Gamma-aminobutyric acid composition as well as preparation method and application thereof

Abstract

The invention provides a gamma-aminobutyric acid composition as well as a preparation method and application thereof. The gamma-aminobutyric acid composition is prepared from the following components in parts by mass: 5 to 10 parts of microcrystalline cellulose, 3 to 5 parts of gamma-aminobutyric acid, 1 to 2 parts of L-theanine, 0.05 to 0.1 part of vitamin, 2 to 5 parts of maltodextrin, 5 to 8 parts of modified adhesive and 0.1 to 5 parts of additive. The modified adhesive is a product obtained by reacting carboxymethyl cellulose with polyethylene glycol. The modified adhesive is prepared through green reaction to serve as a component, not only has good cohesiveness of carboxymethyl cellulose, but also has excellent water solubility and stability of polyethylene glycol, has a good bonding effect on a composition preparation, and has better affinity among the components, so that the stability of the composition is improved, and the service life of the composition is prolonged. The product is endowed with a longer storage life, the release and absorption of active ingredients are facilitated, and the stable exertion of the effects of soothing the nerves and helping sleep is guaranteed.

Description

Technical Field

[0001] This invention relates to the field of health product technology, and in particular to a γ-aminobutyric acid composition, its preparation method, and its application. Background Technology

[0002] The fast pace of modern life has led to an increasing prevalence of sleep disorders such as insomnia. Sleep aid formulas centered around gamma-aminobutyric acid (GABA) and vitamin B6 have become a mainstream research focus due to their safety and lack of dependence. GABA, as a central inhibitory neurotransmitter, can calm and promote sleep, while vitamin B6, as a coenzyme for its synthesis, can participate in the metabolism of neurotransmitters in the human body. The combination of the two can achieve a synergistic sleep-aiding effect.

[0003] In sleep-aid formulations, besides the core active ingredient, the selection of excipients is crucial. For example, binders significantly affect the formulation's molding effect, stability, solubility, and the release efficiency of the active ingredient. Currently, commonly used binders in health supplements and pharmaceutical tablets include carboxymethyl cellulose, starch, and hydroxypropyl methylcellulose. However, these traditional binders generally have many drawbacks: carboxymethyl cellulose dissolves slowly in water and easily forms aggregates, resulting in slow disintegration after formulation, making it difficult for the active ingredient to be quickly released and absorbed by the body, thus affecting the timely exertion of sleep-aiding effects; starch not only has solubility issues but also easily absorbs moisture and has insufficient bonding strength; hydroxypropyl methylcellulose has the problems of high cost and unsatisfactory binding effect.

[0004] Therefore, conventional adhesives have problems such as insufficient stability, and are easily affected by environmental factors such as temperature and humidity during storage, which can lead to cracking, deformation, and deterioration of the formulation, thus reducing the storage stability of the product.

[0005] Therefore, it is necessary to provide a new technical solution to overcome the defects existing in the prior art. Summary of the Invention

[0006] Based on this, the present invention provides a γ-aminobutyric acid composition, which uses a modified adhesive prepared by a green reaction as a component. This adhesive not only has the good adhesive properties of carboxymethyl cellulose, but also the excellent water solubility and stability of polyethylene glycol. It has a good adhesive effect on the composition formulation and better affinity between components, thereby improving the stability of the composition, giving the product a longer shelf life, and helping the release and absorption of active ingredients, ensuring the stable performance of the calming and sleep-aiding effects.

[0007] One object of the present invention is to provide a γ-aminobutyric acid composition comprising the following components in parts by weight: 5-10 parts of microcrystalline cellulose 3-5 parts of γ-aminobutyric acid L-theanine 1-2 parts Vitamins 0.05-0.1 servings 2-5 parts maltodextrin 5-8 parts of modified adhesive Additives: 0.1-5 parts; The modified adhesive is a product of the reaction between carboxymethyl cellulose and polyethylene glycol.

[0008] Furthermore, the vitamins include vitamin B6.

[0009] Furthermore, the additives are selected from one or more of the following: flavorings, colorings, sweeteners, dispersants, lubricants, and disintegrants.

[0010] Another object of the present invention is to provide a method for preparing the above-mentioned γ-aminobutyric acid composition, the method comprising the following steps: S1. Carboxymethyl cellulose, polyethylene glycol and catalyst are mixed and heated to react, resulting in a modified adhesive; S2. Mix the modified adhesive and other components evenly, sieve, and compress into tablets to obtain a γ-aminobutyric acid composition.

[0011] Furthermore, the catalyst includes phytic acid.

[0012] Furthermore, the mass ratio of carboxymethyl cellulose to polyethylene glycol is 1:(0.5-3).

[0013] Furthermore, the heating reaction is carried out at a temperature of 50-100°C for a duration of 4-8 hours.

[0014] Another object of the present invention is to provide the application of the above-described γ-aminobutyric acid composition in medicine.

[0015] Another object of the present invention is to provide the application of the above-described γ-aminobutyric acid composition in health products.

[0016] The present invention has the following beneficial effects: This invention discloses a γ-aminobutyric acid (GABA) composition, using GABA, L-theanine, vitamin B6, and other substances as functional components. Through the synergistic effect of multiple active substances, it alleviates anxiety, improves mood, calms the nerves, soothes, and promotes sleep. Simultaneously, this invention also prepares a modified binder using a green process. Using non-toxic and safe phytic acid as a catalyst, a network-like modified binder is obtained through esterification of carboxymethyl cellulose and polyethylene glycol. This binder possesses the adhesive properties of carboxymethyl cellulose, and the branched structure of this component, along with the introduced hydroxyl, ether, and ester groups, can form intermolecular forces, thereby improving the binding effect between different components, giving the composition better stability, and reducing deterioration during storage. Furthermore, the modified binder also provides better water solubility, promoting disintegration and preventing the components from agglomerating upon contact with water, which is beneficial for improving the release rate of the product during administration. Moreover, the modified binder has good affinity with microcrystalline cellulose and active substances, improving the drug-carrying matrix and further optimizing the stability and release effect of the tablet. Detailed Implementation

[0017] To more clearly illustrate the technical solution of the present invention, the following embodiments are provided. Unless otherwise stated, the raw materials, reactions, and post-processing methods appearing in the embodiments are all commercially available raw materials and technical methods well known to those skilled in the art.

[0018] The terms "preferred," "more preferably," and "more suitable" used in this invention refer to embodiments of the invention that provide certain beneficial effects under certain circumstances. However, other embodiments may also be preferred under the same or other circumstances. Furthermore, the description of one or more preferred embodiments does not imply that other embodiments are unavailable, nor is it intended to exclude other embodiments from the scope of this invention.

[0019] It should be understood that, except in any operational instance or otherwise indicated, all figures representing the amounts of ingredients used, for example, in the specification and claims, should be understood to be modified in all cases by the term "about". Therefore, unless otherwise stated, the numerical parameters set forth in the following specification and appended claims are approximations varying with the desired performance to be obtained according to the invention.

[0020] Unless otherwise specified, the raw materials used in the embodiments of this invention are all food-grade, pharmaceutical-grade, or chemically pure.

[0021] In the embodiments and comparative examples of this invention, the carboxymethyl cellulose underwent acidification pretreatment, including the following steps: Sodium carboxymethyl cellulose (Lihong FVH9) was added to an acetic acid solution (concentration 20 wt / %) at a ratio of 0.1 g / mL, stirred at 40℃ for 4 h, filtered, washed, and dried to obtain the product.

[0022] The disintegrant in this embodiment of the invention is crospovidone (Ashland XL-10).

[0023] The lubricant used in this embodiment of the invention is magnesium stearate. Example 1

[0024] A γ-aminobutyric acid composition comprising the following components in parts by weight: 5 parts microcrystalline cellulose 3 parts of γ-aminobutyric acid 1 part L-theanine Vitamin B6 0.05 parts 2 parts maltodextrin 5 parts of modified adhesive 0.2 parts disintegrant 0.3 parts lubricant; The preparation method of the γ-aminobutyric acid composition includes the following steps: S1. Carboxymethyl cellulose, PEG-400 and phytic acid were mixed in a mass ratio of 1:8:0.05, stirred at 85°C for 8 h, and the modified adhesive was obtained after centrifugation, washing and drying. S2. According to the above-mentioned mass proportions, the modified adhesive and other components except the lubricant are mixed and stirred evenly, rolled and crushed through a 20-mesh sieve, and finally the lubricant is added and compressed into tablets (0.5 g / tablet) to obtain the γ-aminobutyric acid composition. Example 2

[0025] A γ-aminobutyric acid composition comprising the following components in parts by weight: 7 parts microcrystalline cellulose 4 parts of γ-aminobutyric acid 1.3 parts L-theanine Vitamin B6 0.07 parts 2.6 parts maltodextrin 7 parts modified adhesive 0.25 parts disintegrant 0.4 parts lubricant; The preparation method of the γ-aminobutyric acid composition includes the following steps: S1. Carboxymethyl cellulose, PEG-400 and phytic acid were mixed in a mass ratio of 1:8:0.05, stirred at 85°C for 8 h, and the modified adhesive was obtained after centrifugation, washing and drying. S2. According to the above-mentioned mass proportions, the modified adhesive and other components except the lubricant are mixed and stirred evenly, rolled and crushed through a 20-mesh sieve, and finally the lubricant is added and compressed into tablets (0.5 g / tablet) to obtain the γ-aminobutyric acid composition. Example 3

[0026] A γ-aminobutyric acid composition comprising the following components in parts by weight: 9 parts microcrystalline cellulose 5 parts of γ-aminobutyric acid 1.8 parts L-theanine Vitamin B6 0.09 parts 3.5 parts maltodextrin 9 parts of modified adhesive 0.3 parts disintegrant 0.5 parts lubricant; The preparation method of the γ-aminobutyric acid composition includes the following steps: S1. Carboxymethyl cellulose, PEG-400 and phytic acid were mixed in a mass ratio of 1:8:0.05, stirred at 85°C for 8 h, and the modified adhesive was obtained after centrifugation, washing and drying. S2. According to the above-mentioned mass proportions, the modified adhesive and other components except the lubricant are mixed and stirred evenly, rolled and crushed through a 20-mesh sieve, and finally the lubricant is added and compressed into tablets (0.5 g / tablet) to obtain the γ-aminobutyric acid composition.

[0027] Comparative Example 1 The difference between this comparative example and Example 1 is that step S1 is replaced by mixing carboxymethyl cellulose and PEG-400 in a mass ratio of 1:2 and stirring evenly to obtain a modified adhesive. Other components and preparation methods are the same as in Example 1.

[0028] Comparative Example 2 The difference between this comparative example and Example 1 is that step S1 is deleted, and the modified carboxymethyl cellulose is replaced with an equal mass of carboxymethyl cellulose. The other components and preparation methods are the same as in Example 1.

[0029] Test Example 1 Stability testing.

[0030] Test method: Place the sample at 30℃ and 25% humidity for 15 days and check its appearance after placement to see if there are any cracks, deformations, discoloration, or other phenomena.

[0031] The test results are shown in Table 1.

[0032] Table 1 Stability Test Results

[0033] As can be seen from Table 1, the samples prepared in the examples have good stability. However, in Comparative Example 1, the modified adhesive was replaced with a physical mixture of polyethylene glycol and carboxymethyl cellulose, which could not obtain a stable cross-linked network structure and had strong hygroscopicity and poor stability. Comparative Example 2 did not modify carboxymethyl cellulose and also lacked a branched network structure, resulting in reduced stability.

[0034] Test Example 2 Solubility and sleep-aiding effects were tested.

[0035] Test method: Solubility test: The test was conducted according to the disintegration time test method in the Chinese Pharmacopoeia.

[0036] Sleep aid effect test: 20 volunteers aged 20-30 years were recruited. They took 0.5 g of the γ-aminobutyric acid composition prepared in Example 1 one hour before bedtime for 15 days. Before and after the test, the subjects were asked to score according to the Pittsburgh Sleep Quality Index (PSQI) (the total score range was 0-21, with higher scores indicating poorer sleep quality). The average score before the test and the average score after the test were calculated.

[0037] The test results are shown in Table 2.

[0038] Table 2 Performance Test Results

[0039] As shown in Table 2, the γ-aminobutyric acid composition of the present invention exhibits good solubility. The disintegration effect is enhanced synergistically by modified binders and disintegrants. In contrast, Comparative Example 1 uses a physical mixture of CMC and PEG as a binder, which makes it difficult to form a network hydrophilic structure, resulting in insufficient structural uniformity and affecting solubility. Comparative Example 2, lacking the introduction of polyethylene glycol, further reduces the dissolution rate. The sleep-aiding effect test results show that the composition of Example 1 of the present invention, after continuous use, significantly improves sleep quality and significantly reduces the PSQI score, demonstrating that the γ-aminobutyric acid composition of the present invention has good application prospects in the fields of health products and pharmaceuticals for calming the nerves and aiding sleep.

[0040] It will be apparent to those skilled in the art that the present invention is not limited to the details of the exemplary embodiments described above, and that the invention can be implemented in other specific forms without departing from the spirit or essential characteristics of the invention. Therefore, the embodiments should be considered in all respects as exemplary and non-limiting, and the scope of the invention is defined by the appended claims rather than the foregoing description. Thus, it is intended that all variations falling within the meaning and scope of equivalents of the claims be included within the present invention.

[0041] Furthermore, it should be understood that although this specification describes embodiments, not every embodiment contains only one independent technical solution. This narrative style is merely for clarity. Those skilled in the art should consider the specification as a whole, and the technical solutions in each embodiment can also be appropriately combined to form other embodiments that can be understood by those skilled in the art.

Claims

1. A γ-aminobutyric acid composition, characterized in that, The γ-aminobutyric acid composition comprises the following components in parts by weight: 5-10 parts of microcrystalline cellulose 3-5 parts of γ-aminobutyric acid L-theanine 1-2 parts Vitamins 0.05-0.1 servings 2-5 parts maltodextrin 5-8 parts of modified adhesive Additives: 0.1-5 parts; The modified adhesive is a product of the reaction between carboxymethyl cellulose and polyethylene glycol.

2. The γ-aminobutyric acid composition according to claim 1, characterized in that, The vitamins mentioned include vitamin B6.

3. The γ-aminobutyric acid composition according to claim 1, characterized in that, The additives are selected from one or more of the following: flavorings, colorings, sweeteners, dispersants, lubricants, and disintegrants.

4. A method for preparing the γ-aminobutyric acid composition according to any one of claims 1-3, characterized in that, The preparation method of the γ-aminobutyric acid composition includes the following steps: S1. Carboxymethyl cellulose, polyethylene glycol and catalyst are mixed and heated to react, resulting in a modified adhesive; S2. Mix the modified adhesive and other components evenly, sieve, and compress into tablets to obtain a γ-aminobutyric acid composition.

5. The method for preparing the γ-aminobutyric acid composition according to claim 4, characterized in that, The catalyst includes phytic acid.

6. The method for preparing the γ-aminobutyric acid composition according to claim 4, characterized in that, The mass ratio of carboxymethyl cellulose to polyethylene glycol is 1:(0.5-3).

7. The method for preparing the γ-aminobutyric acid composition according to claim 4, characterized in that, The heating reaction is carried out at a temperature of 50-100℃ for 4-8 hours.

8. The use of the γ-aminobutyric acid composition according to any one of claims 1-3 in medicine.

9. The use of the γ-aminobutyric acid composition according to any one of claims 1-3 in health products.

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