Moisture-proof Anti-caking α-lipoic acid

Abstract

A moisture-proof anti-caking α-lipoic acid and a preparation method therefor. The moisture-proof anti-caking α-lipoic acid comprises not less than 20% by weight of α-lipoic acid, and may also comprise other auxiliary materials. By means of auxiliary material selection and treatment with a formulation method on the α-lipoic acid raw material, the problem of α-lipoic acid easily caking is solved, thereby improving the stability of the α-lipoic acid, meeting the requirement for high content, and facilitating transportation, storage and application scenarios.

Description

Moisture-proof and anti-caking alpha-lipoic acid Technical Field

[0001] The invention belongs to the technical field of dietary supplement preparations, and particularly relates to moisture-proof and anti-caking alpha-lipoic acid and a preparation method thereof. Background Art

[0002] α-lipoic acid (alpha lipoic acid) is a coenzyme present in the mitochondria, similar to vitamins, which can eliminate free radicals that accelerate aging and cause disease. After being absorbed through the intestines, lipoic acid enters the cells in the body and has both fat-soluble and water-soluble properties. As a coenzyme, α-lipoic acid plays a role in two key oxidative decarboxylation reactions, namely, in the pyruvate dehydrogenase complex and the α-ketoglutarate dehydrogenase complex, catalyzing the production and transfer of acyl groups. α-lipoic acid can accept the acyl group and the acetyl group of pyruvate to form a thioester bond, and then transfer the acetyl group to the sulfur atom of the coenzyme A molecule. The dihydrolipoamide that forms the cofactor can then be catalyzed by dihydrolipoamide dehydrogenase (which requires NAD + ) is oxidized to form oxidized lipoamide. Alpha-lipoic acid contains a five-membered disulfide ring structure with a high electron density, significant electrophilicity, and the ability to react with free radicals. This gives it antioxidant properties and significant health benefits and medicinal value (such as combating fatty liver disease and lowering plasma cholesterol). Furthermore, the sulfhydryl group of alpha-lipoic acid readily undergoes redox reactions, protecting sulfhydryl enzymes from heavy metal ion toxicity. Alpha-lipoic acid is widely distributed in nature, with liver and yeast cells being particularly abundant. In food, alpha-lipoic acid is often found alongside vitamin B1. It also has benefits such as fatigue relief and improvement in dementia. Therefore, alpha-lipoic acid holds significant research value in the healthcare field.

[0003] The molecular formula of α-lipoic acid is C8H 14 O2S2, with a relative molecular mass of 206.3, is slightly soluble in water and readily soluble in ethanol. However, it often absorbs moisture and hardens during transportation, storage, and application, causing numerous inconveniences. Therefore, there is an urgent need to develop a moisture-resistant, anti-caking α-lipoic acid product to address these issues. Such a product would have a very broad market prospect.

[0004] Summary of the Invention

[0005] In order to solve the above problems, the present invention provides a moisture-proof and anti-caking α-lipoic acid and a preparation method thereof. By selecting auxiliary materials and processing the α-lipoic acid raw material with a preparation method, the α-lipoic acid raw material solves its own characteristic of being easily hygroscopic and hardening, improves the stability of the α-lipoic acid, and at the same time meets the demand for high content, brings great convenience to transportation, storage and application scenarios, and brings extremely high applicability to users; in addition, the preparation process is simple and the production cost is low.

[0006] In one aspect, the present invention provides a moisture-proof and anti-caking α-lipoic acid, which contains not less than 20% by weight of α-lipoic acid.

[0007] In some embodiments, the moisture resistant, caking alpha-lipoic acid comprises no less than 25%, 30%, 35%, 40%, 45%, 50%, 55%, 60% alpha-lipoic acid by weight. In some embodiments, the moisture resistant, caking alpha-lipoic acid comprises no less than 61%, 62%, 63%, 64%, 65%, 66%, 67%, 68%, 69%, 70%, 71%, 72%, 73%, 74%, 75%, 76%, 77%, 78%, 79%, 80%, 85%, 90%, 95%, 97%, 99% alpha-lipoic acid by weight.

[0008] In some embodiments, the moisture-resistant, anti-caking alpha-lipoic acid comprises 10-99%, 15-98%, 20-97%, 25-96%, 30-95%, 35-94%, 40-93%, 45-92%, 50-90% alpha-lipoic acid by weight. In some embodiments, the moisture-resistant, anti-caking alpha-lipoic acid comprises 20-99%, 21-98%, 22-97%, 25-96%, 28-95%, 30-95%, 35-92%, 40-90% alpha-lipoic acid by weight.

[0009] In some embodiments, the moisture-proof and anti-caking alpha-lipoic acid comprises 40-98% by weight of alpha-lipoic acid; 1-40% of one or more excipients selected from microcrystalline cellulose, compressible starch, lactose or mannitol; and 1-10% of one or more excipients selected from silicon dioxide, magnesium stearate, calcium hydrogen phosphate, calcium silicate, and micropowdered silica gel.

[0010] In some embodiments, the moisture-proof and anti-caking α-lipoic acid comprises, by weight, 50-95% α-lipoic acid; 2-40% one or more excipients selected from microcrystalline cellulose and mannitol; and 2-8% silicon dioxide.

[0011] In some embodiments, the moisture-proof and anti-caking alpha-lipoic acid comprises, by weight, 60-90% alpha-lipoic acid; 2-33% of one or more excipients selected from microcrystalline cellulose and mannitol; and 2-5% silicon dioxide. In some embodiments, the moisture-proof and anti-caking alpha-lipoic acid comprises, by weight, 60-90% alpha-lipoic acid; 7-33% of one or more excipients selected from microcrystalline cellulose and mannitol; and 2-5% silicon dioxide.

[0012] In some embodiments, the moisture-proof and anti-caking α-lipoic acid further comprises 1-8% by weight of one or more excipients selected from the group consisting of hypromellose, maltodextrin, and gum arabic. In some embodiments, the moisture-proof and anti-caking α-lipoic acid further comprises 1-2% by weight of one or more excipients selected from the group consisting of hypromellose, maltodextrin, and gum arabic. In some embodiments, the moisture-proof and anti-caking α-lipoic acid further comprises 1-2% by weight of hypromellose. In some embodiments, the moisture-proof and anti-caking α-lipoic acid further comprises 1-3% by weight of ethyl cellulose.

[0013] In some embodiments, the moisture-resistant and caking-resistant alpha-lipoic acid is in granular or powdered form.

[0014] In some embodiments, the particle size of the moisture-resistant and anti-caking alpha-lipoic acid is 10-100 mesh. In some embodiments, the particle size of the moisture-resistant and anti-caking alpha-lipoic acid is 20-80 mesh.

[0015] In some embodiments, the moisture-resistant and caking-resistant alpha-lipoic acid is formulated into a nutritional supplement, food, beverage, or animal feed.

[0016] In some embodiments, the moisture-resistant and anti-caking α-lipoic acid is prepared as a solid formulation or a liquid formulation.

[0017] On the other hand, the present invention provides a method for preparing moisture-proof and anti-caking α-lipoic acid, which comprises mixing the following components according to the formula amount: α-lipoic acid, one or more auxiliary materials selected from microcrystalline cellulose, compressible starch, lactose or mannitol, and one or more auxiliary materials selected from silicon dioxide, magnesium stearate, calcium hydrogen phosphate, calcium silicate, and micropowder silica gel; granulating; and obtaining moisture-proof and anti-caking α-lipoic acid.

[0018] In some embodiments, the moisture-proof and anti-caking alpha-lipoic acid comprises, by weight, 60-90% alpha-lipoic acid; 2-33% of one or more excipients selected from microcrystalline cellulose and mannitol; and 2-5% silicon dioxide. In some embodiments, the moisture-proof and anti-caking alpha-lipoic acid comprises, by weight, 60-90% alpha-lipoic acid; 7-33% of one or more excipients selected from microcrystalline cellulose and mannitol; and 2-5% silicon dioxide.

[0019] In some embodiments, mixing further comprises mixing a formulated amount of one or more excipients selected from the group consisting of hypromellose, maltodextrin, and gum arabic. In some embodiments, mixing further comprises mixing a formulated amount of hypromellose. In some embodiments, mixing further comprises mixing a formulated amount of ethyl cellulose.

[0020] In some embodiments, the moisture-proof and anti-caking α-lipoic acid comprises 1-8% by weight of one or more excipients selected from the group consisting of hypromellose, maltodextrin, and gum arabic. In some embodiments, the moisture-proof and anti-caking α-lipoic acid comprises 1-2% by weight of one or more excipients selected from the group consisting of hypromellose, maltodextrin, and gum arabic. In some embodiments, the moisture-proof and anti-caking α-lipoic acid comprises 1-2% by weight of hypromellose. In some embodiments, the moisture-proof and anti-caking α-lipoic acid comprises 1-3% by weight of ethylcellulose.

[0021] In some embodiments, the granulation is dry granulation.

[0022] In some embodiments, the moisture-resistant and anti-caking α-lipoic acid prepared by the method is used to prepare food, beverages, nutritional products, skin care products, or cosmetics.

[0023] This Summary is provided to introduce a selection of concepts in a simplified form that are further described below in the Detailed Description. This Summary is not intended to identify key features or essential features of the claimed subject matter, nor is it intended to be used to limit the scope of the claimed subject matter. DETAILED DESCRIPTION

[0024] The preferred embodiments of the present invention will now be described in detail with reference to the embodiments thereof. Although the present invention will be described in conjunction with the preferred embodiments, it should be understood that they are not intended to limit the present invention to these embodiments. On the contrary, the present invention is intended to cover substitutions, modifications and equivalents, which may be included within the spirit and scope of the present invention as defined in the claims.

[0025] As used herein, the term "or" is intended to include "and" and "or." In other words, the term "or" can also be replaced with "and / or."

[0026] As used herein, the singular forms "a," "an," and "the" are intended to include the plural forms as well, unless the context clearly indicates otherwise.

[0027] As used herein, the term "comprises" or "includes" or variations thereof refers to instances where the term is used in its non-limiting sense, meaning that items following the term are included, but items not specifically mentioned are not excluded. It also includes the more restrictive verbs 'consisting essentially of' and 'consisting of.'

[0028] Example

[0029] In the present invention, unless otherwise specified, the scientific and technical terms used herein have the meanings commonly understood by those skilled in the art. In addition, the laboratory procedures used herein are all conventional procedures widely used in the relevant fields.

[0030] Unless otherwise specified, the raw materials and reagents used in the present invention are commercially available. All reagents are of commercial grade and used according to the standards received.

[0031] The following examples are illustrative of selected embodiments of the present invention and are not intended to limit the scope of the invention.

[0032] Example 1: Preparation of moisture-proof and anti-caking α-lipoic acid

[0033] A moisture-proof and anti-caking alpha-lipoic acid comprises the following components in percentage by weight:

[0034] Alpha-lipoic acid 80%

[0035] Microcrystalline cellulose 15%

[0036] Silicon dioxide 5%.

[0037] Pass α-lipoic acid through a 30-mesh sieve, weigh the prescribed amount of α-lipoic acid, microcrystalline cellulose, and silicon dioxide, put them into a three-dimensional mixer, and use a dry granulator to granulate to obtain moisture-proof and anti-caking α-lipoic acid.

[0038] Example 2: Preparation of moisture-proof and anti-caking α-lipoic acid

[0039] A moisture-proof and anti-caking alpha-lipoic acid comprises the following components in percentage by weight:

[0040] Pass α-lipoic acid and mannitol through a 30-mesh sieve, weigh the prescribed amount of α-lipoic acid, mannitol, microcrystalline cellulose and silicon dioxide, put them into a three-dimensional mixer, and use a dry granulator to granulate to obtain moisture-proof and anti-caking α-lipoic acid.

[0041] Example 3: Preparation of moisture-proof and anti-caking α-lipoic acid

[0042] A moisture-proof and anti-caking alpha-lipoic acid comprises the following components in percentage by weight:

[0043] Pass α-lipoic acid and mannitol through a 30-mesh sieve, weigh the prescribed amount of α-lipoic acid, mannitol, microcrystalline cellulose, hypromellose and silicon dioxide, put them into a three-dimensional mixer, and use a dry granulator to granulate to obtain moisture-proof and anti-caking α-lipoic acid.

[0044] Example 4: Preparation of moisture-proof and anti-caking α-lipoic acid

[0045] A moisture-proof and anti-caking alpha-lipoic acid comprises the following components in percentage by weight:

[0046] Pass α-lipoic acid and mannitol through a 30-mesh sieve, weigh the prescribed amount of α-lipoic acid, mannitol, microcrystalline cellulose, hypromellose and silicon dioxide, put them into a three-dimensional mixer, and use a dry granulator to granulate to obtain moisture-proof and anti-caking α-lipoic acid.

[0047] Example 5: Preparation of moisture-proof and anti-caking α-lipoic acid

[0048] A moisture-proof and anti-caking alpha-lipoic acid comprises the following components in percentage by weight:

[0049] Pass α-lipoic acid and mannitol through a 30-mesh sieve, weigh the prescribed amount of α-lipoic acid, mannitol, microcrystalline cellulose, hypromellose and silicon dioxide, put them into a three-dimensional mixer, and use a dry granulator to granulate to obtain moisture-proof and anti-caking α-lipoic acid.

[0050] Example 6: Preparation of moisture-proof and anti-caking α-lipoic acid

[0051] A moisture-proof and anti-caking alpha-lipoic acid comprises the following components in percentage by weight:

[0052] Pass α-lipoic acid and mannitol through a 30-mesh sieve, weigh the prescribed amount of α-lipoic acid, mannitol, microcrystalline cellulose, hypromellose and silicon dioxide, put them into a three-dimensional mixer, and use a dry granulator to granulate to obtain moisture-proof and anti-caking α-lipoic acid.

[0053] Example 7: Moisture-proof and anti-caking of α-lipoic acid samples

[0054] The specific test method is as follows: Take a dry glass bottle (outer diameter 50mm, height 100mm), weigh an appropriate amount of the test sample and place it in the open box at a temperature of 40℃±2℃ and a relative humidity of 75%±5%. Take out the glass bottle at regular intervals (respectively at 0.5h, 1h, 1.5h, 2h, 3h, 5h, and 7h) and test the pass rate through a 24-mesh sieve. According to the calculation formula: The percentage of weight gain was calculated. The properties and test results of the moisture-proof and anti-caking α-lipoic acid sample are shown in Table 1.

[0055] Table 1

[0056] As can be seen from Table 1, compared with the raw materials, the moisture-proof and anti-caking α-lipoic acid samples of each embodiment of the present invention are at a temperature of 40 ° C ± 2 ° C, a relative humidity of 75% ± 5%, and while having a high load of not less than 60%, the performance of its moisture-proof and anti-caking is significantly improved. Some embodiment samples are particularly excellent, and have excellent moisture-proof and anti-caking effects and good stability under the temperature and humidity conditions of the accelerated experiment. For example, Example 4 sample is mixed with auxiliary materials such as mannitol and microcrystalline cellulose for dry granulation. While the load is as high as 80%, the pass rate after being placed for 7 hours at a temperature of 40 ° C ± 2 ° C and a relative humidity of 75% ± 5% remains at nearly 90%, with excellent stability and fluidity, and has excellent moisture-proof and anti-caking effects. After lofting, the moisture-proof and anti-caking α-lipoic acid sample of the present invention looks obviously not easy to absorb moisture and form a compaction, and both fluidity and stability are significantly improved.

[0057] The moisture-proof and anti-caking alpha-lipoic acid of the present invention can achieve more obvious moisture-proof and anti-caking effects, fluidity and stability than the raw material under the conditions of a temperature of 40°C±2°C, a relative humidity of 75%±5% and storage at room temperature when the alpha-lipoic acid contains not less than 20%, 25%, 30%, 35%, 40%, 45%, 50%, 55%, 60%, 61%, 62%, 63%, 64%, 65%, 66%, 67%, 68%, 69%, 70%, 71%, 72%, 73%, 74%, 75%, 76%, 77%, 78%, 79%, 80%, 85%, 90%, 95%, 97% or 99% by weight of the alpha-lipoic acid, or contains 10-99%, 15-98%, 20-97%, 25-96%, 30-95%, 35-94%, 40-93%, 45-92% or 50-90% by weight of the alpha-lipoic acid.

[0058] Although specific embodiments and examples of the present invention have been described herein, it will be understood by those skilled in the art that any modifications and variations may be made without departing from the principles of the present invention. The above examples and descriptions do not limit the scope of the present invention. Any combination of the embodiments of the present invention, as well as any obvious extensions or analogs thereof, are within the scope of the present invention. Furthermore, the present invention encompasses any arrangement intended to achieve the same purpose, as well as all such variations and modifications that fall within the scope of the appended claims.

Claims

1. A moisture-proof and anti-caking alpha-lipoic acid, characterized in that: Contains not less than 20% by weight of alpha-lipoic acid.

2. The moisture-proof and anti-caking alpha-lipoic acid according to claim 1, characterized in that Containing not less than 25%, 30%, 35%, 40%, 45%, 50%, 55%, 60% by weight of alpha-lipoic acid.

3. The moisture-proof and anti-caking alpha-lipoic acid according to claim 1 or 2, characterized in that: The invention comprises 40-98% by weight of alpha-lipoic acid; 1-40% of one or more auxiliary materials selected from microcrystalline cellulose, compressible starch, lactose or mannitol; and 1-10% of one or more auxiliary materials selected from silicon dioxide, magnesium stearate, calcium hydrogen phosphate, calcium silicate and micro powder silica gel.

4. The moisture-proof and anti-caking alpha-lipoic acid according to any one of claims 1 to 3, characterized in that The invention comprises 50-95% by weight of alpha-lipoic acid; 2-40% of one or more auxiliary materials selected from microcrystalline cellulose and mannitol; and 2-8% of silicon dioxide.

5. The moisture-proof and anti-caking alpha-lipoic acid according to any one of claims 1 to 4, characterized in that The invention comprises 60-90% by weight of alpha-lipoic acid, 2-33% of one or more auxiliary materials selected from microcrystalline cellulose and mannitol, and 2-5% of silicon dioxide.

6. The moisture-proof and anti-caking alpha-lipoic acid according to any one of claims 3 to 5, characterized in that The invention also contains 1-2% by weight of one or more auxiliary materials selected from the group consisting of hydroxypropyl methylcellulose, maltodextrin and gum arabic.

7. The moisture-proof and anti-caking alpha-lipoic acid according to any one of claims 1 to 6, characterized in that The moisture-proof and anti-caking alpha-lipoic acid is in the form of granules or powder.

8. The moisture-proof and anti-caking alpha-lipoic acid according to claim 7, characterized in that: The particle size of the moisture-proof and anti-caking alpha-lipoic acid is 10-100 meshes.

9. The moisture-proof and anti-caking alpha-lipoic acid according to any one of claims 1 to 8, characterized in that The moisture-proof and anti-caking alpha-lipoic acid is formulated into a nutritional supplement, food, beverage or animal feed.

10. The moisture-proof and anti-caking alpha-lipoic acid according to any one of claims 1 to 9, characterized in that The moisture-proof and anti-caking alpha-lipoic acid is prepared as a solid preparation or a liquid preparation.

11. A method for preparing moisture-proof and anti-caking alpha-lipoic acid, characterized in that: The method comprises mixing the following components according to the formula amount: alpha-lipoic acid, one or more auxiliary materials selected from microcrystalline cellulose, compressible starch, lactose or mannitol, and one or more auxiliary materials selected from silicon dioxide, magnesium stearate, calcium hydrogen phosphate, calcium silicate, and micro-powder silica gel; granulating; and obtaining the moisture-proof and anti-caking alpha-lipoic acid.

12. The method according to claim 11, characterized in that The moisture-proof and anti-caking alpha-lipoic acid comprises, by weight, 60-90% of alpha-lipoic acid; 2-33% of one or more auxiliary materials selected from microcrystalline cellulose and mannitol; and 2-5% of silicon dioxide.

13. The method according to claim 11 or 12, characterized in that: The mixing further comprises mixing a formula amount of one or more auxiliary materials selected from hydroxypropyl methylcellulose, maltodextrin, and gum arabic.

14. The method according to claim 13, characterized in that The moisture-proof and anti-caking alpha-lipoic acid contains 1-2% by weight of one or more auxiliary materials selected from hydroxypropyl methylcellulose, maltodextrin and gum arabic.

15. The method according to any one of claims 11 to 14, characterized in that The granulation is dry granulation.

16. The method according to any one of claims 11 to 15, characterized in that The moisture-proof and anti-caking alpha-lipoic acid prepared by the method is used for preparing food, beverage, nutrition product, skin care product or cosmetic.

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