CN108743552A - A kind of compound sulfamethoxazole and trimethoprim tablets agent and preparation method thereof - Google Patents
A kind of compound sulfamethoxazole and trimethoprim tablets agent and preparation method thereof Download PDFInfo
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2095—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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- A—HUMAN NECESSITIES
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- 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
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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
- A61K31/63—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
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- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
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- 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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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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Abstract
The invention discloses a kind of compound sulfamethoxazole and trimethoprim tablets agent and preparation method thereof, which is added with filler, adhesive, disintegrant, surfactant, lubricant and coating agent using Sulfamethoxazole and trimethoprim as main effect medicine；Then compound sulfamethoxazole and trimethoprim tablets agent has been prepared by operating procedures such as mixing, granulation, drying, tabletting, coatings.Gained compound sulfamethoxazole and trimethoprim tablets agent composition of the invention effectively prevents the side's Fu Sulfamethoxazole solid pharmaceutical preparation loose pieces caused by particle viscosity is not strong, and significantly improve the dissolution of said preparation, ensure the stability of preparation, improve the product quality of preparation, it ensure that the quality and curative effect of said preparation, there is good application prospect.
Description
Technical field
The invention belongs to field of medicine preparations, and in particular to a kind of compound sulfamethoxazole and trimethoprim tablets agent and preparation method thereof.
Technical background
The side's Fu Sulfamethoxazole preparation is disulfonamide, is Sulfamethoxazole and the compound preparation of trimethoprim, right
Non- producing enzyme staphylococcus aureus, micrococcus scarlatinae, streptococcus pneumonia, escherichia coli, Klebsiella, Salmonella,
The enterobacteriaceae lactobacteriaceaes such as Proteus, Morganella, Shigella, gonococcus, Neisseria meningitidis, haemophilus influenzae are equal
With good antibacterial action, especially to escherichia coli, haemophilus influenzae, staphylococcus aureus antibacterial action compared with sulphur
An Jia oxazole list medicines are remarkably reinforced.In addition, the tablet exerts the tools such as card bacterium, protozoon, toxoplasma to chlamydia trachomatis, star in vitro
There is good antimicrobial acivity.
Sulfamethoxazole in the side's Fu Sulfamethoxazole preparation acts on dihydrofolate synthetase, and the of interference synthesis folic acid
One step；Trimethoprim therein acts on the anabolic second step of folic acid, the effect of selective depression dihyrofolate reductase.
The sharing of the two can make the folic acid metabolism of bacterium by double blocking, generate apparent synergistic effect, drug effect is better than any one
The single medicine of kind is remarkably reinforced, and is significantly reduced to its show resistance bacterial strain.Therefore, it is with Sulfamethoxazole, trimethoprim etc.
The disulfonamide of main effect medicine obtains quick research and development.
Currently, the problem that the multiple side's Sulfamethoxazole class preparation generally existing dissolution rate prepared is slow, and dissolution rate subtracts
Slowly absorption of the drug in human body can be largely effected on so that the drug loses its due value.Preparation process in this field
In in order to solve this problem, most of is that a large amount of disintegrant is added, although the addition of a large amount of disintegrants can significantly improve
The dissolution rate of preparation, but the presence of a large amount of disintegrants can cause loose pieces phenomenon, and the quality of preparation is seriously affected, reduce drug
Qualification rate, influence drug use.
Invention content
To solve the above-mentioned problems, the present invention provides a kind of compound sulfamethoxazole and trimethoprim tablets agent and preparation method thereof.This is multiple
Square Gamazole Tab greatly reduces the addition of disintegrant, and obtained tablet quality is stablized, and dissolution in vitro is high；This hair
The preparation method of bright offer can effectively prevent from affecting quality and curative effect because bare die loses powder.
The present invention is achieved by the following technical solutions
A kind of compound sulfamethoxazole and trimethoprim tablets agent, the tablet further include using Sulfamethoxazole and trimethoprim as main component
Filler, adhesive, disintegrant, surfactant, lubricant and coating agent.
The mass percentage of the compound sulfamethoxazole and trimethoprim tablets agent, the Sulfamethoxazole is 70~80%, described
The mass percentage of trimethoprim is 10~20%, and the mass percentage of the filler is 2~8% (preferably 3%),
The mass percentage of described adhesive is 0.5~4% (preferably 2%), the mass percentage of the disintegrant is 2~
8% (is preferably 2~5%, more preferably 3%), the mass percentage of the surfactant (is preferably for 0.1~2.0%
1.5%), the mass percentage of the lubricant is 0.3~0.8% (preferably 0.5%)；
The mass percentage that the coating agent accounts for above-mentioned substance total amount is 2.0~5.0% (preferably 3.0%).
The compound sulfamethoxazole and trimethoprim tablets agent, the filler are starch or pregelatinized starch；The adhesive
For starch；The lubricant is magnesium stearate or sodium stearyl fumarate.
The compound sulfamethoxazole and trimethoprim tablets agent, the disintegrant are sodium carboxymethyl starch, low substituted hydroxy-propyl fiber
Element or croscarmellose sodium.
The compound sulfamethoxazole and trimethoprim tablets agent, the surfactant are Tween-80, cetyltrimethylammonium
Amine, lauryl sodium sulfate, stearyl alcohol sodium sulfonate or docusate sodium；The coating agent is enteric film coating agent.
The preparation method of above-mentioned compound sulfamethoxazole and trimethoprim tablets agent, this approach includes the following steps：
(1) prepare raw material and auxiliary material, all raw materials and the auxiliary material of preparation are sieved with 100 mesh sieve；
(2) it takes starch to be dissolved in purified water, be uniformly mixed starch slurry；It takes surfactant in purified water, makes it
Surfactant is completely dissolved to obtain the aqueous solution (as long as surfactant is completely dissolved) of surfactant；Surface is lived
The aqueous solution of property agent, which is added in starch slurry, to be mixed evenly, and the mixture of surfactant and starch slurry is obtained；
(3) it takes Sulfamethoxazole, trimethoprim and filler to be uniformly mixed, after mixing, is added what step (2) obtained
The mixture of surfactant and starch slurry is pelletized；It is dried after the completion of granulation, obtains dry particl；
(4) dry particl for obtaining step (3) and the ready disintegrant of step (1) and mix lubricant are uniform, carry out
Tabletting obtains tablet；
(5) coating agent that step (1) prepares is used to carry out film coating to the tablet that step (4) obtains, after the completion of coating
Obtain compound sulfamethoxazole and trimethoprim tablets agent composition.
The mass concentration of the preparation method of the compound sulfamethoxazole and trimethoprim tablets agent composition, step (2) described starch slurry is 3
~15%, preferably 8%.
The preparation method of the compound sulfamethoxazole and trimethoprim tablets agent composition, step (3) instrument used of pelletizing is height
The rotating speed of fast mixer-granulator, pelletization high speed mixer-granulator agitating paddle is 150rpm, and the rotating speed of cutter is
2000rpm；Described pair granulation be dried for use boiling drier be dried (dry when inlet air temperature for 65 DEG C, go out
Air temperature is 35 DEG C), water content≤3% of gained dry particl after the completion of drying.
The preparation method of the compound sulfamethoxazole and trimethoprim tablets agent composition, pressure when step (4) described tabletting is 45~
55KN；Step (5) is described to be coated specially tablet：It is coated using seed-coating machine, in seed-coating machine coating process, turntable
Speed be 20HZ, inlet air temperature when coating is 40~50 DEG C, 5.0~9.0rpm of peristaltic pump, spray gun pressure 0.15
~0.2MPa.
The preparation method of the compound sulfamethoxazole and trimethoprim tablets agent, which is characterized in that step (5) is described will to be wrapped using high purity water
The mass concentration of coating agent is 12~15% in the solution that clothing agent is prepared.
Compared with prior art, the present invention has following positive beneficial effect
The present invention is reduced the addition of disintegrant, is effectively avoided by the optimal addition of adhesive and surfactant
The side the Fu Sulfamethoxazole solid pharmaceutical preparation loose pieces caused by particle viscosity is not strong, and the dissolution of said preparation is significantly improved,
The stability for ensuring preparation improves the product quality of preparation, has good application prospect；
The present invention effectively prevents bare die in preparation process and loses powder, further ensure said preparation by wet granulation
Quality and curative effect；
The reference preparation that compound sulfamethoxazole and trimethoprim tablets agent prepared by the present invention is developed with SUN PHARM INDS companies of the U.S.
Both tetra- stripping curves of BACTRIM are consistent, greatly reduce imitation medicine and grind the difference of medicine in terms of quality with former, improve
Bioequivalence.To pushing current China's imitation medicine Conformance Assessment to have great significance.
Description of the drawings
Fig. 1 is that 4 of Sulfamethoxazole and Sulfamethoxazole in reference preparation BACTRIM in 4 products obtained therefrom of embodiment are molten
Go out curve comparison figure；
Fig. 2 is that 4 dissolutions of trimethoprim and trimethoprim in reference preparation BACTRIM in 4 products obtained therefrom of embodiment are bent
Line comparison diagram.
Specific implementation mode
The present invention is described in more details below by specific implementation mode, but is not intended to restrict the invention
Protection domain.
The coating agent used in following embodiment is Opadry enteric film coating agent.
Embodiment 1
A kind of compound sulfamethoxazole and trimethoprim tablets agent composition, is prepared by the ingredient of following weight percentage：
The coating agent is enteric film coating agent, which accounts for above-mentioned raw materials and the quality percentage of auxiliary material total amount contains
Amount is 2%
The preparation method of the compound sulfamethoxazole and trimethoprim tablets agent composition is as follows：
(1) prepare Sulfamethoxazole, trimethoprim, starch (filler), starch (bonding according to above-mentioned prescription requirements
Agent), low-substituted hydroxypropyl cellulose, stearyl alcohol sodium sulfonate, magnesium stearate, enteric film coating agent, sieve with 100 mesh sieve；
(2) it takes step (1) ready starch (adhesive) to be dissolved in purified water and is uniformly mixing to obtain starch slurry (gained shallow lake
5%) mass concentration of slurry is；Then it takes the ready stearyl alcohol sodium sulfonate of step (1) to be dissolved in purified water, waits being completely dissolved
The aqueous solution of stearyl alcohol sodium sulfonate is obtained afterwards；Then the starch slurry for being 5% by the aqueous solution of stearyl alcohol sodium sulfonate and mass concentration
It is uniformly mixed to get to the mixture of stearyl alcohol sodium sulfonate and starch slurry；
(3) the ready Sulfamethoxazole of step (1), trimethoprim and starch (filler) is taken to be uniformly mixed, then
The mixture of stearyl alcohol sodium sulfonate and starch slurry that step (2) is prepared is added, is uniformly mixed；After mixing, using height
Fast mixer-granulator is pelletized, and is 150rpm, is sliced in the rotating speed of the agitating paddle of pelletization high speed mixer-granulator
Rotating speed is 2000rpm, and granulation can be completed in high-speed mixing granulating machine effect 3min；After the completion of granulation, using boiling drier pair
The particle of preparation is dried, and inlet air temperature when dry is 65 DEG C, 35 DEG C of leaving air temp, gained dry particl after the completion of drying
Water content≤3% (is detected) using fast tester for water content；
(4) dry particl for taking the ready low-substituted hydroxypropyl cellulose of step (1), magnesium stearate and step (3) to obtain
It is mixed；After mixing, tabletting is carried out using tablet press machine, pressure when tabletting is 45KN, and tabletting is completed to obtain tablet；
(5) it and then takes the ready coating agent of step (1), high purity water is used to be formulated as mass concentration as 12% packet
Clothing agent aqueous solution；After the completion of preparation, the tablet obtained to step (4) using seed-coating machine is coated processing, is wrapped to tablet
The speed of turntable is 20HZ when clothing processing, and inlet air temperature is 45 ± 5 DEG C, and the pressure of peristaltic pump 6.0rpm, spray gun are
0.15~0.2MPa.
Embodiment 2
A kind of compound sulfamethoxazole and trimethoprim tablets agent composition, is prepared by the ingredient of following weight percentage：
The coating agent is enteric film coating agent, and the coating agent accounts for the quality hundred of above-mentioned raw materials and auxiliary material total amount
It is 3% to divide content
The preparation method of the compound sulfamethoxazole and trimethoprim tablets agent composition is as follows：
(1) prepare Sulfamethoxazole, trimethoprim, starch (filler), starch (bonding according to above-mentioned prescription requirements
Agent), croscarmellose sodium, cetab, sodium stearyl fumarate, enteric film coating agent, mistake
100 mesh sieve；
(2) it takes step (1) ready starch (adhesive) to be dissolved in purified water and is uniformly mixing to obtain starch slurry (gained shallow lake
10%) mass concentration of slurry is；Then it takes step (1) ready cetab to be dissolved in purified water, waits for
The aqueous solution of cetab is obtained after being completely dissolved；Then by the aqueous solution of cetab and matter
A concentration of 10% starch slurry is measured to be uniformly mixed to get to the mixture of cetab and starch slurry；
(3) the ready Sulfamethoxazole of step (1), trimethoprim and starch (filler) is taken to be uniformly mixed, then
The mixture of cetab and starch slurry that step (2) is prepared is added, is uniformly mixed；After mixing,
Pelletized using high-speed mixing granulating machine, pelletization high speed mixer-granulator agitating paddle rotating speed be 150rpm,
The rotating speed of slice is 2000rpm, and granulation can be completed in high-speed mixing granulating machine effect 3min；It is dry using boiling after the completion of granulation
The particle of preparation is dried in dry machine, and inlet air temperature when dry is 65 DEG C, 35 DEG C of leaving air temp, and gained is dry after the completion of drying
Water content≤3% (being detected using fast tester for water content) of particle；
(4) the ready croscarmellose sodium of step (1), sodium stearyl fumarate and step (3) is taken to obtain dry
Particle is mixed；After mixing, tabletting is carried out using tablet press machine, pressure when tabletting is 45KN, and tabletting is completed to obtain piece
Agent；(5) step (1) ready coating agent is taken, using high purity water to prepare becomes mass concentration as 12% coating agent aqueous solution；
After the completion of preparation, the tablet obtained to step (4) using seed-coating machine is coated processing, turntable when being coated processing to tablet
Speed be 20HZ, inlet air temperature is 45 ± 5 DEG C, peristaltic pump 6.0rpm, and the pressure of spray gun is 0.15~0.2MPa.
Embodiment 3
A kind of compound sulfamethoxazole and trimethoprim tablets agent composition, is prepared by the ingredient of following weight percentage：
The coating agent is enteric film coating agent, and the coating agent accounts for the quality hundred of above-mentioned raw materials and auxiliary material total amount
It is 3% to divide content
The preparation method of the compound sulfamethoxazole and trimethoprim tablets agent composition is as follows：
(1) prepare Sulfamethoxazole, trimethoprim, starch (filler), starch (bonding according to above-mentioned prescription requirements
Agent), croscarmellose sodium, cetab, sodium stearyl fumarate, enteric film coating agent, mistake
100 mesh sieve；
(2) it takes step (1) ready starch (adhesive) to be dissolved in purified water and is uniformly mixing to obtain starch slurry (gained shallow lake
8%) mass concentration of slurry is；Then it takes step (1) ready cetab to be dissolved in purified water, has waited for
The aqueous solution of hard cetab is obtained after fully dissolved；Then by the aqueous solution of cetab and matter
A concentration of 8% starch slurry is measured to be uniformly mixed to get to the mixture of cetab and starch slurry；
(3) the ready Sulfamethoxazole of step (1), trimethoprim and starch (filler) is taken to be uniformly mixed, then
The mixture of cetab and starch slurry that step (2) is prepared is added, is uniformly mixed；After mixing,
Pelletized using high-speed mixing granulating machine, pelletization high speed mixer-granulator agitating paddle rotating speed be 150rpm,
The rotating speed of slice is 2000rpm, and granulation can be completed in high-speed mixing granulating machine effect 3min；It is dry using boiling after the completion of granulation
The particle of preparation is dried in dry machine, and inlet air temperature when dry is 65 DEG C, 35 DEG C of leaving air temp, and gained is dry after the completion of drying
Water content≤3% (being measured using fast tester for water content) of particle；
(4) the ready croscarmellose sodium of step (1), sodium stearyl fumarate and step (3) is taken to obtain dry
Particle is mixed；After mixing, tabletting is carried out using tablet press machine, pressure when tabletting is 45KN, and tabletting is completed to obtain piece
Agent；(5) step (1) ready coating agent is taken, using high purity water to prepare coating agent becomes mass concentration as 12% coating
Agent aqueous solution；After the completion of preparation, the tablet obtained to step (4) using seed-coating machine is coated processing, is coated to tablet
The speed of turntable is 20HZ when processing, and inlet air temperature is 45 ± 5 DEG C, peristaltic pump 6.0rpm, and the pressure of spray gun is 0.15
~0.2MPa.
Embodiment 4
A kind of compound sulfamethoxazole and trimethoprim tablets agent composition, is prepared by the ingredient of following weight percentage：
The coating agent is enteric film coating agent, and the coating agent accounts for the quality hundred of above-mentioned raw materials and auxiliary material total amount
It is 3% to divide content
The preparation method of the compound sulfamethoxazole and trimethoprim tablets agent composition is as follows：
(1) prepare Sulfamethoxazole, trimethoprim, starch (filler), starch (bonding according to above-mentioned prescription requirements
Agent), sodium carboxymethyl starch, lauryl sodium sulfate, magnesium stearate, enteric film coating agent, sieve with 100 mesh sieve；
(2) it takes step (1) ready starch (adhesive) to be dissolved in purified water and is uniformly mixing to obtain starch slurry (gained shallow lake
8%) mass concentration of slurry is；Then it takes step (1) ready lauryl sodium sulfate to be dissolved in purified water, waits for completely molten
The aqueous solution of lauryl sodium sulfate is obtained after solution；Then it is 8% by the aqueous solution of lauryl sodium sulfate and mass concentration
Starch slurry is uniformly mixed to get to the mixture of lauryl sodium sulfate and starch slurry；
(3) the ready Sulfamethoxazole of step (1), trimethoprim and starch (filler) is taken to be uniformly mixed, then
The mixture of lauryl sodium sulfate and starch slurry that step (2) is prepared is added, is uniformly mixed；After mixing, it uses
High-speed mixing granulating machine is pelletized, and is 150rpm, is sliced in the rotating speed of the agitating paddle of pelletization high speed mixer-granulator
Rotating speed be 2000rpm, high-speed mixing granulating machine effect 3min granulation can be completed；After the completion of granulation, using boiling drier
The particle of preparation is dried, inlet air temperature when dry is 65 DEG C, 35 DEG C of leaving air temp, gained dry particl after the completion of drying
Water content≤3% (being measured using fast tester for water content)；
(4) dry particl that the ready sodium carboxymethyl starch of step (1), magnesium stearate and step (3) obtain is taken to be mixed
It closes；After mixing, tabletting is carried out using tablet press machine, pressure when tabletting is 45KN, and tabletting is completed to obtain tablet；
(5) step (1) ready coating agent is taken, using high purity water to prepare coating agent becomes mass concentration as 12%
Coating agent aqueous solution；After the completion of preparation, processing is coated to obtained tablet using seed-coating machine, processing is coated to tablet
When turntable speed be 20HZ, inlet air temperature is 45 ± 5 DEG C, peristaltic pump 6.0rpm, the pressure of spray gun is 0.15~
0.2MPa。
For the reference preparation BACTRIM of compound sulfamethoxazole tablets agent composition and the U.S. that embodiment 4 is prepared
4 stripping curve comparisons are carried out, curve graph is as shown in Figures 1 and 2, and result is as shown in table 1 and table 2.
The dissolution pair of Sulfamethoxazole and Sulfamethoxazole in reference preparation BACTRIM in 1 embodiment of table, 4 products obtained therefrom
Than
The dissolution of trimethoprim and trimethoprim in reference preparation BACTRIM compares in 2 embodiment of table, 4 products obtained therefrom
From the above results：The side's Fu Sulfamethoxazole preparation prepared by the method according to the invention is carried out with reference preparation
The comparisons of 4 stripping curves, as a result dissolved corrosion is consistent.The product that i.e. prepared by the present invention grinds product with original and reaches in vitro
" quality is equivalent ", can obtain the present invention the side's Fu Sulfamethoxazole preparation interior quality ground with original it is close, in view of dissolution in vitro
With the correlation of vivo biodistribution availability, it can show that the consistent probability of the two vivo biodistribution availability is high, and then have identical face
Bed curative effect.
Then use Chinese Pharmacopoeia version standard in 2015, in the side's Fu Sulfamethoxazole that embodiment 4 is prepared main effect at
Point content is detected, and the results are shown in Table 3：
The content detection result of main ingredient in 3 embodiment of table, 4 products obtained therefrom
Compound sulfamethoxazole and trimethoprim tablets agent prepared by 1~embodiment of embodiment 3 is identical as the testing result of embodiment 4.By
The above can obtain, and the present invention increases the stability of compound sulfamethoxazole and trimethoprim tablets agent, improves under conditions of disintegrant is less
Dissolving out capability, preparation method is simple, quick, is very beneficial for industrialized mass production, has good application prospect.
Claims (10)
1. a kind of compound sulfamethoxazole and trimethoprim tablets agent, which is characterized in that the compound sulfamethoxazole and trimethoprim tablets agent is with Sulfamethoxazole and first
Oxygen benzyl pyridine is main component, further includes filler, adhesive, disintegrant, surfactant, lubricant and coating agent.
2. compound sulfamethoxazole and trimethoprim tablets agent according to claim 1, which is characterized in that
The mass percentage of the Sulfamethoxazole is 70~80%,
The mass percentage of the trimethoprim is 10~20%,
The mass percentage of the filler is 2~8%,
The mass percentage of described adhesive is 0.5~4%,
The mass percentage of the disintegrant is 2~8%,
The mass percentage of the surfactant is 0.1~2.0%,
The mass percentage of the lubricant is 0.3~0.8%；
The mass percentage that the coating agent accounts for above-mentioned substance total amount is 2.0~5.0%.
3. compound sulfamethoxazole and trimethoprim tablets agent according to claim 1 or 2, which is characterized in that the filler is starch
Or pregelatinized starch；The adhesive is starch；The lubricant is magnesium stearate or sodium stearyl fumarate.
4. compound sulfamethoxazole and trimethoprim tablets agent according to claim 1 or 2, which is characterized in that the disintegrant is carboxymethyl
Sodium starch, low-substituted hydroxypropyl cellulose or croscarmellose sodium.
5. compound sulfamethoxazole and trimethoprim tablets agent according to claim 1 or 2, which is characterized in that the surfactant is
Tween-80, cetab, lauryl sodium sulfate, stearyl alcohol sodium sulfonate or docusate sodium；The coating agent
For enteric film coating agent.
6. the preparation method of compound sulfamethoxazole and trimethoprim tablets agent described in a kind of claim 1, which is characterized in that this method includes following
Step：
(1) prepare raw material and auxiliary material, the raw material of preparation is sieved with 100 mesh sieve with auxiliary material；
(2) take step (1) ready starch be dissolved in purified water, be uniformly mixed obtain starch slurry；Take step (1) ready table
Face activating agent is completely dissolved in purified water, obtains the aqueous solution of surfactant；Then the aqueous solution of surfactant is added
Enter into starch slurry and be uniformly mixed, obtains the mixture of surfactant and starch slurry；
(3) it takes the ready Sulfamethoxazole of step (1), trimethoprim and filler to be uniformly mixed, step is added after mixing
Suddenly the mixture for the surfactant and starch slurry that (2) obtain is uniformly mixed, pelletizes, carried out after granulation after mixing
It is dry, obtain dry particl；
(4) dry particl for obtaining step (3) and the ready disintegrant of step (1), mix lubricant are uniform, after mixing
Tabletting is carried out, tablet is obtained；
(5) using the coating agent that high purity water prepares step (1) to prepare becomes solution, the tablet then obtained to step (4)
Film coating is carried out, compound sulfamethoxazole and trimethoprim tablets agent is obtained after the completion of coating.
7. the preparation method of compound sulfamethoxazole and trimethoprim tablets agent according to claim 6, which is characterized in that step (2) described shallow lake
The mass concentration of slurry is 3~15%.
8. the preparation method of compound sulfamethoxazole and trimethoprim tablets agent according to claim 6, which is characterized in that step (3) described system
For the instrument that grain uses for high-speed mixing granulating machine, the rotating speed of pelletization high speed mixer-granulator agitating paddle is 150rpm, is cut
The rotating speed of piece is 2000rpm；Described pair of granulation is dried to be dried using boiling drier, inlet air temperature when dry
It it is 65 DEG C, leaving air temp is 35 DEG C, water content≤3% of gained dry particl after the completion of drying.
9. the preparation method of compound sulfamethoxazole and trimethoprim tablets agent according to claim 6, which is characterized in that step (4) described pressure
Pressure when piece is 45~55KN；Step (5) is described to be coated specially tablet：Tablet is wrapped using seed-coating machine
Clothing, the frequency of coating process turntable are 20HZ, and inlet air temperature when coating is 40~50 DEG C, 5.0~9.0rpm of peristaltic pump, spray
Rifle pressure is 0.15~0.2MPa.
10. according to the preparation method of the compound sulfamethoxazole and trimethoprim tablets agent of claim 6 or 9, which is characterized in that step (5) institute
The mass concentration of coating agent in the solution for using high purity water to prepare coating agent is stated as 12~15%.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111023705A (en) * | 2019-12-27 | 2020-04-17 | 上海华源安徽锦辉制药有限公司 | Drying method in acetaminophen tablet granulation procedure |
| CN112190557A (en) * | 2020-09-18 | 2021-01-08 | 河北君临药业有限公司 | Compound sulfamethoxazole tablets and preparation method thereof |
| CN112190556A (en) * | 2020-09-18 | 2021-01-08 | 河北君临药业有限公司 | Compound sulfamethoxazole trimethoprim tablet and preparation method thereof |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1480145A (en) * | 2002-09-05 | 2004-03-10 | 上海曼迪新科技合作公司 | Multilayer tablet and multicolor capsule of compound Sulphamethoxazole |
| CN103690546A (en) * | 2013-12-23 | 2014-04-02 | 聊城大学 | Orally disintegrating tablet for preventing and treating toxoplasmosis and preparation method thereof |
| 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 |
-
2018
- 2018-06-30 CN CN201810703066.5A patent/CN108743552A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1480145A (en) * | 2002-09-05 | 2004-03-10 | 上海曼迪新科技合作公司 | Multilayer tablet and multicolor capsule of compound Sulphamethoxazole |
| CN103690546A (en) * | 2013-12-23 | 2014-04-02 | 聊城大学 | Orally disintegrating tablet for preventing and treating toxoplasmosis and preparation method thereof |
| 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 |
Non-Patent Citations (4)
| Title |
|---|
| 史向文等: ""复方磺胺甲噁唑片崩解度问题的工艺改进"", 《安徽医药》 * |
| 宿永成: ""羧甲基淀粉钠对复方磺胺甲噁唑片崩解剂的改善作用"", 《科技园地》 * |
| 张汉忠等: ""几种崩解剂在复方磺胺甲基异嗯哩片中的崩解时限比较"", 《中国药业》 * |
| 陈华萍等: ""复方磺胺甲噁唑片崩解工艺的改进"", 《浙江医学院学报》 * |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111023705A (en) * | 2019-12-27 | 2020-04-17 | 上海华源安徽锦辉制药有限公司 | Drying method in acetaminophen tablet granulation procedure |
| CN112190557A (en) * | 2020-09-18 | 2021-01-08 | 河北君临药业有限公司 | Compound sulfamethoxazole tablets and preparation method thereof |
| CN112190556A (en) * | 2020-09-18 | 2021-01-08 | 河北君临药业有限公司 | Compound sulfamethoxazole trimethoprim tablet and preparation method thereof |
| CN112190556B (en) * | 2020-09-18 | 2022-08-12 | 河北君临药业有限公司 | Compound sulfamethoxazole trimethoprim tablet and preparation method thereof |
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