CN111557920A - Lipoic acid-containing tablet and preparation method thereof - Google Patents

Abstract

The invention discloses a lipoic acid-containing tablet and a preparation method thereof, belonging to the technical field of pharmaceutical preparations. The lipoic acid-containing tablet or the tablet core thereof comprises active components of lipoic acid, a filling agent, an adhesive, a release agent, a disintegrating agent, a flow aid and a lubricant, wherein in the preparation process, the active components are uniformly mixed with the filling agent and the adhesive, then an ethanol solution of the release agent is added to prepare a soft material, then granulation is carried out, and the obtained wet granules are dried, then mixed with the disintegrating agent, the flow aid and the lubricant, and finally tabletted. The tablet prepared by the method has the advantages of high lipoic acid content of active components, no less than 70%, rapid dissolution, smooth tablet core surface, no color spots, no any sticking sign, high bioavailability and rapid disintegration speed, and solves the problems of low lipoic acid melting point and easy sticking of tabletting.

Description

Lipoic acid-containing tablet and preparation method thereof

Technical Field

The invention belongs to the technical field of pharmaceutical preparations, and particularly relates to a lipoic acid-containing tablet and a preparation method thereof.

Background

Lipoic Acid (Thioctic Acid), chemically (±) -5- [3- (1, 2-dithiolane) ] -pentanoic Acid, is a light yellow crystal with a strong pungent odor. Lipoic acid is a coenzyme present in mitochondria, like vitamins, and eliminates free radicals that accelerate aging and cause disease. The lipoic acid enters cells after being absorbed by intestinal tracts in vivo, has the characteristics of fat solubility and water solubility, can pass through the whole body without hindrance and reach any cell part to provide comprehensive efficiency for a human body, is a universal antioxidant with fat solubility and water solubility, is quickly absorbed in vivo, and has certain application value in stabilizing blood sugar value, strengthening liver function, improving fatigue, dementia, beautifying and resisting aging. In the seventies of the twentieth century, germany approved it as a drug for the treatment of hepatitis, in the nineties approved it for the treatment of diabetes, and in 1997 FDA approved lipoic acid for marketing as a health product.

Clinical researches have proved that the lipoic acid can remarkably increase the sugar metabolism of diabetics and relieve symptoms of peripheral nerve numbness, stabbing pain and the like induced by diabetes, so that lipoic acid preparations are currently marketed at home, and the indications are treating diabetic peripheral polyneuropathy, and the lipoic acid preparations are mainly tablets, capsules and injection.

The lipoic acid is rapidly absorbed by oral administration, and the compliance of patients who develop the lipoic acid into oral dosage forms relative to injection is stronger. The product has unstable physical properties and strong pungent odor, and can be developed into coated tablet for masking taste and increasing storage stability. However, the oral tablet specification on the market at home is 0.3g at most, and the number of manufacturers is small, while the specification of 0.6g is on the market for years abroad, which is due to the great difficulty of the preparation process. According to the physical property of the lipoic acid, the melting point of the lipoic acid is lower (about 60 ℃), the process has the common problems of sticking, so that the preparation process difficulty is higher, and if large-size tablets are developed and diluted by using more auxiliary materials to improve the sticking, the tablet weight is increased, and the swallowing difficulty is caused, so that the development of a tablet production technology which has the advantages of less auxiliary material consumption and simple and feasible production process is urgently needed.

The Chinese patent application CN103655495A discloses a tablet preparation technology, which adopts the steps of firstly preparing auxiliary materials into a blank tablet with the diameter of 5-6mm, and then spraying and coating the raw materials on a tablet core layer by layer in a coating mode, thereby avoiding the sticking phenomenon caused by the tabletting process. However, the process is complex and tedious, the main drug can be coated on the tablet core only by spraying and coating multiple layers, the industrial production control is not facilitated, and the cost is high.

The Chinese patent application CN103099793B discloses a direct tabletting technology, which adopts magnesium stearate with fine particle size to fully mix raw materials and auxiliary materials to improve the sticking problem, but the proportion of main drugs in the prescription is low, and the increase of the proportion of main drugs can require more magnesium stearate to improve the sticking, thereby bringing the risks in the product quality aspects of disintegration, dissolution and the like.

Chinese patent application CN105267164A discloses a preparation technology of lipoic acid dispersible tablets with good dispersion uniformity and stability, but the content of main drugs is low, and the effect of inhibiting sticking is achieved mainly by combining talcum powder and micro-powder silica gel.

In order to overcome the problems of low melting point and easy sticking of the pressed tablet, the above patent avoids the pressing procedure in the process preparation way, but causes the process to be more complicated and difficult to operate; or the types and the granularity of the lubricant are explored, but the formula and the process of the tablet which have high occupation ratio of main medicines and simple production process and can overcome the sticking problem cannot be provided.

Disclosure of Invention

The invention aims to provide a lipoic acid-containing tablet which has the advantages of high content of active component lipoic acid, quick dissolution, smooth surface of a tablet core, no color spots, no any sticking sign, high bioavailability and quick disintegration speed on the basis of the prior art, and solves the problems of low melting point and easy sticking of the lipoic acid during tabletting.

The invention also provides a preparation method of the lipoic acid-containing tablet.

The technical scheme of the invention is as follows:

a tablet containing lipoic acid or a tablet core thereof comprises active components of lipoic acid, a filling agent, an adhesive, a release agent, a disintegrating agent, a flow aid and a lubricant.

The tablet or tablet core containing the lipoic acid provided by the invention comprises the active component lipoic acid and auxiliary materials. The auxiliary materials adopted by the invention comprise a filling agent, an adhesive, a release agent, a disintegrating agent, a flow aid and a lubricant. Wherein the filler is selected from one or more of microcrystalline cellulose, lactose, mannitol or pregelatinized starch.

In a preferred embodiment, the filler is selected from microcrystalline cellulose and/or lactose.

The adhesive adopted by the invention can be one or more of hydroxypropyl methylcellulose, povidone or hydroxypropyl cellulose.

In a preferred embodiment, the binder may be hypromellose, e.g., hypromellose E15.

The release agent adopted by the invention is selected from the dimeticone, and the dimeticone is dissolved in the ethanol to prepare the ethanol solution of the dimeticone in the preparation process of the lipoic acid tablet, thereby solving the problems of low melting point of the lipoic acid and easy sticking of tabletting, meanwhile, the dosage of auxiliary materials such as an auxiliary agent and a lubricant can be reduced, the negative influence of a larger dosage of a glidant and a lubricant on the quality of the lipoic acid tablet is avoided, the proportion among the components is further optimized, under the coordination of other conditions, the content of the active component lipoic acid in the prepared tablet is high (not less than 70 percent), the dosage of auxiliary materials is obviously reduced, can be prepared into large-scale preparations to reduce administration times, improve patient compliance, dissolve out rapidly, have smooth tablet core surface, no color spot, high bioavailability, and high disintegration speed, under the condition of high proportion of raw materials and medicines, the sticking problem commonly existing in the production process of the thioctic acid tablet is solved.

In a preferable scheme, the mass concentration of the dimeticone in the ethanol solution of the dimeticone is 0.5-5%; more preferably, the mass concentration of the dimeticone is 1-2%.

In one embodiment, the disintegrant is selected from croscarmellose sodium and/or sodium starch glycolate; preferably croscarmellose sodium.

In a preferred embodiment, the glidant is selected from silicon dioxide, and more preferably, the lubricant is selected from magnesium stearate.

In a preferred scheme, in the preparation process of the lipoic acid tablet, a release agent (dimeticone) is dissolved in ethanol to prepare an ethanol solution of dimeticone, then the ethanol solution is mixed with the uniformly mixed active components, the filling agent and the binder to prepare a soft material, the soft material is sieved and granulated, the obtained wet granules are dried, sieved and granulated, and then the wet granules are mixed with a disintegrating agent, a glidant and a lubricant, tabletted and coated. Experiments show that the addition sequence of the components in the preparation process of the lipoic acid tablet influences the active component lipoic acid content, sticking problem, dissolution speed and related substance content of the tablet.

In the preparation process, the active component, the filling agent and the adhesive are uniformly mixed, then the ethanol solution of the release agent is added to prepare a soft material, then granulation is carried out, and finally other auxiliary materials are added after the granulation. Experiments show that compared with other wet granulation modes, the mode provided by the invention can improve the dissolution speed of the preparation, solve the problems of low melting point of lipoic acid and easiness in sticking and flushing of tabletting, improve the content of active substances in the preparation, effectively improve the content of each preparation, and enable the surface of a tablet core to be smooth, have no color spots, and meet the requirements on disintegration time and friability.

In one scheme, the lipoic acid-containing tablet comprises a tablet core and a coating, wherein the tablet core comprises the following components in percentage by mass: 70-80% of lipoic acid, 14-18% of a filler, 2-4% of an adhesive, 0.25-0.5% of a release agent, 2-4% of a disintegrant, 1-3% of a glidant and 1-3% of a lubricant.

Experiments show that the tablet can maintain higher dissolution speed and higher lipoic acid content of active ingredients only when the dosage of the release agent is kept within a reasonable range, the sticking problem commonly existing in the production process of lipoic acid tablets is solved under the condition of high raw material-medicine ratio, and the effect is difficult to achieve by using too high or too low dosage of the release agent. The preferable usage amount of the release agent is 0.25-0.5%.

In a preferred embodiment, the lipoic acid-containing tablet comprises a tablet core and a coating, wherein the tablet core comprises the following components in parts by mass: 70-80 parts of lipoic acid, 4-9 parts of microcrystalline cellulose, 8-13 parts of lactose, 152-4 parts of hydroxypropyl methylcellulose E, 0.25-0.5 part of dimethicone, 2-4 parts of croscarmellose sodium, 1-3 parts of silicon dioxide and 1-3 parts of magnesium stearate.

In a more preferable scheme, the lipoic acid-containing tablet comprises a tablet core and a coating, 75 parts of lipoic acid, 5-7 parts of microcrystalline cellulose, 11 parts of lactose, 153 parts of hydroxypropyl methylcellulose E, 0.25-0.5 part of dimethicone, 2 parts of croscarmellose sodium, 1-2 parts of silicon dioxide and 1-2 parts of magnesium stearate.

The coating of the tablet of the invention can adopt the existing gastric soluble film coating material, such as gastric soluble coating powder, and the weight gain of the coating is 3-5%.

The invention provides a preparation method of the lipoic acid-containing tablet, which comprises the following steps:

(1) pretreatment: sieving active component lipoic acid, filler and adhesive for later use;

(2) preparing ethanol solution of release agent: dissolving a release agent in ethanol to prepare an ethanol solution of the release agent;

(3) granulating, tabletting and coating: mixing pretreated active components, filler and binder uniformly, adding ethanol solution of mold release agent to make soft mass, sieving, granulating, drying the obtained wet granule, sieving, grading, mixing with disintegrant, glidant and lubricant, tabletting, and coating.

In one embodiment, the filler is selected from one or more of microcrystalline cellulose, lactose, mannitol, or pregelatinized starch.

In a preferred embodiment, the filler is selected from microcrystalline cellulose and/or lactose.

In one embodiment, the binder may be one or more of hypromellose, povidone, or hydroxypropyl cellulose.

In a preferred embodiment, the binder may be hypromellose, e.g., hypromellose E15.

In the preparation process of the lipoic acid tablet, the release agent is dissolved in ethanol to prepare an ethanol solution of the release agent, and preferably, the release agent is simethicone. The invention adopts the dimeticone as the release agent, solves the problems of low melting point of the lipoic acid and easy sticking of the pressed tablet, can reduce the dosage of auxiliary materials such as an auxiliary agent and a lubricant, and avoids the negative influence of the glidant and the lubricant with larger dosage on the quality of the lipoic acid tablet. In a preferable scheme, the mass concentration of the dimeticone in the ethanol solution of the dimeticone is 0.5-5%; more preferably, the mass concentration of the dimeticone is 1-2%.

In one embodiment, the disintegrant is selected from croscarmellose sodium and/or sodium starch glycolate; preferably croscarmellose sodium.

In a preferred embodiment, the glidant is selected from silicon dioxide, and more preferably, the lubricant is selected from magnesium stearate.

In the preparation method of the tablet, in the step (3), the drying temperature is 35-45 ℃, and the drying weight loss is controlled to be less than 4%; preferably, the drying temperature is 40 ℃.

In a preferred embodiment, step (1) is carried out by sieving with a 60-mesh sieve.

Further, obtaining a soft material in the step (3), granulating by 20 meshes, drying at 35-45 ℃, grading by 20 meshes, and controlling the weight gain of the coating by 3-5% by adopting a gastric-soluble film coating material, such as gastric-soluble coating powder.

In the preparation of tablets, the preferred granulation process is as follows: uniformly mixing the pretreated active component, microcrystalline cellulose, lactose and hydroxypropyl methylcellulose E15, adding an ethanol solution of dimeticone with the mass concentration of 0.5-5% to prepare a soft material, sieving with a 20-mesh sieve, granulating, drying the obtained wet granules at 35-45 ℃, controlling the drying weight loss to be less than 4%, sieving with the 20-mesh sieve, grading, mixing with croscarmellose sodium, silicon dioxide and magnesium stearate, tabletting, and coating.

The preparation method of the lipoic acid-containing tablet provided by the invention comprises the following more detailed steps:

(1) pretreatment: respectively sieving active components of lipoic acid, microcrystalline cellulose, lactose and hydroxypropyl methylcellulose E15 through a 60-mesh sieve, and mixing in a high-speed wet mixer for 20 minutes;

(2) preparing ethanol solution of release agent: dissolving dimeticone in ethanol to prepare an ethanol solution of dimeticone with the mass concentration of 0.5-5%;

(3) granulating, tabletting and coating: uniformly mixing pretreated active components of lipoic acid, microcrystalline cellulose, lactose and hydroxypropyl methylcellulose E15, adding an ethanol solution with the mass concentration of 0.5-5% of dimethicone to prepare a soft material, sieving with a 20-mesh sieve, granulating, putting the obtained wet granules into a fluidized bed for drying, setting the air inlet temperature to be 40 ℃, drying until the drying weight loss of the granules is less than 4%, sieving the dried granules with the 20-mesh sieve, granulating, mixing with croscarmellose sodium, silicon dioxide and magnesium stearate in a three-dimensional mixer for 10 minutes, detecting the content of an intermediate, tabletting after determining the tablet weight, controlling the hardness of a tablet core to be 12-18kg, coating, and controlling the weight gain of the coating to be 3-5%.

In the lipoic acid coated tablet prepared by the method, the content of active component lipoic acid is high (not less than 70%), and in the preparation process, an ethanol solution with the mass concentration of 0.5-5% of dimethicone is added to prepare a soft material, so that the problems of low melting point of the lipoic acid and easiness in sticking and flushing of tabletting are solved, the using amount of auxiliary materials can be reduced, the lipoic acid coated tablet can be used for preparing large-size (0.6g) preparations, the tablet weight is not increased too much, the special spicy and pungent odor of the lipoic acid is covered by coating, the administration frequency of patients can be reduced clinically, the swallowing difficulty is not increased, and the administration compliance of the patients is increased.

The lipoic acid tablet core prepared by the method has smooth surface, no color spots and no sticking and stamping signs, the friability and the disintegration time limit meet the requirements, the lipoic acid tablet core is coated with a good appearance, and the disintegration time limit meets the requirements.

By adopting the technical scheme of the invention, the advantages are as follows:

the lipoic acid-containing tablet provided by the invention has the advantages that the content of active component lipoic acid is high (not less than 70%), the dissolution is rapid, the surface of a tablet core is smooth, no color spots and no sticking and washing signs exist, the bioavailability is high, the disintegration speed is high, and the problems of low melting point and easiness in sticking and washing of a pressed tablet of the lipoic acid are solved.

In the preparation method of the lipoic acid tablet, the conventional wet granulation process and common solid preparation production equipment are adopted to prepare the lipoic acid tablet, the tablet core surface is smooth, no color spots and no sticking and punching signs exist, the friability and the disintegration time limit meet the requirements, the coated lipoic acid tablet has good appearance, and the disintegration time limit meets the requirements.

Detailed Description

The tablets containing lipoic acid according to the present invention are further illustrated by the following examples, which are not intended to limit the present invention in any way.

Example 1

(1) Formulation and weight percentage content (1000 tablets dosage)

(2) Preparation method

(1) Pretreatment: respectively sieving active components of lipoic acid, microcrystalline cellulose, lactose and hydroxypropyl methylcellulose E15 through a 60-mesh sieve, and mixing in a high-speed wet mixer for 20 minutes;

(2) preparing ethanol solution of release agent: dissolving dimeticone in ethanol to prepare an ethanol solution of dimeticone with the mass concentration of 1%;

(3) granulating, tabletting and coating: uniformly mixing pretreated active components of lipoic acid, microcrystalline cellulose, lactose and hydroxypropyl methylcellulose E15, adding 200g of an ethanol solution with the mass concentration of 1% of dimethicone to prepare a soft material, sieving with a 20-mesh sieve, granulating, putting the obtained wet granules into a fluidized bed for drying, setting the air inlet temperature to be 40 ℃, drying until the drying weight loss of the granules is less than 4%, sieving the dried granules with the 20-mesh sieve, granulating, mixing with croscarmellose sodium, silicon dioxide and magnesium stearate in a three-dimensional mixer for 10 minutes, detecting the content of an intermediate, tabletting after determining the tablet weight, controlling the hardness of a tablet core to be 12-18kg, coating, and controlling the weight gain of the coating to be 4%.

Example 2

(1) Formulation and weight percentage content (1000 tablets dosage)

(2) Preparation method

(1) Pretreatment: respectively sieving active components of lipoic acid, microcrystalline cellulose, lactose and hydroxypropyl methylcellulose E15 through a 60-mesh sieve, and mixing in a high-speed wet mixer for 20 minutes;

(2) preparing ethanol solution of release agent: dissolving dimeticone in ethanol to prepare an ethanol solution of dimeticone with the mass concentration of 2%;

(3) granulating, tabletting and coating: uniformly mixing pretreated active components of lipoic acid, microcrystalline cellulose, lactose and hydroxypropyl methylcellulose E15, adding 200g of an ethanol solution with the mass concentration of 2% of dimethicone to prepare a soft material, sieving with a 20-mesh sieve, granulating, putting the obtained wet granules into a fluidized bed for drying, setting the air inlet temperature to be 40 ℃, drying until the drying weight loss of the granules is less than 4%, sieving the dried granules with the 20-mesh sieve, granulating, mixing with croscarmellose sodium, silicon dioxide and magnesium stearate in a three-dimensional mixer for 10 minutes, detecting the content of an intermediate, tabletting after determining the tablet weight, controlling the hardness of a tablet core to be 12-18kg, coating, and controlling the weight gain of the coating to be 4%.

Comparative example 1

We examined the preparation of thioctic acid tablets without release agent (dimethicone).

(1) Formulation and weight percentage content (1000 tablets dosage)

(2) Preparation method

(1) Pretreatment: respectively sieving active components of lipoic acid, microcrystalline cellulose, lactose and hydroxypropyl methylcellulose E15 through a 60-mesh sieve, and mixing in a high-speed wet mixer for 20 minutes;

(2) granulating, tabletting and coating: uniformly mixing pretreated active components of lipoic acid, microcrystalline cellulose, lactose and hydroxypropyl methylcellulose E15, adding 200g of ethanol to prepare a soft material, sieving with a 20-mesh sieve, granulating, putting the obtained wet granules into a fluidized bed for drying, setting the air inlet temperature to be 40 ℃, drying until the drying weight loss of the granules is less than 4%, sieving the dried granules with the 20-mesh sieve, granulating, mixing with croscarmellose sodium, silicon dioxide and magnesium stearate in a three-dimensional mixer for 10 minutes, detecting the content of an intermediate, tabletting after determining the tablet weight, controlling the hardness of a tablet core to be 12-18kg, coating, and controlling the weight gain of the coating to be 4%.

Comparative example 2

We examined the preparation and quality testing of thioctic acid tablets when the tablet core contained the components of the release agent (dimethicone) in parts by mass which were not within the scope of protection of the present application.

(1) Formulation and weight percentage content (1000 tablets dosage)

(2) Preparation method

(1) Pretreatment: respectively sieving active components of lipoic acid, microcrystalline cellulose, lactose and hydroxypropyl methylcellulose E15 through a 60-mesh sieve, and mixing in a high-speed wet mixer for 20 minutes;

(2) preparing ethanol solution of release agent: dissolving dimeticone in ethanol to prepare an ethanol solution of dimeticone with the mass concentration of 4%;

(3) granulating, tabletting and coating: uniformly mixing pretreated active components of lipoic acid, microcrystalline cellulose, lactose and hydroxypropyl methylcellulose E15, adding 200g of an ethanol solution of dimethyl silicone oil with the mass concentration of 4% to prepare a soft material, sieving with a 20-mesh sieve, granulating, putting the obtained wet granules into a fluidized bed, drying until the drying weight loss of the granules is less than 4% by setting the air inlet temperature at 40 ℃, sieving the dried granules with the 20-mesh sieve, granulating, mixing with croscarmellose sodium, silicon dioxide and magnesium stearate in a three-dimensional mixer for 10 minutes, detecting the content of an intermediate, tabletting after determining the weight of the tablet, controlling the hardness of a tablet core to be 12-18kg, coating, and controlling the weight gain of the coating to be 4%.

Comparative example 3

Lipoic acid tablets prepared according to the composition and method of example 1 of chinese patent application CN 103099793B.

Comparative example 4

Lipoic acid tablets prepared according to the composition and method of example 1 of chinese patent application CN 105267164A.

The results of the evaluation of the indexes of the thioctic acid tablets prepared in examples 1 and 2 and comparative examples 1,2, 3 and 4 are shown in Table 1.

TABLE 1 examination results of thioctic acid tablets prepared in examples and comparative examples

The tablet cores prepared in the above examples 1 and 2 are smooth and have no sticking, and the disintegration time limit and friability meet the requirements of Chinese pharmacopoeia; the dissolution determination method adopts a method recommended by United states pharmacopoeia: the paddle method takes 900ml of water as a dissolution medium, and the dissolution rate in 60 minutes is more than 95 percent, and the dissolution rate in 60 minutes meeting the requirements of United states pharmacopoeia is not less than 70 percent. The lipoic acid content of the lipoic acid prepared by the method is obviously higher, and the main quality index is not inferior to that of the prior art.

The above examples are merely representative of embodiments of the present invention, and the description thereof is more detailed and specific, but not to be construed as limiting the present invention. It should be noted that, for a person skilled in the art, several variations and modifications can be made without departing from the inventive concept, which falls within the scope of the present invention.

Claims (10)

1. A tablet containing lipoic acid is characterized in that the tablet or a tablet core thereof comprises active ingredients of lipoic acid, a filling agent, an adhesive, a mold release agent, a disintegrating agent, a flow aid and a lubricant, wherein in the preparation process of the tablet, the active ingredients are uniformly mixed with the filling agent and the adhesive, then an ethanol solution of the mold release agent is added to prepare a soft material, then granulation is carried out, the obtained wet granules are dried, and then the mixture is mixed with the disintegrating agent, the flow aid and the lubricant to carry out tabletting.

2. The lipoic acid containing tablet of claim 1, characterised in that said filler is selected from one or more of microcrystalline cellulose, lactose, mannitol or pregelatinized starch; preferably microcrystalline cellulose and/or lactose; the adhesive is selected from one or more of hydroxypropyl methylcellulose, povidone or hydroxypropyl cellulose; preferably hypromellose; more preferably hypromellose E15.

3. The lipoic acid containing tablet of claim 1, characterised in that said release agent is selected from dimethicone, preferably, dimethicone in ethanol solution has a mass concentration of 0.5-5% during the lipoic acid tablet preparation process; more preferably, the mass concentration of the dimeticone is 1-2%.

4. The lipoic acid containing tablet according to claim 1, characterised in that said disintegrant is selected from the group consisting of croscarmellose sodium and/or sodium starch glycolate; preferably croscarmellose sodium; the glidant is selected from silicon dioxide; the lubricant is selected from magnesium stearate.

5. The lipoic acid containing tablet of claims 1,2, 3 or 4, characterized in that the lipoic acid tablet comprises a core and a coating, wherein the core comprises the following components in parts by mass: 70-80 parts of lipoic acid, 4-9 parts of microcrystalline cellulose, 8-13 parts of lactose, 152-4 parts of hydroxypropyl methylcellulose E, 0.25-0.5 part of dimethicone, 2-4 parts of croscarmellose sodium, 1-3 parts of silicon dioxide and 1-3 parts of magnesium stearate.

6. The lipoic acid containing tablet of claim 5, comprising a core and a coating, wherein the core comprises the following components in parts by mass: 75 parts of lipoic acid, 5-7 parts of microcrystalline cellulose, 11 parts of lactose, 153 parts of hydroxypropyl methylcellulose E, 0.25-0.5 part of dimethicone, 2 parts of croscarmellose sodium, 1-2 parts of silicon dioxide and 1-2 parts of magnesium stearate.

7. A method for preparing a lipoic acid containing tablet according to claim 1, characterized in that it comprises the following steps:

(1) pretreatment: sieving active component lipoic acid, filler and adhesive for later use;

(2) preparing ethanol solution of release agent: dissolving a release agent in ethanol to prepare an ethanol solution of the release agent;

(3) granulating, tabletting and coating: mixing pretreated active components, filler and binder uniformly, adding ethanol solution of mold release agent to make soft mass, sieving, granulating, drying the obtained wet granule, sieving, grading, mixing with disintegrant, glidant and lubricant, tabletting, and coating.

8. The method for preparing lipoic acid containing tablets of claim 7, characterised in that said filler is selected from one or more of microcrystalline cellulose, lactose, mannitol or pregelatinized starch; preferably microcrystalline cellulose and/or lactose; the adhesive is selected from one or more of hydroxypropyl methylcellulose, povidone or hydroxypropyl cellulose; preferably hypromellose; more preferably hypromellose E15; the release agent is selected from dimeticone; the disintegrant is selected from croscarmellose sodium and/or sodium carboxymethyl starch; preferably croscarmellose sodium; the glidant is selected from silicon dioxide; the lubricant is selected from magnesium stearate.

9. The method for preparing lipoic acid containing tablets of claim 8, wherein in step (2), the mass concentration of dimethicone in the ethanol solution of dimethicone is 0.5-5%, preferably, the mass concentration of dimethicone is 1-2%; in the step (3), the drying temperature is 35-45 ℃, and the drying weight loss is controlled to be less than 4%; preferably, the drying temperature is 40 ℃.

10. The method for preparing lipoic acid containing tablets of claim 9, wherein in step (1), 60 mesh sieve is passed; and (4) granulating by 20 meshes after obtaining a soft material in the step (3), finishing granules by 20 meshes after drying, wherein the coating is made of a gastric-soluble film coating material, and the weight of the coating is controlled to be increased by 3-5%.