferably 5-10℃). The extract is filtered and centrifuged to obtain centrifuged liquid and crude starch. The centrifuged liquid is concentrated by reverse osmosis until the liquid density reaches 1.2-1.7 g / ml to obtain the first concentrate and reverse osmosis water. The density of the first concentrate is preferably 1.55 g / ml.
[0032] (3) Add 1 to 10 times (preferably 5 times) of distilled water to crude starch to form a suspension, heat to 55 to 60°C, add 20 U / g α-glucosidase, and stir. React for 20 to 60 hours (preferably 40 hours). After the reaction is completed, heat to boiling, inactivate the enzyme, and filter to obtain ginseng isomaltooligosaccharide filtrate. The filtrate is concentrated by reverse osmosis concentrator to a liquid density of 1.2 to 1.7 g / ml to obtain a second concentrate. The density of the second concentrate is preferably 1.55 g / ml. The second concentrate is freeze-dried to obtain ginseng isomaltooligosaccharide freeze-dried powder.
[0033] Optionally, the ginseng in step (1) can be fresh forest ginseng, garden ginseng, or American ginseng, preferably fresh forest ginseng aged 15 to 18 years.
[0034] Optionally, in step (2), distilled water or reverse osmosis water is used as the extraction solvent during ultrasonic extraction. Reverse osmosis water is recycled as the extraction solvent to achieve green production.
[0035] Optionally, in step (2), the particles are crushed into 60-100 mesh; the extract is filtered through a 100-mesh sieve; and the centrifugation speed is 5000-25000 r / min, preferably 20000 r / min.
[0036] Optionally, in step (3), the stirring speed is 120 r / min.
[0037] Optionally, in step (3), the freeze-drying conditions are as follows: Pre-freezing stage: The product is placed in the freeze-drying chamber and cooled to -50°C, and maintained at -50°C for 3 to 5 hours, at which point the pre-freezing stage ends; Sublimation stage: The plate temperature is controlled at 10 to 15°C, and the product temperature is maintained at -20 to -25°C until the frozen ice in the product has sublimated completely; Desorption stage: The product temperature is heated to 20 to 33°C and maintained until the freeze-drying is completed. Preferably, to ensure that the active ginseng isomaltooligosaccharide does not absorb moisture, after the freeze-drying process is completed, the freeze-drying chamber is filled with dry high-purity nitrogen.
[0038] Compared with the prior art, the present invention has the following advantages:
[0039] 1. This invention provides a low-temperature culture method for increasing the content of active polysaccharides in ginseng.
[0040] 2. The active ginseng orally disintegrating tablets of the present invention are prepared by freeze-drying a mixture of fresh ginseng extract and disintegrant ginseng isomaltooligosaccharide. The average disintegration time of the active ginseng orally disintegrating tablets of the present invention is 1 second to 30 seconds. The active ginseng orally disintegrating tablets of the present invention do not contain any artificial chemical additives.
[0041] 3. The temperature is controlled to not exceed 35°C throughout the preparation process of the active ginseng orally disintegrating tablets of the present invention, so as to prevent the active enzymes from being destroyed by high temperature.
[0042] 4. The orally disintegrating ginseng tablets of this invention do not contain other chemical excipients, making the product safer. These orally disintegrating ginseng tablets promote the recovery of patients with pharyngeal cancer after surgery and radiotherapy / chemotherapy, and can be used in the development of pharmaceuticals, food, and health foods.
[0043] 5. The starch content in fresh ginseng is generally above 20% of the dry weight of ginseng, and the ginseng starch particles are relatively large. Ginseng active polysaccharides are important active ingredients in ginseng. In order to increase the content of ginseng active polysaccharides, this invention adopts low temperature culture technology to make the content of ginseng active polysaccharides reach more than 5% of the dry weight of ginseng. Detailed Implementation
[0044] The specific embodiments of this invention will be described in detail below with examples. In this specification, active polysaccharides refer to the pharmacologically active polysaccharides in ginseng polysaccharides other than starch, with pectin as the main component.
[0045] Example 1: Low-temperature culture of fresh ginseng
[0046] Freshly harvested ginseng was spread 15cm thick on breathable trays and placed on shelves, with a 10cm gap between each tray. The shelves were then placed in a well-ventilated cold storage room, maintaining a relative humidity of 80% and a temperature of 3℃. The cold storage was ventilated once daily at 6:00 AM for 15 minutes each time, for a total cultivation period of 30 days. After cultivation, the starch content in the ginseng decreased to 6.5% of its dry weight, while the content of active polysaccharides reached 8.2% of its dry weight. The content of active polysaccharides was determined using the phenol-sulfuric acid colorimetric method.
[0047] Example 2: Preparation of Orally Disintegrating Ginseng Tablets
[0048] 2.1 Extraction of fresh ginseng
[0049] Freshly cultivated ginseng is washed with deionized water and pulverized into 60-100 mesh particles. Extraction is performed at 5-10℃ using a continuous countercurrent ultrasonic extraction device with distilled water as the extraction solvent. The extract is filtered through a 100-mesh sieve, and the filtrate is centrifuged (20,000 rpm) to obtain a centrifuged liquid and crude starch. The centrifuged liquid is then concentrated using a reverse osmosis concentrator (Hefei Zhixuan Membrane Separation Technology Co., Ltd.) until the liquid density reaches 1.55 g / ml, yielding a concentrated liquid and reverse osmosis water. The reverse osmosis water is recycled as the extraction solvent, achieving green production.
[0050] 2.2 Preparation of Ginseng Isomaltooligosaccharide
[0051] A suspension was formed by adding five times its weight of distilled water to crude starch, heating to 55–60°C, adding 20 U / g α-glucosidase, and stirring at 120 rpm for 40 hours. After the reaction, the mixture was heated to boiling to inactivate the enzyme and filtered to obtain ginseng isomaltooligosaccharide filtrate. The filtrate was concentrated using a reverse osmosis concentrator (Hefei Zhixuan Membrane Separation Technology Co., Ltd.) to a liquid density of 1.55 g / ml to obtain a concentrated solution. The concentrated solution was then freeze-dried to obtain ginseng isomaltooligosaccharide freeze-dried powder. Freeze-drying (pre-freezing stage: the product is placed in the chamber and cooled to -50℃, and maintained at -50℃ for 3-5 hours, ending the pre-freezing stage. Sublimation stage: the plate temperature is controlled at 10-15℃, maintaining the product temperature at -20--25℃ until the frozen ice in the product has sublimated completely. Desorption stage: the product temperature is heated to 20-33℃ and maintained until the freeze-drying is complete). To ensure that the active ginseng isomaltooligosaccharide does not absorb moisture, the freeze-drying chamber is filled with dry, high-purity nitrogen after the freeze-drying process. Ginseng isomaltooligosaccharide has excellent hygroscopic properties and can be used as a disintegrant for ginseng disintegrating tablets.
[0052] 2.3 Preparation of Orally Disintegrating Ginseng Tablets
[0053] Add 2% (by weight of the dry matter) of ginseng oligoisomaltose to the above-mentioned fresh ginseng concentrate, mix well to form a solution, add the solution quantitatively into a cold aluminum blister pack, and freeze-dry after quick freezing in a liquid nitrogen tunnel.
[0054] Freeze-drying conditions: Pre-freezing stage: The product is placed in the freeze-drying chamber and cooled to -50°C, and maintained at -50°C for 3-5 hours, ending the pre-freezing stage; Sublimation stage: The plate temperature is controlled at 10-15°C, maintaining the product temperature at -20--25°C until the frozen ice in the product has sublimated completely; Desorption stage: The product temperature is heated to 20-33°C and maintained until the freeze-drying is complete. To ensure that the active ginseng orally disintegrating tablets are not oxidized or absorb moisture from the air, after the freeze-drying process, the freeze-drying chamber is filled with dry high-purity nitrogen gas to obtain the active ginseng orally disintegrating tablets of this invention, with a tablet weight of 0.7 grams and a ginsenoside Rg1 content of 3.2%. The ginseng orally disintegrating tablets are packaged in aluminum foil.
[0055] The content of ginsenoside Rg1 in the active ginseng orally disintegrating tablets was tested by high performance liquid chromatography.
[0056] Example 3: Determination of disintegration time of orally disintegrating active ginseng tablets
[0057] Following the method for determining disintegration time in the 2020 edition of the Chinese Pharmacopoeia, six orally disintegrating ginseng tablets were tested using water as the medium at a temperature of (37.0±1)℃. One tablet was tested at a time, and the disintegration time was measured from the moment the tablet touched the water surface until all the particles passed through the sieve. A total of six tests were performed. The average disintegration time was calculated. The average disintegration time of the orally disintegrating ginseng tablets was 5 seconds.
[0058] Example 4: Comparison of novel disintegrant ginseng isomaltooligosaccharide with traditional disintegrants
[0059] Take 20 ml of ginseng concentrate with a density of 1.55 g / ml and add the following disintegrants: microcrystalline cellulose (MCC), crospovidone (PVPP), low-substituted hydroxypropyl methylcellulose (L-HPC), sodium crospovidone carboxymethyl cellulose (CMC-Na), and 60 mg of ginseng isomaltooligosaccharide. Mix well to obtain a suspension. Quantitatively add the suspension to a pre-made cold aluminum blister pack, and after rapid freezing in a liquid nitrogen tunnel, freeze-dry (freeze-drying conditions: pre-freezing stage: the product is placed in the chamber and cooled to -50℃, and then at -5℃...). Pre-freezing stage: Pre-freezing is carried out at 0℃ for 3-5 hours. Sublimation stage: The plate temperature is controlled at 10-15℃, maintaining the product temperature at -20 to -25℃ until the frozen ice in the product has sublimated completely. Desorption stage: The product temperature is heated to 20-33℃ and maintained until the freeze-drying is completed. To ensure that the active ginseng orally disintegrating tablets are not oxidized or absorb moisture from the air, after the freeze-drying process is completed, the freeze-drying chamber is filled with dry high-purity nitrogen gas to obtain the active ginseng orally disintegrating tablets of this invention. These tablets are then packaged to obtain active ginseng orally disintegrating tablets with different disintegrants, each weighing 0.7 grams.
[0060] Determination of disintegration time of orally disintegrating ginseng tablets prepared with different disintegrants
[0061] Following the method for determining disintegration time in the 2020 edition of the Chinese Pharmacopoeia, six tablets of orally disintegrating active ginseng were taken and tested in water at a temperature of (37.0±1)℃. One tablet was tested at a time, and the disintegration time was measured from the moment the tablet touched the water surface until all the particles passed through the sieve. A total of six tests were conducted, and the average disintegration time was calculated. The results are as follows:
[0062] Table 1. Disintegration time of orally disintegrating tablets of fresh ginseng active extract with different disintegrants.
[0063]
[0064] The results showed that ginseng isomaltooligosaccharide has excellent disintegration properties.
[0065] Example 5: The effect of active ginseng orally disintegrating tablets on the recovery of patients with pharyngeal cancer after surgery and radiotherapy / chemotherapy.
[0066] Pharyngeal cancer is a common malignant tumor of the head and neck. Clinical treatment for pharyngeal cancer mainly involves surgery and radiotherapy, but both can cause varying degrees of pharyngeal damage, including congestion, edema, and partial or even complete loss of function. Postoperative complications and the toxic side effects of radiotherapy and chemotherapy often rely solely on the patient's own body for repair. Currently, there is a lack of effective treatments to promote the patient's recovery, as well as effective further consolidation treatments.
[0067] Active ginseng orally disintegrating tablets can rapidly disintegrate in the oral cavity and be absorbed through the oral mucosa. The active ingredients and enzymes in the active ginseng orally disintegrating tablets act on the lesions of pharyngeal cancer and surgical wounds through oral blood and lymph circulation, repairing wounds and inhibiting tumor growth. They have a significant promoting effect on the recovery of pharyngeal cancer patients after surgery and radiotherapy and chemotherapy.
[0068] Clinical efficacy trial of active ginseng orally disintegrating tablets
[0069] (I) Case Studies:
[0070] A clinical observation study was conducted on 128 patients with pharyngeal cancer. The treatment group (n=64) received active ginseng orally disintegrating tablets, while the control group (n=64) received anti-cancer tablets.
[0071] (II) Research Methods:
[0072] 1. Treatment group of 64 patients: After surgery and after radiotherapy and chemotherapy, they took active ginseng orally disintegrating tablets, with a daily dose of 6 tablets, each tablet weighing 0.7 grams.
[0073] 2. Xiaoyaping Group (64 cases): After surgery and after radiotherapy and chemotherapy, Xiaoyaping tablets were taken at a daily dose of 24 tablets.
[0074] Both groups took the medication continuously for 5 days, followed by a 2-day rest period, with 4 weeks constituting one course of treatment.
[0075] Clinical efficacy observation items:
[0076] 1. Does the gastrointestinal reaction lessen after chemotherapy?
[0077] The main gastrointestinal reactions after chemotherapy are nausea and vomiting, loss of appetite, constipation, and diarrhea. If nausea is reduced after 3 doses, the number of vomitings is reduced by more than 2 times compared to before taking the medication, appetite increases, constipation is relieved, and the number of diarrheas is reduced by more than 2 times, it is considered effective and counted as 1. If there is no change before and after taking the medication, it is considered ineffective and counted as 0.
[0078] 2. Is the white blood cell count increased?
[0079] Bone marrow suppression is a common side effect of radiotherapy and chemotherapy, mainly manifested as a decrease in white blood cell count. After taking the medication, the white blood cell count increased by 1*10 compared to before the medication. 9 / L is 1, 2*10 9 The / L count is 2, 3 * 10 9 A count of 3 or higher ( / L or above) indicates effectiveness; an increase of less than 1*10-1 in white blood cells after medication compared to before medication is also considered effective. 9 / L count is 0, invalid.
[0080] 3. Does the oral ulcer lessen after radiotherapy?
[0081] The incidence of oral ulcers after head and neck radiotherapy is relatively high, almost 100%. Some chemotherapy patients may also develop oral ulcers. The area and depth of oral ulcers are recorded before and after medication. A reduction of 25% in area is counted as 0 (ineffective); a reduction of 25%-50% is counted as 1; 50%-75% as 2; and a reduction of more than 75% as 3, all of which are effective. The disappearance of superficial ulcers or the transformation of deep ulcers into superficial ulcers is counted as 1; the disappearance of deep ulcers is counted as 2; and no significant change before and after medication is counted as 0.
[0082] 4. Whether the pain in the mouth and throat is relieved: If there is no significant change or no change after taking the medication, the count is 0, which is ineffective; if the pain is slightly relieved, the count is 1, and if the pain is significantly relieved, the count is 2, which are both effective.
[0083] The results of the comparison of the efficacy of active ginseng orally disintegrating tablets and anti-cancer tablets are shown in Table 1.
[0084] Table 1. Comparison of therapeutic effects between active ginseng orally disintegrating tablets and anti-cancer tablets.
[0085]
[0086] (III) Results:
[0087] Clinical studies have shown that the use of orally disintegrating active ginseng tablets after surgery for laryngeal cancer or during radiotherapy and chemotherapy has a sensitizing effect, enhancing the efficacy of radiotherapy and chemotherapy, reducing the toxic side effects of radiotherapy and chemotherapy such as gastrointestinal reactions, significantly reducing oral and pharyngeal mucosal reactions, oral ulcers and pain caused by radiotherapy, and significantly enhancing the body's cellular immunity and anti-tumor ability. Orally disintegrating active ginseng tablets also promote postoperative wound healing in patients after laryngeal cancer surgery.
Claims
1. A method for preparing orally disintegrating ginseng tablets, characterized in that, Includes the following steps: S1, Fresh ginseng is cultured at low temperature for 20-40 days in an environment of 0-5℃ and 70-90% relative humidity; S2, the ginseng cultured at low temperature in step S1 is washed with deionized water, crushed into granules, and extracted using ultrasound at 1~35 ℃. The extract is filtered, centrifuged, and then centrifuged to obtain centrifuged liquid and crude starch. The centrifuged liquid is concentrated by reverse osmosis until the liquid density reaches 1.2~1.7 g / ml to obtain the first concentrate and reverse osmosis water. S3, add 1-10 times the weight of distilled water to the crude starch obtained in step S2 to form a suspension, heat to 55-60℃, add 20 U / g α-glucosidase, and stir. React for 20-60 hours. After the reaction is completed, heat to boiling, inactivate the enzyme, and filter to obtain ginseng isomaltooligosaccharide filtrate. The filtrate is concentrated by reverse osmosis concentrator to a liquid density of 1.2-1.7 g / ml to obtain a second concentrate. The second concentrate is freeze-dried to obtain ginseng isomaltooligosaccharide freeze-dried powder. S4, add 1-5% of the dry matter weight of the first concentrate to the first concentrate, freeze-dried ginseng isomaltooligosaccharide powder, mix evenly to form a solution, add the solution quantitatively to a cold aluminum blister pack, freeze-dry after being rapidly frozen in a liquid nitrogen tunnel, and obtain active ginseng orally disintegrating tablets.
2. The preparation method according to claim 1, characterized in that, In step S2, during the ultrasonic extraction process, distilled water or reverse osmosis water is used as the extraction solvent.
3. The preparation method according to claim 1, characterized in that, In step S2, the particles are crushed into 60-100 mesh; the extract is filtered through a 100 mesh sieve; the centrifugation speed is 5000-25000 r / min; in step S3, the stirring speed is 120 r / min.
4. The preparation method according to claim 1, characterized in that, In step S3, the freeze-drying conditions are as follows: Pre-freezing stage: The product is placed in the chamber and cooled to -50 ℃, and maintained at -50 ℃ for 3~5 hours, at which point the pre-freezing stage ends; Sublimation stage: The plate temperature is controlled at 10~15 ℃, and the product temperature is maintained at -20~-25 ℃ until the frozen ice in the product has completely sublimated; Desorption stage: The product temperature is heated to 20~33 ℃ and maintained until the freeze-drying is completed.
5. The preparation method according to claim 1, characterized in that, In step S4, the freeze-drying conditions are as follows: Pre-freezing stage: The product is placed in the chamber and cooled to -50 ℃, and maintained at -50 ℃ for 3~5 hours, at which point the pre-freezing stage ends; Sublimation stage: The plate temperature is controlled at 10~15 ℃, and the product temperature is maintained at -20~-25 ℃ until the frozen ice in the product has completely sublimated; Desorption stage: The product temperature is heated to 20-33 ℃ and maintained until the freeze-drying is completed.
6. The preparation method according to claim 1, characterized in that, In step S1, the low-temperature culture is specifically cultured at 3°C and 80% relative humidity for 30 days; in step S2, the density of the first concentrate is 1.55 g / ml; in step S3, the density of the second concentrate is 1.55 g / ml; in step S4, the amount of ginseng isomaltooligosaccharide freeze-dried powder added is 2% of the dry matter weight of the first concentrate.
7. An active ginseng orally disintegrating tablet, prepared by the preparation method described in any one of claims 1 to 6.
8. The use of the active ginseng orally disintegrating tablets according to claim 7 in the preparation of rehabilitation drugs for patients with pharyngeal cancer after surgery and radiotherapy / chemotherapy.
9. A method for preparing a ginseng isomaltooligosaccharide disintegrant, comprising the following steps: (1) Fresh ginseng is cultured at low temperature for 20 to 40 days in an environment of 0 to 5 ℃ and 70 to 90% relative humidity; (2) The ginseng after low-temperature culture was washed with deionized water, crushed into granules, and extracted by ultrasound at 1~35 ℃. The extract was filtered and centrifuged to obtain centrifuged liquid and crude starch. The centrifuged liquid was concentrated by reverse osmosis until the liquid density reached 1.2~1.7 g / ml to obtain the first concentrate and reverse osmosis water. (3) Add 1 to 10 times the weight of crude starch in distilled water to form a suspension, heat to 55 to 60 °C, add 20 U / g of α-glucosidase and stir, react for 20 to 60 hours, heat to boiling after the reaction is completed, inactivate the enzyme and filter to obtain ginseng isomaltooligosaccharide filtrate, concentrate the filtrate through a reverse osmosis concentrator until the liquid density reaches 1.2 to 1.7 g / ml to obtain a second concentrate, and freeze-dry the second concentrate to obtain ginseng isomaltooligosaccharide freeze-dried powder.