CN114432256A - Paracetamol coated tablet and preparation method thereof - Google Patents
Paracetamol coated tablet and preparation method thereof Download PDFInfo
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- CN114432256A CN114432256A CN202111672845.1A CN202111672845A CN114432256A CN 114432256 A CN114432256 A CN 114432256A CN 202111672845 A CN202111672845 A CN 202111672845A CN 114432256 A CN114432256 A CN 114432256A
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- RZVAJINKPMORJF-UHFFFAOYSA-N Acetaminophen Chemical compound CC(=O)NC1=CC=C(O)C=C1 RZVAJINKPMORJF-UHFFFAOYSA-N 0.000 title claims abstract description 105
- 229960005489 paracetamol Drugs 0.000 title claims abstract description 55
- 238000002360 preparation method Methods 0.000 title claims abstract description 14
- 239000000463 material Substances 0.000 claims abstract description 77
- 238000000576 coating method Methods 0.000 claims abstract description 53
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims abstract description 49
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims abstract description 49
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims abstract description 49
- 239000011248 coating agent Substances 0.000 claims abstract description 47
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims abstract description 36
- 235000019359 magnesium stearate Nutrition 0.000 claims abstract description 18
- 229920000881 Modified starch Polymers 0.000 claims abstract description 11
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims abstract description 11
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims abstract description 11
- 229940075614 colloidal silicon dioxide Drugs 0.000 claims abstract description 11
- 229960000913 crospovidone Drugs 0.000 claims abstract description 11
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 claims abstract description 11
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 claims abstract description 11
- UIIMBOGNXHQVGW-UHFFFAOYSA-M Sodium bicarbonate Chemical compound [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 claims abstract description 10
- 229910000030 sodium bicarbonate Inorganic materials 0.000 claims abstract description 5
- 235000017557 sodium bicarbonate Nutrition 0.000 claims abstract description 5
- 239000000843 powder Substances 0.000 claims description 83
- 239000000203 mixture Substances 0.000 claims description 39
- 238000000034 method Methods 0.000 claims description 38
- 238000002156 mixing Methods 0.000 claims description 37
- 238000007873 sieving Methods 0.000 claims description 34
- 238000005303 weighing Methods 0.000 claims description 21
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims description 20
- 238000004090 dissolution Methods 0.000 claims description 17
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 14
- 238000005469 granulation Methods 0.000 claims description 13
- 230000003179 granulation Effects 0.000 claims description 13
- UIIMBOGNXHQVGW-DEQYMQKBSA-M Sodium bicarbonate-14C Chemical compound [Na+].O[14C]([O-])=O UIIMBOGNXHQVGW-DEQYMQKBSA-M 0.000 claims description 7
- 238000000889 atomisation Methods 0.000 claims description 7
- 238000007664 blowing Methods 0.000 claims description 7
- 239000002775 capsule Substances 0.000 claims description 7
- 238000001035 drying Methods 0.000 claims description 7
- 230000002572 peristaltic effect Effects 0.000 claims description 7
- 230000000750 progressive effect Effects 0.000 claims description 7
- 239000007787 solid Substances 0.000 claims description 7
- 239000007916 tablet composition Substances 0.000 claims description 7
- 238000000265 homogenisation Methods 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000003814 drug Substances 0.000 abstract description 5
- 230000000694 effects Effects 0.000 abstract description 4
- 208000002193 Pain Diseases 0.000 abstract description 3
- 230000036407 pain Effects 0.000 abstract description 3
- 239000000853 adhesive Substances 0.000 abstract description 2
- 230000001070 adhesive effect Effects 0.000 abstract description 2
- 230000005611 electricity Effects 0.000 abstract description 2
- 230000003068 static effect Effects 0.000 abstract description 2
- 229920003023 plastic Polymers 0.000 description 10
- 238000001514 detection method Methods 0.000 description 3
- BSYNRYMUTXBXSQ-UHFFFAOYSA-N Aspirin Chemical compound CC(=O)OC1=CC=CC=C1C(O)=O BSYNRYMUTXBXSQ-UHFFFAOYSA-N 0.000 description 2
- FZERHIULMFGESH-UHFFFAOYSA-N N-phenylacetamide Chemical group CC(=O)NC1=CC=CC=C1 FZERHIULMFGESH-UHFFFAOYSA-N 0.000 description 2
- 229960001138 acetylsalicylic acid Drugs 0.000 description 2
- 230000000202 analgesic effect Effects 0.000 description 2
- 230000015572 biosynthetic process Effects 0.000 description 2
- 230000001186 cumulative effect Effects 0.000 description 2
- 230000002401 inhibitory effect Effects 0.000 description 2
- 150000003180 prostaglandins Chemical class 0.000 description 2
- 238000003786 synthesis reaction Methods 0.000 description 2
- 208000000114 Pain Threshold Diseases 0.000 description 1
- 102000004005 Prostaglandin-endoperoxide synthases Human genes 0.000 description 1
- 108090000459 Prostaglandin-endoperoxide synthases Proteins 0.000 description 1
- 206010037660 Pyrexia Diseases 0.000 description 1
- 229960001413 acetanilide Drugs 0.000 description 1
- 230000001754 anti-pyretic effect Effects 0.000 description 1
- 239000003907 antipyretic analgesic agent Substances 0.000 description 1
- 210000004211 gastric acid Anatomy 0.000 description 1
- 230000002267 hypothalamic effect Effects 0.000 description 1
- 230000037040 pain threshold Effects 0.000 description 1
- 210000005259 peripheral blood Anatomy 0.000 description 1
- 239000011886 peripheral blood Substances 0.000 description 1
- 230000002093 peripheral effect Effects 0.000 description 1
- 230000035900 sweating Effects 0.000 description 1
- 230000028016 temperature homeostasis Effects 0.000 description 1
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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
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
- A61K31/167—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
-
- 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
- A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
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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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- 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
- A61K9/2095—Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
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- 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
- A61K9/2893—Tablet coating processes
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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Abstract
The invention discloses an acetaminophen coated tablet and a preparation method thereof, wherein the acetaminophen coated tablet comprises the following materials in percentage by mass: acetaminophen 74%, pregelatinized starch 11.2%, hydroxypropylcellulose 5%, sodium bicarbonate 4%, colloidal silicon dioxide 0.5%, crospovidone (pvpp XL-10) 2%, Hydroxypropylcellulose (HPC) 3%, magnesium stearate 0.3%. The acetaminophen content of the invention reaches 74%, the acetaminophen material has serious static electricity and poor viscosity, and is easy to crack and short tablets during tabletting and coating, and hydroxypropyl cellulose is used as an adhesive, so that the condition can be better improved; the disintegrating and dissolving speed of the medicine is accelerated, and the pain relieving effect can be exerted more quickly after the medicine is taken.
Description
Technical Field
The invention belongs to the technical field of pharmacy, and particularly relates to an acetaminophen coated tablet and a preparation method thereof.
Background
The acetaminophen coated tablet is acetanilide antipyretic analgesic. By inhibiting cyclooxygenase, synthesis of prostaglandin at hypothalamic thermoregulation center is selectively inhibited, peripheral blood vessel is expanded and sweating is caused to achieve the effect of relieving fever, and the intensity of the antipyretic effect is similar to that of aspirin; the traditional Chinese medicine composition has an analgesic effect by inhibiting synthesis and release of prostaglandin and the like and increasing pain threshold, belongs to a peripheral analgesic, has weaker effect than aspirin, and is only effective on light and moderate pain. In the process of improving the process research, the original preparation is found to be slow in disintegration and dissolution, the process is improved, sodium bicarbonate is added in the prescription, the tablet is rapidly disintegrated under the action of gastric acid after oral administration, and the dissolution is measured in 0.1mol/L hydrochloric acid solution at the speed of 30r/min of a paddle board, so that the dissolution can reach more than 80% in 3 min.
Disclosure of Invention
In view of the above, the main object of the present invention is to provide a paracetamol coated tablet and a preparation method thereof.
In order to achieve the purpose, the technical scheme of the invention is realized as follows:
the embodiment of the invention provides an acetaminophen coated tablet, which consists of the following materials in percentage by mass: acetaminophen 74%, pregelatinized starch 11.2%, hydroxypropylcellulose 5%, sodium bicarbonate 4%, colloidal silicon dioxide 0.5%, crospovidone (pvpp XL-10) 2%, Hydroxypropylcellulose (HPC) 3%, magnesium stearate 0.3%.
In the scheme, the coating powder is also included by 2.5 percent.
An embodiment of the present invention further provides a method for preparing an acetaminophen-coated tablet as described in any one of the above schemes, the method comprising:
weighing 74% of acetaminophen, 11.2% of pregelatinized starch, 5% of hydroxypropyl cellulose, 4% of sodium bicarbonate, 0.5% of colloidal silicon dioxide and 2% of crospovidone (pvpp XL-10) according to mass percentage;
preliminarily mixing the weighed materials by a three-dimensional mixer, sieving the materials by a 24-mesh sieve to disperse lumps, and uniformly mixing the materials by the three-dimensional mixer again to obtain a mixed material;
granulating the mixed materials by a dry method granulator, sieving the obtained materials by a 50-mesh sieve, weighing the weights of the coarse powder and the fine powder respectively, granulating the fine powder again, continuously sieving the obtained materials by the 50-mesh sieve, and circulating the steps to obtain the final coarse powder and the final fine powder;
weighing 3% of hydroxypropyl cellulose (HPC) and 0.3% of magnesium stearate according to the granulation yield;
and (3) sieving the hydroxypropyl cellulose (HPC) and the fine powder in an equivalent progressive addition mode by a 50-mesh sieve for premixing, then mixing with the coarse powder by a three-dimensional mixer, adding magnesium stearate after uniformly mixing, continuing mixing for 2min, and obtaining a total mixed material, namely acetaminophen powder after mixing.
In the above scheme, the preparation method further comprises: the total blend was tableted according to the capsule tablet formulation.
In the above scheme, the preparation method further comprises: after tabletting, coating solution is prepared by 50 percent of ethanol, the solid content of the coating solution is 8 percent (g/g), and the tablet is coated to obtain the acetaminophen coated tablet.
In the scheme, the materials are uniformly mixed again through the three-dimensional mixer, specifically, the materials are uniformly mixed again through the three-dimensional mixer until the RSD is less than or equal to 3.0%, and the bulk density of the obtained materials is 0.35-0.45 g/cm3。
In the scheme, the dry granulating machine is operated under the condition that the no-load pressure is 3-4.0MPa, and the coarse powder accounts for not less than 85% of the final coarse powder and fine powder.
In the scheme, the bulk density of the total mixed material is 0.6-0.7 g/cm3The tap density is 0.7 to 0.8g/cm3。
In the scheme, the tablet weight difference is controlled to be +/-2% in the tabletting process, and the hardness is in the range of 90-120N; taking plain tablets to determine weight difference, friability and content, and a dissolution curve of 0.05mol/L hydrochloric acid medium and 30r/min by a paddle method.
In the scheme, the air inlet temperature is 40 ℃, the air outlet temperature is controlled to be 32-40 ℃, the atomization pressure and the blowing pressure are both 0.1MPa, the rotating speed of a peristaltic pump is 11r/min, the rotating speed of a pot body is 8r/min, the coating is preheated before coating, and the rotating speed of the coating pot is 2r/min during preheating; and drying the coated tablets at the coating pan rotation speed of 2 r/min.
Compared with the prior art, the content of the acetaminophen reaches 74%, the acetaminophen material has serious static electricity and poor viscosity, and is easy to crack and short during tabletting and coating, and the hydroxypropyl cellulose is used as an adhesive, so that the condition can be better improved; the disintegrating and dissolving speed of the medicine is accelerated, and the pain relieving effect can be exerted more quickly after the medicine is taken.
Drawings
The accompanying drawings, which are included to provide a further understanding of the invention and are incorporated in and constitute a part of this specification, illustrate embodiment(s) of the invention and together with the description serve to explain the invention without limiting the invention. In the drawings:
FIG. 1 is a graph showing the measured dissolution profile of acetaminophen-coated tablets prepared in accordance with the present invention.
Detailed Description
In order to make the objects, technical solutions and advantages of the present invention more apparent, the present invention is described in further detail below with reference to the accompanying drawings and embodiments. It should be understood that the specific embodiments described herein are merely illustrative of the invention and are not intended to limit the invention.
It should be noted that, in this document, the terms "comprises," "comprising," or any other variation thereof, are intended to cover a non-exclusive inclusion, such that a process, article, or apparatus that comprises a list of elements does not include only those elements but may include other elements not expressly listed or inherent to such process, article, or apparatus. Without further limitation, an element defined by the phrase "comprising an … …" does not exclude the presence of other like elements in a process, article, or apparatus that comprises the element.
The embodiment of the invention provides an acetaminophen coated tablet, which consists of the following materials in percentage by mass: acetaminophen 74%, pregelatinized starch 11.2%, hydroxypropylcellulose 5%, sodium bicarbonate 4%, colloidal silicon dioxide 0.5%, crospovidone (pvpp XL-10) 2%, Hydroxypropylcellulose (HPC) 3%, magnesium stearate 0.3%.
Further, the coating powder is also included by 2.5 percent.
The embodiment of the invention also provides a preparation method of the acetaminophen coated tablet, which is realized by the following steps:
step 101: weighing 74% of acetaminophen, 11.2% of pregelatinized starch, 5% of hydroxypropyl cellulose, 4% of sodium bicarbonate, 0.5% of colloidal silicon dioxide and 2% of crospovidone (pvpp XL-10) according to mass percentage;
step 102: preliminarily mixing the weighed materials by a three-dimensional mixer, sieving the materials by a 24-mesh sieve to disperse lumps, and uniformly mixing the materials by the three-dimensional mixer again to obtain a mixed material;
specifically, the materials are uniformly mixed again by a three-dimensional mixer until the RSD is less than or equal to 3.0 percent, and the bulk density of the obtained materials is 0.35-0.45 g/cm3。
Step 103: granulating the mixed materials by a dry granulating machine, sieving the obtained materials by a 50-mesh sieve, weighing the weights of the coarse powder and the fine powder respectively, granulating the fine powder again, continuously sieving the obtained materials by the 50-mesh sieve, and circulating the steps to obtain final coarse powder and fine powder;
specifically, the dry granulator granulation is operated under an unloaded pressure of 3-4.0MPa, and the ratio of coarse powder to fine powder in the final coarse powder and fine powder is not less than 85%.
Step 104: weighing 3% of hydroxypropyl cellulose (HPC) and 0.3% of magnesium stearate according to the granulation yield;
step 105: and (3) sieving the hydroxypropyl cellulose (HPC) and the fine powder in an equivalent progressive addition mode, sieving the mixture with a 50-mesh sieve, premixing the mixture, mixing the mixture with the coarse powder through a three-dimensional mixer, adding magnesium stearate after the mixture is uniformly mixed, continuously mixing for 2min, and obtaining a total mixed material, namely acetaminophen powder after the mixing is finished.
Specifically, the bulk density of the total mixed material is 0.6-0.7 g/cm3The tap density is 0.7 to 0.8g/cm3。
Step 106: the total blend was compressed according to the capsule tablet formulation.
Specifically, the difference of tablet weight in the tabletting process is controlled to be +/-2%, and the hardness is in the range of 90-120N; taking plain tablets to determine weight difference, friability and content, and a dissolution curve of 0.05mol/L hydrochloric acid medium and 30r/min by a paddle method.
Step 107: after tabletting, coating solution is prepared by 50 percent of ethanol, the solid content of the coating solution is 8 percent (g/g), and the tablet is coated to obtain the acetaminophen coated tablet.
Specifically, the air inlet temperature is 40 ℃ in the coating process, the air exhaust temperature is controlled to be 32-40 ℃, the atomization pressure and the blowing pressure are both 0.1MPa, the rotating speed of a peristaltic pump is 11r/min, the rotating speed of a pot body is 8r/min, the coating is preheated before coating, and the rotating speed of the coating pot is 2r/min during preheating; and drying the coated tablets at the coating pan rotation speed of 2 r/min.
Step 108: the aluminum-plastic blister package is adopted, and the number of each plate is determined according to the actual aluminum-plastic die condition.
Example 1
The embodiment 1 of the invention provides a preparation method of an acetaminophen coated tablet, which is realized by the following steps:
step 101: weighing 74% of acetaminophen, 11.2% of pregelatinized starch, 5% of hydroxypropyl cellulose, 4% of sodium bicarbonate, 0.5% of colloidal silicon dioxide and 2% of crospovidone (pvpp XL-10) according to mass percentage;
step 102: preliminarily mixing the weighed materials by a three-dimensional mixer, sieving the materials by a 24-mesh sieve to disperse lumps, and uniformly mixing the materials by the three-dimensional mixer again to obtain a mixed material;
specifically, again, the mixture was mixed by the three-dimensional mixer until the RSD became 2.0%, and the bulk density of the material obtained was 0.35g/cm3。
Step 103: granulating the mixed materials by a dry method granulator, sieving the obtained materials by a 50-mesh sieve, weighing the weights of the coarse powder and the fine powder respectively, granulating the fine powder again, continuously sieving the obtained materials by the 50-mesh sieve, and circulating the steps to obtain the final coarse powder and the final fine powder;
specifically, the dry granulator granulation is operated under an unloaded pressure of 3MPa, and the ratio of coarse powder to fine powder in the final coarse powder and fine powder is not less than 85%.
Step 104: weighing 3% of hydroxypropyl cellulose (HPC) and 0.3% of magnesium stearate according to the granulation yield;
step 105: and (3) sieving the hydroxypropyl cellulose (HPC) and the fine powder in an equivalent progressive addition mode, sieving the mixture with a 50-mesh sieve, premixing the mixture, mixing the mixture with the coarse powder through a three-dimensional mixer, adding magnesium stearate after the mixture is uniformly mixed, continuously mixing for 2min, and obtaining a total mixed material, namely acetaminophen powder after the mixing is finished.
Specifically, the bulk density of the total mixture is 0.6g/cm3Tap density of 0.7g/cm3。
Step 106: the total blend was tableted according to the capsule tablet formulation.
Specifically, the weight difference of tablets in the tabletting process is controlled to be +/-2 percent, and the hardness is in the range of 90N; taking plain tablets to determine weight difference, friability and content, and a dissolution curve of 0.05mol/L hydrochloric acid medium and 30r/min by a paddle method.
Step 107: after tabletting, coating solution is prepared by 50 percent of ethanol, the solid content of the coating solution is 8 percent (g/g), and the tablet is coated to obtain the acetaminophen coated tablet.
Specifically, the air inlet temperature is 40 ℃ in the coating process, the air exhaust temperature is controlled to be 32 ℃, the atomization pressure and the blowing pressure are both 0.1MPa, the rotating speed of a peristaltic pump is 11r/min, the rotating speed of a pan body is 8r/min, the coating is preheated before coating, and the rotating speed of the coating pan is 2r/min during preheating; and drying the coated tablets at the coating pan rotation speed of 2 r/min.
Step 108: the aluminum-plastic blister package is adopted, and the number of each plate is determined according to the actual aluminum-plastic die condition.
Example 2
The embodiment 2 of the invention provides a preparation method of an acetaminophen coated tablet, which is realized by the following steps:
step 101: weighing 74% of acetaminophen, 11.2% of pregelatinized starch, 5% of hydroxypropyl cellulose, 4% of sodium bicarbonate, 0.5% of colloidal silicon dioxide and 2% of crospovidone (pvpp XL-10) according to mass percentage;
step 102: preliminarily mixing the weighed materials by a three-dimensional mixer, sieving the materials by a 24-mesh sieve to disperse lumps, and uniformly mixing the materials by the three-dimensional mixer again to obtain a mixed material;
specifically, again, the mixture was mixed by a three-dimensional mixer until the RSD was 3%, and the bulk density of the obtained material was 0.45g/cm3。
Step 103: granulating the mixed materials by a dry method granulator, sieving the obtained materials by a 50-mesh sieve, weighing the weights of the coarse powder and the fine powder respectively, granulating the fine powder again, continuously sieving the obtained materials by the 50-mesh sieve, and circulating the steps to obtain the final coarse powder and the final fine powder;
specifically, the dry granulator granulation is operated at an unloaded pressure of 4.0MPa, and the ratio of coarse powder to fine powder in the final coarse powder and fine powder is not less than 85%.
Step 104: weighing 3% of hydroxypropyl cellulose (HPC) and 0.3% of magnesium stearate according to the granulation yield;
step 105: and (3) sieving the hydroxypropyl cellulose (HPC) and the fine powder in an equivalent progressive addition mode, sieving the mixture with a 50-mesh sieve, premixing the mixture, mixing the mixture with the coarse powder through a three-dimensional mixer, adding magnesium stearate after the mixture is uniformly mixed, continuously mixing for 2min, and obtaining a total mixed material, namely acetaminophen powder after the mixing is finished.
Specifically, the bulk density of the total mixture is 0.7g/cm3Tap density of 0.8g/cm3。
Step 106: the total blend was compressed according to the capsule tablet formulation.
Specifically, the weight difference of tablets in the tabletting process is controlled to be +/-2 percent, and the hardness is within the range of 120N; taking plain tablets to determine weight difference, friability and content, and a dissolution curve of 0.05mol/L hydrochloric acid medium and 30r/min by a paddle method.
Step 107: after tabletting, coating solution is prepared by 50 percent of ethanol, the solid content of the coating solution is 8 percent (g/g), and the tablet is coated to obtain the acetaminophen coated tablet.
Specifically, the air inlet temperature is 40 ℃ in the coating process, the air exhaust temperature is controlled to be 40 ℃, the atomization pressure and the blowing pressure are both 0.1MPa, the rotating speed of a peristaltic pump is 11r/min, the rotating speed of a pan body is 8r/min, the coating is preheated before coating, and the rotating speed of the coating pan is 2r/min during preheating; and drying the coated tablets at the coating pan rotation speed of 2 r/min.
Step 108: the aluminum-plastic blister package is adopted, and the number of each plate is determined according to the actual aluminum-plastic die condition.
Example 3
Embodiment 3 of the present invention provides a method for preparing a paracetamol coated tablet, which is implemented by the following steps:
step 101: weighing 74% of acetaminophen, 11.2% of pregelatinized starch, 5% of hydroxypropyl cellulose, 4% of sodium bicarbonate, 0.5% of colloidal silicon dioxide and 2% of crospovidone (pvpp XL-10) according to mass percentage;
step 102: preliminarily mixing the weighed materials by a three-dimensional mixer, sieving the materials by a 24-mesh sieve to disperse lumps, and uniformly mixing the materials by the three-dimensional mixer again to obtain a mixed material;
specifically, the materials are uniformly mixed again by a three-dimensional mixer until the RSD is 1.0 percent, and the bulk density of the obtained materials is 0.35-0.45 g/cm3。
Step 103: granulating the mixed materials by a dry method granulator, sieving the obtained materials by a 50-mesh sieve, weighing the weights of the coarse powder and the fine powder respectively, granulating the fine powder again, continuously sieving the obtained materials by the 50-mesh sieve, and circulating the steps to obtain the final coarse powder and the final fine powder;
specifically, the dry granulator granulation is operated under an unloaded pressure of 3.1MPa, and the ratio of coarse powder to fine powder in the final coarse powder and fine powder is not less than 85%.
Step 104: weighing 3% of hydroxypropyl cellulose (HPC) and 0.3% of magnesium stearate according to the granulation yield;
step 105: and (3) sieving the hydroxypropyl cellulose (HPC) and the fine powder in an equivalent progressive addition mode, sieving the mixture with a 50-mesh sieve, premixing the mixture, mixing the mixture with the coarse powder through a three-dimensional mixer, adding magnesium stearate after the mixture is uniformly mixed, continuously mixing for 2min, and obtaining a total mixed material, namely acetaminophen powder after the mixing is finished.
Specifically, the bulk density of the total mixture is 0.65g/cm3Tap density of 0.75g/cm3。
Step 106: the total blend was compressed according to the capsule tablet formulation.
Specifically, the weight difference of tablets in the tabletting process is controlled to be +/-2%, and the hardness is within 1050N; taking plain tablets to determine weight difference, friability and content, and a dissolution curve of 0.05mol/L hydrochloric acid medium and 30r/min by a paddle method.
Step 107: after tabletting, coating solution is prepared by 50 percent of ethanol, the solid content of the coating solution is 8 percent (g/g), and the tablet is coated to obtain the acetaminophen coated tablet.
Specifically, the air inlet temperature is 40 ℃ in the coating process, the air exhaust temperature is controlled to be 36 ℃, the atomization pressure and the blowing pressure are both 0.1MPa, the rotating speed of a peristaltic pump is 11r/min, the rotating speed of a pan body is 8r/min, the coating is preheated before coating, and the rotating speed of the coating pan is 2r/min during preheating; and drying the coated tablets at the coating pan rotation speed of 2 r/min.
Step 108: the aluminum-plastic blister package is adopted, and the number of each plate is determined according to the actual aluminum-plastic die condition.
Example 4
Embodiment 4 of the present invention provides a method for preparing a paracetamol coated tablet, which is implemented by the following steps:
step 101: weighing 74% of acetaminophen, 11.2% of pregelatinized starch, 5% of hydroxypropyl cellulose, 4% of sodium bicarbonate, 0.5% of colloidal silicon dioxide and 2% of crospovidone (pvpp XL-10) according to mass percentage;
step 102: preliminarily mixing the weighed materials by a three-dimensional mixer, sieving the materials by a 24-mesh sieve to disperse lumps, and uniformly mixing the materials by the three-dimensional mixer again to obtain a mixed material;
specifically, uniformly mixing the materials again through a three-dimensional mixer until the RSD is 1.5%, and obtaining the bulk density of the materials of 0.35-0.45g/cm3。
Step 103: granulating the mixed materials by a dry method granulator, sieving the obtained materials by a 50-mesh sieve, weighing the weights of the coarse powder and the fine powder respectively, granulating the fine powder again, continuously sieving the obtained materials by the 50-mesh sieve, and circulating the steps to obtain the final coarse powder and the final fine powder;
specifically, the dry granulator granulation is operated under an unloaded pressure of 3.1MPa, and the ratio of coarse powder to fine powder in the final coarse powder and fine powder is not less than 85%.
Step 104: weighing 3% of hydroxypropyl cellulose (HPC) and 0.3% of magnesium stearate according to the granulation yield;
step 105: and (3) sieving the hydroxypropyl cellulose (HPC) and the fine powder in an equivalent progressive addition mode, sieving the mixture with a 50-mesh sieve, premixing the mixture, mixing the mixture with the coarse powder through a three-dimensional mixer, adding magnesium stearate after the mixture is uniformly mixed, continuously mixing for 2min, and obtaining a total mixed material, namely acetaminophen powder after the mixing is finished.
Specifically, the bulk density of the total mixture is 0.64g/cm3Tap density of 0.74g/cm3。
Detection indexes of the total mixed materials are as follows: angle of repose, content
| Detecting items | Control standard |
| Angle of repose (°) | ≤45 |
| Content (mg/g) | 717.81～762.2 |
Step 106: the total blend was compressed according to the capsule tablet formulation.
Specifically, the weight difference of tablets in the tabletting process is controlled to be +/-2 percent, and the hardness is within the range of 110N; taking plain tablets to determine weight difference, friability and content, and a dissolution curve of 0.05mol/L hydrochloric acid medium and 30r/min by a paddle method.
Detection indexes of the plain film are as follows: the difference of tablet weight, friability, content and dissolution profile (0.03mol/L hydrochloric acid medium, 30r/min by paddle method) are shown in FIG. 1.
| Detecting items | Control standard |
| Difference in tablet weight | ±3.0％ |
| Degree of friability | ≤0.6％ |
| Dissolution curve | The cumulative dissolution amount is more than or equal to 80 percent in 3min |
| Content (wt.) | 97％～103％ |
Step 107: after tabletting, coating solution is prepared by 50 percent of ethanol, the solid content of the coating solution is 8 percent (g/g), and the tablet is coated to obtain the acetaminophen coated tablet.
Specifically, the air inlet temperature is 40 ℃ in the coating process, the air exhaust temperature is controlled to be 36 ℃, the atomization pressure and the blowing pressure are both 0.1MPa, the rotating speed of a peristaltic pump is 11r/min, the rotating speed of a pan body is 8r/min, the coating is preheated before coating, and the rotating speed of the coating pan is 2r/min during preheating; and drying the coated tablets at the coating pan rotation speed of 2 r/min.
Detection indexes of the coated tablets are as follows: tablet weight difference and dissolution curve (0.03mol/L hydrochloric acid medium, 30r/min by paddle method).
| Detecting items | Control standard |
| Difference in tablet weight | ±3.0％ |
| Dissolution curve | The cumulative dissolution amount is more than or equal to 80 percent in 3min |
Step 108: the aluminum-plastic blister package is adopted, and the number of each plate is determined according to the actual aluminum-plastic die condition.
The above description is only a preferred embodiment of the present invention, and is not intended to limit the scope of the present invention.
Claims (10)
1. An acetaminophen coated tablet is characterized by comprising the following materials in percentage by mass: acetaminophen 74%, pregelatinized starch 11.2%, hydroxypropylcellulose 5%, sodium bicarbonate 4%, colloidal silicon dioxide 0.5%, crospovidone (pvpp XL-10) 2%, Hydroxypropylcellulose (HPC) 3%, magnesium stearate 0.3%.
2. The acetaminophen coated tablet of claim 1, further comprising a coating powder of 2.5%.
3. A method for preparing the acetaminophen-coated tablet of any one of claims 1-2, comprising:
weighing 74% of acetaminophen, 11.2% of pregelatinized starch, 5% of hydroxypropyl cellulose, 4% of sodium bicarbonate, 0.5% of colloidal silicon dioxide and 2% of crospovidone (pvpp XL-10) according to mass percentage;
preliminarily mixing the weighed materials by a three-dimensional mixer, sieving the materials by a 24-mesh sieve to disperse lumps, and uniformly mixing the materials by the three-dimensional mixer again to obtain a mixed material;
granulating the mixed materials by a dry method granulator, sieving the obtained materials by a 50-mesh sieve, weighing the weights of the coarse powder and the fine powder respectively, granulating the fine powder again, continuously sieving the obtained materials by the 50-mesh sieve, and circulating the steps to obtain the final coarse powder and the final fine powder;
weighing 3% of hydroxypropyl cellulose (HPC) and 0.3% of magnesium stearate according to the granulation yield;
and (3) sieving the hydroxypropyl cellulose (HPC) and the fine powder in an equivalent progressive addition mode, sieving the mixture with a 50-mesh sieve, premixing the mixture, mixing the mixture with the coarse powder through a three-dimensional mixer, adding magnesium stearate after the mixture is uniformly mixed, continuously mixing for 2min, and obtaining a total mixed material, namely acetaminophen powder after the mixing is finished.
4. A method of preparing an acetaminophen coated tablet according to claim 3, wherein the method further comprises: the total blend was compressed according to the capsule tablet formulation.
5. The method of preparing an acetaminophen coated tablet according to claim 4, further comprising: after tabletting, coating solution is prepared by 50 percent of ethanol, the solid content of the coating solution is 8 percent (g/g), and the tablet is coated to obtain the acetaminophen coated tablet.
6. Method for the preparation of an acetaminophen coated tablet according to any one of claims 3-5, wherein the homogenisation is performed again by means of a three-dimensional mixer, in particular again to RSDNot more than 3.0 percent, and the bulk density of the obtained material is 0.35 to 0.45g/cm3。
7. A process for the preparation of acetaminophen coated tablets as claimed in claim 6 wherein the dry granulator granulation is operated at an idling pressure of between 3 and 4.0MPa and the ratio of coarse to fine in the final coarse and fine powders is not less than 85%.
8. The method for producing an acetaminophen-coated tablet according to claim 7, wherein the bulk density of the total blend is 0.6 to 0.7g/cm3The tap density is 0.7 to 0.8g/cm3。
9. The method for preparing an acetaminophen-coated tablet according to claim 8, wherein the difference in tablet weight during tabletting is controlled to ± 2%, and the hardness is in the range of 90 to 120N; taking plain tablets to determine weight difference, friability and content, and a dissolution curve of 0.05mol/L hydrochloric acid medium and 30r/min by a paddle method.
10. The preparation method of acetaminophen coated tablet as claimed in claim 9, wherein the air inlet temperature in the coating process is 40 ℃, the air outlet temperature is controlled to be 32-40 ℃, the atomization pressure and the blowing pressure are both 0.1MPa, the rotation speed of a peristaltic pump is 11r/min, the rotation speed of a pot body is 8r/min, the coating is preheated before coating, and the rotation speed of the coating pot is 2r/min during preheating; and drying the coated tablets at the coating pan rotation speed of 2 r/min.
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