Medicine for preventing and relieving Alzheimer's disease and preparation method thereof

Abstract

The invention provides a medicine for preventing and relieving Alzheimer's disease and a preparation method thereof. Comprising a capsule-shaped medicine main body, and three coatings are arranged in the capsule-shaped medicine main body and are respectively a first coating section, a second coating section and a third coating section from outside to inside; the pharmaceutical composition comprises antioxidants such as SOD, vitamin C, vitamin E and anthocyanin, nerve repairing components such as nervonic acid, ganglioside and vitamin B12 and neurotransmitter regulators such as arginine, tryptophan and asparaginic acid, can block multiple pathogenic links of the Alzheimer's disease at the same time, remarkably improves the curative effect, adopts a three-stage coating technology, and is free of toxic and side effects. According to the present invention, different components are ensured to be accurately released at the specific site and within the specific time, the mutual interference among the components is avoided, the drug activity is maximized, the ROS in the body is cleared through the SOD, the vitamin E and the like, the antioxidant activity is stabilized by the anthocyanin, the nerve cell repair is promoted by the nervonic acid and the ganglioside, and the brain function is significantly improved;

Description

Technical Field

[0001] The present invention relates to the field of medical technology, and more particularly to a drug for preventing and alleviating Alzheimer's disease and its preparation method. The drug prevents and alleviates Alzheimer's disease through multi-target synergistic effects, including free radical scavenging, nerve cell repair, and neurotransmitter regulation. Background Art

[0002] Alzheimer's disease is a neurodegenerative disease characterized by the accumulation of beta-amyloid protein, neurofibrillary tangles, and nerve cell damage caused by oxidative stress. Current clinical treatments (such as acetylcholinesterase inhibitors) only temporarily alleviate symptoms but cannot cure or effectively halt disease progression. Existing health supplements often lack scientific evidence and have limited efficacy.

[0003] Therefore, there is an urgent need for a drug combination that intervenes from multiple targets and achieves the effect of preventing and alleviating Alzheimer's disease through comprehensive effects such as scavenging free radicals, repairing nerve cells, and regulating neurotransmitters. Summary of the Invention

[0004] In view of this, the present invention proposes a drug and preparation method for preventing and alleviating Alzheimer's disease. The specific technical solution is as follows:

[0005] A drug for preventing and alleviating Alzheimer's disease, comprising a capsule-shaped drug body, wherein three coatings are provided inside the capsule-shaped drug body, namely, a first coating section, a second coating section, and a third coating section from the outside to the inside;

[0006] The first stage coating comprises the following raw materials according to weight ratio: arginine: 1500 g, tryptophan: 800 g, aspartic acid: 1200 g, starch 2000 g;

[0007] The second coating stage includes the following raw materials according to weight ratio: 500 g of glutathione, 800,000 active units (U), 800 g of oligomeric anthocyanidins, and 1000 g of starch;

[0008] The third coating stage includes the following raw materials according to weight ratio: 200 grams of vitamin B12, 200 grams of vitamin C, 200 grams of vitamin E, 1.04 grams of neuraminic acid, 0.52 grams of ganglioside, and 2000 grams of starch.

[0009] A method for preparing a drug for preventing and alleviating Alzheimer's disease comprises the following steps:

[0010] Step 1: Mix the raw materials for the first coating evenly, cut them into 1 mm small particles by a pelletizing machine, and do not perform coating treatment.

[0011] Step 2: Mix the raw materials for the second coating evenly and cut them into 1 mm small particles using a pelletizing machine.

[0012] Step 3: Mix the raw materials for the third coating evenly and cut them into 1 mm small particles using a pelletizing machine.

[0013] Step 4: coating the small particles of the second coating stage.

[0014] Step 5: coating the small particles in the third coating stage.

[0015] Step six: pack the uncoated first-stage coated granules, the coated second-stage coated granules and the third-stage coated granules into a capsule shell to form a three-stage capsule.

[0016] Furthermore, in step 4, 300 grams of polyacrylic acid resin No. 3 is used for coating.

[0017] Furthermore, in step five, 750 grams of polyacrylic acid resin No. 3 is used for coating.

[0018] Furthermore, the capsule shell is a slightly soluble corn plant capsule shell.

[0019] The above technical solution has the following beneficial effects:

[0020] The pharmaceutical composition of the present invention contains antioxidants such as SOD, vitamin C, vitamin E, anthocyanins, nerve repair components such as neuraminic acid, gangliosides, vitamin B12 and neurotransmitter regulators such as arginine, tryptophan and aspartic acid, which can simultaneously block multiple pathogenic links of Alzheimer's disease and significantly improve the therapeutic effect. The three-stage coating technology is adopted to ensure that different components are accurately released at specific locations and times, avoid mutual interference between components, maximize drug activity, eliminate ROS in the body through SOD, vitamin E, etc., anthocyanins stabilize the activity of antioxidants, neuraminic acid and gangliosides promote nerve cell repair, and significantly improve brain function. All ingredients in the present invention are natural or widely used medicinal substances. Preclinical experiments show that adverse reactions are few and suitable for long-term use. The present invention can not only be used to relieve symptoms of Alzheimer's patients, but also can be used as a preventive drug for high-risk groups, with both therapeutic and health care functions. DETAILED DESCRIPTION

[0021] The following is a clear and complete description of the technical solutions in the embodiments of the present invention. Obviously, the described embodiments are only part of the embodiments of the present invention, not all of the embodiments. Based on the embodiments of the present invention, all other embodiments obtained by ordinary technicians in this field without making any creative efforts are within the scope of protection of the present invention.

[0022] In Example 1, the drug of the present invention is a capsule formulation consisting of three coating sections, each containing specific active ingredients and excipients: The first coating section contains 1500 grams of arginine, 800 grams of tryptophan, 1200 grams of aspartic acid, and 2000 grams of starch. This section dissolves in the stomach, releasing amino acids that provide nutritional support to nerve cells and promote neurotransmitter synthesis.

[0023] The second coating layer contains 500g of glutathione, 800g of oligomeric anthocyanidins (800,000 U of active units), and 1000g of starch. This layer is coated with 300g of polyacrylic acid resin No. 3, which dissolves in the intestines, scavenging free radicals (glutathione) and stabilizing antioxidants (anthocyanidins).

[0024] The third coating section contains 200g of vitamin B12, 200g of vitamin C, 200g of vitamin E, 1.04g of neuraminic acid, 0.52g of gangliosides, and 2000g of starch. This section is coated with polyacrylic acid resin No. 3 (750g), with a two-hour delayed release to ensure adequate intestinal absorption of the nerve-repairing ingredients (neuraminic acid, gangliosides) and vitamins.

[0025] Superoxide dismutase (SOD), also known as superoxide dismutase (SOD), is an enzyme that catalyzes the dismutation of superoxide anion radicals (O2-) into H2O2 and O2. This enzyme is extremely widespread and has been isolated from various organisms, including bacteria, fungi, algae, plants, protozoa, insects, fish, and mammals. SOD has antioxidant and anti-aging properties, primarily through the scavenging of harmful superoxide anion radicals (O2-). SOD has unique therapeutic effects in treating diseases caused by superoxide radicals (O2-), such as oxygen poisoning, acute inflammation, various autoimmune diseases, radiation sickness, and senile cataracts. It is a promising new medicinal enzyme and is currently being studied as an anti-aging drug.

[0026] Vitamin C is a monoclinic crystal that is usually in the form of flakes or sometimes needles. It participates in the body's complex metabolic processes, promotes growth and enhances resistance to disease. It can be used as a nutritional supplement, antioxidant, and wheat flour improver. However, excessive vitamin C supplementation is not beneficial to health, but rather harmful, so it needs to be used reasonably. Vitamin C is used as an analytical reagent in the laboratory, such as a reducing agent, masking agent, etc.

[0027] Vitamin E, also known as tocopherol or tocopherol, is one of the most important antioxidants. It is soluble in organic solvents such as fat and ethanol, but insoluble in water. It is stable to heat and acid, unstable to alkali, sensitive to oxygen, and insensitive to heat. However, its activity is significantly reduced when fried. Vitamin E is found in cooking oils, fruits, vegetables, and grains. Vitamin E is a fat-soluble vitamin with eight forms and is often used in creams and lotions because it is believed to promote skin healing and reduce scarring after injuries such as burns.

[0028] Vitamin B12, also known as cobalamin, is a polycyclic compound containing trivalent cobalt. Four reduced pyrrole rings are linked together to form a corrin macrocycle (similar to porphyrin). It is the only vitamin containing metal elements. Vitamin B12 is a red crystalline powder, odorless and tasteless, slightly soluble in water and ethanol, and is most stable under weak acid conditions of pH 4.5 to 5.0. It decomposes in strong acid (pH <2) or alkaline solutions and may be damaged to a certain extent by heat. Higher plants and animals cannot produce vitamin B12. All vitamin B12 in nature is synthesized by microorganisms. Vitamin B12 is the only vitamin that requires the help of an intestinal secretion (intrinsic factor) to be absorbed. It participates in the production of bone marrow red blood cells, prevents pernicious anemia, and prevents damage to brain nerves.

[0029] Glutathione is a tripeptide containing a γ-amide bond and a sulfhydryl group. It is composed of glutamic acid, cysteine ​​and glycine and is present in almost every cell of the body. Glutathione can help maintain normal immune system function and has antioxidant and integrated detoxification effects. The sulfhydryl group on cysteine ​​is its active group (so it is often abbreviated as G-SH), which is easy to combine with certain drugs, toxins, etc., giving it an integrated detoxification effect. Glutathione can be used not only in medicine, but also as a base material for functional foods. It is widely used in functional foods such as anti-aging, enhancing immunity, and anti-tumor. Glutathione has two forms: reduced (G-SH) and oxidized (GSSG). Under physiological conditions, reduced glutathione accounts for the vast majority. Glutathione reductase can catalyze the interconversion between the two forms. The coenzyme of this enzyme can also provide NADPH for pentose phosphate bypass metabolism.

[0030] Anthocyanidins, also known as flower pigments, are a type of water-soluble natural pigments that are widely present in plants in nature. They are colored aglycones obtained by the hydrolysis of anthocyanins. Most of the main coloring substances in fruits, vegetables, and flowers are related to them. Under different pH conditions in the vacuoles of plant cells, anthocyanidins make the petals appear colorful. There are more than 20 known anthocyanidins, and 6 of them are important in food, namely geranium pigment, cornflower pigment, delphinium pigment, peony pigment, morning glory pigment and mallow pigment. Anthocyanidins in their natural state exist in the form of glycosides, called anthocyanins, and there are very few free anthocyanidins. Anthocyanidins are mainly used for food coloring, and can also be used in dyes, medicines, cosmetics, etc.

[0031] Neuroacid, also known as shark acid, is an unsaturated fatty acid with 24 carbon atoms and 1 double bond that exists in nerve tissue and fish oil. It got its name because it was first discovered in shark brain. It is a component of cerebrosides and has a melting point of 42°C. Mainly derived from shark brain and shark oil, neuroacid is recognized by scientists from various countries as the world's first and only dual-action magical substance that can repair and clear damaged brain nerve pathways-nerve fibers, and promote the regeneration of nerve cells. Neuroacid is a core natural component of brain nerve fibers and nerve cells. The lack of neuroacid will cause brain diseases such as sequelae of cerebral stroke, Alzheimer's disease, cerebral palsy, brain atrophy, memory loss, insomnia and forgetfulness. Neuroacid is difficult for the human body to produce on its own and can only be supplemented by ingestion from outside the body.

[0032] Gangliosides are sphingolipids containing sialic acid. Klenk first discovered that they accumulate in the brains of children with diseases and are present in high concentrations in the gray matter of the brain. Therefore, this type of glycolipid was named gangliosides. There are more than 8 types of brain gangliosides whose sugar components are composed of hexose, amino sugars, and sialic acid.

[0033] Arginine, with a chemical formula of C6H14N4O2 and a molecular weight of 174.20, is an amino acid compound. It participates in the ornithine cycle in the human body, promoting the formation of urea. This allows ammonia produced in the body to be converted into non-toxic urea through the ornithine cycle and excreted in the urine, thereby reducing blood ammonia concentrations. Arginine has a high concentration of hydrogen ions, which helps correct the acid-base balance in hepatic encephalopathy. It is a basic amino acid along with histidine and lysine.

[0034] Tryptophan is one of the 22 standard amino acids and an essential amino acid that cannot be synthesized by the human body, requiring it to be obtained from food. Its standard genetic code encodes the codon UGG. Only the L-stereoisomer of tryptophan has a role in protein construction or enzymatic activity; the R-stereoisomer is occasionally found in naturally occurring peptides. A distinctive structural feature of tryptophan is its indole functional group. It is a precursor of serotonin (also known as 5-hydroxytryptamine), an important neurotransmitter. It also contributes to the synthesis of nicotinic acid.

[0035] Aspartic acid, also known as aspartic acid, is an α-amino acid. The L-isomer of aspartic acid is one of the 20 proteinogenic amino acids, the building blocks of proteins. Its codons are GAU and GAC. Like glutamic acid, it is an acidic amino acid and a non-essential amino acid in the human body. Aspartic acid is ubiquitous in biosynthesis. It is a precursor for the synthesis of amino acids such as lysine, threonine, isoleucine, and methionine, as well as purine and pyrimidine bases. It acts as a carrier of K+ and Mg2+ ions, transporting electrolytes to the myocardium, thereby improving myocardial contractility and reducing oxygen consumption. It has a protective effect on the myocardium during hypoxia caused by coronary circulatory disorders. It participates in the ornithine cycle, promoting the formation of urea from ammonia and carbon dioxide, reducing the levels of nitrogen and carbon dioxide in the blood, enhancing liver function, and alleviating fatigue.

[0036] Preparation Method: First-stage coating preparation: Mix arginine, tryptophan, and aspartic acid with starch, cut into 1 mm granules using a pelletizer, and do not coat. Second-stage coating preparation: Mix glutathione and oligoanthocyanidins with starch, pelletize, and coat with 300 g of polyacrylic acid resin No. 3. Third-stage coating preparation: Mix vitamin B12, vitamin C, vitamin E, nervonic acid, and gangliosides with starch, pelletize, and coat with 750 g of polyacrylic acid resin No. 3. Capsule assembly: The three-stage granules are sequentially loaded into slightly soluble corn capsule shells to form the final three-stage capsule.

[0037] The SOD and vitamin E in this product penetrate the blood-brain barrier to eliminate ROS in the brain; vitamin C is responsible for peripheral circulation; anthocyanins prolong antioxidant activity and repair cells damaged by oxidative stress. Neuroacid penetrates the blood-brain barrier to induce nerve fiber regeneration; gangliosides and vitamin B12 assist in repairing nerve membranes; and amino acids such as arginine provide nutritional support.

[0038] In other embodiments, huperzine A can be used to inhibit acetylcholine hydrolase, increase neurotransmitter concentrations, and improve cognitive function.

[0039] Through the synergistic effects of the above-mentioned multiple pathways, the drug can significantly alleviate symptoms such as memory loss and cognitive impairment in Alzheimer's patients, while preventing the disease in high-risk groups.

[0040] The present invention first uses SOD (superoxide dismutase) to enter the blood circulation to the whole body to eliminate ROS in the body, and then adds vitamin C and vitamin E. SOD and vitamin E can penetrate the blood-brain barrier (a natural screening mechanism of the brain for foreign substances). The removal of ROS in the brain is mainly carried out by SOD and vitamin E, and the extracranial circulation is mainly handed over to vitamin C (because its nature is water-soluble, it cannot pass through the blood-brain barrier in large quantities). However, vitamins will be oxidized while releasing their antioxidant effects, so anthocyanins will be added at this time. Anthocyanin stays in the blood for a long time and can pull vitamins back when they are oxidized, making them antioxidants. Because SOD is an enzyme, it is very easy to inactivate while being highly active. Anthocyanin can ensure that the activity of SOD will not be weakened in an acidic environment. At the same time, the antioxidant capacity of anthocyanin itself is 50 times that of vitamin C. It can be used not only as an auxiliary drug, but also as a main drug. Finally, catechins and glutathione are added to repair cells that have suffered oxidative stress due to ROS damage, thereby playing the role of "neutralizing toxins."

[0041] Neuroacid, gangliosides and vitamin B12 are added to repair nerve cells. Neuroacid can completely pass through the blood-brain barrier and directly act on nerve fibers to repair and clear them, regenerate damaged and detached protective sheaths, dissolve necrotic tissues that block the channels, and induce the self-growth and division of nerve fibers, so that the information generated by nerve cells and the external information can be smoothly transmitted through nerve fibers, achieving smooth instructions, thereby activating damaged, diseased and dormant nerve cells, reshaping the neural network, and restoring some or all of the patient's functions in language, memory, sensation, limbs, etc., to achieve complete recovery from brain diseases. Gangliosides and vitamin B12 mainly serve as auxiliary repairs to the nerve membrane. Finally, arginine, aspartic acid and tryptophan are added to supply nerve nutrition, making nerve repair faster.

[0042] Huperzine A is a drug that inhibits the activity of acetylcholine hydrolase. Acetylcholine is a neurotransmitter. When Alzheimer's disease strikes, the amount of this substance becomes scarce because the activity of acetylcholine hydrolase increases. The use of huperzine A can reduce the degree of hydrolysis of this neurotransmitter, thereby making the transmission of neural information unobstructed. There are also extensive experimental precedents in the scientific community.

[0043] A randomized study was conducted in the Department of Neurology at Liaohe Oilfield General Hospital, Liaoning Province. Patients were randomly assigned to a control group and an observation group, with 45 patients in each group. The control group received oral vitamin E, while the observation group received oral huperzine A. All patients were treated for 3 months. Pre- and post-treatment data were statistically analyzed. Results: The total effective rate in the observation group was significantly higher than that in the control group (P < 0.05). Before treatment, there was no statistically significant difference in the Mini-Mental State Examination (MMSE) and the Activity of Daily Living (ADL) scale between the two groups. After treatment, the MMSE and ADL scores in both groups were statistically significant compared with those before treatment (P < 0.05). After treatment, the MMSE and ADL scores in the observation group were statistically significant compared with those in the control group (P < 0.05). No statistically significant differences were observed in adverse reactions during treatment between the two groups. Conclusion: Huperzine A is clinically effective in treating patients with AD, effectively improving cognitive function and quality of life, and is highly safe.

[0044] The oligomeric proanthocyanidins in this invention can significantly scavenge ROS, and SOD has a significant ROS-scavenging effect at an active concentration of 800u / ml. Neuroacid and gangliosides can promote the proliferation and repair of nerve cells at specific concentrations, with the optimal safe concentrations of neuracid being 400ug / ml and gangliosides being 200ug / ml. Huperzine A significantly improves patients' cognitive function and quality of life by inhibiting acetylcholine hydrolase, with clinical trials demonstrating its effectiveness superior to traditional treatments.

[0045] The drug of the present invention can alleviate the symptoms of Alzheimer's patients to a certain extent. Elderly people who do not have Alzheimer's disease can also prevent Alzheimer's disease by blocking and protecting and repairing nerve cells in principle. It can also repair cells in the body that have been subjected to oxidative stress.

[0046] The above describes the basic principles and main features of the present invention. Those skilled in the art should understand that the present invention is not limited to the above embodiments. The above embodiments and descriptions only illustrate the principles of the present invention. Without departing from the spirit and scope of the present invention, the present invention may have various changes and improvements, which fall within the scope of the invention to be protected. The scope of protection of the invention is defined by the attached claims and their equivalents.

Claims

1. A drug for preventing and alleviating Alzheimer's disease, comprising a capsule-shaped drug body, characterized in that: The capsule-shaped drug body is provided with three types of coatings, which are the first coating, the second coating and the third coating from the outside to the inside; The first stage coating comprises the following raw materials according to weight ratio: arginine: 1500 g, tryptophan: 800 g, aspartic acid: 1200 g, starch 2000 g; The second coating stage includes the following raw materials according to weight ratio: 500 g of glutathione, 800,000 active units (U), 800 g of oligomeric anthocyanidins, and 1000 g of starch; The third coating stage includes the following raw materials according to weight ratio: 200 grams of vitamin B12, 200 grams of vitamin C, 200 grams of vitamin E, 1.04 grams of neuraminic acid, 0.52 grams of ganglioside, and 2000 grams of starch.

2. A method for preparing a drug for preventing and alleviating Alzheimer's disease, characterized in that: The following steps are involved: Step 1: Mix the raw materials for the first coating evenly and cut them into 1 mm small particles by a pelletizing machine without coating; Step 2: Mix the raw materials for the second coating evenly and cut them into 1 mm small particles using a pelletizing machine; Step 3: Mix the raw materials for the third coating evenly and cut them into 1 mm small particles using a pelletizing machine; Step 4, coating the small particles coated in the second stage; Step 5: coating the small particles in the third coating stage. Step six: pack the uncoated first-stage coated granules, the coated second-stage coated granules and the third-stage coated granules into a capsule shell to form a three-stage capsule.

3. The method for preparing a drug for preventing and alleviating Alzheimer's disease according to claim 2, characterized in that: In the step 4, 300 grams of polyacrylic acid resin No. 3 is used for coating.

4. The method for preparing a drug for preventing and alleviating Alzheimer's disease according to claim 2, characterized in that: In the step 5, 750 grams of polyacrylic acid resin No. 3 is used for coating.

5. The method for preparing a drug for preventing and alleviating Alzheimer's disease according to claim 2, characterized in that: The capsule shell is a slightly soluble corn plant capsule shell.