Moisture-proof acetyl-l-carnitine

Abstract

A moisture-proof acetyl-L-carnitine, comprising not less than 10% of acetyl-L-carnitine, or a hydrochloride thereof, or a mixture of both by weight. The preparation method comprises mixing the following components by prescription amount: acetyl-L-carnitine, or a hydrochloride thereof, or a mixture of both, one or more adjuvants selected from microcrystalline cellulose, compressible starch, lactose or mannitol, one or more adjuvants selected from silicon dioxide, magnesium stearate, calcium hydrogen phosphate, calcium silicate, and micro-powder silica gel; granulating; obtaining the moisture-proof acetyl-L-carnitine. The moisture-proof acetyl-L-carnitine is formulated into a nutritional supplement, a food, a beverage, or an animal feed.

Description

Moisture-proof acetyl-L-carnitine Technical Field

[0001] The invention belongs to the technical field of dietary supplement preparations, and particularly relates to moisture-proof acetyl-L-carnitine and a preparation method thereof. Background Art

[0002] Acetyl L-Carnitine is an ester of L-carnitine. It is a white powder that is soluble in water but insoluble in acetone. Acetyl L-Carnitine is a naturally occurring substance in the body, particularly abundant in muscle, brain, and sperm. It participates in a number of important metabolic processes in the human body and has beneficial effects on the brain and reproductive systems. Its primary physiological functions include lowering blood lipids, improving athletic performance, and promoting weight loss; protecting cells; preventing lactic acid accumulation; promoting energy utilization of carbohydrates and other substances; and increasing sperm count and motility.

[0003] However, acetyl-L-carnitine is very easy to absorb moisture, so it often causes moisture absorption and brings many inconveniences during transportation, storage and application. Therefore, it is urgent to develop a moisture-proof acetyl-L-carnitine product to solve the problems of its easy moisture absorption, and this product will have a very broad market prospect. Summary of the Invention

[0004] In order to solve the above problems, the present invention provides a moisture-proof acetyl-L-carnitine and a preparation method thereof. By selecting auxiliary materials and treating the raw materials of acetyl-L-carnitine with a preparation method, the strong hygroscopic deliquescence when exposed to the air is solved, and an excellent moisture-proof and deliquescence-resistant effect is achieved. The stability of acetyl-L-carnitine is improved, while meeting the demand for high content, bringing great convenience to transportation, storage and application scenarios, and bringing extremely high applicability to users. In addition, the preparation process of the present invention is simple and the production cost is low; no organic solvent is involved in the production process, which is environmentally friendly and has no risk of residual dissolution of the product.

[0005] In one aspect, the present invention provides a moisture-proof acetyl-L-carnitine comprising not less than 10% by weight of acetyl-L-carnitine, or its hydrochloride, or a mixture thereof.

[0006] In some embodiments, the moisture-proof acetyl-L-carnitine comprises not less than 15%, 20%, 25%, 30%, 35%, 40%, 45%, 50% by weight of acetyl-L-carnitine, or its hydrochloride salt, or a mixture thereof. In some embodiments, the moisture-proof acetyl-L-carnitine comprises not less than 12%, 14%, 16%, 18%, 22%, 24%, 26%, 28%, 32%, 34%, 36%, 38%, 42%, 44%, 46%, 48%, 52%, 55%, 58%, 60%, 62%, 65%, 68%, 70%, 72%, 75%, 78%, 80%, 85%, 90%, 95%, 97%, 99% by weight of acetyl-L-carnitine, or its hydrochloride salt, or a mixture thereof.

[0007] In some embodiments, the moisture-proof acetyl-L-carnitine comprises 10-99%, 15-98%, 20-97%, 25-96%, 30-95%, 35-94%, 40-93%, 45-92%, 50-90% acetyl-L-carnitine, or its hydrochloride salt, or a mixture thereof by weight. In some embodiments, the moisture-proof acetyl-L-carnitine comprises 10-99%, 11-98%, 12-97%, 15-96%, 18-95%, 20-95%, 25-92%, 35-90% acetyl-L-carnitine, or its hydrochloride salt, or a mixture thereof by weight.

[0008] In some embodiments, the moisture-proof acetyl-L-carnitine comprises, by weight, 20-98% of acetyl-L-carnitine, or its hydrochloride, or a mixture thereof; 1-60% of one or more excipients selected from microcrystalline cellulose, compressible starch, lactose, or mannitol; and 1-20% of one or more excipients selected from silicon dioxide, magnesium stearate, calcium hydrogen phosphate, calcium silicate, and micropowdered silica gel.

[0009] In some embodiments, the moisture-proof acetyl-L-carnitine comprises, by weight, 40-90% of acetyl-L-carnitine, or its hydrochloride, or a mixture thereof; 2-50% of one or more excipients selected from microcrystalline cellulose and mannitol; and 2-10% of one or more excipients selected from silicon dioxide and magnesium stearate.

[0010] In some embodiments, the moisture-proof acetyl-L-carnitine comprises, by weight, 50-80% of acetyl-L-carnitine, or its hydrochloride, or a mixture thereof; 5-45% of one or more excipients selected from microcrystalline cellulose and mannitol; and 2-5% of magnesium stearate.

[0011] In some embodiments, the moisture-proof acetyl-L-carnitine is in granular or powdered form.

[0012] In some embodiments, the particle size of the moisture-proof acetyl-L-carnitine is 10-100 mesh. In some embodiments, the particle size of the moisture-proof acetyl-L-carnitine is 20-80 mesh.

[0013] In some embodiments, the moisture-protected acetyl-L-carnitine is formulated as a nutritional supplement, food, beverage, or animal feed.

[0014] In some embodiments, the moisture-proof acetyl-L-carnitine is prepared as a solid formulation or a liquid formulation.

[0015] In another aspect, the present invention provides a method for preparing moisture-proof acetyl-L-carnitine, comprising mixing the following components according to a formula: acetyl-L-carnitine, or its hydrochloride or a mixture of the two, one or more excipients selected from microcrystalline cellulose, compressible starch, lactose or mannitol, and one or more excipients selected from silicon dioxide, magnesium stearate, calcium hydrogen phosphate, calcium silicate, and micropowdered silica gel; granulating; and obtaining moisture-proof acetyl-L-carnitine.

[0016] In some embodiments, the moisture-proof acetyl-L-carnitine comprises, by weight, 40-90% of acetyl-L-carnitine, or its hydrochloride, or a mixture thereof; 2-50% of one or more excipients selected from microcrystalline cellulose and mannitol; and 2-10% of one or more excipients selected from silicon dioxide and magnesium stearate.

[0017] In some embodiments, the moisture-proof acetyl-L-carnitine comprises, by weight, 50-80% of acetyl-L-carnitine, or its hydrochloride, or a mixture thereof; 5-45% of one or more excipients selected from microcrystalline cellulose and mannitol; and 2-5% of magnesium stearate.

[0018] In some embodiments, the granulation is one of wet granulation, spray granulation, melt granulation, and dry granulation.

[0019] In some embodiments, the granulation is dry granulation.

[0020] In some embodiments, the moisture-proof acetyl-L-carnitine prepared by the above method is used to prepare food, beverages, nutritional products, skin care products or cosmetics.

[0021] In some embodiments, the method includes a sieving step. In some embodiments, acetyl-L-carnitine, or its hydrochloride, or a mixture thereof, and / or mannitol are sieved through a 10-100 mesh sieve. In some embodiments, acetyl-L-carnitine, or its hydrochloride, or a mixture thereof, and / or mannitol are sieved through a 20-80 mesh sieve.

[0022] 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

[0023] 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.

[0024] 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."

[0025] 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.

[0026] As used herein, the term "comprises" or "includes" or variations thereof refer to instances where the term is used in its non-limiting sense, meaning that items following the word are included, but items not specifically mentioned are not excluded. It also includes the more restrictive verbs 'consisting essentially of' and 'consisting of. Examples

[0027] 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.

[0028] 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.

[0029] On the one hand, the present invention provides a moisture-proof acetyl-L-carnitine, or its hydrochloride or a mixture thereof, wherein the moisture-proof acetyl-L-carnitine, or its hydrochloride or a mixture thereof has excellent moisture-proof and deliquescence-resistant effects, improves the stability of acetyl-L-carnitine or its hydrochloride, and provides users with extremely high applicability. The acetyl-L-carnitine or its hydrochloride used in the present invention can be prepared and obtained by known methods.

[0030] On the other hand, the present invention is screened by granulation mode to acetyl-L-carnitine or its hydrochloride raw material, and granulation modes such as wet granulation, spray granulation, melt granulation, and dry granulation can be screened, and preferably dry granulation mode is granulated; The dry granulation process adopted is applicable to the formula of the present invention, and bed collapse phenomenon will not be caused, and process energy consumption is small, and production cost is low, and preparation process is solvent-free and intervenes, and production process flow is green and environmentally friendly, and no waste gas and waste water are produced. The addition of microcrystalline cellulose, mannitol, etc. can achieve a good anti-caking effect in this formula, and magnesium stearate, etc. have a good anti-caking and anti-sticking effect, and these several material combinations have the advantages that production yield is high, anti-hygroscopic effect is remarkable, and auxiliary materials are economically easy to get. This method can select 10-100 mesh, and preferably 20-80 mesh sieve granulation obtains moisture-proof acetyl-L-carnitine.

[0031] The method achieves the preparation of high-content moisture-proof acetyl-L-carnitine, or its hydrochloride, or a mixture of the two by screening suitable auxiliary materials and granulation methods. The prepared moisture-proof acetyl-L-carnitine, or its hydrochloride, or a mixture of the two achieves excellent moisture-proof and deliquescence-resistant effects, improves the stability of acetyl-L-carnitine or its hydrochloride, and provides users with extremely high applicability.

[0032] The following examples are illustrative of selected embodiments of the present invention and are not intended to limit the scope of the present invention. Example 1 Preparation of moisture-proof acetyl-L-carnitine

[0033] A moisture-proof acetyl-L-carnitine comprises the following components in weight percentage: 50% acetyl-L-carnitine, 45% microcrystalline cellulose, and 5% magnesium stearate. The acetyl-L-carnitine is passed through a 30-mesh sieve, and the prescribed amount of acetyl-L-carnitine, microcrystalline cellulose, and magnesium stearate are weighed and placed in a three-dimensional mixer. Granulation is performed using a dry granulator to obtain moisture-proof acetyl-L-carnitine. Example 2 Preparation of moisture-proof acetyl-L-carnitine

[0034] A moisture-proof acetyl-L-carnitine comprises the following components in percentage by weight: Acetyl L-carnitine and mannitol were passed through a 30-mesh sieve, and the prescribed amount of acetyl L-carnitine, mannitol, microcrystalline cellulose, and magnesium stearate were weighed and placed in a three-dimensional mixer. Granulation was performed using a dry granulator to obtain moisture-proof acetyl L-carnitine. Example 3 Preparation of moisture-proof acetyl L-carnitine

[0035] A moisture-proof acetyl-L-carnitine comprises the following components in percentage by weight: Acetyl L-carnitine and mannitol were passed through a 30-mesh sieve, and the prescribed amount of acetyl L-carnitine, mannitol, microcrystalline cellulose, and magnesium stearate were weighed and placed in a three-dimensional mixer. Granulation was performed using a dry granulator to obtain moisture-proof acetyl L-carnitine. Example 4 Preparation of moisture-proof acetyl L-carnitine

[0036] A moisture-proof acetyl-L-carnitine comprises the following components in percentage by weight: Acetyl L-carnitine and mannitol were passed through a 30-mesh sieve, and the prescribed amount of acetyl L-carnitine, mannitol, microcrystalline cellulose, and magnesium stearate were weighed and placed in a three-dimensional mixer. Granulation was performed using a dry granulator to obtain moisture-proof acetyl L-carnitine. Example 5 Preparation of moisture-proof acetyl L-carnitine hydrochloride

[0037] A moisture-proof acetyl-L-carnitine hydrochloride comprises the following components in percentage by weight: Acetyl-L-carnitine hydrochloride and mannitol were passed through a 30-mesh sieve, and the prescribed amount of acetyl-L-carnitine hydrochloride, mannitol, microcrystalline cellulose, and magnesium stearate were weighed and placed in a three-dimensional mixer. Granulation was performed using a dry granulator to obtain moisture-proof acetyl-L-carnitine hydrochloride. Example 6 Preparation of moisture-proof acetyl-L-carnitine and acetyl-L-carnitine hydrochloride mixture

[0038] A moisture-proof mixture of acetyl-L-carnitine and acetyl-L-carnitine hydrochloride comprises the following components in percentage by weight: Acetyl-L-carnitine, acetyl-L-carnitine hydrochloride, and mannitol were passed through a 30-mesh sieve, and the prescribed amount of acetyl-L-carnitine, acetyl-L-carnitine hydrochloride, mannitol, microcrystalline cellulose, and magnesium stearate were weighed and placed in a three-dimensional mixer. The mixture was granulated using a dry granulator to obtain a moisture-proof acetyl-L-carnitine and acetyl-L-carnitine hydrochloride mixture. Example 7: Investigation of moisture-proof properties of moisture-proof acetyl-L-carnitine

[0039] 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, place it in a temperature of 40℃±2℃, relative humidity of 75%±5%, take out the glass bottle at regular intervals (respectively at 0.5h, 1h, 1.5h, 2h, 3h, 5h, 7h), and test the pass rate through the 24-mesh sieve and the moisture content. According to the calculation formula: Calculate the sieve pass rate.

[0040] The test results of the moisture-proof acetyl L-carnitine sample passing through a 24-mesh sieve are shown in Table 1.

[0041] The moisture test results of moisture-proof acetyl L-carnitine samples are shown in Table 2.

[0042] As can be seen from Table 1 and Table 2, compared with the raw materials, the moisture-proof acetyl L-carnitine samples of each embodiment of the present invention have a high load of not less than 50% at a temperature of 40°C ± 2°C and a relative humidity of 75% ± 5%. At the same time, the pass rate of the 24-mesh sieve is high and the moisture content increases little, and the moisture-proof effect is excellent; in addition, the auxiliary materials screened during the dry granulation preparation process are conducive to tableting and granulation, and the material fluidity is good. The moisture-proof acetyl L-carnitine of the present invention contains not less than 10%, 12%, 14%, 15%, 16%, 18%, 20%, 22%, 24%, 25%, 26%, 28%, 30%, 32%, 34%, 35%, 36%, 38%, 40%, 42%, 44%, 45%, 46%, 48%, 50%, 52%, 55%, 58%, 60%, 62%, 65%, 68%, 70%, 72%, 75%, 78% by weight. %, 80%, 85%, 90%, 95%, 97%, 99% of acetyl-L-carnitine, or its hydrochloride or a mixture of the two, or containing 10-99%, 15-98%, 20-97%, 25-96%, 30-95%, 35-94%, 40-93%, 45-92%, 50-90% of acetyl-L-carnitine, or its hydrochloride or a mixture of the two, can achieve more obvious moisture-proof and deliquescence-resistant effects and fluidity enhancement under high humidity conditions than the raw materials.

[0043] 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 acetyl-L-carnitine, characterized in that: The invention contains not less than 10% by weight of acetyl-L-carnitine, or its hydrochloride, or a mixture of the two.

2. Moisture-proof acetyl-L-carnitine according to claim 1, characterized in that The invention comprises not less than 15%, 20%, 25%, 30%, 35%, 40%, 45%, 50% by weight of acetyl-L-carnitine, or its hydrochloride or a mixture of the two.

3. Moisture-proof acetyl-L-carnitine according to claim 1 or 2, characterized in that The invention comprises 20-98% by weight of acetyl-L-carnitine, or its hydrochloride or a mixture of the two; 1-60% of one or more auxiliary materials selected from microcrystalline cellulose, compressible starch, lactose or mannitol; and 1-20% 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 acetyl-L-carnitine according to any one of claims 1 to 3, characterized in that The invention comprises 40-90% by weight of acetyl-L-carnitine, or its hydrochloride or a mixture of the two; 2-50% by weight of one or more auxiliary materials selected from microcrystalline cellulose and mannitol; and 2-10% by weight of one or more auxiliary materials selected from silicon dioxide and magnesium stearate.

5. The moisture-proof acetyl-L-carnitine according to any one of claims 1 to 4, characterized in that The invention comprises 50-80% by weight of acetyl-L-carnitine, or its hydrochloride or a mixture of the two; 5-45% of one or more auxiliary materials selected from microcrystalline cellulose and mannitol; and 2-5% of magnesium stearate.

6. The moisture-proof acetyl-L-carnitine according to any one of claims 1 to 5, characterized in that The moisture-proof acetyl-L-carnitine is in the form of granules or powder.

7. The moisture-proof acetyl-L-carnitine according to claim 6, characterized in that The particle size of the moisture-proof acetyl-L-carnitine is 10-100 meshes.

8. The moisture-proof acetyl-L-carnitine according to any one of claims 1 to 7, characterized in that The moisture-proof acetyl-L-carnitine is formulated into a nutritional supplement, food, beverage or animal feed.

9. The moisture-proof acetyl-L-carnitine according to any one of claims 1 to 8, characterized in that The moisture-proof acetyl-L-carnitine is prepared as a solid preparation or a liquid preparation.

10. A method for preparing moisture-proof acetyl-L-carnitine, characterized in that: The method comprises mixing the following components according to the formula amount: acetyl-L-carnitine, or its hydrochloride or a mixture of the two, 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 acetyl-L-carnitine.

11. The method according to claim 10, characterized in that The moisture-proof acetyl-L-carnitine comprises, by weight, 50-80% of acetyl-L-carnitine, or its hydrochloride or a mixture of the two; 5-45% of one or more auxiliary materials selected from microcrystalline cellulose and mannitol; and 2-5% of magnesium stearate.

12. The method according to claim 10 or 11, characterized in that: The granulation is one of wet granulation, spray granulation, melt granulation and dry granulation.

13. The method according to claim 12, characterized in that The granulation is dry granulation.

14. The method according to any one of claims 10 to 13, characterized in that: The moisture-proof acetyl-L-carnitine prepared by the method is used for preparing food, beverage, nutrition product, skin care product or cosmetic.