CN108743555B - Aspirin enteric-coated tablet and preparation method thereof - Google Patents
Aspirin enteric-coated tablet and preparation method thereof Download PDFInfo
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- 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
- A61K9/2886—Dragees; Coated pills or tablets, e.g. with film or compression coating having two or more different drug-free coatings; Tablets of the type inert core-drug layer-inactive layer
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- 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
- A61K31/60—Salicylic acid; Derivatives thereof
- A61K31/612—Salicylic acid; Derivatives thereof having the hydroxy group in position 2 esterified, e.g. salicylsulfuric acid
- A61K31/616—Salicylic acid; Derivatives thereof having the hydroxy group in position 2 esterified, e.g. salicylsulfuric acid by carboxylic acids, e.g. acetylsalicylic acid
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- 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
- A61K9/2009—Inorganic compounds
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- 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
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- 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
- A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
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- 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
- A61K9/2806—Coating materials
- A61K9/2833—Organic macromolecular compounds
- A61K9/284—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone
Abstract
The invention relates to the field of pharmaceutical engineering, in particular to an aspirin enteric-coated tablet and a preparation method thereof. The preparation method of the aspirin enteric-coated tablet comprises the following steps: the first enteric coating layer and the second enteric coating layer are sequentially arranged outside the aspirin tablet core without solvent. The first enteric coating layer is obtained by spraying the first coating solution to the aspirin tablet core. Each part of the first coating solution comprises 1.8 to 2.2 parts of enteric coating material, 0.2 to 0.4 part of plasticizer, 0.8 to 1.2 parts of anti-sticking agent and 20 to 25 parts of solvent by weight. The aspirin tablet core is coated by the first enteric coating layer and the second enteric coating layer, so that external moisture can be effectively prevented from permeating, aspirin is prevented from hydrolyzing, and meanwhile, aspirin is prevented from disintegrating in gastric juice, but the disintegrating and dissolving effects of aspirin in intestinal juice can be guaranteed.
Description
Technical Field
The invention relates to the field of pharmaceutical engineering, in particular to an aspirin enteric-coated tablet and a preparation method thereof.
Background
Aspirin (Aspirin, acetylsalicylic acid) is a white crystal or crystalline powder, odorless or slightly acetogenic, slightly soluble in water, readily soluble in ethanol, soluble in ether and chloroform, and acidic in aqueous solution. Aspirin is stable in dry air, and slowly hydrolyzes into salicylic acid and acetic acid when meeting tide, so that the stability and the drug effect of the aspirin are easily influenced, and meanwhile, the aspirin is easily decomposed in an acidic environment, so that the toxic and side effects of the aspirin are increased, and the drug effect of the aspirin is reduced. Therefore, aspirin is prepared into the enteric-coated tablet in the prior art, but in the aspirin enteric-coated tablet in the prior art, the aspirin is deteriorated too much due to the fact that a tablet core is granulated by a wet method, and meanwhile, an isolation layer is arranged in the aspirin enteric-coated tablet, so that the disintegration effect of the aspirin enteric-coated tablet in intestinal juice is reduced.
Disclosure of Invention
The invention provides a preparation method of an aspirin enteric-coated tablet, and aims to solve the technical problem that an isolating layer influences the disintegration of the aspirin enteric-coated tablet.
The invention also provides an aspirin enteric-coated tablet which is high in stability and is insoluble in gastric juice and decomposed in intestinal tracts.
The invention is realized by the following steps:
a preparation method of aspirin enteric-coated tablets comprises the following steps:
sequentially arranging a first enteric coating layer and a second enteric coating layer outside the aspirin tablet core without a solvent;
the first enteric coating layer is obtained by spraying a first coating solution onto the aspirin tablet core, and each part of the first coating solution comprises, by weight, 1.8-2.2 parts of an enteric coating material, 0.2-0.4 part of a plasticizer, 0.8-1.2 parts of an anti-sticking agent and 20-25 parts of a solvent.
An aspirin enteric-coated tablet, which is prepared by the preparation method of the aspirin enteric-coated tablet.
The invention has the beneficial effects that: according to the preparation method of the aspirin enteric-coated tablet, the first enteric-coated layer and the second enteric-coated layer are arranged to coat the aspirin tablet core, so that external moisture can be effectively prevented from permeating, aspirin is prevented from hydrolyzing, aspirin is prevented from disintegrating in gastric juice, and the disintegrating and dissolving effects of aspirin in intestinal juice can be guaranteed. Meanwhile, the aspirin tablet core does not contain a solvent, so that the aspirin can be effectively inhibited from hydrolyzing, and the drug effect of the aspirin is further ensured.
Detailed Description
In order to make the objects, technical solutions and advantages of the embodiments of the present invention clearer, the technical solutions in the embodiments of the present invention will be clearly and completely described below. The examples, in which specific conditions are not specified, were conducted under conventional conditions or conditions recommended by the manufacturer. The reagents or instruments used are not indicated by the manufacturer, and are all conventional products available commercially.
The aspirin enteric-coated tablet of the embodiment of the present invention and the preparation method thereof are specifically described below.
A preparation method of aspirin enteric-coated tablets comprises the following steps:
s1, preparing an aspirin tablet core;
each part of aspirin tablet core is a tablet core obtained by directly tabletting after mixing 0.8-1.2 parts of aspirin, 0.10-0.14 part of adhesive, 0.09-0.13 part of filler and 0.02-0.03 part of lubricant in parts by weight. Or a tablet core obtained by directly tabletting after mixing 0.9-1.1 parts of aspirin, 0.11-0.13 parts of adhesive, 0.1-0.12 parts of filling agent and 0.023-0.029 parts of lubricant; or a tablet core obtained by directly tabletting after mixing 1 to 1.05 parts of aspirin, 0.12 to 0.15 part of adhesive, 0.105 to 0.11 part of filler and 0.025 to 0.028 part of lubricant.
Aspirin is stable in dry air, can be slowly hydrolyzed into salicylic acid and acetic acid when meeting tide, and if aspirin is contacted with water, ethanol or other solvents, and then is heated and dried under the condition of damp heat, so that the decomposition of aspirin raw material can be promoted, and the excessive free salicylic acid is easily caused. In order to solve the problem that aspirin is easily decomposed when meeting a solvent, the embodiment adopts direct tabletting of powder, and no solvent is introduced in the mixing and tabletting processes, so that the content of aspirin is ensured, and the content of free salicylic acid is reduced.
The aspirin tablet core can be directly tabletted only by mixing the auxiliary materials in the step 3 with aspirin, and the compressibility of mixed powder can be ensured only by adopting the interaction of the auxiliary materials in the step 3, so that the possibility of the aspirin tablet core being affected with damp is reduced, and the materials are uniformly mixed.
In particular, the binder is a cellulose depolymerization product, preferably microcrystalline cellulose, more preferably microcrystalline cellulose type 102. Microcrystalline cellulose (MCC) is a purified, partially depolymerized cellulose, white, odorless, tasteless, crystalline powder composed of porous particles, and is available in a wide variety of forms, with different types of microcrystalline cellulose having different properties, such as MCC-101, MCC-102, MCC-103, MCC-105, and MCC-CG, among many other types. However, the present application prefers type 102 microcrystalline cellulose, i.e., MCC-102, which has better flowability and compressibility than other microcrystalline celluloses, and in turn, can facilitate direct tableting of the blended powder.
Further, the filler is a starch filler, preferably corn starch, and the starch filler also includes other starches such as pregelatinized starch, carboxymethyl starch, and the like. Corn starch is more stable in property and low in hygroscopicity compared with other starch, so that an aspirin tablet core is not easy to damp, but the compressibility of powder is reduced by using the corn starch, so that the corn starch also needs to interact with MCC-102 of the application to ensure the compressibility of the powder, further ensure the stable structure of the aspirin tablet core, and prevent loose tablets or loose tablets from being formed.
Furthermore, the lubricant can reduce the friction force between the powder and is convenient for the uniform mixing of the materials. The lubricant is talcum powder, the pH value of the talcum powder is 7-9, the aspirin tablet core is prevented from disintegrating in gastric juice, the chemical property of the aspirin tablet core is inactive, the aspirin tablet core does not change the property of aspirin, the aspirin tablet core has covering capacity, and the surface smoothness of the aspirin tablet core can be improved.
The specific operation of mixing aspirin, binder, filler and lubricant and tabletting in this example is well known in the art and will not be described in detail herein.
S2, preparing a first coating solution and a second coating solution;
s2.1, preparing a first coating solution;
each part of the first coating solution comprises 1.8 to 2.2 parts of enteric coating material, 0.2 to 0.4 part of plasticizer, 0.8 to 1.2 parts of anti-sticking agent and 20 to 25 parts of solvent by weight. Or comprises 1.9-2.1 parts of enteric coating material, 0.25-0.35 part of plasticizer, 0.9-1.1 part of antisticking agent and 22-23 parts of solvent. Or comprises 2 to 2.05 parts of enteric coating material, 0.27 to 0.3 part of plasticizer, 1 to 1.05 parts of anti-sticking agent and 22.5 to 24 parts of solvent.
The first coating liquid is obtained by mixing enteric coating material, plasticizer, antisticking agent and solvent. A dense film layer is formed on the surface of the aspirin tablet core through the synergistic effect of the substances, so that external water is effectively prevented from permeating, aspirin is prevented from decomposing and deteriorating, and the drug effect of the aspirin enteric-coated tablet is ensured. The first coating layer is arranged through the first coating liquid, the isolation layer is avoided being arranged, the effect of isolating moisture can be achieved, the coating layer playing a role in isolating moisture in the prior art is the isolation layer, but the isolation layer only isolates moisture, and meanwhile, as the raw materials adopted by the isolation layer are cellulose polymers (such as hydroxypropyl methyl cellulose and ethyl cellulose) or mucilage and other substances which are difficult to be degraded by intestinal juice, the disintegration effect of the disintegrated aspirin enteric-coated tablet is inhibited, and the drug effect of the drug is inhibited. The first enteric coating material is arranged in the first coating liquid, so that the first enteric coating layer can be rapidly decomposed by the intestinal liquid after the second enteric coating layer is decomposed by the intestinal liquid, the disintegration effect of the aspirin enteric tablet is improved, the formation of the first enteric coating layer can be accelerated through the interaction of the enteric coating material and the plasticizer, and the moisture isolation effect of the first enteric coating layer is ensured. Furthermore, the enteric coating material is a resin material, preferably acrylic resin, preferably methacrylic acid copolymer, and the use of the methacrylic acid copolymer can form a compact and tough film with enzyme resistance, low permeability and rapid decomposition in the intestine on the aspirin tablet core.
Further, the plasticizer is an ester organic matter, preferably triethyl citrate, and the triethyl citrate and the enteric coating material in the proportion range are mutually synergistic to enhance the bonding function of the film.
Furthermore, the anti-sticking agent is talcum powder, and the talcum powder in the enteric coating liquid effectively prevents all substances from being bonded, so that all substances are uniformly dispersed.
Further, the solvent is an alcoholic solvent, preferably a monohydric alcohol, more preferably a C1-C3 monohydric alcohol, and most preferably 95% ethanol.
S2.2, preparing a second coating solution;
each part of the second coating solution comprises, by weight, 1.8-2.2 parts of enteric coating material, 0.1-0.2 part of plasticizer, 0.8-1.2 parts of anti-sticking agent, 0.2-0.4 part of surfactant and 20-25 parts of solvent. Or comprises 1.9-2.1 parts of enteric coating material, 0.12-0.18 part of plasticizer, 0.9-1.1 part of antisticking agent, 0.25-0.35 part of surfactant and 22-23 parts of solvent. Or comprises 2 to 2.05 parts of enteric coating material, 0.15 to 0.17 part of plasticizer, 1 to 1.05 parts of anti-sticking agent, 0.27 to 0.3 part of surfactant and 22.5 to 24 parts of solvent.
The second coating liquid is obtained by mixing enteric coating material, plasticizer, surfactant, antisticking agent and solvent. The second enteric coating layer prepared from the second coating liquid mainly has the function of well coating the aspirin tablet core, so that the aspirin tablet core cannot disintegrate in gastric juice and quickly disintegrates in intestinal juice, and the stable quality and the definite curative effect are achieved. The second enteric coating layer is in direct contact with the oral cavity of a human body, gastric juice and the like, meanwhile, the surfactant is arranged to increase the disintegration speed of the aspirin enteric-coated tablet in the intestinal juice, the surfactant with the proportion is arranged to ensure the disintegration speed of the aspirin enteric-coated tablet in the intestinal juice and prevent the aspirin enteric-coated tablet from disintegrating in the gastric juice, and meanwhile, the content of the plasticizer is reduced, so that the disintegration speed of the aspirin enteric-coated tablet in the intestinal juice can be further increased, and the aspirin enteric-coated tablet can take effect quickly.
The enteric coating material, plasticizer and anti-sticking agent and solvent used in the second coating solution are the same as those used in the first coating solution.
Further, the surfactant is a nonionic surfactant, preferably polysorbate 80, and the surfactant in the above range can promote the disintegration of the film, and the synergistic effect with other substances ensures that the aspirin enteric-coated tablet cannot disintegrate in gastric juice.
S3, preparing a first enteric coating layer;
the preparation method comprises the following steps of arranging a first enteric coating layer outside a solvent-free aspirin tablet core, wherein the first enteric coating layer is obtained by spraying a first coating liquid onto the aspirin tablet core, and specifically, the first enteric coating layer is obtained by spraying 0.03-0.045 part of the first coating liquid onto the surface of each part of the aspirin tablet core and then drying the spraying liquid, or is 0.032-0.037 part of the first coating liquid, or is 0.031-0.034 part of the first coating liquid. By adopting the proportion to spray the first coating solution, the good film forming effect can be ensured, the isolation effect can be ensured, and the disintegration effect of the aspirin can be ensured. If too much first coating liquid is sprayed, although the isolation effect is improved, the disintegration effect is reduced, and then the aspirin enteric-coated tablet cannot be quickly decomposed to take effect after entering the intestinal tract, so that the curative effect is reduced.
Specifically, spraying the first coating solution onto the aspirin tablet core is that the first coating solution peristalses at a rate of 14-16 revolutions per minute and acts on the aspirin tablet core with a tablet temperature of 27-30 ℃.
Specifically, the first coating solution is placed in a peristaltic pump, the peristaltic pump rotates at the speed of 14-16 r/min and discharges the first coating solution, the aspirin tablet core is arranged in a coating pot, the temperature of the aspirin tablet core is 27-30 ℃, meanwhile, hot air at the temperature of 55-65 ℃ is introduced into the coating pot, so that the aspirin tablet core is dried while the first coating solution acts on the aspirin tablet core, and a first enteric coating layer is formed, wherein the whole coating time is 1.5-2 hours. The aspirin tablet core has a certain temperature, so that the first coating liquid and the aspirin tablet core are more favorably acted, meanwhile, the first coating liquid can be quickly dried, and a compact film can be quickly formed on the surface of the aspirin tablet core.
S4, preparing a second enteric coating layer;
and then arranging a second enteric coating layer outside the first enteric coating layer, specifically, spraying 0.05-0.09 part of second coating liquid on the surface of each part of aspirin tablet core after the first enteric coating layer is arranged, and drying to obtain the coating layer, or 0.06-0.08 part of second coating liquid, or 0.065-0.075 part of second coating liquid.
Specifically, the second coating liquid is placed in a peristaltic pump, then the peristaltic pump rotates at the speed of 14-16 r/min and discharges the second coating liquid, the aspirin tablet core is arranged in a coating pot, the temperature of the aspirin tablet core is 27-30 ℃, meanwhile, hot air at the temperature of 55-65 ℃ is introduced into the coating pot, so that the aspirin tablet core is dried while the second coating liquid acts on the aspirin tablet core, and a second enteric coating layer is formed, wherein the whole coating time is 4-4.5 hours. The aspirin tablet core has a certain temperature, so that the second coating liquid and the aspirin tablet core are more favorably acted, meanwhile, the second coating liquid can be quickly dried, and a compact film can be quickly formed on the surface of the aspirin tablet core.
The first enteric coating layer can play a good role in isolation, reduce the generation of free salicylic acid, but cannot influence the disintegration of the aspirin enteric-coated tablet, and can promote the disintegration of the aspirin enteric-coated tablet. The second enteric coating layer can improve the swallowing feeling of the aspirin enteric-coated tablet, accelerate the disintegration and dissolution speed of the aspirin enteric-coated tablet in intestinal juice and further improve the treatment effect of the aspirin enteric-coated tablet. The first enteric coating layer and the second enteric coating layer are mutually synergistic, so that the stability, the content and the disintegration effect of the aspirin enteric-coated tablet are ensured. The invention also provides an aspirin enteric-coated tablet which is prepared by the preparation method of the aspirin enteric-coated tablet.
The features and properties of the present invention are described in further detail below with reference to examples.
Example 1
The embodiment provides a preparation method of an aspirin enteric-coated tablet, which comprises the following steps:
s1, preparing an aspirin tablet core;
56Kg of aspirin, 5.8Kg of MCC-102, 6Kg of corn starch and 1.4Kg of talcum powder are mixed and directly subjected to powder tabletting.
S2, preparing a first coating solution and a second coating solution;
s2.1, preparing a first coating solution;
2Kg of methacrylic acid copolymer, 0.3Kg of triethyl citrate, 1.0Kg of talc and 23Kg of 95% ethanol were mixed to obtain a first coating solution, the methacrylic acid copolymer being a copolymer obtained by polymerizing methacrylic acid and acrylic acid as monomers.
S2.2, preparing a second coating solution;
2Kg of methacrylic acid copolymer, 0.15Kg of triethyl citrate, 0.3Kg of polysorbate 80, 1.0Kg of talc and 23Kg of 95% ethanol were mixed to obtain a second coating solution.
S3, preparing a first enteric coating layer;
spraying 2.6Kg of first coating liquid on the surface of 56 ten thousand aspirin tablet cores, specifically, placing the first coating liquid in a peristaltic pump, rotating the peristaltic pump at the speed of 14 revolutions per minute and discharging the first coating liquid, arranging the aspirin tablet cores in a coating pot, controlling the temperature of the aspirin tablet cores to be 27 ℃, and simultaneously introducing hot air with the temperature of 55 ℃ into the coating pot, wherein the coating time is 1.5 hours.
S4, preparing a second enteric coating layer;
spraying 5.72Kg of second coating liquid on the surface of 56 ten thousand aspirin tablet cores, specifically, placing the second coating liquid in a peristaltic pump, rotating the peristaltic pump at the speed of 14 r/min and discharging the second coating liquid, wherein the aspirin tablet cores are arranged in a coating pot, the temperature of the aspirin tablet cores is 27 ℃, meanwhile, hot air with the temperature of 55 ℃ is introduced into the coating pot, and the whole coating time is 4 hours.
The embodiment also provides an aspirin enteric-coated tablet, which is prepared by the preparation method of the aspirin enteric-coated tablet.
Examples 2 to 7
The preparation method of the aspirin enteric-coated tablet provided in examples 2 to 7 is basically identical to that of the aspirin enteric-coated tablet provided in example 1 in operation, except that the ratio of raw materials is changed and the operation conditions are different.
Example 2
The aspirin tablet core is prepared by mixing 44.8Kg of aspirin, 5.6Kg of MCC-102, 5.04Kg of corn starch and 1.12Kg of talcum powder, and directly tabletting.
1.8Kg of methacrylic acid copolymer, 0.2Kg of triethyl citrate, 0.8Kg of talc and 22Kg of 95% ethanol were mixed to obtain a first coating solution, the methacrylic acid copolymer being a copolymer obtained by polymerizing methacrylic acid and ethylene as monomers.
1.8Kg of methacrylic acid copolymer, 0.1Kg of triethyl citrate, 0.8Kg of talc, 0.2Kg of polysorbate 80 and 20Kg of 95% ethanol were mixed to obtain a second coating solution.
The amount of the first coating solution used is 1.6968Kg, the rotating speed of a peristaltic pump is 15 r/min, the temperature of the aspirin tablet core is 30 ℃, the temperature of the introduced hot air is 65 ℃, and the coating time is 2 hours.
The amount of the second coating solution used is 2.828Kg, the rotating speed of the peristaltic pump is 15 r/min, the temperature of the aspirin tablet core is 30 ℃, the temperature of the introduced hot air is 65 ℃, and the coating time is 4 hours.
Example 3
The aspirin tablet core is prepared by mixing 67.2Kg of aspirin, 7.84Kg of MCC-102, 7.28Kg of corn starch and 1.68Kg of talcum powder, and directly performing powder tabletting.
2.2Kg of methacrylic acid copolymer, 0.4Kg of triethyl citrate, 1.2Kg of talcum powder and 25Kg of 95% ethanol are mixed to obtain a first coating solution, wherein the methacrylic acid copolymer is a copolymer obtained by polymerizing methacrylic acid and hydroxypropyl acrylate as monomers.
2.2Kg of methacrylic acid copolymer, 0.2Kg of triethyl citrate, 1.2Kg of talc, 0.4Kg of polysorbate 80 and 25Kg of 95% ethanol were mixed to obtain a second coating solution.
The amount of the first coating solution used is 2.688Kg, the rotation speed of a peristaltic pump is 16 r/min, the temperature of the aspirin tablet core is 28 ℃, the temperature of the introduced hot air is 60 ℃, and the coating time is 1.7 hours.
The amount of the second coating solution used is 7.56Kg, the rotating speed of the peristaltic pump is 16 r/min, the temperature of the aspirin tablet core is 28 ℃, the temperature of the introduced hot air is 60 ℃, and the coating time is 4.5 hours.
Example 4
The aspirin tablet core is prepared by directly performing powder tabletting after mixing 50.4Kg of aspirin, 6.16Kg of MCC-102, 5.6Kg of corn starch and 1.288Kg of talcum powder.
1.9Kg of methacrylic acid copolymer, 0.25Kg of triethyl citrate, 0.9Kg of talcum powder and 22Kg of 95% ethanol were mixed to obtain a first coating solution, wherein the methacrylic acid copolymer was a copolymer polymerized from methacrylic acid and hydroxyethyl acrylate as monomers.
1.9Kg of methacrylic acid copolymer, 0.12Kg of triethyl citrate, 0.9Kg of talc, 0.25Kg of polysorbate 80 and 22Kg of 95% ethanol were mixed to obtain a second coating solution.
The amount of the first coating solution used is 2.348Kg, the rotating speed of the peristaltic pump is 15 r/min, the temperature of the aspirin tablet core is 29 ℃, the temperature of the introduced hot air is 57 ℃, and the coating time is 1.8 hours.
The amount of the second coating solution used is 3.807Kg, the rotating speed of the peristaltic pump is 15 r/min, the temperature of the aspirin tablet core is 29 ℃, the temperature of the introduced hot air is 57 ℃, and the coating time is 4.2 hours.
Example 5
The aspirin tablet core is prepared by directly performing powder compression on 61.6Kg of aspirin, 7.28Kg of MCC-102, 6.72Kg of corn starch and 1.624Kg of talcum powder after mixing.
2.1Kg of methacrylic acid copolymer, 0.35Kg of triethyl citrate, 1.1Kg of talc and 23Kg of 95% ethanol were mixed to obtain a first coating solution, the methacrylic acid copolymer being a copolymer obtained by polymerizing methacrylic acid and styrene as monomers.
2.1Kg of methacrylic acid copolymer, 0.18Kg of triethyl citrate, 1.1Kg of talc, 0.35Kg of polysorbate 80 and 23Kg of 95% ethanol were mixed to obtain a second coating solution.
The amount of the first coating solution used is 3.475Kg, the rotating speed of the peristaltic pump is 14 r/min, the temperature of the aspirin tablet core is 30 ℃, the temperature of the introduced hot air is 62 ℃, and the coating time is 1.5 hours.
The amount of the second coating solution used is 6.178Kg, the rotating speed of the peristaltic pump is 14 r/min, the temperature of the aspirin tablet core is 30 ℃, the temperature of the introduced hot air is 62 ℃, and the coating time is 4.3 hours.
Example 6
The aspirin tablet core is prepared by directly performing powder tabletting after mixing 56Kg of aspirin, 6.72Kg of MCC-102, 5.88Kg of corn starch and 1.4Kg of talcum powder.
2.05Kg of methacrylic acid copolymer, 0.3Kg of triethyl citrate, 1.05Kg of talc and 24Kg of 95% ethanol were mixed to obtain a first coating solution, the methacrylic acid copolymer being a copolymer obtained by polymerizing methacrylic acid and styrene as monomers.
2Kg of methacrylic acid copolymer, 0.17Kg of triethyl citrate, 1.05Kg of talc, 0.3Kg of polysorbate 80 and 22.5Kg of 95% ethanol were mixed to obtain a second coating solution.
The amount of the first coating solution used is 2.17Kg, the rotating speed of the peristaltic pump is 15 r/min, the temperature of the aspirin tablet core is 27 ℃, the temperature of the introduced hot air is 63 ℃, and the coating time is 2 hours.
The amount of the second coating solution used is 4.55Kg, the rotating speed of the peristaltic pump is 15 r/min, the temperature of the aspirin tablet core is 27 ℃, the temperature of the introduced hot air is 63 ℃, and the coating time is 4.4 hours.
Example 7
The aspirin tablet core is prepared by mixing 58.8Kg of aspirin, 8.4Kg of MCC-102, 6.16Kg of corn starch and 1.568Kg of talcum powder, and directly tabletting.
2Kg of methacrylic acid copolymer, 0.27Kg of triethyl citrate, 1Kg of talcum powder and 22.5Kg of 95% ethanol were mixed to obtain the first coating solution, and the methacrylic acid copolymer was polymerized from methacrylic acid and itaconic acid as monomers.
2.05Kg of methacrylic acid copolymer, 0.15Kg of triethyl citrate, 1Kg of talc, 0.27Kg of polysorbate 80 and 24Kg of 95% ethanol were mixed to obtain a second coating solution.
The amount of the first coating solution used is 2.548Kg, the rotation speed of a peristaltic pump is 16 r/min, the temperature of the aspirin tablet core is 29 ℃, the temperature of the introduced hot air is 59 ℃, and the coating time is 2 hours.
The amount of the second coating solution used is 5.395Kg, the rotating speed of a peristaltic pump is 16 r/min, the temperature of the aspirin tablet core is 29 ℃, the temperature of the introduced hot air is 59 ℃, and the coating time is 4 hours.
Comparative example 1: commercially available aspirin enteric-coated tablets
Comparative example 2: an aspirin enteric tablet was prepared in accordance with the preparation method provided in example 1, except that the first enteric coating layer of example 1 was replaced with a second enteric coating layer, that is, the aspirin enteric tablet of this comparative example was provided with the second enteric coating layer having a thickness equal to the sum of the thicknesses of the first enteric coating layer and the second enteric coating layer of the aspirin enteric tablet of example 1.
Comparative example 3: an aspirin enteric tablet was prepared in accordance with the preparation method provided in example 1, except that the second enteric coating layer of example 1 was replaced with the first enteric coating layer, that is, the aspirin enteric tablet of this comparative example was provided with the first enteric coating layer having a thickness equal to the sum of the thicknesses of the first enteric coating layer and the second enteric coating layer of the aspirin enteric tablet of example 1. Comparative example 4: an aspirin enteric tablet was prepared according to the preparation method provided in example 1, except that the second coating liquid contained no surfactant.
Comparative example 5: an aspirin enteric tablet was prepared in accordance with the preparation method provided in example 1, except that the amount of triethyl citrate used in the first coating solution was 0.9 Kg.
Comparative example 6: an aspirin enteric tablet was prepared according to the preparation method provided in example 1, except that the amount of enteric coating material used in the first coating solution was 5 Kg.
Examples of the experiments
The aspirin enteric-coated tablets of example 1 and comparative examples 1 to 7 were placed at 40 ± 2 ℃ and a relative humidity of 75% ± 5% for 6 months, and sampled at the end of 0, 1, 3 and 6 months to detect the content of free salicylic acid, the release rate in acid within 120 minutes and the release rate in buffer within 45 minutes, respectively, and the results are shown in table 1.
TABLE 1 test results of aspirin enteric-coated tablets
According to the results in table 1, the stability, the release rate and the content of related substances of the aspirin enteric-coated tablet provided by the invention are superior to those of the aspirin enteric-coated tablet in the prior art, and meanwhile, the synergistic effect among the substances can be damaged by changing the components of the coating layer in the embodiment of the invention, so that the stability, the release rate and the content of the aspirin enteric-coated tablet are greatly reduced, and the drug effect of the aspirin enteric-coated tablet is further reduced.
In conclusion, the preparation method of the aspirin enteric-coated tablet provided by the invention has the advantages that the first enteric-coated layer and the second enteric-coated layer are arranged to coat the aspirin tablet core, so that external moisture can be effectively prevented from permeating, aspirin is prevented from hydrolyzing, aspirin is prevented from disintegrating in gastric juice at the same time, and the disintegrating and dissolving effects of aspirin in intestinal juice can be guaranteed. Meanwhile, the aspirin tablet core does not contain a solvent, so that the aspirin can be effectively inhibited from hydrolyzing, and the drug effect of the aspirin is further ensured.
The above description is only a preferred embodiment of the present invention and is not intended to limit the present invention, and various modifications and changes may be made by those skilled in the art. Any modification, equivalent replacement, or improvement made within the spirit and principle of the present invention should be included in the protection scope of the present invention.
Claims (6)
1. A preparation method of aspirin enteric-coated tablets is characterized by comprising the following steps:
sequentially arranging a first enteric coating layer and a second enteric coating layer outside the aspirin tablet core without a solvent;
the first enteric coating layer is obtained by spraying a first coating solution to the aspirin tablet core, and each part of the first coating solution comprises, by weight, 1.8-2.2 parts of an enteric coating material, 0.2-0.4 part of a plasticizer, 0.8-1.2 parts of an anti-sticking agent and 20-25 parts of a solvent;
the second enteric coating layer is obtained by spraying a second coating solution to the aspirin tablet core provided with the first enteric coating layer, and each part of the second coating solution comprises, by weight, 1.8-2.2 parts of an enteric coating material, 0.1-0.2 part of a plasticizer, 0.8-1.2 parts of an anti-sticking agent, 0.2-0.4 part of a surfactant and 20-25 parts of a solvent;
the tablet core is obtained by directly tabletting after mixing 0.8-1.2 parts of aspirin, 0.10-0.14 parts of adhesive, 0.09-0.13 parts of filler and 0.02-0.03 parts of lubricant;
the first enteric coating layer is obtained by spraying 0.03-0.045 parts of the first coating liquid on the surface of each part of the aspirin tablet core;
the second enteric coating layer is obtained by spraying 0.05-0.09 part of second coating liquid on the surface of each part of aspirin tablet core after the first enteric coating layer is arranged and drying;
the plasticizer is an ester organic matter; the solvent is an alcohol solvent; the surfactant is a nonionic surfactant, and the binder is a cellulose depolymerization product; the filler is a starch filler; the enteric coating material is methacrylic acid copolymer; the antisticking agent is talcum powder.
2. The method for preparing aspirin enteric tablets according to claim 1, characterized in that the binder is microcrystalline cellulose.
3. The method for preparing aspirin enteric tablets according to claim 2, characterized in that the binder is type 102 microcrystalline cellulose.
4. A process for preparing an aspirin enteric tablet according to claim 1, characterized in that spraying the first coating solution onto the aspirin tablet core is performed such that the first coating solution peristalses at a rate of 14-16 revolutions per minute and acts on the aspirin tablet core with a tablet temperature of 27-30 ℃.
5. The method for preparing an aspirin enteric-coated tablet according to claim 4, characterized in that the first enteric coating layer is a coating layer obtained by spraying the first coating solution onto the aspirin tablet core and then drying the coating layer.
6. An aspirin enteric-coated tablet, characterized in that it is prepared by the method for preparing an aspirin enteric-coated tablet according to any one of claims 1 to 5.
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Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4775536A (en) * | 1986-02-24 | 1988-10-04 | Bristol-Myers Company | Enteric coated tablet and process for making |
| US4857337A (en) * | 1988-05-24 | 1989-08-15 | American Home Products Corp. (Del) | Enteric coated aspirin tablets |
| CN101088494A (en) * | 2006-06-16 | 2007-12-19 | 信越化学工业株式会社 | Enteric coated granule and method for preparing the same |
| CN102641254A (en) * | 2012-05-07 | 2012-08-22 | 山东新华制药股份有限公司 | Preparation method of aspirin enteric-coated sustained-release preparation |
| CN102973534A (en) * | 2012-12-14 | 2013-03-20 | 贵州信邦制药股份有限公司 | Enteric coating suitable for tablets |
-
2018
- 2018-08-03 CN CN201810878432.0A patent/CN108743555B/en active Active
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4775536A (en) * | 1986-02-24 | 1988-10-04 | Bristol-Myers Company | Enteric coated tablet and process for making |
| US4857337A (en) * | 1988-05-24 | 1989-08-15 | American Home Products Corp. (Del) | Enteric coated aspirin tablets |
| CN101088494A (en) * | 2006-06-16 | 2007-12-19 | 信越化学工业株式会社 | Enteric coated granule and method for preparing the same |
| CN102641254A (en) * | 2012-05-07 | 2012-08-22 | 山东新华制药股份有限公司 | Preparation method of aspirin enteric-coated sustained-release preparation |
| CN102973534A (en) * | 2012-12-14 | 2013-03-20 | 贵州信邦制药股份有限公司 | Enteric coating suitable for tablets |
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