A formulation of matatabi and a method for preparing the same

Abstract

The present application provides a preparation of pinitol, which comprises the following components: pinitol 5-58 parts by weight; filler 32-84 parts by weight; disintegrant 5-12 parts by weight; binder 0-5 parts by weight; lubricant 0.1-2 parts by weight; the filler comprises pregelatinized starch. The present application uses pregelatinized starch as the filler, and combines with the rest of the disintegrant, binder and lubricant, so that the final pinitol tablet is smooth in surface, appropriate in thickness and hardness, qualified in friability and good in dissolution.

Description

Technical Field

[0001] This invention relates to the field of pharmaceutical formulation technology, and in particular to a echinacoside formulation and its preparation method. Background Technology

[0002] In the process of drug use, to meet the needs of different routes of administration, effects, and patient populations, drugs need to be formulated into different dosage forms, such as tablets, pills, injections, aerosols, and ointments. Through research in pharmaceutics, various biological drugs, chemical raw materials, and traditional Chinese medicine extracts have been formulated into drugs that can be directly used by the human body, ensuring not only efficacy but also improving absorption and utilization. Because pharmaceutical preparations possess characteristics such as effectiveness, stability, uniformity, and economy, they not only ensure convenience for patients but also guarantee controllable drug quality and reduce the risks associated with drug use. Therefore, research in pharmaceutics not only brings greater convenience to people but also provides more services to patients.

[0003] Traditional Chinese medicine (TCM), as a traditional medicine, has a long history in my country. It is an important part of the splendid culture of the Chinese nation and one of the most influential disciplines in the world. Throughout history, TCM has made positive contributions to human health and development, especially in disease prevention, treatment, rehabilitation, and health maintenance, possessing unique advantages and appeal, and is highly sought after by the medical community both domestically and internationally. However, traditional dosage forms such as pills, decoctions, and powders are no longer keeping pace with modern development. Therefore, utilizing modern science and technology, applying new processes, excipients, and equipment, and developing new dosage forms and preparing new formulations of TCM have improved the overall level of TCM, ensuring the efficacy, stability, and quality control of TCM preparations. This lays a solid foundation for the modernization of TCM, its entry onto the world stage, and its participation in international competition. In recent years, the development of TCM preparations in my country has been rapid, with various new dosage forms being applied, such as ordinary preparations, sustained-release capsules, soft capsules, dispersible tablets, effervescent tablets, injections, gels, and chewable tablets.

[0004] Echinacoside (ECH), also known as echinacea glycoside or sea urchin glycoside, is derived from the rhizomes of plants in the genus *Echinacea*, primarily extracted from *Cistanche deserticola*. It is a phenylethanoid glycoside compound. Traditional Chinese medicine considers *Cistanche deserticola* to have extremely high medicinal value, possessing effects such as tonifying kidney yang, nourishing essence and blood, and moistening the intestines to relieve constipation. Modern medical research has discovered that echinacoside is one of the most important active components of *Cistanche deserticola*.

[0005] Modern research indicates that echinacoside can reverse and protect against rotenone-induced, middle cerebral artery occlusion, and 6-hydroxydopamine-induced dopaminergic neuronal damage. Echinacoside can also freely cross the blood-brain barrier, potentially offering treatment for neurodegenerative diseases such as Parkinson's and Alzheimer's, as well as preventing and treating ischemic brain diseases. Echinacoside may also exert significant neuroprotective effects through pathways such as reversing mitochondrial function and apoptosis, inhibiting TNF-α (tumor necrosis factor-α)-induced apoptosis in human neuroblastoma cells, and promoting cholinergic neurotransmitter levels in the brains of vascular dementia mice, making it suitable for intervention in neurodegenerative diseases. Echinacoside also possesses estrogen-like effects and can be used to treat estrogen deficiency-induced postmenopausal osteoporosis. It can protect against acute lung injury and is used to treat acute respiratory distress syndrome, as well as protect against carbon tetrachloride-induced acute liver injury in mice. Furthermore, echinacoside also exhibits anti-damage, antioxidant, anti-inflammatory, skin-protecting, and anti-aging effects.

[0006] The pharmacological and metabolic effects of echinacoside are constantly being explored. From its initial research on anti-damage, anti-infection, antioxidant, and neuroprotective effects, to its current research on life extension, immune regulation, anti-tumor, and anti-fibrotic effects, it is clear that echinacoside is a highly promising traditional Chinese medicine extract.

[0007] Current research on echinacoside mainly focuses on animal and cellular levels. The echinacoside samples used are primarily derived from raw materials produced by domestic and international companies (such as Sigma-Aldrich in the US and Chengdu Manster Co., Ltd. in China), and these samples have not been prepared into formulations. However, pharmacological activity studies of echinacoside have shown its promising application prospects in various areas. Therefore, it is necessary to prepare echinacoside into various oral solid dosage forms for clinical trials to accelerate its development and use. Echinacoside has a large amount of active pharmaceutical ingredient (API), which is highly hygroscopic and prone to agglomeration during wet granulation. Dry granulation is preferable, but dry granulation results in a high proportion of API, low tablet hardness, and difficulty in forming the tablets. Summary of the Invention

[0008] In view of this, the technical problem to be solved by the present invention is to provide a echinacoside preparation, wherein the echinacoside preparation of the present invention has a smooth surface, appropriate thickness and hardness, qualified brittleness and good dissolution.

[0009] This invention provides a echinacoside preparation, the raw materials of which include the following components:

[0010]

[0011] The filler includes pregelatinized starch.

[0012] Preferably, the filler may also include one or more of microcrystalline cellulose and lactose.

[0013] Preferably, the pregelatinized starch accounts for more than 20% of the mass percentage of the filler.

[0014] Preferably, the disintegrant is one or more of sodium carboxymethyl starch, croscarmellose sodium, and croscarmellose polyvinylpyrrolidone.

[0015] Preferably, the adhesive is one or more of methylcellulose, hydroxypropylcellulose, povidone, and sodium carboxymethylcellulose.

[0016] Preferably, the lubricant is one or more of talc, micronized silica gel, and magnesium stearate.

[0017] Preferably, the raw material comprises the following components:

[0018]

[0019] The preferred particle size of echinacoside is: passing through a 60-150 mesh sieve.

[0020] Preferably, the dosage form of the preparation is a tablet.

[0021] This invention provides a method for preparing echinacoside tablets, comprising:

[0022] Echinacoside was pulverized and sieved to obtain pretreated echinacoside.

[0023] The pretreated echinacoside, filler, disintegrant, binder, and lubricant are stirred and mixed, then compressed into tablets, coated, and dried to obtain the tablets.

[0024] Alternatively, pretreated echinacoside, filler, disintegrant, binder, and lubricant can be initially mixed, granulated, and sized. The granules can then be further mixed with the remaining lubricant, compressed, coated, and dried to obtain the final product.

[0025] Preferably, the initial stirring speed is 50-100 rpm and the time is 10-20 min; the continued stirring speed is 3-15 rpm and the time is 4-10 min.

[0026] The specific coating parameters are: inlet air temperature 65-80℃; outlet air temperature 40-50℃; coating pan rotation speed: 6-15 rpm; liquid spraying speed: 8-15 ml / min.

[0027] The drying time is 2 to 16 hours.

[0028] Compared with the prior art, the present invention provides a echinacoside formulation, the raw materials of which include the following components: 5-58 parts by weight of echinacoside; 32-84 parts by weight of filler; 5-12 parts by weight of disintegrant; 0-5 parts by weight of binder; and 0.1-2 parts by weight of lubricant; wherein the filler includes pregelatinized starch. The present invention uses pregelatinized starch as a filler, combined with the remaining disintegrant, binder, and lubricant, to finally obtain echinacoside tablets with smooth surface, suitable thickness and hardness, acceptable friability, and good dissolution. Detailed Implementation

[0029] This invention provides a echinacoside preparation and its preparation method. Those skilled in the art can refer to the content of this document and appropriately modify the process parameters to achieve the desired result. It should be particularly noted that all similar substitutions and modifications are obvious to those skilled in the art and fall within the scope of protection of this invention. The method and application of this invention have been described through preferred embodiments. Those skilled in the art can obviously modify or appropriately change and combine the method and application described herein without departing from the content, spirit, and scope of this invention to realize and apply the technology of this invention.

[0030] This invention provides a echinacoside preparation, the raw materials of which include the following components:

[0031]

[0032] The filler includes pregelatinized starch.

[0033] The present invention provides a echinacoside preparation, the raw materials of which include 5 to 58 parts by weight of echinacoside; preferably 8 to 55 parts by weight of echinacoside; more preferably 20 to 52 parts by weight; and most preferably 40 to 50 parts by weight.

[0034] The preferred particle size of echinacoside is: passing through a 60-150 mesh sieve.

[0035] The present invention provides a echinacoside preparation, the raw materials of which include 32 to 82 parts by weight of filler; preferably 34 to 82 parts by weight of filler; more preferably 36 to 60 parts by weight of filler.

[0036] The filler of this invention includes pregelatinized starch. The filler of this invention also includes one or more of microcrystalline cellulose and lactose.

[0037] That is, the filler can be pregelatinized starch; it can be a combination of pregelatinized starch and microcrystalline cellulose; it can be a combination of pregelatinized starch and lactose; or it can be a combination of pregelatinized starch, microcrystalline cellulose and lactose.

[0038] In the above combination, the pregelatinized starch accounts for more than 20% of the mass percentage of the filler.

[0039] This invention uses pregelatinized starch alone, or pregelatinized starch together with one or more of microcrystalline cellulose, lactose, etc., as a filler. Pregelatinized starch can increase tablet hardness and improve forming rate; improve tablet appearance and improve coating texture; improve the flowability of powder under direct compression and reduce tablet weight variation; and increase dissolution.

[0040] The present invention provides a echinacoside preparation, the raw materials of which include 5-12 parts by weight of disintegrant; preferably 6-11 parts by weight of disintegrant; more preferably 6-10 parts by weight of disintegrant.

[0041] The disintegrant described in this invention is one or more of sodium carboxymethyl starch, croscarmellose sodium, and croscarmellose. This invention does not limit the source of the disintegrant; any commercially available product well-known to those skilled in the art is acceptable.

[0042] The present invention provides a echinacoside preparation, the raw materials of which include 0 to 5 parts by weight of binder; preferably 0 to 4 parts by weight of binder; more preferably 0.5 to 4 parts by weight of binder.

[0043] The adhesive described in this invention is one or more of methylcellulose, hydroxypropylcellulose, povidone, and sodium carboxymethylcellulose; the source of the adhesive is not limited in this invention, and commercially available adhesives known to those skilled in the art are acceptable.

[0044] The present invention provides a echinacoside preparation, the raw materials of which include 0.1 to 2 parts by weight of lubricant; preferably 0.2 to 1.8 parts by weight of lubricant; more preferably 0.5 to 1.5 parts by weight of lubricant.

[0045] The lubricant described in this invention is one or more of talc, micronized silica gel, and magnesium stearate. This invention does not limit the source of the lubricant; commercially available products well-known to those skilled in the art are acceptable.

[0046] In a preferred embodiment of the present invention, the raw material comprises the following components:

[0047]

[0048] In a preferred embodiment of the present invention, the raw material comprises the following components:

[0049]

[0050] The preferred dosage form of the formulation described in this invention is a tablet.

[0051] The present invention comprises echinacoside and fillers, disintegrants, binders, lubricants, etc., commonly used in pharmaceutical preparations. The excipients used in the formulation of the present invention include: microcrystalline cellulose, lactose, pregelatinized starch, etc., which act as fillers; hydroxypropyl starch, sodium carboxymethyl starch, sodium carboxymethyl cellulose, croscarmellose sodium, croscarmellose ketone, etc., which act as disintegrants; methylcellulose, hydroxypropyl cellulose, povidone, sodium carboxymethyl cellulose, etc., which act as binders; and magnesium stearate, etc., which act as lubricants.

[0052] This invention provides a method for preparing echinacoside tablets, comprising:

[0053] Echinacoside was pulverized and sieved to obtain pretreated echinacoside.

[0054] The pretreated echinacoside, filler, disintegrant, binder, and lubricant are stirred and mixed, then compressed into tablets, coated, and dried to obtain the tablets.

[0055] Alternatively, pretreated echinacoside, filler, disintegrant, binder, and lubricant can be initially mixed, granulated, and sized. The granules can then be further mixed with the remaining lubricant, compressed, coated, and dried to obtain the final product.

[0056] The specific composition and proportions of the above-mentioned components have been clearly described above and will not be repeated here.

[0057] The method for preparing echinacoside tablets provided by the present invention first involves pulverizing and sieving echinacoside to obtain pretreated echinacoside.

[0058] The preferred method is as follows: the echinacoside raw material is pulverized, the particle size of the raw material is controlled, the powder is passed through a 60-150 mesh sieve (120 mesh sieve is preferred), and each raw and auxiliary material is weighed according to the prescription amount.

[0059] The pretreated echinacoside, filler, disintegrant, binder, and lubricant are initially mixed. More preferably, the echinacoside, filler, disintegrant, binder, and lubricant are mixed and stirred sequentially; the initial mixing rpm is 50-100 rpm, more preferably 60-90 rpm, and most preferably 80 rpm; the stirring time is preferably 10-20 min, more preferably 12-18 min, and most preferably 15 min. The mixing is preferably performed in a V-type mixer. This invention does not limit the type of instrument used; any instrument known to those skilled in the art is acceptable.

[0060] Alternatively, the mixture can be prepared as described above and then granulated and sized. More preferably, the echinacoside mixture is granulated in a dry granulator and then sized; the parameters of the dry granulator are: pressure roller speed 5-12 r / min, vertical feeding speed 12-40 r / min, horizontal feeding speed 40-140 r / min, and pressure 5-18 MPa. More preferably, the pressure roller speed is 8-12 r / min, vertical feeding speed is 18-40 r / min, horizontal feeding speed is 40-100 r / min, and pressure is 10-18 MPa. Most preferably, the pressure roller speed is 9 r / min, vertical feeding speed is 20 r / min, horizontal feeding speed is 70 r / min, and pressure is 16 MPa. A 24-mesh sieve is used for granulation. Then, the mixture is further stirred and mixed with a lubricant. Preferably, the mixed material is transferred to a three-dimensional mixer. The stirring speed is preferably 3–15 rpm; more preferably 5–12 rpm; and the mixing time is preferably 4–10 min; more preferably 5–8 min. This invention does not limit the instrument used; any instrument well-known to those skilled in the art is acceptable.

[0061] After mixing, the mixture is compressed into tablets using a tableting machine. The hardness is controlled between 6.0 and 12.0 kg, with the optimal hardness being 9.0 kg.

[0062] After compression, the tablets are coated. The uncoated tablets are placed in a coating pan, and the coating parameters are as follows: the inlet air temperature is preferably 65-80℃; more preferably 68-78℃; and most preferably 75℃; the outlet air temperature is preferably 40-50℃; more preferably 42-48℃; and most preferably 45℃; the coating pan rotation speed is preferably 6-15 rpm, more preferably 8-12 rpm; and the liquid spraying speed is preferably 8-15 ml / min; and more preferably 10-13 ml / min.

[0063] After drying the coated tablets, echinacoside tablets are obtained. The drying time is preferably 2-16 hours; more preferably 4-10 hours.

[0064] This invention provides a echinacoside formulation, the raw materials of which include the following components: 5-58 parts by weight of echinacoside; 32-84 parts by weight of filler; 5-12 parts by weight of disintegrant; 0-5 parts by weight of binder; and 0.1-2 parts by weight of lubricant; wherein the filler includes pregelatinized starch. This invention uses pregelatinized starch as a filler, combined with the remaining disintegrant, binder, and lubricant, to obtain echinacoside tablets with smooth surfaces, suitable thickness and hardness, acceptable friability, and good dissolution.

[0065] To further illustrate the present invention, the following detailed description, in conjunction with embodiments, provides a echinacoside preparation and its preparation method. All embodiments and comparative examples of the present invention are in parts by weight, and the total weight of all components is consistent.

[0066] Methods for determining disintegration degree in embodiments and comparative examples of this invention:

[0067] Methods: Dissolution and release determination method (General Chapter 0931, Method II, Slurry method) of Part IV of the 2015 edition of the Chinese Pharmacopoeia.

[0068] Temperature: 37℃±0.5℃; Dissolution medium: water; Medium volume: 900mL; Rotation speed: 50 rpm; Sampling time: 45min.

[0069] Reference solution: The self-comparison method was used, and the concentration of echinacoside in the reference solution was 0.02 mg / mL.

[0070] Test solution: Accurately transfer 5 mL to a 50 mL volumetric flask, dilute to volume with aqueous medium, shake well, and set aside.

[0071] Detection method: Ultraviolet spectrophotometry. Detection wavelength: 330 nm.

[0072] Examples 1-8

[0073] Table 1

[0074]

[0075] Example: Preparation method of echinacoside ordinary tablets:

[0076] Take echinacoside according to the weight proportions in Table 1, add filler, appropriate amount of disintegrant, binder, magnesium stearate lubricant, mix well, and prepare tablets by tableting machine; or mix well and make into granules, and then prepare tablets by tableting machine.

[0077] Preparation method 1: Examples 1-6

[0078] (1) Pulverize the echinacoside raw material, control the particle size of the raw material, and pass the powder through a 60-150 mesh pharmacopoeia sieve (120 mesh pharmacopoeia sieve is best). Weigh each raw and auxiliary material according to the prescription amount.

[0079] (2) Add echinacoside, filler, disintegrant, binder and lubricant to a V-type mixer in sequence and stir for 50-100 rpm (80 rpm is best) for 10-20 min (15 min is best).

[0080] (3) Tableting: Tablets are compressed using a tablet press, with the hardness controlled at 6.0-12.0 kg (9.0 kg being optimal).

[0081] (4) Prepare the coating solution. Place the uncoated tablets in the coating pan. Coating parameters: inlet air temperature 65-80℃ (optimal 75℃); outlet air temperature 40-50℃ (optimal 45℃); coating pan rotation speed: 6-15rpm (optimal 12rpm); spraying speed: 8-15ml / min (optimal 10ml / min).

[0082] (6) Dry the sheets for 2-16 hours (4 hours is best).

[0083] Preparation method 2: Examples 7-8

[0084] (1) Pulverize the echinacoside raw material, control the particle size of the raw material, and pass the powder through a 60-150 mesh pharmacopoeia sieve (120 mesh pharmacopoeia sieve is best). Weigh each raw and auxiliary material according to the prescription amount.

[0085] (2) Add echinacoside, filler, disintegrant, binder and some lubricant into a V-type mixer in sequence, stir for 50-100 rpm (80 rpm is best) for 10-20 min (15 min is best);

[0086] (3) Dry granulation of the mixture: roller speed 5-12 r / min (optimal 9 r / min), vertical feeding speed 12-40 r / min (optimal 20 r / min), horizontal feeding speed 40-140 r / min (optimal 70 r / min), pressure 5-18 MPa (optimal 16 MPa). Granulation by 24 mesh sieve.

[0087] (4) Transfer the particles into a three-dimensional mixer, add the remaining amount of magnesium stearate, speed: 3-15 rpm (12 rpm is optimal), time: 4-10 min (5 min is optimal).

[0088] (5) Tableting: Tablets are compressed using a tablet press, with the hardness controlled at 6.0-12.0 kg (9.0 kg being optimal).

[0089] (6) Prepare the coating solution. Place the uncoated tablets in the coating pan. Coating parameters: inlet air temperature 65-80℃ (optimal 75℃); outlet air temperature 40-50℃ (optimal 45℃); coating pan rotation speed: 6-15rpm (optimal 12rpm); spraying speed: 8-15ml / min (optimal 10ml / min).

[0090] (7) Dry the slices for 2-16 hours (4 hours is best).

[0091] The results showed that the tablets obtained in Examples 1-8 had smooth surfaces, appropriate thickness and hardness, and qualified friability and dissolution.

[0092] Comparative Examples 1-10

[0093] Table 2

[0094]

[0095] Preparation method of echinacoside ordinary tablets for comparative examples 1-10:

[0096] According to the weight proportions in Table 2, echinacoside was taken, and fillers, disintegrants, binders, and magnesium stearate lubricants were added. The mixture was then prepared into tablets using a tableting machine.

[0097] Specifically:

[0098] (1) Pulverize the echinacoside raw material, control the particle size of the raw material, and pass the powder through a 60-150 mesh pharmacopoeia sieve (120 mesh pharmacopoeia sieve is best). Weigh each raw and auxiliary material according to the prescription amount.

[0099] (2) Add echinacoside, filler, disintegrant, binder and lubricant to a V-type mixer in sequence and stir for 50-100 rpm (80 rpm is best) for 10-20 min (15 min is best).

[0100] (3) Tableting: Tablets are compressed using a tablet press, with the hardness controlled at 6.0-12.0 kg (9.0 kg being optimal).

[0101] (4) Prepare the coating solution. Place the uncoated tablets in the coating pan. Coating parameters: inlet air temperature 65-80℃ (optimal 75℃); outlet air temperature 40-50℃ (optimal 45℃); coating pan rotation speed: 6-15rpm (optimal 12rpm); spraying speed: 8-15ml / min (optimal 10ml / min).

[0102] (5) Dry the sheets for 2-16 hours (4 hours is best).

[0103] The results show that, based on the above data, Comparative Example 10 tablets had low hardness and failed the friability test, making them unsuitable for coating. Comparative Example 2 tablets were too thick, which was detrimental to coating, packaging, and patient swallowing. Comparative Examples 1-5 indicate that when pregelatinized starch was not used as a filler in the formulation, or when one or more of microcrystalline cellulose and lactose were used alone, or when other excipients were used to replace pregelatinized starch, the tablets exhibited edge chipping, cracking, and an uneven surface (with bumps or cracks), and failed the hardness test. Comparative Examples 6-9 indicate that adding pregelatinized starch to the formulation and using one or more of microcrystalline cellulose and lactose can improve the appearance and increase the hardness of the tablets, but when used in combination with other excipients, all indicators met the requirements, but the effect was significantly lower than that of the other examples. The other examples had moderate hardness, and the friability was all below 0.2%. In contrast, Comparative Examples 6, 8, and 9 had hardness close to the limit of 6.0 kg and a friability of approximately 0.4%.

[0104] The above experimental data analysis shows that, within the material ratio range of this patent, an oral solid dosage form of echinacoside with good formability, suitable hardness, and dissolution rate that meets the standards can be obtained.

[0105] Verification test

[0106] 1. Production process verification test:

[0107]

[0108] Experimental results show that the oral solid dosage form of echinacoside has a stable process, high yield, and the obtained samples meet the quality standards and can be used to treat patients' diseases.

[0109] 2. Pharmacological activity verification

[0110] (1) Animal behavioral studies

[0111] 120 SPF-grade ICR mice were screened using a water maze test, and mice that were not sensitive to the test (could not find the platform within 60 seconds) were excluded. The mice were randomly divided into 6 groups: a blank control group, a model control group, and groups 1-4 (Examples 1-4). Scopolamine was injected intraperitoneally at 9:00 AM daily to induce the ICR model (the blank control group received sterile saline). The drugs were administered by gavage at 3:00 PM daily (the blank control and model control groups received saline, while the drugs in the example groups were prepared to contain the same concentration of echinacoside), for 14 consecutive days. Five days before the end of the experiment, the animals underwent a 5-day orientation navigation experiment (each mouse was trained once a day for 60 seconds, for 5 consecutive days. A fixed entry point was selected, and the mouse was placed in the water with its head facing the pool wall. If it could not find the platform within 60 seconds, it was led to a safe area and left there for 20 seconds; the escape latency period was recorded as 60 seconds. The above operation was repeated from day 2 to day 5). On day 6, a spatial exploration experiment was conducted. The reference points around the pool remained unchanged, the platform was removed, and the mouse was placed in the water at the same location and allowed to swim freely for 60 seconds. The time to reach the platform location for the first time and the number of times the mouse crossed the platform location within 60 seconds were recorded as indicators of its spatial memory ability.

[0112] Blank control group 16.3±1.0 5.4±1.1 Model control group <![CDATA[34.8±1.1 ** ]]> <![CDATA[1.8±0.4 ** ]]> Formula 1 set <![CDATA[25.8±1.4 ## ]]> <![CDATA[3.8±0.6 ## ]]> Formula 2 sets <![CDATA[26.5±1.1 ## ]]> <![CDATA[3.5±0.7 ## ]]> Formula 3 sets <![CDATA[25.9±1.4 ## ]]> <![CDATA[3.9±0.7 ## ]]> Formula 4 sets <![CDATA[25.2±1.1 ## ]]> <![CDATA[4.1±0.7 ## ]]> Formula 5 sets <![CDATA[26.0±0.5 ## ]]> <![CDATA[3.8±1.0 ## ]]> Formula 6 sets <![CDATA[26.1±0.4 ## ]]> <![CDATA[3.9±0.7 ## ]]> Formula 7 sets <![CDATA[25.9±0.5 ## ]]> <![CDATA[3.9±1.0 ## ]]> Formula 8 sets <![CDATA[25.5±0.5 ## ]]> <![CDATA[3.8±0.8 ## ]]>

[0113] Note: Compared with the blank control group, **P<0.01; compared with the model group, ## P<0.01;

[0114] Compared with the blank control group, the time for mice in the model control group to reach the platform for the first time was significantly increased, and the number of times they crossed the platform was significantly reduced (P<0.01), indicating that the memory impairment model was successfully established.

[0115] Compared with the model control group, the time for mice in the example group to reach the platform for the first time was significantly shorter and the number of times they crossed the platform was significantly increased (P<0.01), indicating that the sample of the example can improve the spatial learning and memory ability of mice.

[0116] (2) Biochemical indicator verification

[0117] After the water maze experiment, the mice were euthanized by cervical dislocation, and the brain tissue was immediately removed. The tissue was rinsed with cold physiological saline, weighed, and homogenized in 0.9% ice-cold physiological saline to prepare a 10% brain tissue homogenate. The homogenate was centrifuged at 3000 rpm for 10 minutes at 4°C, and the supernatant was collected. The 10% brain tissue homogenate was used to determine AChE activity and protein content using an AChE assay kit and a protein assay kit, following the kit instructions.

[0118] Blank control group 0.40±0.01 255.58±6.95 Model control group <![CDATA[0.56±0.02 ** ]]> <![CDATA[167.95±7.88 ** ]]> Example 1 Group <![CDATA[0.43±0.03 ## ]]> <![CDATA[237.20±5.75 ## ]]> Example 2 group <![CDATA[0.44±0.02 ## ]]> <![CDATA[227.3.±9.75 ## ]]> Example 3 Group <![CDATA[0.45±0.02 ## ]]> <![CDATA[225.76±6.26 ## ]]> Example 4 group <![CDATA[0.44±0.02 ## ]]> <![CDATA[240.74±6.73 ## ]]> Example 5 group <![CDATA[0.47±0.01 ## ]]> <![CDATA[225.18±3.37 ## ]]> Example 6 group <![CDATA[0.45±0.01 ## ]]> <![CDATA[227.24±4.18 ## ]]> Example 7 group <![CDATA[0.46±0.03 ## ]]> <![CDATA[224.57±6.21 ## ]]> Example 8 group <![CDATA[0.45±0.03 ## ]]> <![CDATA[231.56±5.89 ## ]]>

[0119] Note: Compared with the blank control group, **P<0.01; compared with the model group, ## P<0.01;

[0120] The central cholinergic system is closely related to learning and memory. Acetylcholine is a neurotransmitter that promotes learning and memory, and the degeneration of cholinergic neurons is considered a cause of dementia. Compared with the blank control group, the activity of AChE in the model control group mice was significantly increased, while the activity of AChE in the example control group was significantly reduced, indicating that the drug in the example can inhibit the activity of acetylcholinesterase and reduce the breakdown of acetylcholine.

[0121] Protein is the building block of brain memory function. Compared with the blank control group, the protein content of mice in the model control group was significantly reduced, while the drug in this example can promote the synthesis of brain tissue proteins, thereby enhancing learning and memory function.

[0122] The above description is only a preferred embodiment of the present invention. It should be noted that for those skilled in the art, several improvements and modifications can be made without departing from the principle of the present invention, and these improvements and modifications should also be considered within the scope of protection of the present invention.

Claims

1. A echinacoside preparation, characterized in that, Its raw materials consist of the following components: Echinacoside 40-50 parts by weight; 32-84 parts by weight of filler; 5-12 parts by weight of disintegrant; 0-5 parts by weight of adhesive; Lubricant 0.1 to 2 parts by weight; The filler is selected from one or more of pregelatinized starch, microcrystalline cellulose and lactose, and the pregelatinized starch accounts for more than 20% of the mass percentage of the filler. The adhesive is hydroxypropyl cellulose; The disintegrant is croscarmellose sodium cellulose; The lubricant is magnesium stearate; The method for preparing the echinacoside preparation includes: Echinacoside was pulverized and sieved to obtain pretreated echinacoside. The pretreated echinacoside is mixed with filler, disintegrant, binder and lubricant, then compressed into tablets, coated and dried to obtain tablets, with the drying time being 4 to 10 hours. The coating parameters are as follows: inlet air temperature 75℃; outlet air temperature 45℃; coating pan rotation speed: 8~12rpm; spraying speed: 10~13ml / min.

2. The formulation of eriodicytol according to claim 1, characterized in that, The dosage form of the preparation is tablets.

Images