CN114053234A - Acarbose tablet and preparation method thereof - Google Patents
Acarbose tablet and preparation method thereof Download PDFInfo
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- CN114053234A CN114053234A CN202111632399.1A CN202111632399A CN114053234A CN 114053234 A CN114053234 A CN 114053234A CN 202111632399 A CN202111632399 A CN 202111632399A CN 114053234 A CN114053234 A CN 114053234A
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- acarbose
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- corn starch
- magnesium stearate
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- XUFXOAAUWZOOIT-SXARVLRPSA-N (2R,3R,4R,5S,6R)-5-[[(2R,3R,4R,5S,6R)-5-[[(2R,3R,4S,5S,6R)-3,4-dihydroxy-6-methyl-5-[[(1S,4R,5S,6S)-4,5,6-trihydroxy-3-(hydroxymethyl)-1-cyclohex-2-enyl]amino]-2-oxanyl]oxy]-3,4-dihydroxy-6-(hydroxymethyl)-2-oxanyl]oxy]-6-(hydroxymethyl)oxane-2,3,4-triol Chemical compound O([C@H]1O[C@H](CO)[C@H]([C@@H]([C@H]1O)O)O[C@H]1O[C@@H]([C@H]([C@H](O)[C@H]1O)N[C@@H]1[C@@H]([C@@H](O)[C@H](O)C(CO)=C1)O)C)[C@@H]1[C@@H](CO)O[C@@H](O)[C@H](O)[C@H]1O XUFXOAAUWZOOIT-SXARVLRPSA-N 0.000 title claims abstract description 77
- 229960002632 acarbose Drugs 0.000 title claims abstract description 77
- XUFXOAAUWZOOIT-UHFFFAOYSA-N acarviostatin I01 Natural products OC1C(O)C(NC2C(C(O)C(O)C(CO)=C2)O)C(C)OC1OC(C(C1O)O)C(CO)OC1OC1C(CO)OC(O)C(O)C1O XUFXOAAUWZOOIT-UHFFFAOYSA-N 0.000 title claims abstract description 77
- 238000002360 preparation method Methods 0.000 title claims abstract description 20
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims abstract description 74
- 229920002261 Corn starch Polymers 0.000 claims abstract description 44
- 239000008120 corn starch Substances 0.000 claims abstract description 44
- 235000019359 magnesium stearate Nutrition 0.000 claims abstract description 37
- 238000007873 sieving Methods 0.000 claims abstract description 35
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims abstract description 34
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims abstract description 34
- 239000008108 microcrystalline cellulose Substances 0.000 claims abstract description 34
- 229940016286 microcrystalline cellulose Drugs 0.000 claims abstract description 34
- 238000002156 mixing Methods 0.000 claims abstract description 29
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims abstract description 26
- 229940075614 colloidal silicon dioxide Drugs 0.000 claims abstract description 26
- 238000004806 packaging method and process Methods 0.000 claims abstract description 23
- 238000000034 method Methods 0.000 claims abstract description 20
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 16
- 238000005303 weighing Methods 0.000 claims abstract description 16
- 239000004033 plastic Substances 0.000 claims abstract description 13
- 230000008569 process Effects 0.000 claims abstract description 13
- 239000000463 material Substances 0.000 claims abstract description 12
- 239000000843 powder Substances 0.000 claims abstract description 11
- 239000000945 filler Substances 0.000 claims abstract description 9
- 238000004519 manufacturing process Methods 0.000 claims abstract description 7
- 239000000835 fiber Substances 0.000 claims description 6
- 239000000314 lubricant Substances 0.000 claims description 6
- 238000003825 pressing Methods 0.000 claims description 5
- 238000000338 in vitro Methods 0.000 abstract description 5
- 238000007907 direct compression Methods 0.000 abstract description 3
- 239000000825 pharmaceutical preparation Substances 0.000 abstract description 3
- 229940099112 cornstarch Drugs 0.000 abstract 1
- 238000004090 dissolution Methods 0.000 description 13
- 230000000052 comparative effect Effects 0.000 description 8
- 238000007789 sealing Methods 0.000 description 6
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 4
- 238000012360 testing method Methods 0.000 description 4
- 238000000227 grinding Methods 0.000 description 3
- 239000000243 solution Substances 0.000 description 3
- 239000008280 blood Substances 0.000 description 2
- 210000004369 blood Anatomy 0.000 description 2
- 238000001727 in vivo Methods 0.000 description 2
- 229920001542 oligosaccharide Polymers 0.000 description 2
- 150000002482 oligosaccharides Chemical class 0.000 description 2
- 238000011160 research Methods 0.000 description 2
- 238000005550 wet granulation Methods 0.000 description 2
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 description 1
- 102100026189 Beta-galactosidase Human genes 0.000 description 1
- 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 1
- 108090000604 Hydrolases Proteins 0.000 description 1
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- 108010059881 Lactase Proteins 0.000 description 1
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- 201000010538 Lactose Intolerance Diseases 0.000 description 1
- 229910019142 PO4 Inorganic materials 0.000 description 1
- 102000001746 Pancreatic alpha-Amylases Human genes 0.000 description 1
- 108010029785 Pancreatic alpha-Amylases Proteins 0.000 description 1
- 230000002159 abnormal effect Effects 0.000 description 1
- 239000008351 acetate buffer Substances 0.000 description 1
- 230000009471 action Effects 0.000 description 1
- XAGFODPZIPBFFR-UHFFFAOYSA-N aluminium Chemical compound [Al] XAGFODPZIPBFFR-UHFFFAOYSA-N 0.000 description 1
- 229910052782 aluminium Inorganic materials 0.000 description 1
- 108010005774 beta-Galactosidase Proteins 0.000 description 1
- 230000004071 biological effect Effects 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 150000001720 carbohydrates Chemical class 0.000 description 1
- 235000014633 carbohydrates Nutrition 0.000 description 1
- 230000015556 catabolic process Effects 0.000 description 1
- 230000006957 competitive inhibition Effects 0.000 description 1
- 238000006731 degradation reaction Methods 0.000 description 1
- 230000003111 delayed effect Effects 0.000 description 1
- 206010012601 diabetes mellitus Diseases 0.000 description 1
- 230000004069 differentiation Effects 0.000 description 1
- 230000029087 digestion Effects 0.000 description 1
- 239000003085 diluting agent Substances 0.000 description 1
- 208000016097 disease of metabolism Diseases 0.000 description 1
- 238000007922 dissolution test Methods 0.000 description 1
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- 230000002401 inhibitory effect Effects 0.000 description 1
- 230000003914 insulin secretion Effects 0.000 description 1
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- 229940116108 lactase Drugs 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
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- 239000000203 mixture Substances 0.000 description 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 1
- 239000010452 phosphate Substances 0.000 description 1
- 239000008055 phosphate buffer solution Substances 0.000 description 1
- 238000003908 quality control method Methods 0.000 description 1
- 230000001105 regulatory effect Effects 0.000 description 1
- 230000006965 reversible inhibition Effects 0.000 description 1
- 238000005070 sampling Methods 0.000 description 1
- 230000035945 sensitivity Effects 0.000 description 1
- XUIMIQQOPSSXEZ-OUBTZVSYSA-N silicon-29 atom Chemical group [29Si] XUIMIQQOPSSXEZ-OUBTZVSYSA-N 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 description 1
Images
Classifications
-
- 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
- A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
- A61K31/7036—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin having at least one amino group directly attached to the carbocyclic ring, e.g. streptomycin, gentamycin, amikacin, validamycin, fortimicins
-
- 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
-
- 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
- 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
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
Abstract
The invention relates to the technical field of pharmaceutical preparations, and particularly discloses an acarbose tablet and a preparation method thereof, wherein the acarbose tablet comprises the following steps: sieving corn starch, microcrystalline cellulose and magnesium stearate respectively; after the sieving is finished, weighing, adding the weighed acarbose, corn starch, colloidal silicon dioxide and microcrystalline cellulose into a three-dimensional motion mixer, mixing, and adding magnesium stearate for mixing; respectively adding the mixed materials into a hopper, and starting a tablet press to perform tabletting; and (4) carrying out aluminum-plastic packaging by adopting a high-speed blister packaging machine. The invention adopts a powder direct compression process and a filler with high water content, improves the hardness of the tablet and regulates the release of the tablet. The tablet is prepared by directly mixing the acarbose and the colloidal silicon dioxide, adding the magnesium stearate, and tabletting, and has the advantages of simple preparation process, short production period and high efficiency. The prepared acarbose tablet can ensure that the in-vitro release behavior is similar to that of the original product, and can also ensure the stability of the tablet.
Description
Technical Field
The invention relates to the technical field of pharmaceutical preparations, in particular to acarbose tablets and a preparation method thereof.
Background
Diabetes is a widespread metabolic disease that is initiated primarily by elevated blood glucose due to abnormal insulin secretion or impaired other biological effects. Acarbose is a complex oligosaccharide, and the action mechanism of acarbose is mainly competitive and reversible inhibition of pancreatic alpha-amylase and intestinal alpha-glucoside hydrolase, so that digestion of ingested carbohydrates is delayed, and the purpose of reducing blood sugar is achieved. Acarbose has no inhibitory effect on lactase and therefore does not cause lactose intolerance.
Acarbose is an oligosaccharide obtained by microbial fermentation, and is mainly used for treating type 2 diabetes. Acarbose currently exists in related dosage forms such as tablets and capsules. The tablet is imported domestically at present, the specifications are 50mg and 100mg, the imported countries are Germany and Portugal, wherein 'Baitang apple' of Germany Bayer is a primary product, and the tablet is marketed in Germany in 1990 and domestic in 1995.
Acarbose is hygroscopic and unstable to heat. The conventional wet granulation process is liable to cause degradation of acarbose, and thus is not suitable for the wet granulation process. If dry granulation and tabletting are adopted, the process is complex and the production cost is high. For the reasons mentioned above, acarbose tablets were prepared by direct powder pressing. Through experiments, the conventional commercial auxiliary materials such as microcrystalline cellulose, lactose, corn starch and the like are used as diluents, the water content is low, the compressibility of the powder is general, although the stability of the tablet can meet corresponding requirements, the hardness of the tablet is lower than that of the original tablet, and the dissolution behavior of the tablet is greatly different from that of the original tablet.
Disclosure of Invention
The invention aims to provide an acarbose tablet and a preparation method thereof, so that the prepared acarbose tablet can ensure that the in-vitro release behavior is similar to that of the original product, and the stability of the tablet can be ensured.
In order to achieve the purpose, the acarbose tablet adopted by the invention is prepared by mixing and directly pressing powders according to the weight percentage and comprises the following components:
40-60 parts of acarbose, 40-100 parts of a filling agent, 0.1-0.5 part of a glidant and 0.2-1 part of a lubricant.
Wherein the filler is corn starch and microcrystalline cellulose.
Wherein the glidant is colloidal silicon dioxide.
Wherein the lubricant is magnesium stearate.
Wherein the water content of the corn starch is 11-14%.
The invention also provides a preparation method of the acarbose tablets, which comprises the following steps:
sieving said corn starch, said microcrystalline fiber, and said magnesium stearate separately;
weighing after the sieving is finished, adding the weighed acarbose, the corn starch, the colloidal silicon dioxide and the microcrystalline cellulose into a three-dimensional motion mixer for mixing, and then adding the magnesium stearate for mixing;
respectively adding the mixed materials into a hopper, and starting a tablet press to perform tabletting;
and (4) carrying out aluminum-plastic packaging by adopting a high-speed blister packaging machine.
Wherein, the specific steps of respectively sieving the corn starch, the microcrystalline fibers and the magnesium stearate are as follows:
and sieving the corn starch and the microcrystalline cellulose by a 80-mesh sieve, and sieving the magnesium stearate by a 40-mesh sieve.
Wherein, the concrete steps of weighing after the sieving is completed are as follows:
weighing the acarbose, the corn starch, the microcrystalline cellulose, the colloidal silicon dioxide and the magnesium stearate according to a mass ratio.
Wherein, the three-dimensional motion mixer adopts an SYH-50 type three-dimensional motion mixer.
According to the acarbose tablet and the preparation method thereof, the corn starch, the microcrystalline fiber and the magnesium stearate are respectively sieved; weighing after the sieving is finished, adding the weighed acarbose, the corn starch, the colloidal silicon dioxide and the microcrystalline cellulose into a three-dimensional motion mixer for mixing, and then adding the magnesium stearate for mixing; respectively adding the mixed materials into a hopper, and starting a tablet press to perform tabletting; and (4) carrying out aluminum-plastic packaging by adopting a high-speed blister packaging machine. The invention adopts a powder direct compression process and the filler with high water content, improves the hardness of the tablet and regulates the release of the tablet. The acarbose and the colloidal silicon dioxide are directly mixed and added with the magnesium stearate for tabletting, and the preparation method has the advantages of simple preparation process, short production period and high production efficiency. The prepared acarbose tablet can ensure that the in-vitro release behavior of the acarbose tablet is similar to that of the original ground product 'baitang apple', and can also ensure the stability of the acarbose tablet.
Drawings
In order to more clearly illustrate the embodiments of the present invention or the technical solutions in the prior art, the drawings used in the description of the embodiments or the prior art will be briefly described below, it is obvious that the drawings in the following description are only some embodiments of the present invention, and for those skilled in the art, other drawings can be obtained according to the drawings without creative efforts.
FIG. 1 is a graph showing the dissolution profiles of the acarbose tablets of cases 1 to 5 and the comparative example in hydrochloric acid at pH 1.2.
FIG. 2 is a graph of the dissolution profiles of the acarbose tablets of cases 1 to 5 and the comparative example in acetate at pH 4.0.
FIG. 3 is a graph showing the dissolution profiles of the acarbose tablets of cases 1 to 5 and the comparative example in phosphate at pH 6.8.
Fig. 4 is a graph showing the dissolution profile of acarbose tablets in water for cases 1 to 5 and comparative example.
Detailed Description
Reference will now be made in detail to embodiments of the present invention, examples of which are illustrated in the accompanying drawings, wherein like or similar reference numerals refer to the same or similar elements or elements having the same or similar function throughout. The embodiments described below with reference to the drawings are illustrative and intended to be illustrative of the invention and are not to be construed as limiting the invention. Further, in the description of the present invention, "a plurality" means two or more unless specifically defined otherwise.
Referring to fig. 1 to 4, the present invention provides an acarbose tablet, which is prepared by mixing powders by weight and directly pressing, and comprises the following components:
40-60 parts of acarbose, 40-100 parts of a filling agent, 0.1-0.5 part of a glidant and 0.2-1 part of a lubricant.
The filler is corn starch and microcrystalline cellulose.
The glidant is colloidal silicon dioxide.
The lubricant is magnesium stearate.
The water content of the corn starch is 11-14%.
The invention also provides a preparation method of the acarbose tablets, which comprises the following steps:
sieving said corn starch, said microcrystalline fiber, and said magnesium stearate separately;
weighing after the sieving is finished, adding the weighed acarbose, the corn starch, the colloidal silicon dioxide and the microcrystalline cellulose into a three-dimensional motion mixer for mixing, and then adding the magnesium stearate for mixing;
respectively adding the mixed materials into a hopper, and starting a tablet press to perform tabletting;
and (4) carrying out aluminum-plastic packaging by adopting a high-speed blister packaging machine.
The specific steps of respectively sieving the corn starch, the microcrystalline fibers and the magnesium stearate are as follows:
and sieving the corn starch and the microcrystalline cellulose by a 80-mesh sieve, and sieving the magnesium stearate by a 40-mesh sieve.
The specific steps of weighing after the sieving is finished are as follows:
weighing the acarbose, the corn starch, the microcrystalline cellulose, the colloidal silicon dioxide and the magnesium stearate according to a mass ratio.
The three-dimensional motion mixer adopts an SYH-50 type three-dimensional motion mixer.
Adding the weighed acarbose, the corn starch, the colloidal silicon dioxide and the microcrystalline cellulose into a three-dimensional motion mixer for mixing, and adding the magnesium stearate for mixing, wherein the specific steps of:
adding the weighed acarbose, the corn starch, the colloidal silicon dioxide and the microcrystalline cellulose into a three-dimensional motion mixer to be mixed for 50 revolutions per minute, wherein the mixing time is 20 minutes, closing the three-dimensional motion mixer, then adding the magnesium stearate, starting the three-dimensional motion mixer to be mixed for 50 revolutions per minute, and the mixing time is 5 minutes.
Respectively adding the mixed materials into a hopper, and starting a tablet press to perform tabletting, namely: samples need to be spot inspected during tabletting to determine hardness and friability.
The specific steps of the aluminum plastic package by adopting the high-speed blister packaging machine are as follows:
and (3) carrying out aluminum-plastic packaging by using a DPH-220A high-speed blister packaging machine, wherein the temperature of an upper plate for PVC blister forming is 110 ℃, the temperature of a lower plate is 110 ℃, the temperature of heat sealing is 170 ℃, the air pressure is 0.6Mpa, and the blanking rate is 15-40 times/min.
Case 1, referring to table 1, a method for preparing acarbose tablets according to the present invention comprises the following steps:
sieving the corn starch and the microcrystalline cellulose by a sieve of 80 meshes, and sieving the magnesium stearate by a sieve of 40 meshes;
weighing the acarbose, the corn starch, the colloidal silicon dioxide and the microcrystalline cellulose after the sieving is finished;
adding 50 parts of the weighed acarbose, 46 parts of the corn starch with the water content of 5%, 0.3 part of the colloidal silicon dioxide and 39 parts of the microcrystalline cellulose into an SYH-50 type three-dimensional motion mixer to mix for 50 revolutions per minute, wherein the mixing time is 20 minutes, closing the three-dimensional motion mixer, then adding 0.7 part of the magnesium stearate, starting the three-dimensional motion mixer to mix for 50 revolutions per minute, and the mixing time is 5 minutes;
respectively adding the mixed materials into a hopper, starting a PGG-40 high-speed rotary tablet press for tabletting to obtain 3000 tablets, then performing spot check on samples in the tabletting process, and detecting the hardness and friability;
and (3) carrying out aluminum-plastic packaging by using a DPH-220A high-speed blister packaging machine, wherein the temperature of an upper plate for PVC blister forming is 110 ℃, the temperature of a lower plate is 110 ℃, the temperature of heat sealing is 170 ℃, the air pressure is 0.6Mpa, and the blanking rate is 15-40 times/min.
TABLE 1
Case 2, referring to table 2, the preparation method of acarbose tablets of the present invention comprises the following steps:
sieving the corn starch and the microcrystalline cellulose by a sieve of 80 meshes, and sieving the magnesium stearate by a sieve of 40 meshes;
weighing the acarbose, the corn starch, the colloidal silicon dioxide and the microcrystalline cellulose after the sieving is finished;
adding 50 parts of the weighed acarbose, 56 parts of the corn starch with the water content of 5 percent, 0.3 part of the colloidal silicon dioxide and 29 parts of the microcrystalline cellulose into an SYH-50 type three-dimensional motion mixer to be mixed for 50 revolutions per minute, wherein the mixing time is 20 minutes, closing the three-dimensional motion mixer, then adding 0.7 part of the magnesium stearate, starting the three-dimensional motion mixer to be mixed for 50 revolutions per minute, and the mixing time is 5 minutes;
respectively adding the mixed materials into a hopper, starting a PGG-40 high-speed rotary tablet press for tabletting to obtain 3000 tablets, then performing spot check on samples in the tabletting process, and detecting the hardness and friability;
and (3) carrying out aluminum-plastic packaging by using a DPH-220A high-speed blister packaging machine, wherein the temperature of an upper plate for PVC blister forming is 110 ℃, the temperature of a lower plate is 110 ℃, the temperature of heat sealing is 170 ℃, the air pressure is 0.6Mpa, and the blanking rate is 15-40 times/min.
TABLE 2
Case 3, referring to table 3, a method for preparing acarbose tablets according to the present invention comprises the following steps:
sieving the corn starch and the microcrystalline cellulose by a sieve of 80 meshes, and sieving the magnesium stearate by a sieve of 40 meshes;
weighing the acarbose, the corn starch, the colloidal silicon dioxide and the microcrystalline cellulose after the sieving is finished;
adding 50 parts of the weighed acarbose, 48 parts of the corn starch with the water content of 9 percent, 0.3 part of the colloidal silicon dioxide and 37 parts of the microcrystalline cellulose into an SYH-50 type three-dimensional motion mixer to be mixed for 50 revolutions per minute, wherein the mixing time is 20 minutes, closing the three-dimensional motion mixer, then adding 0.7 part of the magnesium stearate, starting the three-dimensional motion mixer to be mixed for 50 revolutions per minute, and the mixing time is 5 minutes;
respectively adding the mixed materials into a hopper, starting a PGG-40 high-speed rotary tablet press for tabletting to obtain 3000 tablets, then performing spot check on samples in the tabletting process, and detecting the hardness and friability;
and (3) carrying out aluminum-plastic packaging by using a DPH-220A high-speed blister packaging machine, wherein the temperature of an upper plate for PVC blister forming is 110 ℃, the temperature of a lower plate is 110 ℃, the temperature of heat sealing is 170 ℃, the air pressure is 0.6Mpa, and the blanking rate is 15-40 times/min.
TABLE 3
Case 4, referring to table 4, a method for preparing acarbose tablets according to the present invention comprises the following steps:
sieving the corn starch and the microcrystalline cellulose by a sieve of 80 meshes, and sieving the magnesium stearate by a sieve of 40 meshes;
weighing the acarbose, the corn starch, the colloidal silicon dioxide and the microcrystalline cellulose after the sieving is finished;
adding 50 parts of the weighed acarbose, 49 parts of the corn starch with the water content of 11 percent, 0.3 part of the colloidal silicon dioxide and 36 parts of the microcrystalline cellulose into an SYH-50 type three-dimensional motion mixer to be mixed for 50 revolutions per minute, wherein the mixing time is 20 minutes, closing the three-dimensional motion mixer, then adding 0.7 part of the magnesium stearate, starting the three-dimensional motion mixer to be mixed for 50 revolutions per minute, and the mixing time is 5 minutes;
respectively adding the mixed materials into a hopper, starting a PGG-40 high-speed rotary tablet press for tabletting to obtain 3000 tablets, then performing spot check on samples in the tabletting process, and detecting the hardness and friability;
and (3) carrying out aluminum-plastic packaging by using a DPH-220A high-speed blister packaging machine, wherein the temperature of an upper plate for PVC blister forming is 110 ℃, the temperature of a lower plate is 110 ℃, the temperature of heat sealing is 170 ℃, the air pressure is 0.6Mpa, and the blanking rate is 15-40 times/min.
TABLE 4
sieving the corn starch and the microcrystalline cellulose by a sieve of 80 meshes, and sieving the magnesium stearate by a sieve of 40 meshes;
weighing the acarbose, the corn starch, the colloidal silicon dioxide and the microcrystalline cellulose after the sieving is finished;
adding 50 parts of the weighed acarbose, 51 parts of the corn starch with the water content of 14 percent, 0.3 part of the colloidal silicon dioxide and 34 parts of the microcrystalline cellulose into an SYH-50 type three-dimensional motion mixer to be mixed for 50 revolutions per minute, wherein the mixing time is 20 minutes, closing the three-dimensional motion mixer, then adding 0.7 part of the magnesium stearate, starting the three-dimensional motion mixer to be mixed for 50 revolutions per minute, and the mixing time is 5 minutes;
respectively adding the mixed materials into a hopper, starting a PGG-40 high-speed rotary tablet press for tabletting to obtain 3000 tablets, then performing spot check on samples in the tabletting process, and detecting the hardness and friability;
and (3) carrying out aluminum-plastic packaging by using a DPH-220A high-speed blister packaging machine, wherein the temperature of an upper plate for PVC blister forming is 110 ℃, the temperature of a lower plate is 110 ℃, the temperature of heat sealing is 170 ℃, the air pressure is 0.6Mpa, and the blanking rate is 15-40 times/min.
TABLE 5
Comparative example: bayer "Bhattang apple" tablets, Germany, were sold under batch No. BXHABK 1.
The invention adopts the quality standard of 2020 version Chinese pharmacopoeia acarbose tablets to check the content, related substances and dissolution rate.
The dissolution curve measuring method comprises the following steps: measuring according to a dissolution and release measuring method (second method of 0931 general rule) in the 2020 edition of Chinese pharmacopoeia; the media are selected as follows: hydrochloric acid solution with pH value of 1.2, acetate buffer solution with pH value of 4.0, phosphate buffer solution with pH value of 6.8 and water; the volume is 900 ml; rotating speed: 75 revolutions per minute; the sampling time points are 5min, 10min, 15min and 30 min.
Table 6 results for angle of repose, acarbose tablet appearance, friability and hardness, content uniformity of the mixtures obtained in the different cases:
TABLE 6
The results in Table 6 show that increasing the water content of the corn starch increases the compressibility of the powder and thus the hardness of the acarbose tablets, and that only case 4 and case 5 ensure a hardness consistent with the original grinding and a satisfactory friability. Case 1 and case 2 are very different in hardness from the original grinding and unsatisfactory in friability. Case 3 has a large difference between hardness and original grinding, and has an edge with friability within a standard limit; the content uniformity result shows that the mixing uniformity of the powder can be ensured by adopting the powder direct-pressing preparation process.
The dissolution curves of the acarbose tablets of cases 1 to 5 and comparative examples at pH1.2, pH 4.5, pH6.8 and water are shown in the figure.
In most cases, the in vitro dissolution test has higher sensitivity and stronger differentiation ability than the in vivo test. The quality control significance of the dissolution control curve on the prediction of the in-vivo behavior of the pharmaceutical preparation is obviously improved. The dissolution curve results show that the hardness has a greater influence on the dissolution curve. Cases 4 and 5 f2The factors are all larger than 50, and the dissolution curve of the acarbose tablets is similar to the release behavior of the comparative example.
The invention adopts the aluminum-plastic package to simultaneously carry out stability investigation with the original product, and accelerates the test conditions: 40 ℃ plus or minus 2 ℃ and RH75 percent plus or minus 5 percent.
Table 7, case 5 accelerated test results:
TABLE 7
Table 8, comparative example accelerated test results:
TABLE 8
The results in tables 7 and 8 show that the quality of case 5 and the original research still meets the requirements after being accelerated for 6 months, and the preparation process using case 5 has good stability and less total impurities than the original research.
In conclusion, the invention adopts the powder direct compression process and the filler with high water content, thereby improving the hardness of the tablet and regulating the release of the tablet. The acarbose and the colloidal silicon dioxide are directly mixed and added with the magnesium stearate for tabletting, and the preparation method has the advantages of simple preparation process, short production period and high production efficiency. The prepared acarbose tablet can ensure that the in-vitro release behavior of the acarbose tablet is similar to that of the original ground product 'baitang apple', and can also ensure the stability of the acarbose tablet.
While the invention has been described with reference to a preferred embodiment, it will be understood by those skilled in the art that various changes in form and detail may be made therein without departing from the spirit and scope of the invention as defined by the appended claims.
Claims (10)
1. Acarbose tablets are characterized by being prepared by mixing and directly pressing powders according to the weight percentage:
40-60 parts of acarbose, 40-100 parts of a filling agent, 0.1-0.5 part of a glidant and 0.2-1 part of a lubricant.
2. The acarbose tablet according to claim 1,
the filler is corn starch and microcrystalline cellulose.
3. The acarbose tablet according to claim 2,
the glidant is colloidal silicon dioxide.
4. The acarbose tablet according to claim 3,
the lubricant is magnesium stearate.
5. The acarbose tablet according to claim 4,
the water content of the corn starch is 11-14%.
6. A process for the preparation of acarbose tablets according to claim 5, comprising the following steps:
sieving said corn starch, said microcrystalline fiber, and said magnesium stearate separately;
weighing after the sieving is finished, adding the weighed acarbose, the corn starch, the colloidal silicon dioxide and the microcrystalline cellulose into a three-dimensional motion mixer for mixing, and then adding the magnesium stearate for mixing;
respectively adding the mixed materials into a hopper, and starting a tablet press to perform tabletting;
and (4) carrying out aluminum-plastic packaging by adopting a high-speed blister packaging machine.
7. The process for preparing acarbose tablets according to claim 6, wherein the corn starch, the microcrystalline cellulose and the magnesium stearate are separately sieved by the following steps:
and sieving the corn starch and the microcrystalline cellulose by a 80-mesh sieve, and sieving the magnesium stearate by a 40-mesh sieve.
8. The process for the preparation of acarbose tablets according to claim 7, wherein the weighing after sieving is carried out comprises the specific steps of:
weighing the acarbose, the corn starch, the microcrystalline cellulose, the colloidal silicon dioxide and the magnesium stearate according to a mass ratio.
9. The process for the preparation of acarbose tablets according to claim 8,
the three-dimensional motion mixer adopts an SYH-50 type three-dimensional motion mixer.
10. The process for the preparation of acarbose tablets according to claim 9,
the tablet press adopts a PGG-40 high-speed rotary tablet press.
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| CN114306258A (en) * | 2022-03-11 | 2022-04-12 | 天津睿创康泰生物技术有限公司 | Acarbose solid oral preparation and preparation method thereof |
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