CN112190557B - Compound sulfamethoxazole tablets and preparation method thereof - Google Patents
Compound sulfamethoxazole tablets and preparation method thereof Download PDFInfo
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- CN112190557B CN112190557B CN202010991597.6A CN202010991597A CN112190557B CN 112190557 B CN112190557 B CN 112190557B CN 202010991597 A CN202010991597 A CN 202010991597A CN 112190557 B CN112190557 B CN 112190557B
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- sulfamethoxazole
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- 229960005404 sulfamethoxazole Drugs 0.000 title claims abstract description 100
- JLKIGFTWXXRPMT-UHFFFAOYSA-N sulphamethoxazole Chemical compound O1C(C)=CC(NS(=O)(=O)C=2C=CC(N)=CC=2)=N1 JLKIGFTWXXRPMT-UHFFFAOYSA-N 0.000 title claims abstract description 100
- 150000001875 compounds Chemical class 0.000 title claims abstract description 76
- 238000002360 preparation method Methods 0.000 title claims abstract description 31
- 229920002472 Starch Polymers 0.000 claims abstract description 80
- 239000008107 starch Substances 0.000 claims abstract description 80
- 235000019698 starch Nutrition 0.000 claims abstract description 80
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims abstract description 58
- 239000011734 sodium Substances 0.000 claims abstract description 30
- 229910052708 sodium Inorganic materials 0.000 claims abstract description 30
- 235000019359 magnesium stearate Nutrition 0.000 claims abstract description 29
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims abstract description 28
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims abstract description 28
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims abstract description 28
- IEDVJHCEMCRBQM-UHFFFAOYSA-N trimethoprim Chemical compound COC1=C(OC)C(OC)=CC(CC=2C(=NC(N)=NC=2)N)=C1 IEDVJHCEMCRBQM-UHFFFAOYSA-N 0.000 claims abstract description 14
- 229960001082 trimethoprim Drugs 0.000 claims abstract description 13
- 238000002156 mixing Methods 0.000 claims description 36
- 238000003756 stirring Methods 0.000 claims description 27
- 238000010008 shearing Methods 0.000 claims description 24
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 23
- 239000008187 granular material Substances 0.000 claims description 22
- 239000007779 soft material Substances 0.000 claims description 20
- 238000001035 drying Methods 0.000 claims description 19
- 239000004677 Nylon Substances 0.000 claims description 18
- 239000000853 adhesive Substances 0.000 claims description 18
- 230000001070 adhesive effect Effects 0.000 claims description 18
- 229920001778 nylon Polymers 0.000 claims description 18
- 238000003825 pressing Methods 0.000 claims description 18
- 238000009826 distribution Methods 0.000 claims description 17
- 239000000463 material Substances 0.000 claims description 17
- 239000002245 particle Substances 0.000 claims description 17
- 235000015424 sodium Nutrition 0.000 claims description 17
- 238000007873 sieving Methods 0.000 claims description 16
- 239000002002 slurry Substances 0.000 claims description 12
- ZCSOPTJSZZUCPE-UHFFFAOYSA-N N-methoxy-1-phenylmethanamine pyrimidine Chemical class N1=CN=CC=C1.CONCC1=CC=CC=C1 ZCSOPTJSZZUCPE-UHFFFAOYSA-N 0.000 claims description 10
- 239000002994 raw material Substances 0.000 claims description 10
- WZRJTRPJURQBRM-UHFFFAOYSA-N 4-amino-n-(5-methyl-1,2-oxazol-3-yl)benzenesulfonamide;5-[(3,4,5-trimethoxyphenyl)methyl]pyrimidine-2,4-diamine Chemical compound O1C(C)=CC(NS(=O)(=O)C=2C=CC(N)=CC=2)=N1.COC1=C(OC)C(OC)=CC(CC=2C(=NC(N)=NC=2)N)=C1 WZRJTRPJURQBRM-UHFFFAOYSA-N 0.000 claims description 9
- 239000002671 adjuvant Substances 0.000 claims description 9
- 239000011230 binding agent Substances 0.000 claims description 9
- 238000007599 discharging Methods 0.000 claims description 9
- 239000000843 powder Substances 0.000 claims description 9
- 238000012216 screening Methods 0.000 claims description 9
- 229940006995 sulfamethoxazole and trimethoprim Drugs 0.000 claims description 9
- 230000006835 compression Effects 0.000 claims description 2
- 238000007906 compression Methods 0.000 claims description 2
- 230000006641 stabilisation Effects 0.000 claims 1
- 238000011105 stabilization Methods 0.000 claims 1
- 238000004090 dissolution Methods 0.000 abstract description 39
- 239000000203 mixture Substances 0.000 abstract description 12
- 238000000338 in vitro Methods 0.000 abstract description 5
- 230000000694 effects Effects 0.000 abstract description 4
- 239000012535 impurity Substances 0.000 abstract description 2
- 238000009472 formulation Methods 0.000 abstract 1
- 230000000052 comparative effect Effects 0.000 description 16
- 238000001514 detection method Methods 0.000 description 11
- 239000003814 drug Substances 0.000 description 7
- OVBPIULPVIDEAO-LBPRGKRZSA-N folic acid Chemical compound C=1N=C2NC(N)=NC(=O)C2=NC=1CNC1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 OVBPIULPVIDEAO-LBPRGKRZSA-N 0.000 description 6
- 238000000034 method Methods 0.000 description 5
- OVBPIULPVIDEAO-UHFFFAOYSA-N N-Pteroyl-L-glutaminsaeure Natural products C=1N=C2NC(N)=NC(=O)C2=NC=1CNC1=CC=C(C(=O)NC(CCC(O)=O)C(O)=O)C=C1 OVBPIULPVIDEAO-UHFFFAOYSA-N 0.000 description 3
- 230000000844 anti-bacterial effect Effects 0.000 description 3
- 229940079593 drug Drugs 0.000 description 3
- 229960000304 folic acid Drugs 0.000 description 3
- 235000019152 folic acid Nutrition 0.000 description 3
- 239000011724 folic acid Substances 0.000 description 3
- 241000588724 Escherichia coli Species 0.000 description 2
- 241000606768 Haemophilus influenzae Species 0.000 description 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 2
- 241000191967 Staphylococcus aureus Species 0.000 description 2
- 230000015572 biosynthetic process Effects 0.000 description 2
- 239000007884 disintegrant Substances 0.000 description 2
- 238000000227 grinding Methods 0.000 description 2
- 229940047650 haemophilus influenzae Drugs 0.000 description 2
- 229940031703 low substituted hydroxypropyl cellulose Drugs 0.000 description 2
- VZSRBBMJRBPUNF-UHFFFAOYSA-N 2-(2,3-dihydro-1H-inden-2-ylamino)-N-[3-oxo-3-(2,4,6,7-tetrahydrotriazolo[4,5-c]pyridin-5-yl)propyl]pyrimidine-5-carboxamide Chemical compound C1C(CC2=CC=CC=C12)NC1=NC=C(C=N1)C(=O)NCCC(N1CC2=C(CC1)NN=N2)=O VZSRBBMJRBPUNF-UHFFFAOYSA-N 0.000 description 1
- YLZOPXRUQYQQID-UHFFFAOYSA-N 3-(2,4,6,7-tetrahydrotriazolo[4,5-c]pyridin-5-yl)-1-[4-[2-[[3-(trifluoromethoxy)phenyl]methylamino]pyrimidin-5-yl]piperazin-1-yl]propan-1-one Chemical compound N1N=NC=2CN(CCC=21)CCC(=O)N1CCN(CC1)C=1C=NC(=NC=1)NCC1=CC(=CC=C1)OC(F)(F)F YLZOPXRUQYQQID-UHFFFAOYSA-N 0.000 description 1
- 241000894006 Bacteria Species 0.000 description 1
- 241000606153 Chlamydia trachomatis Species 0.000 description 1
- 241000588921 Enterobacteriaceae Species 0.000 description 1
- 102000004190 Enzymes Human genes 0.000 description 1
- 108090000790 Enzymes Proteins 0.000 description 1
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 1
- 241000588748 Klebsiella Species 0.000 description 1
- 241000588771 Morganella <proteobacterium> Species 0.000 description 1
- 241000588653 Neisseria Species 0.000 description 1
- 241000588650 Neisseria meningitidis Species 0.000 description 1
- 241000187654 Nocardia Species 0.000 description 1
- 241000588769 Proteus <enterobacteria> Species 0.000 description 1
- 241000607142 Salmonella Species 0.000 description 1
- 241000607768 Shigella Species 0.000 description 1
- 241000193998 Streptococcus pneumoniae Species 0.000 description 1
- 241000193996 Streptococcus pyogenes Species 0.000 description 1
- 108010022394 Threonine synthase Proteins 0.000 description 1
- 241000223996 Toxoplasma Species 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 239000008351 acetate buffer Substances 0.000 description 1
- 230000000845 anti-microbial effect Effects 0.000 description 1
- 229940124350 antibacterial drug Drugs 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 125000002057 carboxymethyl group Chemical group [H]OC(=O)C([H])([H])[*] 0.000 description 1
- 239000003153 chemical reaction reagent Substances 0.000 description 1
- 229940038705 chlamydia trachomatis Drugs 0.000 description 1
- 238000007796 conventional method Methods 0.000 description 1
- 102000004419 dihydrofolate reductase Human genes 0.000 description 1
- 108010014404 dihydrofolate synthetase Proteins 0.000 description 1
- 239000012738 dissolution medium Substances 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 230000004060 metabolic process Effects 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 239000008363 phosphate buffer Substances 0.000 description 1
- 238000012797 qualification Methods 0.000 description 1
- 238000013112 stability test Methods 0.000 description 1
- 229940031000 streptococcus pneumoniae Drugs 0.000 description 1
- FDDDEECHVMSUSB-UHFFFAOYSA-N sulfanilamide Chemical compound NC1=CC=C(S(N)(=O)=O)C=C1 FDDDEECHVMSUSB-UHFFFAOYSA-N 0.000 description 1
- 229940124530 sulfonamide Drugs 0.000 description 1
- 230000002195 synergetic effect Effects 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- 238000010998 test method Methods 0.000 description 1
- 229940096949 trimethoprim 80 mg Drugs 0.000 description 1
Classifications
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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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
-
- 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
- A61K31/63—Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide
- A61K31/635—Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide having a heterocyclic ring, e.g. sulfadiazine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
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- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
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- General Health & Medical Sciences (AREA)
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- Molecular Biology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
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Abstract
The invention provides a compound sulfamethoxazole tablet and a preparation method thereof, wherein the compound sulfamethoxazole tablet comprises 70-75% of sulfamethoxazole, 14-15% of trimethoprim, 9-10.0% of starch, 0.45-0.65% of magnesium stearate, 0.9-1.4% of hydroxypropyl cellulose and 2-3% of sodium carboxymethyl starch by weight, and the compound sulfamethoxazole tablet provided by the invention has stable quality and low impurity content; a reference formulation developed with the company sunpherm INDS, usa (trade name:
Description
Technical Field
The invention belongs to the technical field of pharmaceutical preparations, and particularly relates to a compound sulfamethoxazole tablet and a preparation method thereof.
Background
The compound sulfamethoxazole and sulfanilamide antibacterial drug is a compound preparation of Sulfamethoxazole (SMZ) and Trimethoprim (TMP), has good antibacterial effect on non-enzyme-producing staphylococcus aureus, streptococcus pyogenes, streptococcus pneumoniae, escherichia coli, klebsiella, salmonella, proteus, morganella, shigella and other enterobacteriaceae bacteria, gonococcus, neisseria meningitidis and haemophilus influenzae, and particularly has obviously enhanced antibacterial effect on escherichia coli, haemophilus influenzae and staphylococcus aureus compared with the single SMZ drug. In addition, the compound also has good antimicrobial activity in vitro against chlamydia trachomatis, Nocardia stellata, protozoa, toxoplasma and the like.
Sulfamethoxazole acts on dihydrofolate synthetase to interfere the first step of folic acid synthesis, trimethoprim acts on the second step of folic acid anabolism to selectively inhibit the action of dihydrofolate reductase, and the two are combined to enable the folic acid metabolism of bacteria to be doubly blocked. The product has synergistic antibacterial effect, and has reduced drug-resistant strains compared with single medicine.
The existing compound sulfamethoxazole tablets have certain difference with the original product due to different prescriptions and processes, particularly the problem of slow dissolution rate, and the slow dissolution rate can greatly influence the absorption of the medicine in a human body, so that the medicine loses the value of the medicine. Therefore, the prescription and the preparation process of the compound sulfamethoxazole tablets need to be further optimized, and the quality qualification and the medication safety of the product are ensured.
Disclosure of Invention
In order to solve the problems, the invention provides the compound sulfamethoxazole tablet and the preparation method thereof, the compound sulfamethoxazole tablet greatly reduces the addition of a disintegrant, and the obtained tablet has stable quality and high in-vitro dissolution rate.
In order to achieve the purpose, the invention adopts the following technical scheme:
the compound sulfamethoxazole tablet comprises the following components in parts by weight:
in the compound sulfamethoxazole tablets, each compound sulfamethoxazole tablet contains 0.4g of compound sulfamethoxazole and 80mg of trimethoprim.
In one embodiment of the invention, the compound sulfamethoxazole tablet comprises the following components in parts by weight:
| components | Weight percent of |
| Sulfamethoxazole | 72.01％ |
| Methoxybenzylamine pyrimidines | 14.40％ |
| Starch | 9.81％ |
| Magnesium stearate | 0.54％ |
| Hydroxypropyl cellulose | 1.08％ |
| Sodium carboxymethyl starch | 2.16％ |
Further, the invention provides a preparation method of the compound sulfamethoxazole tablets.
A preparation method of compound sulfamethoxazole tablets comprises the following steps:
(1) preparing raw materials and auxiliary materials:
firstly, screening sulfamethoxazole and trimethoprim through a 80-mesh sieve; sieving magnesium stearate, hydroxypropyl cellulose, sodium carboxymethyl starch and starch with 120 mesh sieve;
preparing 25-28% of starch into 8.5-9.5% of starch slurry; as a binder; controlling the temperature to be 40-45 ℃ for standby;
(2) mixing and preparing a soft material:
firstly, the sulfamethoxazole, the trimethoprim and the residual starch are placed in a groove type mixer to be mixed for 10 to 20 minutes, the stirring speed is 100 plus 150rpm, and the shearing speed is 600 plus 800 rpm;
② the stirring speed is 100-150rpm, the shearing speed is 1000-1200rpm, and the adhesive with the temperature of 40-45 ℃ is added within 7-10 minutes;
thirdly, stirring at the speed of 100-1200 rpm and the shear at the speed of 1000-150 rpm for 13-15 minutes to prepare a proper soft material and then discharging the soft material;
(3) and (3) granulating: granulating with 14 mesh nylon sieve swing granulator, and making into uniform granule with appropriate hardness and size.
(4) And (3) drying: drying at 60-70 ℃ for 210 minutes, and controlling the water content to be 1.5-3.0%.
(5) Straightening: adding additional adjuvants such as magnesium stearate, hydroxypropyl cellulose, and sodium carboxymethyl starch before granulating. Sieving with 14 mesh nylon sieve, granulating, and collecting fine powder;
(6) total mixing: adding the granules after finishing the granules into a V-shaped mixer, and totally mixing for 28-32 minutes; rotate positively and negatively for 14-16 minutes respectively
(7) Tabletting: pressing into tablets, wherein the pressing pressure is 70-90KN, and obtaining the compound sulfamethoxazole tablets.
In the preparation method, in the step (1), 9.0% of starch slurry is prepared.
In the above preparation method, in the step (4), the drying is performed for 180 minutes.
In the preparation method, in the step (4), the water content is controlled to be 1.7-2.5%.
In the preparation method, in the step (5), the particle size distribution after finishing is as follows:
| particle size distribution | Percentage of |
| 20 mesh or larger (%) | 2％-5％ |
| 20-60 mesh (%) | 7％-12％ |
| 60-100 mesh (%) | 20％-32％ |
| 100-140 mesh (%) | 28％-40％ |
| 140-200 mesh (%) | 12％-18％ |
| 200 mesh or less (%) | 7％-10％ |
In the above production method, in the step (6), the total mixing is preferably carried out for 30 minutes.
In the above preparation method, in the step (7), the tabletting pressure is 75-85N, preferably 80N.
Compared with the prior art, the invention has the beneficial effects that:
1) the compound sulfamethoxazole tablets provided by the invention have stable quality and low impurity content.
2) The compound sulfamethoxazole tablet provided by the invention and a reference preparation (trade name:
) The four dissolution curves are consistent and have the same in-vitro dissolution behavior, namely the dissolution curve f2 factor is not less than 50, and the four dissolution curves have the same treatment effect.
Detailed Description
The invention discloses a compound sulfamethoxazole tablet and a preparation method thereof, and a person skilled in the art can realize the compound sulfamethoxazole tablet by properly improving process parameters by taking the contents of the compound sulfamethoxazole tablet as reference. It is expressly intended that all such similar substitutes and modifications apparent to those skilled in the art are deemed to be within the scope of the invention. While the invention has been described in terms of preferred embodiments, it will be apparent to those skilled in the art that variations may be applied, or changes and combinations may be made, in the methods and applications described herein to achieve and use the inventive techniques without departing from the spirit, scope, and content of the invention.
The present invention is further illustrated by the following examples, which are not intended to limit the invention in any way.
The test methods in the following examples are all conventional methods unless otherwise specified, and the raw materials, reagent materials and the like used in the following examples are all commercially available products unless otherwise specified.
Original grinding products: sun PHARM INDS company (specification: sulfamethoxazole 0.4 g/trimethoprim 80mg, trade name:
)。
friability, content uniformity: detecting according to the standard of pharmacopoeia in 2015.
Dissolution curve: the dissolution curves in dissolution medium (water, hydrochloric acid pH1.2, acetate buffer pH4.0, phosphate buffer pH 6.8) in 4 were measured separately and compared with the original ground product.
Example 1: compound sulfamethoxazole tablet
The prescription composition is as follows:
| components | 10 ten thousand tablets per material | Weight percent of |
| Sulfamethoxazole | 40kg | 72.01％ |
| Methoxybenzylamine pyrimidines | 8kg | 14.40％ |
| Starch | 5.45kg | 9.81％ |
| Magnesium stearate | 0.3Kg | 0.54％ |
| Hydroxypropyl cellulose | 0.6Kg | 1.08％ |
| Sodium carboxymethyl starch | 1.2Kg | 2.16％ |
The preparation method comprises the following steps:
(1) preparing raw materials and auxiliary materials: firstly, screening sulfamethoxazole and trimethoprim through a 80-mesh sieve; sieving magnesium stearate, hydroxypropyl cellulose, sodium carboxymethyl starch and starch with 120 mesh sieve; ② preparing 0.09 percent starch slurry by taking 1.45Kg (26.6 percent) of starch; as a binder; controlling the temperature to be 40-45 ℃ for standby;
(2) mixing and preparing a soft material: firstly, mixing sulfamethoxazole, trimethoprim and residual starch in a groove type mixer for 15 minutes, wherein the stirring speed is 120rpm, and the shearing speed is 700 rpm; ② the stirring speed is 120rpm, the shearing speed is 1100rpm, and the 42 ℃ adhesive is added within 8 minutes; thirdly, stirring at the speed of 120rpm and the shearing speed of 1100rpm for 14 minutes to prepare a soft material, and then discharging;
(3) and (3) granulating: granulating with 14 mesh nylon sieve swing granulator to obtain uniform granules with appropriate hardness and size;
(4) and (3) drying: drying at 60-70 deg.C for 180 min with water content of 2.1%;
(5) straightening: adding additional adjuvants such as magnesium stearate, hydroxypropyl cellulose, and sodium carboxymethyl starch before granulating. Sieving with 14 mesh nylon sieve, granulating, and collecting fine powder; the particle size distribution after finishing is as follows:
| particle size distribution | Percentage of |
| 20 mesh or larger (%) | 4.2％ |
| 20-60 mesh (%) | 10.0％ |
| 60-100 mesh (%) | 22.2％ |
| 100-140 mesh (%) | 36.80％ |
| 140-200 mesh (%) | 17.7％ |
| 200 mesh or less (%) | 9.1％ |
(6) Adding the granules after the total mixing and finishing into a V-shaped mixer, and totally mixing for 28 minutes, and rotating positively and negatively for 14 minutes respectively;
(7) tabletting: pressing into tablets, wherein the pressing pressure is 80KN, and obtaining the compound sulfamethoxazole tablets.
The prepared compound sulfamethoxazole tablets are subjected to weight difference, friability and four dissolution curve detections in pH1.2, pH4.0, pH6.8, water and the like, and compared with the original ground product, f2 is calculated, and the results are as follows:
example 2: compound sulfamethoxazole tablet
The prescription composition is as follows:
| components | 40 ten thousand tablets per material | Weight percent of |
| Sulfamethoxazole | 160kg | 72.01％ |
| Methoxybenzylamine pyrimidines | 32kg | 14.40％ |
| Starch | 21.8kg | 9.81％ |
| Magnesium stearate | 1.2kg | 0.54％ |
| Hydroxypropyl cellulose | 2.4kg | 1.08％ |
| Sodium carboxymethyl starch | 4.8Kg | 2.16％ |
The preparation method comprises the following steps:
(1) preparing raw materials and auxiliary materials: firstly, screening sulfamethoxazole and trimethoprim through a 80-mesh sieve; sieving magnesium stearate, hydroxypropyl cellulose, sodium carboxymethyl starch and starch with 120 mesh sieve; ② preparing 0.09 percent starch slurry by taking 5.8Kg (26.6 percent) of starch; as an adhesive; controlling the temperature to be 40-45 ℃ for standby;
(2) mixing and preparing a soft material: firstly, mixing sulfamethoxazole, trimethoprim and residual starch in a groove type mixer for 15 minutes, wherein the stirring speed is 120rpm, and the shearing speed is 700 rpm; ② the stirring speed is 120rpm, the shearing speed is 1100rpm, and the adhesive with the temperature of 43 ℃ is added within 8 minutes; thirdly, stirring at the speed of 120rpm and the shearing speed of 1100rpm for 14 minutes to prepare a soft material, and then discharging;
(3) and (3) granulating: granulating with 14 mesh nylon sieve swing granulator to obtain uniform granules with appropriate hardness and size;
(4) and (3) drying: drying at 60-70 deg.C for 180 min with water content of 2.3%;
(5) straightening: adding additional adjuvants such as magnesium stearate, hydroxypropyl cellulose, and sodium carboxymethyl starch before granulating. Sieving with 14 mesh nylon sieve, granulating, and collecting fine powder; the particle size distribution after finishing is as follows:
| particle size distribution | Percentage of |
| 20 mesh or larger (%) | 2.7％ |
| 20-60 mesh (%) | 8.3％ |
| 60-100 mesh (%) | 30.0％ |
| 100-140 mesh (%) | 35.20％ |
| 140-200 mesh (%) | 16.5％ |
| 200 mesh or less (%) | 7.3％ |
(6) Adding the granules after the total mixing and finishing into a V-shaped mixer, and totally mixing for 28 minutes, and rotating positively and negatively for 14 minutes respectively;
(7) tabletting: pressing into tablets, wherein the pressing pressure is 80KN, and obtaining the compound sulfamethoxazole tablets.
The prepared compound sulfamethoxazole tablets are subjected to weight difference, friability and four dissolution curve detections in pH1.2, pH4.0, pH6.8, water and the like, and compared with the original ground product, f2 is calculated, and the results are as follows:
example 3: compound sulfamethoxazole tablets
The prescription composition is as follows:
| components | 1 ten thousand tablets per material | Weight percent of |
| Sulfamethoxazole | 4kg | 72.01％ |
| Methoxybenzylamine pyrimidines | 0.8kg | 14.40％ |
| Starch | 0.545kg | 9.81％ |
| Magnesium stearate | 0.03Kg | 0.54％ |
| Hydroxypropyl cellulose | 0.06Kg | 1.08％ |
| Sodium carboxymethyl starch | 0.12Kg | 2.16％ |
The preparation method comprises the following steps:
(1) preparing raw materials and auxiliary materials: firstly, screening sulfamethoxazole and trimethoprim through a 80-mesh sieve; sieving magnesium stearate, hydroxypropyl cellulose, sodium carboxymethyl starch and starch with 120 mesh sieve; ② 0.09 percent of starch slurry is prepared by taking 0.145Kg (26.6 percent) of starch; as a binder; controlling the temperature to be 40-45 ℃ for standby;
(2) mixing and preparing a soft material: firstly, mixing sulfamethoxazole, trimethoprim and residual starch in a groove type mixer for 15 minutes, wherein the stirring speed is 120rpm, and the shearing speed is 700 rpm; ② the stirring speed is 120rpm, the shearing speed is 1100rpm, and the 42 ℃ adhesive is added within 8 minutes; thirdly, stirring at the speed of 120rpm and the shearing speed of 1100rpm for 14 minutes to prepare a soft material, and then discharging;
(3) and (3) granulating: granulating with 14 mesh nylon sieve swing granulator to obtain uniform granules with appropriate hardness and size;
(4) and (3) drying: drying at 60-70 deg.C for 180 min with water content of 1.8%;
(5) straightening: adding additional adjuvants such as magnesium stearate, hydroxypropyl cellulose, and carboxymethyl starch sodium before grading. Sieving with 14 mesh nylon sieve, granulating, and collecting fine powder; the particle size distribution after finishing is as follows:
| particle size distribution | Percentage of |
| 20 mesh or larger (%) | 2.3％ |
| 20-60 mesh (%) | 9.4％ |
| 60-100 mesh (%) | 28.3％ |
| 100-140 mesh (%) | 34.80％ |
| 140-200 mesh (%) | 17.3％ |
| 200 mesh or less (%) | 7.9％ |
(6) Adding the granules after the total mixing and finishing into a V-shaped mixer, and totally mixing for 28 minutes, and rotating positively and negatively for 14 minutes respectively;
(7) tabletting: pressing into tablets, wherein the pressing pressure is 80KN, and obtaining the compound sulfamethoxazole tablets.
The prepared compound sulfamethoxazole tablets are subjected to weight difference, friability and four dissolution curve detections in pH1.2, pH4.0, pH6.8, water and the like, and compared with the original ground product, f2 is calculated, and the results are as follows:
example 4: compound sulfamethoxazole tablet
The prescription composition is as follows:
the preparation method comprises the following steps:
(1) preparing raw materials and auxiliary materials: firstly, screening sulfamethoxazole and trimethoprim through a 80-mesh sieve; sieving magnesium stearate, hydroxypropyl cellulose, sodium carboxymethyl starch and starch with 120 mesh sieve; ② taking 1.4Kg (25.7%) of starch to prepare 0.087% of starch slurry; as a binder; controlling the temperature to be 40-45 ℃ for standby;
(2) mixing and preparing a soft material: firstly, mixing sulfamethoxazole, trimethoprim and residual starch in a groove type mixer for 12 minutes, wherein the stirring speed is 140rpm, and the shearing speed is 750 rpm; ② the stirring speed is 140rpm, the shearing speed is 1100rpm, and the 44 ℃ adhesive is added within 8 minutes; stirring at 140rpm and 1100rpm for 14 min to obtain soft material, and discharging;
(3) and (3) granulating: granulating with 14 mesh nylon sieve swing granulator to obtain uniform granules with appropriate hardness and size;
(4) and (3) drying: drying at 60-70 deg.C for 175 min with water content of 2.2%;
(5) straightening: adding additional adjuvants such as magnesium stearate, hydroxypropyl cellulose, and sodium carboxymethyl starch before granulating. Sieving with 14 mesh nylon sieve, granulating, and collecting fine powder; the particle size distribution after finishing is as follows:
| particle size distribution | Percentage of |
| 20 mesh or larger (%) | 4.4％ |
| 20-60 mesh (%) | 11.3％ |
| 60-100 mesh (%) | 21.3％ |
| 100-140 mesh (%) | 36.60％ |
| 140-200 mesh (%) | 17.9％ |
| 200 mesh or less (%) | 8.5％ |
(6) Adding the granules after the total mixing and finishing into a V-shaped mixer, and totally mixing for 28 minutes, and rotating positively and negatively for 14 minutes respectively;
(7) tabletting: pressing into tablets, wherein the pressing pressure is 75KN, and obtaining the compound sulfamethoxazole tablets.
The prepared compound sulfamethoxazole tablets are subjected to weight difference, friability and four dissolution curve detections in pH1.2, pH4.0, pH6.8, water and the like, and compared with the original ground product, f2 is calculated, and the results are as follows:
example 5: compound sulfamethoxazole tablet
The prescription composition is as follows:
| components | 10 ten thousand tablets per material | Weight percent of |
| Sulfamethoxazole | 40kg | 72.01％ |
| Methoxybenzylamine pyrimidines | 8kg | 14.40％ |
| Starch | 5.45kg | 9.81％ |
| Magnesium stearate | 0.3Kg | 0.54％ |
| Hydroxypropyl cellulose | 0.6Kg | 1.08％ |
| Sodium carboxymethyl starch | 1.2Kg | 2.16％ |
The preparation method comprises the following steps:
(1) preparing raw materials and auxiliary materials: firstly, screening sulfamethoxazole and trimethoprim through a 80-mesh sieve; sieving magnesium stearate, hydroxypropyl cellulose, sodium carboxymethyl starch and starch with 120 mesh sieve; ② taking 1.5Kg (27.5%) of starch to prepare 0.092% of starch slurry; as a binder; controlling the temperature to be 40-45 ℃ for standby;
(2) mixing and preparing a soft material: firstly, mixing sulfamethoxazole, trimethoprim and residual starch in a tank type mixer for 18 minutes, wherein the stirring speed is 110rpm, and the shearing speed is 650 rpm; ② the stirring speed is 110rpm, the shearing speed is 1100rpm, and the 42 ℃ adhesive is added within 9 minutes; thirdly, stirring at the speed of 110rpm and the shearing speed of 1100rpm for 14 minutes to prepare a soft material, and then discharging;
(3) and (3) granulating: granulating with 14 mesh nylon sieve swing granulator to obtain uniform granules with appropriate hardness and size;
(4) and (3) drying: drying at 60-70 deg.C for 200 min with water content of 1.7%;
(5) straightening: adding additional adjuvants such as magnesium stearate, hydroxypropyl cellulose, and sodium carboxymethyl starch before granulating. Sieving with 14 mesh nylon sieve, granulating, and collecting fine powder; the particle size distribution after finishing is as follows:
| particle size distribution | Percentage of |
| 20 mesh or larger (%) | 4.0％ |
| 20-60 mesh (%) | 9.3％ |
| 60-100 mesh (%) | 25.4％ |
| 100-140 mesh (%) | 37.20％ |
| 140-200 mesh (%) | 15.6％ |
| 200 mesh or less (%) | 8.5％ |
(6) Adding the granules after the total mixing and finishing into a V-shaped mixer, and totally mixing for 28 minutes, and rotating positively and negatively for 14 minutes respectively;
(7) tabletting: pressing into tablets, wherein the pressing pressure is 85KN, and obtaining the compound sulfamethoxazole tablets.
The prepared compound sulfamethoxazole tablets are subjected to weight difference, friability and four dissolution curve detections in pH1.2, pH4.0, pH6.8, water and the like, and compared with the original ground product, f2 is calculated, and the results are as follows:
example 6: compound sulfamethoxazole tablet
The prescription composition is as follows:
| components | 10 ten thousand tablets per material | Weight percent of |
| Sulfamethoxazole | 40kg | 72.01％ |
| Methoxybenzylamine pyrimidines | 8kg | 14.40％ |
| Starch | 5.2kg | 9.36％ |
| Magnesium stearate | 0.35Kg | 0.63％ |
| Hydroxypropyl cellulose | 0.7Kg | 1.26％ |
| Sodium carboxymethyl starch | 1.3Kg | 2.34％ |
The preparation method comprises the following steps:
(1) preparing raw materials and auxiliary materials: firstly, screening sulfamethoxazole and trimethoprim through a 80-mesh sieve; sieving magnesium stearate, hydroxypropyl cellulose, sodium carboxymethyl starch and starch with 120 mesh sieve; ② taking 1.35Kg (25.9%) of starch to prepare 0.085% of starch slurry; as a binder; controlling the temperature to be 40-45 ℃ for standby;
(2) mixing and preparing a soft material: firstly, mixing sulfamethoxazole, trimethoprim and residual starch in a groove type mixer for 10 minutes, wherein the stirring speed is 150rpm, and the shearing speed is 800 rpm; ② the stirring speed is 150rpm, the shearing speed is 1200rpm, and 40 ℃ adhesive is added within 7 minutes; thirdly, stirring at the speed of 150rpm and the shearing speed of 1200rpm for 13 minutes to prepare a soft material, and then discharging;
(3) and (3) granulating: granulating with 14 mesh nylon sieve swing granulator to obtain uniform granules with appropriate hardness and size;
(4) and (3) drying: drying at 60-70 deg.C for 150 min with water content of 2.5%;
(5) straightening: adding additional adjuvants such as magnesium stearate, hydroxypropyl cellulose, and sodium carboxymethyl starch before granulating. Granulating with 14 mesh nylon sieve, with uniform granule and appropriate amount of fine powder; the particle size distribution after finishing is as follows:
(6) adding the granules after the total mixing and finishing into a V-shaped mixer, and totally mixing for 28 minutes, and rotating positively and negatively for 14 minutes respectively;
(7) tabletting: pressing into tablets, wherein the pressing pressure is 70KN, and obtaining the compound sulfamethoxazole tablets.
The prepared compound sulfamethoxazole tablets are subjected to weight difference, friability and four dissolution curve detections in pH1.2, pH4.0, pH6.8, water and the like, and compared with the original ground product, f2 is calculated, and the results are as follows:
example 7: compound sulfamethoxazole tablet
The prescription composition is as follows:
| components | 10 ten thousand tablets per material | Weight percent of |
| Sulfamethoxazole | 40kg | 72.07％ |
| Methoxybenzylamine pyrimidines | 8kg | 14.41％ |
| Starch | 5.55kg | 10.00％ |
| Magnesium stearate | 0.25Kg | 0.45％ |
| Hydroxypropyl cellulose | 0.55Kg | 0.99％ |
| Sodium carboxymethyl starch | 1.15Kg | 2.07％ |
The preparation method comprises the following steps:
(1) preparing raw materials and auxiliary materials: firstly, screening sulfamethoxazole and trimethoprim through a 80-mesh sieve; sieving magnesium stearate, hydroxypropyl cellulose, sodium carboxymethyl starch and starch with 120 mesh sieve; ② taking 1.55Kg (26.6%) of starch to prepare 0.095% of starch slurry; as a binder; controlling the temperature to be 40-45 ℃ for standby;
(2) mixing and preparing a soft material: firstly, mixing sulfamethoxazole, trimethoprim and residual starch in a groove type mixer for 20 minutes, wherein the stirring speed is 100rpm, and the shearing speed is 600 rpm; ② the stirring speed is 100rpm, the shearing speed is 1000rpm, and 45 ℃ adhesive is added within 10 minutes; thirdly, stirring at the speed of 100rpm and the shearing speed of 1000rpm for 15 minutes to prepare a soft material, and then discharging;
(3) and (3) granulating: granulating with 14 mesh nylon sieve swing granulator to obtain uniform granules with appropriate hardness and size;
(4) and (3) drying: drying at 60-70 deg.C for 210 min with water content of 1.6%;
(5) straightening: adding additional adjuvants such as magnesium stearate, hydroxypropyl cellulose, and sodium carboxymethyl starch before granulating. Sieving with 14 mesh nylon sieve, granulating, and collecting fine powder; the particle size distribution after finishing is as follows:
| particle size distribution | Percentage of |
| 20 mesh or larger (%) | 4.5％ |
| 20-60 mesh (%) | 8.8％ |
| 60-100 mesh (%) | 30.6％ |
| 100-140 mesh (%) | 33.00％ |
| 140-200 mesh (%) | 15.2％ |
| 200 mesh or less (%) | 7.9％ |
(6) Adding the granules after the total mixing and finishing into a V-shaped mixer, and totally mixing for 28 minutes, and rotating positively and negatively for 14 minutes respectively;
(7) tabletting: pressing into tablets, wherein the pressing pressure is 90KN, and obtaining the compound sulfamethoxazole tablets.
The prepared compound sulfamethoxazole tablets are subjected to weight difference, friability and four dissolution curve detections in pH1.2, pH4.0, pH6.8, water and the like, and compared with the original ground product, f2 is calculated, and the results are as follows:
comparative example 1: compound sulfamethoxazole tablet
The prescription composition is as follows: the same as in example 3.
The preparation method comprises the following steps: the steps (1) - (1), step (2) - (7) are the same as the example 3, and the steps (1) - (7) are as follows:
the prepared compound sulfamethoxazole tablets are subjected to weight difference, friability and four dissolution curve detections in pH1.2, pH4.0, pH6.8, water and the like, and compared with the original ground product, f2 is calculated, and the results are as follows:
as can be seen from examples 1 to 7 and comparative example 1, the concentration of the binder in step (1) affects the friability and dissolution behavior of the samples; when the concentration of the adhesive is 8% (as in comparative example 1-1), 4 dissolution curves f2 in 4 media of the prepared compound sulfamethoxazole tablets are lower than 50; when the concentration of the adhesive is 11% (as in comparative examples 1-2), the friability of the prepared compound sulfamethoxazole tablets is not satisfactory; the friability of the compound sulfamethoxazole tablets prepared by the invention meets the requirement, and the dissolution curve f2 in 4 media is not lower than 50 (compared with the original ground product), so 8.5-9.5% of starch slurry is prepared to be used as an adhesive.
Comparative example 2: compound sulfamethoxazole tablet
The prescription composition is as follows: the same as in example 3.
The preparation method comprises the following steps: step (1), step (2) - ((c)), step (3) -step (7) are the same as example 3, step (2) - ((c)) is as follows:
the prepared compound sulfamethoxazole tablets are subjected to weight difference, friability and four dissolution curve detections in pH1.2, pH4.0, pH6.8, water and the like, and compared with the original ground product, f2 is calculated, and the results are as follows:
as can be seen from examples 1-7 and comparative example 2, the addition temperature and the addition time of the adhesive in the step (2) influence the weight difference and the dissolution behavior of the sample, and when the addition time of the adhesive is 3 minutes (comparative example 2-1) or the addition temperature of the adhesive is 35 ℃ (comparative example 2-2), the weight difference of the prepared compound sulfamethoxazole tablets is not satisfactory; when the adding temperature of the adhesive is 55 ℃ (comparative example 2-3), 4 dissolution curves f2 in 4 media of the prepared compound sulfamethoxazole tablets are lower than 50; the compound sulfamethoxazole tablets prepared by the invention meet the requirements on weight difference, and the dissolution curve f2 in 4 media is not lower than 50 (compared with the original ground product), so that the adhesive with the temperature of 40-45 ℃ is added within 7-10 minutes.
Comparative example 3: compound sulfamethoxazole tablet
The prescription composition is as follows:
| components | 1 ten thousand tablets per material | Weight percent of |
| Sulfamethoxazole | 4kg | 72.01％ |
| Methoxybenzylamine pyrimidines | 0.8kg | 14.40％ |
| Starch | 0.545kg | 9.81％ |
| Magnesium stearate | 0.03Kg | 0.54％ |
| Low-substituted hydroxypropyl cellulose | See the following Table | See the following Table |
| Sodium carboxymethyl starch | See the following Table | See the following Table |
The preparation method comprises the following steps: the same as in example 3.
The prepared compound sulfamethoxazole tablets are subjected to weight difference, friability and four dissolution curve detections in pH1.2, pH4.0, pH6.8, water and the like, and compared with the original ground product, f2 is calculated, and the results are as follows:
as can be seen from examples 1-7 and comparative example 3, the dosage of the disintegrant low-substituted hydroxypropyl cellulose and sodium carboxymethyl starch affect the dissolution behavior of the sample, and the dissolution curve f2 of the compound sulfamethoxazole tablet prepared by the invention in 4 media is not lower than 50 (compared with the original product).
Comparative example 4: compound sulfamethoxazole tablet
The prescription composition is as follows: the same as in example 3.
The preparation method comprises the following steps: step (1) to step (6) were the same as in example 3, and step (7) was as follows:
the prepared compound sulfamethoxazole tablets are subjected to weight difference, friability and four dissolution curve detections in pH1.2, pH4.0, pH6.8, water and the like, and compared with the original ground product, f2 is calculated, and the results are as follows:
example 8: stability test
Samples of examples 1-7, comparative examples 4-1, comparative examples 4-2, at a temperature of 40 ℃. + -. 2 ℃; the sample was left under 75% + -5% (accelerated) relative humidity for 6 months, and at the end of the 6 th month, the dissolution curve and the like were measured, and the results are shown in the following table.
The compound sulfamethoxazole tablet prepared by the method of the invention is accelerated to stand for 6 months, has a dissolution curve f2 of not less than 50, has the same in vitro dissolution behavior as the original product, and has the same treatment effect.
As can be seen from examples 1 to 7 and comparative example 4, the tablet compression pressure affects the dissolution profile of the sample; the compound sulfamethoxazole tablets prepared in the comparative examples 4-1 and 4-2 are placed for 6 months at an accelerated speed, 1-2 dissolution curves f2 in the four dissolution curves are lower than 50, and the compound sulfamethoxazole tablets have larger difference with the dissolution curves of the original grinding products and larger difference of treatment effects.
Claims (8)
1. The compound sulfamethoxazole tablet comprises the following components in parts by weight:
In the compound sulfamethoxazole tablets, each tablet contains 0.4g of sulfamethoxazole and 80mg of trimethoprim;
the preparation method comprises the following steps:
(1) preparing raw materials and auxiliary materials:
firstly, screening sulfamethoxazole and trimethoprim through a 80-mesh sieve; sieving magnesium stearate, hydroxypropyl cellulose, sodium carboxymethyl starch and starch with 120 mesh sieve;
preparing 25-28% of starch into 8.5-9.5% of starch slurry; as a binder; controlling the temperature to be 40-45 ℃ for standby;
(2) mixing and preparing a soft material:
firstly, the sulfamethoxazole, the trimethoprim and the residual starch are placed in a groove type mixer to be mixed for 10 to 20 minutes, the stirring speed is 100 plus 150rpm, and the shearing speed is 600 plus 800 rpm;
② the stirring speed is 100-150rpm, the shearing speed is 1000-1200rpm, and the adhesive with the temperature of 40-45 ℃ is added within 7-10 minutes;
thirdly, stirring at the speed of 100-1200 rpm and the shear at the speed of 1000-150 rpm for 13-15 minutes to prepare a proper soft material and then discharging the soft material;
(3) and (3) granulating: granulating with 14 mesh nylon sieve swing granulator to obtain uniform granules with appropriate hardness and size;
(4) and (3) drying: drying at 60-70 ℃ for 210 minutes, and controlling the water content to be 1.5-3.0%;
(5) straightening: adding additional adjuvants such as magnesium stearate, hydroxypropyl cellulose, and sodium carboxymethyl starch before granulating; granulating with 14 mesh nylon sieve, and making into uniform granule without long rod and appropriate amount of fine powder;
(6) total mixing: adding the granules after finishing the granules into a V-shaped mixer, and totally mixing for 28-32 minutes; rotating positively and negatively for 14-16 minutes respectively;
(7) tabletting: pressing into tablets, wherein the pressing pressure is 70-90KN, and the compound sulfamethoxazole tablets are obtained;
in the step (5), the particle size distribution after size stabilization is as follows:
。
2. The compound sulfamethoxazole tablet of claim 1, which is composed of the following components in parts by weight:
。
3. The compound sulfamethoxazole tablet according to claim 1, wherein in the step (1), 9.0% of starch slurry is prepared.
4. The compound sulfamethoxazole tablet according to claim 1, wherein in the step (4), the compound sulfamethoxazole tablet is dried for 180 minutes.
5. The compound sulfamethoxazole tablet of claim 1, wherein in the step (4) of the preparation method, the water content is controlled to be 1.7% -2.5%.
6. The compound sulfamethoxazole tablet according to claim 1, wherein in the step (6), the preparation method comprises mixing for 30 minutes.
7. The compound sulfamethoxazole tablet of claim 1, wherein the compression pressure in the preparation method is 75-85N.
8. The compound sulfamethoxazole tablet according to claim 1, wherein the pressure of the tablet is 80N.
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| JP6245786B2 (en) * | 2011-10-17 | 2017-12-13 | 大同化成工業株式会社 | Pharmaceutical binding agent and preparation using the binding agent |
| EP2674149B1 (en) * | 2012-06-15 | 2017-10-04 | Shin-Etsu Chemical Co., Ltd. | Method of preparing composite granule comprising low-substituted hydroxypropyl cellulose and rapid release preparation |
| CN105769883A (en) * | 2014-12-17 | 2016-07-20 | 康普药业股份有限公司 | Compound sulfamethoxazole dispersible tablet and preparation method thereof |
| CN108743552A (en) * | 2018-06-30 | 2018-11-06 | 郑州明泽医药科技有限公司 | A kind of compound sulfamethoxazole and trimethoprim tablets agent and preparation method thereof |
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Address after: No.47 Zhongxing Street, Lincheng Economic Development Zone, Xingtai City, Hebei Province 054300 Applicant after: HEBEI JUNLIN PHARMACEUTICAL Co.,Ltd. Address before: 054300 North Ring East Road, Lincheng Town, Lincheng County, Xingtai City, Hebei Province Applicant before: HEBEI JUNLIN PHARMACEUTICAL Co.,Ltd. |
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Denomination of invention: A compound sulfamethoxazole tablet and its preparation method Granted publication date: 20220809 Pledgee: Xingtai Lincheng Branch of China Construction Bank Co.,Ltd. Pledgor: HEBEI JUNLIN PHARMACEUTICAL CO.,LTD. Registration number: Y2024980003537 |