CN112402387A - Lipoic acid tablet and preparation method thereof - Google Patents
Lipoic acid tablet and preparation method thereof Download PDFInfo
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- CN112402387A CN112402387A CN202011369204.4A CN202011369204A CN112402387A CN 112402387 A CN112402387 A CN 112402387A CN 202011369204 A CN202011369204 A CN 202011369204A CN 112402387 A CN112402387 A CN 112402387A
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- lipoic acid
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- 235000019136 lipoic acid Nutrition 0.000 title claims abstract description 70
- 229960002663 thioctic acid Drugs 0.000 title claims abstract description 70
- 238000002360 preparation method Methods 0.000 title abstract description 17
- AGBQKNBQESQNJD-UHFFFAOYSA-M lipoate Chemical compound [O-]C(=O)CCCCC1CCSS1 AGBQKNBQESQNJD-UHFFFAOYSA-M 0.000 title abstract 6
- 238000001035 drying Methods 0.000 claims abstract description 20
- 239000008187 granular material Substances 0.000 claims abstract description 20
- 239000000945 filler Substances 0.000 claims abstract description 13
- 239000000314 lubricant Substances 0.000 claims abstract description 12
- 239000000853 adhesive Substances 0.000 claims abstract description 11
- 230000001070 adhesive effect Effects 0.000 claims abstract description 11
- 239000007888 film coating Substances 0.000 claims abstract description 11
- 238000009501 film coating Methods 0.000 claims abstract description 11
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 11
- 239000002994 raw material Substances 0.000 claims abstract description 10
- 238000005469 granulation Methods 0.000 claims abstract description 6
- 230000003179 granulation Effects 0.000 claims abstract description 6
- AGBQKNBQESQNJD-UHFFFAOYSA-N lipoic acid Chemical compound OC(=O)CCCCC1CCSS1 AGBQKNBQESQNJD-UHFFFAOYSA-N 0.000 claims description 66
- 238000002156 mixing Methods 0.000 claims description 20
- 238000000034 method Methods 0.000 claims description 12
- AGBQKNBQESQNJD-SSDOTTSWSA-N (R)-lipoic acid Chemical compound OC(=O)CCCC[C@@H]1CCSS1 AGBQKNBQESQNJD-SSDOTTSWSA-N 0.000 claims description 9
- 238000000576 coating method Methods 0.000 claims description 8
- 239000011248 coating agent Substances 0.000 claims description 7
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 6
- 239000000758 substrate Substances 0.000 claims description 6
- MVPICKVDHDWCJQ-UHFFFAOYSA-N ethyl 3-pyrrolidin-1-ylpropanoate Chemical compound CCOC(=O)CCN1CCCC1 MVPICKVDHDWCJQ-UHFFFAOYSA-N 0.000 claims description 5
- 229940045902 sodium stearyl fumarate Drugs 0.000 claims description 5
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims description 4
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 4
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims description 4
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims description 4
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims description 4
- 239000008108 microcrystalline cellulose Substances 0.000 claims description 4
- 229940016286 microcrystalline cellulose Drugs 0.000 claims description 4
- 229920002472 Starch Polymers 0.000 claims description 3
- 239000011230 binding agent Substances 0.000 claims description 3
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims description 3
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 3
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 3
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 claims description 3
- 229940031703 low substituted hydroxypropyl cellulose Drugs 0.000 claims description 3
- 235000019359 magnesium stearate Nutrition 0.000 claims description 3
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims description 3
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims description 3
- 239000008107 starch Substances 0.000 claims description 3
- 235000019698 starch Nutrition 0.000 claims description 3
- 229920000858 Cyclodextrin Polymers 0.000 claims description 2
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims description 2
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims description 2
- 238000009835 boiling Methods 0.000 claims description 2
- 239000008101 lactose Substances 0.000 claims description 2
- 239000007788 liquid Substances 0.000 claims description 2
- 229940037627 magnesium lauryl sulfate Drugs 0.000 claims description 2
- 229940057948 magnesium stearate Drugs 0.000 claims description 2
- HBNDBUATLJAUQM-UHFFFAOYSA-L magnesium;dodecyl sulfate Chemical compound [Mg+2].CCCCCCCCCCCCOS([O-])(=O)=O.CCCCCCCCCCCCOS([O-])(=O)=O HBNDBUATLJAUQM-UHFFFAOYSA-L 0.000 claims description 2
- 238000000643 oven drying Methods 0.000 claims description 2
- 229940069328 povidone Drugs 0.000 claims description 2
- HFHDHCJBZVLPGP-UHFFFAOYSA-N schardinger α-dextrin Chemical compound O1C(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(O)C2O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC2C(O)C(O)C1OC2CO HFHDHCJBZVLPGP-UHFFFAOYSA-N 0.000 claims description 2
- 239000000463 material Substances 0.000 abstract description 8
- 238000004090 dissolution Methods 0.000 abstract description 7
- 239000003814 drug Substances 0.000 abstract description 5
- 238000004519 manufacturing process Methods 0.000 abstract description 5
- 239000000203 mixture Substances 0.000 abstract description 5
- 238000009776 industrial production Methods 0.000 abstract description 4
- 239000000825 pharmaceutical preparation Substances 0.000 abstract description 2
- 239000007767 bonding agent Substances 0.000 abstract 1
- 239000003826 tablet Substances 0.000 description 43
- 238000003756 stirring Methods 0.000 description 9
- 238000007922 dissolution test Methods 0.000 description 4
- 239000000843 powder Substances 0.000 description 4
- 239000008213 purified water Substances 0.000 description 4
- 238000012360 testing method Methods 0.000 description 4
- 229940079593 drug Drugs 0.000 description 3
- 238000002474 experimental method Methods 0.000 description 3
- 239000000080 wetting agent Substances 0.000 description 3
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- 239000008103 glucose Substances 0.000 description 2
- 238000001727 in vivo Methods 0.000 description 2
- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 description 2
- 238000012986 modification Methods 0.000 description 2
- 230000004048 modification Effects 0.000 description 2
- 238000007873 sieving Methods 0.000 description 2
- 239000000126 substance Substances 0.000 description 2
- 238000006467 substitution reaction Methods 0.000 description 2
- 102000004877 Insulin Human genes 0.000 description 1
- 108090001061 Insulin Proteins 0.000 description 1
- 235000014676 Phragmites communis Nutrition 0.000 description 1
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 description 1
- 230000032683 aging Effects 0.000 description 1
- 239000003963 antioxidant agent Substances 0.000 description 1
- 230000003078 antioxidant effect Effects 0.000 description 1
- 235000006708 antioxidants Nutrition 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 239000001768 carboxy methyl cellulose Substances 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 230000001684 chronic effect Effects 0.000 description 1
- 239000005515 coenzyme Substances 0.000 description 1
- 230000001276 controlling effect Effects 0.000 description 1
- -1 crushing Substances 0.000 description 1
- 206010012601 diabetes mellitus Diseases 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 239000007884 disintegrant Substances 0.000 description 1
- 238000009826 distribution Methods 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 210000001035 gastrointestinal tract Anatomy 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 229940125396 insulin Drugs 0.000 description 1
- 238000011835 investigation Methods 0.000 description 1
- 210000004185 liver Anatomy 0.000 description 1
- 238000002844 melting Methods 0.000 description 1
- 230000008018 melting Effects 0.000 description 1
- 230000004060 metabolic process Effects 0.000 description 1
- 229930014626 natural product Natural products 0.000 description 1
- 230000002093 peripheral effect Effects 0.000 description 1
- 238000003825 pressing Methods 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 230000001105 regulatory effect Effects 0.000 description 1
- 238000010008 shearing Methods 0.000 description 1
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 1
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- 238000005507 spraying Methods 0.000 description 1
- 230000006641 stabilisation Effects 0.000 description 1
- 238000013112 stability test Methods 0.000 description 1
- 238000011105 stabilization Methods 0.000 description 1
- 230000004102 tricarboxylic acid cycle Effects 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
- A61K31/385—Heterocyclic compounds having sulfur as a ring hetero atom having two or more sulfur atoms in the same ring
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P39/00—General protective or antinoxious agents
- A61P39/06—Free radical scavengers or antioxidants
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Biochemistry (AREA)
- Toxicology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
The invention belongs to the technical field of pharmaceutical preparations, and particularly relates to a lipoic acid tablet and a preparation method thereof. The tablet comprises a tablet core and a film coating, wherein the tablet core contains lipoic acid, a bonding agent, a filling agent and a lubricating agent, and the preparation method comprises the following steps: the lipoic acid raw material and adhesive are dry-mixed, water is added for granulation, a filling agent and a lubricating agent are added after drying, the granules are sized, the mixture is totally mixed and then tableted, and the lipoic acid tablet is coated. The formula of the invention has simple composition, good product stability, good dissolution and more excellent product quality; the invention has simple and easy production operation, less auxiliary material types and dosage, high main medicine occupation ratio and low cost, solves the problem that the lipoic acid tablet is easy to stick and dash, and is suitable for industrial production.
Description
Technical Field
The invention belongs to the technical field of pharmaceutical preparations, and particularly relates to a lipoic acid tablet and a preparation method thereof.
Background
Lipoic acid (lipoic acid) with the chemical name of 1, 2-dithiolane-3-pentanoic acid and the molecular formula of C8H12S2O2Is a vitaminBoth in water and in fat.
The chemical structure of lipoic acid is as follows:
lipoic acid is a natural product which is separated from pig liver for the first time in 1951 by Reed, and the lipoic acid is used as a coenzyme in vivo to participate in tricarboxylic acid cycle, not only participates in the metabolic process of glucose, but also directly mediates the distribution of insulin-regulated glucose in peripheral tissues, and has good prevention and treatment effects on chronic complications of diabetes. The lipoic acid enters cells after being absorbed by intestinal tracts in vivo, has the characteristics of fat solubility and water solubility, can reach any cell, can eliminate free radicals for accelerating aging and causing diseases, and is a universal antioxidant with fat solubility and water solubility.
At present, the lipoic acid is mainly available in the dosage forms of injection, tablet and capsule. Lipoic acid has pungent odor and taste, and has low melting point and is unstable to light and heat. When the tablet is prepared, the tablet is easy to stick and wash during tabletting, and the preparation difficulty is high.
The Chinese patent application CN103655495A, published by the date 2014.03.26, provides a lipoic acid tablet with less types and dosage of auxiliary materials and a preparation method thereof, in order to overcome the technical problems that the activity may be influenced by the drying process in the conventional granulation method in the preparation of the lipoic acid tablet, and the lipoic acid tablet is easy to stick and punch during tabletting and is easy to have color spots during tabletting. The method is that the auxiliary material tablet is prepared by the filler and the adhesive according to the conventional tabletting method, then the lipoic acid powder is sprayed and coated on the auxiliary material tablet by taking sodium carboxymethyl cellulose as a spraying agent, and then the drying is finished by strictly controlling the drying temperature. The method avoids sticking phenomenon and color spots generated during tabletting of the lipoic acid by pressing the auxiliary material tablets without the lipoic acid. However, compared with direct tabletting, the coating process is complex in operation and high in equipment requirement, and the problems of nonuniform coating, nonuniform drug content, tablet breakage and the like are easily caused.
Chinese patent application CN103622927A, published as 2014.03.12, discloses a lipoic acid common tablet, which is prepared by micronizing lipoic acid, and sieving to obtain lipoic acid fine powder; sieving the filler and disintegrant respectively, mixing with thioctic acid fine powder, mixing, adding binder, stirring at high speed, and shearing to obtain wet granule; and finally, drying the wet granules, adding a lubricant, crushing, finishing granules, mixing uniformly, and tabletting to obtain the tablet. The problem that the common lipoic acid tablets are easy to stick and dash in the tabletting process is solved, but the process is relatively complex, the types of the auxiliary materials are more, and the tablets can not effectively cover the pungent smell of the lipoic acid raw materials.
In conclusion, the prior art can solve the problem that the thioctic acid tablet is easy to stick and dash during tabletting in the preparation process, but the preparation process is complex, can not effectively cover bad smell, is easy to cause uneven medicine content, has low efficiency and is not suitable for industrial production.
Disclosure of Invention
The invention aims to provide a lipoic acid tablet which has simple prescription composition, good stability and good dissolution.
The invention also aims to provide a preparation method of the lipoic acid tablet, which has the advantages of simple production process, less auxiliary material types and dosage, high main drug ratio and low production cost, solves the problem that the lipoic acid tablet is easy to stick and dash, and is suitable for industrial production.
The lipoic acid tablet comprises a tablet core and a film coating, wherein the tablet core contains lipoic acid, a binding agent, a filling agent and a lubricating agent.
Wherein:
the tablet core is prepared from the following raw materials in parts by weight: 600 parts of lipoic acid, 10-40 parts of adhesive, 160 parts of filler 120 and 3-40 parts of lubricant.
In the tablet, the weight percentage of the lipoic acid is 70-85%.
The adhesive is one or more of hydroxypropyl methylcellulose, hydroxypropyl cellulose or povidone.
The filler is one or more of lactose, microcrystalline cellulose, starch, cyclodextrin or low-substituted hydroxypropyl cellulose
The lubricant is one or more of sodium stearyl fumarate, magnesium stearate or magnesium lauryl sulfate.
In the tablet, the mass percentage of the film coating is 2-5%.
The preparation method of the lipoic acid tablet comprises the following steps:
(1) mixing thioctic acid and adhesive, adding water, and granulating to obtain wet granule;
(2) drying the wet granules prepared in the step (1), adding a filler and a lubricant, granulating, uniformly mixing, and tabletting to obtain a base sheet;
(3) coating the substrate prepared in the step (2) with film coating liquid to obtain the lipoic acid tablet.
In step (1), water is used as a wetting agent.
In the step (1), the granulation is performed by adopting a wet granulator.
In the step (2), the drying is boiling drying or oven drying.
The raw materials and the adhesive are mixed, a proper amount of wetting agent is added for granulation, more granules are prepared, and meanwhile, a screen with larger aperture (a screen with the aperture of 2.0 mm) is adopted for granule stabilization, so that the proportion of fine powder in the granules is further reduced, and the sticking problem of the lipoic acid tablets is solved.
Compared with the prior art, the invention has the following beneficial effects:
1. the lipoic acid tablet has simple prescription composition, the weight percentage content of the main drug is as high as 70-85%, the single dose of a patient is reduced, and the compliance is improved; the dosage of auxiliary materials is reduced, and the production cost is obviously reduced.
2. In the preparation method of the lipoic acid tablet, the problem of easy sticking in the tabletting process is solved; meanwhile, the raw materials are not required to be crushed and sieved, and an adhesive solution is not required to be prepared, the raw materials and the adhesive are dry-mixed, a proper amount of wetting agent is added for granulation, a filler and a lubricant are added after drying, the granules are sized, and the mixture is tabletted and coated after total mixing. The process has simple steps and high production efficiency, and is suitable for industrial production.
3. The product of the invention has stable quality and complete dissolution.
4. The product of the invention can effectively cover the pungent smell of the lipoic acid raw material.
Detailed Description
The present invention will be further described with reference to the following embodiments.
The raw materials used in the examples are all commercially available raw materials.
Example 1
The lipoic acid tablet has the following formula (1000 dosage tablets):
the mass percentage content of the film coating is 3.5%.
The preparation method specifically comprises the following steps:
putting lipoic acid and hydroxypropyl methylcellulose into an efficient mixing granulator, firstly operating at a low speed (stirring paddle 100RPM and fly cutter 1500RPM) for 120 seconds, adding 150g of purified water, continuing to operate for 180 seconds, and finally operating at a high speed (stirring paddle 150RPM and fly cutter 3000RPM) for 30 seconds to obtain wet granules. Drying the wet granules by a hot air circulation drying oven, granulating by a crushing and granulating machine, adding starch and sodium stearyl fumarate, mixing by a hopper mixer, tabletting after uniformly mixing, and finally coating the substrate.
The prepared thioctic acid tablet has smooth and clean appearance and no sticking, the disintegration time measured by a disintegration test is 2 minutes, and the dissolution rate measured by the dissolution test is 92 percent, thereby meeting the requirements.
Example 2
The lipoic acid tablet has the following formula (1000 dosage tablets):
the mass percentage content of the film coating is 3.5%.
The preparation method specifically comprises the following steps:
putting thioctic acid and polyvidone into high-efficiency mixing granulator, operating at low speed (stirring paddle 100RPM, fly cutter 1500RPM) for 120 s, adding 150g of purified water, operating for 180 s, and operating at high speed (stirring paddle 150RPM, fly cutter 3000RPM) for 30 s to obtain wet granule. Drying the wet granules by a hot air circulation drying oven, granulating by a crushing and granulating machine, adding low-substituted hydroxypropyl cellulose and sodium stearyl fumarate, mixing by a hopper mixer, tabletting after uniformly mixing, and finally coating the substrate.
The prepared thioctic acid tablet has smooth and clean appearance and no sticking, the disintegration time measured by a disintegration test is 3 minutes, and the dissolution rate measured by the dissolution test is 89 percent, thereby meeting the requirements.
Example 3
The lipoic acid tablet has the following formula (1000 dosage tablets):
the mass percentage content of the film coating is 3.5%.
The preparation method specifically comprises the following steps:
putting lipoic acid and hydroxypropyl cellulose into an efficient mixing granulator, firstly operating at a low speed (stirring paddle 100RPM and fly cutter 1500RPM) for 120 seconds, adding 150g of purified water, continuing operating for 180 seconds, and finally operating at a high speed (stirring paddle 150RPM and fly cutter 3000RPM) for 30 seconds to prepare wet granules. Drying the wet granules by a hot air circulation drying oven, granulating by a crushing and granulating machine, adding microcrystalline cellulose and sodium stearyl fumarate, mixing by a hopper mixer, tabletting after uniformly mixing, and finally coating the substrate.
The prepared thioctic acid tablet has smooth and clean appearance and no sticking, the disintegration time measured by a disintegration test is 3 minutes, and the dissolution rate measured by the dissolution test is 90 percent, thereby meeting the requirements.
Example 4
The lipoic acid tablet has the following formula (1000 dosage tablets):
the mass percentage content of the film coating is 3.5%.
The preparation method specifically comprises the following steps:
putting lipoic acid and hydroxypropyl cellulose into an efficient mixing granulator, firstly operating at a low speed (stirring paddle 100RPM and fly cutter 1500RPM) for 120 seconds, adding 150g of purified water, continuing operating for 180 seconds, and finally operating at a high speed (stirring paddle 150RPM and fly cutter 3000RPM) for 30 seconds to prepare wet granules. Drying the wet granules by a hot air circulation drying oven, granulating by a crushing granulator, adding microcrystalline cellulose and magnesium stearate, mixing by a hopper mixer, tabletting after uniformly mixing, and finally coating the substrate.
The prepared thioctic acid tablet has smooth and clean appearance and no sticking, the disintegration time measured by a disintegration test is 6 minutes, and the dissolution rate measured by the dissolution test is 87 percent.
Example 5
Stability experiments, three batches of samples were produced and packaged according to example 1. And (4) carrying out stability experiments according to the stability investigation experiment requirements of Chinese pharmacopoeia. The results are shown in Table 1.
TABLE 1 stability test results
The above embodiments are preferred embodiments of the present invention, but the present invention is not limited to the above embodiments, and any other changes, modifications, substitutions, combinations, and simplifications which do not depart from the spirit and principle of the present invention should be construed as equivalents thereof, and all such changes, modifications, substitutions, combinations, and simplifications are intended to be included in the scope of the present invention.
Claims (10)
1. A lipoic acid tablet characterized by: the tablet comprises a tablet core and a film coating, wherein the tablet core contains lipoic acid, a binding agent, a filling agent and a lubricating agent.
2. The lipoic acid tablet of claim 1, characterized in that: the tablet core is prepared from the following raw materials in parts by weight: 600 parts of lipoic acid, 10-40 parts of adhesive, 160 parts of filler 120 and 3-40 parts of lubricant.
3. The lipoic acid tablet according to claim 1 or 2, characterized in that: in the tablet, the weight percentage of the lipoic acid is 70-85%.
4. The lipoic acid tablet according to claim 1 or 2, characterized in that: the adhesive is one or more of hydroxypropyl methylcellulose, hydroxypropyl cellulose or povidone.
5. The lipoic acid tablet according to claim 1 or 2, characterized in that: the filler is one or more of lactose, microcrystalline cellulose, starch, cyclodextrin or low-substituted hydroxypropyl cellulose.
6. The lipoic acid tablet according to claim 1 or 2, characterized in that: the lubricant is one or more of sodium stearyl fumarate, magnesium stearate or magnesium lauryl sulfate.
7. The lipoic acid tablet according to claim 1 or 2, characterized in that: in the tablet, the mass percentage of the film coating is 2-5%.
8. A method for preparing the lipoic acid tablet of any one of claims 1-7, comprising: the method comprises the following steps:
(1) mixing thioctic acid and adhesive, adding water, and granulating to obtain wet granule;
(2) drying the wet granules prepared in the step (1), adding a filler and a lubricant, granulating, uniformly mixing, and tabletting to obtain a base sheet;
(3) coating the substrate prepared in the step (2) with film coating liquid to obtain the lipoic acid tablet.
9. The method of preparing a lipoic acid tablet of claim 8, characterized in that: in the step (1), the granulation is performed by adopting a wet granulator.
10. The method of preparing a lipoic acid tablet of claim 8, characterized in that: in the step (2), the drying is boiling drying or oven drying.
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| CN202011369204.4A CN112402387A (en) | 2020-11-30 | 2020-11-30 | Lipoic acid tablet and preparation method thereof |
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| CN202011369204.4A CN112402387A (en) | 2020-11-30 | 2020-11-30 | Lipoic acid tablet and preparation method thereof |
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Citations (3)
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|---|---|---|---|---|
| CN105267164A (en) * | 2014-07-04 | 2016-01-27 | 江苏神龙药业有限公司 | Thioctic acid dispersible tablet and preparation method thereof |
| CN110063942A (en) * | 2018-01-24 | 2019-07-30 | 四川科伦药物研究院有限公司 | Amber love song Ge Lieting solid pharmaceutical preparation and preparation method thereof |
| CN111557920A (en) * | 2020-04-15 | 2020-08-21 | 南京海纳医药科技股份有限公司 | Lipoic acid-containing tablet and preparation method thereof |
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2020
- 2020-11-30 CN CN202011369204.4A patent/CN112402387A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN105267164A (en) * | 2014-07-04 | 2016-01-27 | 江苏神龙药业有限公司 | Thioctic acid dispersible tablet and preparation method thereof |
| CN110063942A (en) * | 2018-01-24 | 2019-07-30 | 四川科伦药物研究院有限公司 | Amber love song Ge Lieting solid pharmaceutical preparation and preparation method thereof |
| CN111557920A (en) * | 2020-04-15 | 2020-08-21 | 南京海纳医药科技股份有限公司 | Lipoic acid-containing tablet and preparation method thereof |
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Application publication date: 20210226 |