CN110051637A - Amoxicillin and clavulanate potassium preparation and preparation method thereof - Google Patents
Amoxicillin and clavulanate potassium preparation and preparation method thereof Download PDFInfo
- Publication number
- CN110051637A CN110051637A CN201910422568.5A CN201910422568A CN110051637A CN 110051637 A CN110051637 A CN 110051637A CN 201910422568 A CN201910422568 A CN 201910422568A CN 110051637 A CN110051637 A CN 110051637A
- Authority
- CN
- China
- Prior art keywords
- preparation
- amoxicillin
- clavulanate
- potassium
- temperature
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/42—Oxazoles
- A61K31/424—Oxazoles condensed with heterocyclic ring systems, e.g. clavulanic acid
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/429—Thiazoles condensed with heterocyclic ring systems
- A61K31/43—Compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula, e.g. penicillins, penems
-
- 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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
-
- 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
- A61K9/2031—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Amoxicillin and clavulanate potassium preparation of the present invention and preparation method thereof, amoxicillin and clavulanate potassium can be prepared into two kinds of dosage forms, one is by Amoxicillin and potassium clavulanate and a certain amount of water-soluble base it is miscible after, dripping pill is prepared into using dripping pill technology of preparing；Another kind is that Amoxicillin and auxiliary material are first carried out micro mist crushing, it is uniformly mixed, as adhesive after using a certain amount of water to dissolve potassium clavulanate, granule is prepared into using spray granulation processes, the amoxicillin and clavulanate potassium preparation prepared using above two method has production simple, and bioavilability is high, it absorbs fastly, proves effective the advantages that rapid.
Description
Technical field
The invention belongs to pharmaceutical technology fields, and in particular to amoxicillin and clavulanate potassium preparation and preparation method thereof.
Background technique
Amoxicillin also known as amoxicillin or Amoxicillin are that a kind of most common semi-synthetic penicillins wide spectrum β-is interior
Amides antibiotic is a kind of white powder, is one of current widely used oral semisynthetic penicillin.
Potassium clavulanate is crystalline powder white or yellowish, and it is invalid to be used alone, and is often combined with penicillin medicine
Using to overcome microorganism to produce drug resistance caused by beta-lactamase, curative effect is improved.
Amoxicillin and potassium clavulanate are used in combination, and are suitable for microorganism and produce beta-lactamase haemophilus influenzae and card
Lower respiratory tract infection caused by his Moraxella, tympanitis, nasosinusitis, microorganism produce beta-lactamase S. aureus L-forms and producing enzyme enterobacteria
Section bacterium urinary tract as caused by escherichia coli, Klebsiella and skin soft-tissue infection etc.；Also can be used for caused by enterococcus
Light, grade and moderate infection.
Patent No. CN200810212280.7 discloses a kind of amoxicillin/clavulanate potassium 8: 1 and its preparation side
Method, the preparation method are the preparation method works using the good intermediate blended stock of quality controllability, mixture homogeneity as main ingredient source
Skill is simply its advantage, but bad in terms of bioavilability and uniformity of dosage units.
Publication No. is that CN200910074500.9 discloses a kind of preparation method of amoxicillin and clavulanate potassium tablets, should
Preparation method is Amoxicillin to be made after particle to mix with potassium clavulanate, then all auxiliary materials are added with equivalent gradually-increased and carry out
Mixing, the tablet prepared with this method, the disadvantage is that incorporation time is longer, feeding requirement is more stringent, is difficult to control technique
Stability.
Publication No. is that CN101897701B discloses a kind of preparation process of amoxicillin and clavulanate potassium tablets, and being will
It after the granulation of Amoxicillin original powder, then is uniformly mixed with potassium clavulanate, hence improves the mobility of major ingredient itself, effectively avoid
Phenomena such as capping, sticking caused by direct tablet compressing.
Number of patent application is 201710569445.5 to disclose a kind of amoxicillin and clavulanate potassium preparation and its preparation side
Method, the amoxicillin and clavulanate potassium dispersible tablet prepared with this method, is that Amoxicillin and trehalose are dissolved in buffer, is led to
After pervaporation granulation, then be uniformly mixed with potassium clavulanate, so that the stability of amoxicillin and clavulanate potassium improves, in relation to object
Matter content reduces.Compared with the above-mentioned published patent, which shortens process flow, reduces production cycle and medicine
Object exposure duration in air, guarantees the stability of drug, further improve the quality of product, still, in production process,
It is dissolved in buffer with Amoxicillin and trehalose, is pelletized by evaporation, reduce the active constituent content of Amoxicillin,
Reduce the curative effect of drug.
Summary of the invention
For solve the prior art deficiency, amoxicillin and clavulanate potassium preparation of the present invention and preparation method thereof, be by Ah
Amdinocillin potassium clavulanate is prepared into two kinds of dosage forms, and one is by Amoxicillin and potassium clavulanate and a certain amount of water-soluble base
After matter is miscible, dripping pill is prepared into using dripping pill technology of preparing, another kind is that Amoxicillin and auxiliary material are carried out micro mist crushing, general gram
Clavulanic acid potassium use a certain amount of water to dissolve after as adhesive, granule is prepared into using cold nebulization method of granulating, in utilization
Amoxicillin and clavulanate potassium preparation prepared by two methods is stated, has bioavilability high, absorbs fastly, is proved effective rapid etc. excellent
Point.
It is prepared using following technical scheme, the present invention can be obtained:
Pill and granule can be made in amoxicillin and clavulanate potassium preparation and preparation method thereof,
1, it is prepared into pill
1.1 prescriptions: raw material: (100.00-150.00) the g potassium clavulanate 31.25 of Amoxicillin 125 (30.00-33.00)
G,
Matrix: polyethylene glycol.
Raw material and substrate composition: as unit of g or kg, by weight, raw material: matrix=1: 0.5~5.
1.2 preparation methods:
1.2.1 according to proportion given by prescription, raw material and matrix are accurately weighed, first matrix is placed in heating container,
Adjusting temperature is (50~90) DEG C, after matrix thawing, under stirring, is slowly added to raw material, continues stirring to medical fluid and is in
Molten liquid and/or emulsion and/or suspension, it is spare；
1.2.2 the temperature control system for adjusting pill dripping machine, makes the water dropper temperature of pill dripping machine be heated and maintained at (50~90)
DEG C, the temperature of condensing agent is cooled and maintained at (40~-5) DEG C；
1.2.3 medical fluid is placed in the drop tank of pill dripping machine, is instilled in condensing agent by water dropper, will shunk by pill dripping machine outlet
Molding dripping pill takes out, and removes surface condensation agent, it is dry to get.
The matrix is cetomacrogol 1000 or polyethylene glycol 1500 or polyethylene glycol 2000 or Macrogol 4000 or gathers
Ethylene glycol 6000 or polyethylene glycol 10000 or the above two or two or more mixture of PEG 20000.
The condensing agent can be atoleine, dimethicone, any one or a few in vegetable oil.
The adjustment temperature is 50~90 DEG C or the water dropper temperature of pill dripping machine to be made to be heated and maintained at 50~90 DEG C, preferably with
55-60℃.The temperature of the condensing agent is cooled and maintained at 40~-5 DEG C, preferably with 10~0 DEG C.
Preparation method preferably with: 4000 468.75g of taking polyethylene glycol is set in material tank, open material tank heating system
System, adjustment temperature is 55-60 DEG C, after polyethylene glycol all melts, opens the agitating paddle of material tank, is slowly added to clavulanic acid
Potassium 31.25g and Amoxicillin 125g adjusts the temperature control system of pill dripping machine, makes pill dripping machine when medical fluid is at melting liquid status
Water dropper temperature be heated and maintained at 55 DEG C, the temperature of condensing agent is cooled and maintained at 3 DEG C, and medical fluid is placed in the drop tank of pill dripping machine
It is interior, it is instilled in dimethicone by water dropper, molding dripping pill will be shunk by pill dripping machine outlet and taken out, surface condensation agent is removed,
It is dry to get.
2, it is prepared into granule
2.1 prescriptions:
31.25 (30.00-33.00) g of (100-150) the g potassium clavulanate of Amoxicillin 125, (diluent is suitable for auxiliary material
Amount) microcrystalline cellulose 31.25 (30.00-33.00) g, (appropriate disintegrating agent) silica 3%~8% (disintegrating agent) carboxylic
First sodium starch 3%~8% (appropriate adhesive) microcrystalline cellulose 2%~4% (appropriate corrigent) mixes essence
0.05%~1.0% (appropriate corrigent) Icing Sugar 1.5kg lubricant is appropriate.
2.2 preparation method
2.2.1 after taking the potassium clavulanate of recipe quantity to be dissolved with suitable water, filtering obtains potassium clavulanate lysate, standby
With；
2.2.2 it after taking the Amoxicillin of recipe quantity and a certain amount of auxiliary material to be pulverized respectively, is uniformly mixed, sets spray
In mist granulating drier, adjustment granulating drier temperature is 50-90 DEG C, using potassium clavulanate lysate as adhesive, is sprayed
The particle prepared 24-40 mesh screen whole grain is added suitable lubricant and carries out total mix by mist granulation, packaging to get.
The potassium clavulanate is dissolved with suitable water, and water refers to distilled water or purified water.
The auxiliary material refers to disintegrating agent, diluent, lubricant and corrigent.
The disintegrating agent include but is not limited to soluble starch, silica, carboxyrnethyl starch sodium, sodium carboxymethylcellulose,
One of crospovidone, two or more mixture；By weight be 3-8%, preferably with silica, dosage
For diluent described in 3-8% include but is not limited to one of Icing Sugar, lactose, microcrystalline cellulose and pre-paying starch, two kinds or
Two kinds or more of composition, by weight be 1-10%, preferably with microcrystalline cellulose, dosage 10-90%.
The lubricant includes but is not limited to silica, talcum powder or magnesium stearate, is by weight 3-8%, preferably
With magnesium stearate, dosage 3-8%.
The corrigent include but is not limited to one of Icing Sugar, lactose, orange essence, flavoring apple essence, hawthorn essence, or
Two kinds or more mixtures, the preferably mixture with Icing Sugar and orange essence, dosage are 0.05%~1.0%.
The adjustment granulator temperature be 50-90 DEG C, preferably with 50-60 DEG C.
The particle that will be prepared 24-40 mesh screen whole grain, preferably and with 24 mesh screen whole grains.
Preparation method preferably with: take a small amount of water of potassium clavulanate 31.25g to dissolve, after filtering, obtain potassium clavulanate dissolution
Liquid, it is spare；Take Amoxicillin 125g, microcrystalline cellulose 3.12%, silica 5%, carboxyrnethyl starch sodium 5%, Icing Sugar 1.5kg and
It after orange essence 0.05% carries out super prestige crushing respectively, is uniformly mixed, sets in spray granulator, adjustment spray granulator temperature is
It 55 DEG C, using potassium clavulanate lysate as adhesive, carries out spraying granulation and adds 24 mesh screen whole grains of the particle prepared
Enter suitable magnesium stearate 3.5% and carry out total mix, packaging to get.
Beneficial effect
Amoxicillin and clavulanate potassium preparation of the present invention and preparation method thereof, is to be prepared into amoxicillin and clavulanate potassium
Two kinds of dosage forms, one is by Amoxicillin and potassium clavulanate and a certain amount of water-soluble base it is miscible after, prepared using dripping pill
Technology is prepared into dripping pill；Another kind is that Amoxicillin and auxiliary material are carried out micro mist crushing, by a certain amount of water of potassium clavulanate
It is used as adhesive after dissolution, is prepared into granule using spray granulation processes, the Amoxicillin prepared using above two method
Potassium clavulanate preparation has production simple, and bioavilability is high, and absorption is fast, proves effective the advantages that rapid.
Specific embodiment
Embodiment 1 (preparation of dripping pill) (best)
Prepared by the preparation method for being prepared as described above pill in method, 4000 468.75g of taking polyethylene glycol sets material
In tank, the heating system of material tank is opened, adjustment temperature is 55 DEG C, after polyethylene glycol all melts, opens stirring for material tank
Paddle is mixed, potassium clavulanate 31.25g and Amoxicillin 125g are slowly added to, when medical fluid is at melting liquid status, adjusts pill dripping machine
Temperature control system makes the water dropper temperature of pill dripping machine be heated and maintained at 55 DEG C, and the temperature of condensing agent is cooled and maintained at 3 DEG C,
Medical fluid is placed in the drop tank of pill dripping machine, is instilled in dimethicone by water dropper, molding drop will be shunk by pill dripping machine outlet
Ball takes out, and removes surface condensation agent, it is dry to get.
Embodiment 2
Prepared by the preparation method for being prepared as described above pill in method, 6000 650g of taking polyethylene glycol sets material tank
In, the heating system of material tank is opened, adjustment temperature is 75 DEG C, after polyethylene glycol all melts, opens the stirring of material tank
Paddle is slowly added to potassium clavulanate 30g and Amoxicillin 100g, when medical fluid is at melting liquid status, adjusts the temperature of pill dripping machine
Control system makes the water dropper temperature of pill dripping machine be heated and maintained at 75 DEG C, and the temperature of condensing agent is cooled and maintained at -1 DEG C, by medicine
Liquid is placed in the drop tank of pill dripping machine, is instilled in dimethicone by water dropper, will be shunk molding dripping pill by pill dripping machine outlet and is taken
Out, remove surface condensation agent, it is dry to get.
Embodiment 3
Prepared by the preparation method for being prepared as described above pill in method, taking polyethylene glycol 10000765g sets material tank
In, the heating system of material tank is opened, adjustment temperature is 75 DEG C, after polyethylene glycol all melts, opens the stirring of material tank
Paddle is slowly added to potassium clavulanate 33g and Amoxicillin 120g, when medical fluid is at melting liquid status, adjusts the temperature of pill dripping machine
Control system makes the water dropper temperature of pill dripping machine be heated and maintained at 65 DEG C, and the temperature of condensing agent is cooled and maintained at 0 DEG C, by medicine
Liquid is placed in the drop tank of pill dripping machine, is instilled in dimethicone by water dropper, will be shunk molding dripping pill by pill dripping machine outlet and is taken
Out, remove surface condensation agent, it is dry to get.
Embodiment 4
Prepared by the preparation method for being prepared as described above pill in method, 20000 688g of taking polyethylene glycol sets material tank
In, the heating system of material tank is opened, adjustment temperature is 85 DEG C, after polyethylene glycol all melts, opens the stirring of material tank
Paddle is slowly added to potassium clavulanate 32g and Amoxicillin 140g, when medical fluid is at melting liquid status, adjusts the temperature of pill dripping machine
Control system makes the water dropper temperature of pill dripping machine be heated and maintained at 65 DEG C, and the temperature of condensing agent is cooled and maintained at 5 DEG C, by medicine
Liquid is placed in the drop tank of pill dripping machine, is instilled in dimethicone by water dropper, will be shunk molding dripping pill by pill dripping machine outlet and is taken
Out, remove surface condensation agent, it is dry to get.
Embodiment 5 (preparation of granule) (being best)
It is prepared by the preparation method of above-mentioned granule, potassium clavulanate 31.25g is taken to be dissolved with a small amount of water, after filtering,
Potassium clavulanate lysate is obtained, it is spare；Take Amoxicillin 125g, microcrystalline cellulose 3.12%, silica 5%, carboxymethylstarch
It after sodium 5%, Icing Sugar 1.5kg and orange essence 0.05% carry out super prestige crushing respectively, is uniformly mixed, sets in spray granulator, adjust
Whole spray granulator temperature is 55 DEG C, using potassium clavulanate lysate as adhesive, carries out spraying granulation, the particle that will be prepared
With 24 mesh screen whole grain, suitable magnesium stearate 3.5% is added and carries out total mix, packaging to get.
Embodiment 6 (preparation of granule)
It is prepared by the preparation method of above-mentioned granule, potassium clavulanate 33.0g is taken to be dissolved with a small amount of water, after filtering,
Potassium clavulanate lysate is obtained, it is spare；Take Amoxicillin 130g, microcrystalline cellulose 33.0g, 3% carboxyrnethyl starch sodium of silica
3%, it after Icing Sugar 1.5kg and orange essence 0.05% carry out super prestige crushing after mixing respectively, is uniformly mixed, sets spray granulator
In, adjustment granulator temperature is 60 DEG C, using potassium clavulanate lysate as adhesive, carries out spraying granulation, that will be prepared
40 mesh screen whole grains of grain are added suitable silica 4% and carry out total mix, pack to get.
Embodiment 7 (preparation of granule)
It is prepared by the preparation method of above-mentioned granule, potassium clavulanate 32.0g is taken to be dissolved with a small amount of water, after filtering,
Potassium clavulanate filtrate is obtained, it is spare；Take Amoxicillin 150g, microcrystalline cellulose 32.0g, 5% carboxyrnethyl starch sodium of silica
3%, it after Icing Sugar 1.5kg and orange essence 0.5% carry out super prestige crushing respectively, is uniformly mixed, sets in spray granulator, adjustment system
Grain machine temperature is 65 DEG C, using potassium clavulanate lysate as adhesive, spraying granulation is carried out, by 24 meshes of the particle prepared
Net whole grain, be added silica 5% carry out total mix, packaging to get.
Embodiment 8 (preparation of granule)
It is prepared by the preparation method of above-mentioned granule, after taking a small amount of water dissolution filter of potassium clavulanate 31.5g, is obtained
Potassium clavulanate lysate, it is spare；Take Amoxicillin 140g, microcrystalline cellulose 31.5g, 6% carboxyrnethyl starch sodium of silica
3%, it after Icing Sugar 1.5kg and orange essence 0.1% carry out super prestige crushing respectively, is uniformly mixed, sets in spray granulator, adjustment system
Grain machine temperature is 75 DEG C, using potassium clavulanate lysate as adhesive, spraying granulation is carried out, by 24 meshes of the particle prepared
Net whole grain, be added silica 7% carry out total mix, packaging to get.
Embodiment 9
Investigate granule prepared by dripping pill and embodiment 5 to embodiment 8 prepared by embodiment 1 to embodiment 4 and specially
Dispersible tablet prepared by patent of the benefit application No. is 201710569445.5 is contrast sample, is that detection refers to amoxicillin content
Mark carries out dissolution rate detection, to prove that the present invention has quickly, efficient feature.
Detection method, by the dissolution test side of dripping pill, granule and dispersible tablet in " Chinese Pharmacopoeia " 2015 editions four
Method is detected respectively, and testing result is as follows:
Upper table shows；Embodiment 1 is all better than the dissolution rate of contrast sample to the dissolution rate of embodiment 8, wherein 1 He of embodiment
No matter embodiment 5 is from dissolution rate or the amount of dissolution, all stronger than other embodiments or contrast sample, thus, made with the present invention
Standby pill or granule has the advantages that prove effective, and fast, bioavilability is high.
Claims (16)
1. amoxicillin and clavulanate potassium preparation and preparation method thereof, being prepared into pill is by raw material: Amoxicillin 100.00-
150.00g potassium clavulanate 30.00-33.00g and matrix polyethylene glycol form, wherein raw material and substrate composition --- with g or kg
For unit, by weight, raw material: matrix=1: 0.5~5, it is characterised in that the preparation method comprises the following steps:
1.1, according to proportion given by prescription, accurately weigh raw material and matrix, and first matrix is placed in heating container, adjustment temperature
Degree be 50~90 DEG C, after matrix thawing after, under stirring, be slowly added to raw material, continue stirring to medical fluid in molten liquid and/
Or emulsion and/or suspension it is spare；
The temperature control system of 1.2 adjustment pill dripping machines, makes the water dropper temperature of pill dripping machine be heated and maintained at 50~90 DEG C, condensing agent
Temperature be cooled and maintained at 40~-5 DEG C；
1.2.3 medical fluid is placed in the drop tank of pill dripping machine, is instilled in condensing agent by water dropper, will shunk and formed by pill dripping machine outlet
Dripping pill take out, remove surface condensation agent, it is dry to get.
2. amoxicillin and clavulanate potassium preparation and preparation method thereof according to claim 1, it is characterised in that the matrix
For cetomacrogol 1000 or polyethylene glycol 1500 or polyethylene glycol 2000 or Macrogol 4000 or Macrogol 6000 or poly- second
Glycol 10000 or the above two or two or more mixture of PEG 20000.
3. amoxicillin and clavulanate potassium preparation and preparation method thereof according to claim 1, it is characterised in that the condensation
Agent can be atoleine, dimethicone, any one or a few in vegetable oil.
4. amoxicillin and clavulanate potassium preparation and preparation method thereof according to claim 1, it is characterised in that the adjustment
Temperature is 50~90 DEG C or the water dropper temperature of pill dripping machine made to be heated and maintained at 50~90 DEG C, temperature preferably with 55-60 DEG C, institute
The temperature for stating condensing agent is cooled and maintained at 40~-5 DEG C, temperature preferably with 10~0 DEG C.
5. amoxicillin and clavulanate potassium preparation and preparation method thereof according to claim 1, it is characterised in that the condensation
The temperature of agent is cooled and maintained at 40~-5 DEG C, preferably with 10~0 DEG C.
6. -5 any one described amoxicillin and clavulanate potassium preparation and preparation method thereof according to claim 1, feature exists
In preparation method preferably with: 4000 468.75g of taking polyethylene glycol is set in material tank, open material tank heating system, adjustment temperature
Degree be 55 DEG C, after polyethylene glycol all melt after, open material tank agitating paddle, be slowly added to potassium clavulanate 31.25g and Ah
Amdinocillin 125g adjusts the temperature control system of pill dripping machine, adds the water dropper temperature of pill dripping machine when medical fluid is at melting liquid status
Heat is simultaneously maintained at 55 DEG C, and the temperature of condensing agent is cooled and maintained at 3 DEG C, and medical fluid is placed in the drop tank of pill dripping machine, water dropper is passed through
Instill in dimethicone, molding dripping pill will be shunk by pill dripping machine outlet and taken out, remove surface condensation agent, it is dry to get.
7. amoxicillin and clavulanate potassium preparation and preparation method thereof, being prepared into granule is by Amoxicillin 100.00-
150.00g potassium clavulanate 30.00-33.00g, right amount of auxiliary materials composition, it is characterised in that the preparation method is as follows:
7.1 take the potassium clavulanate of recipe quantity to be dissolved with suitable water, and filtering obtains potassium clavulanate lysate, spare；
After 7.2 take the Amoxicillin of recipe quantity and a certain amount of auxiliary material to be pulverized respectively, it is uniformly mixed, sets spraying granulation
In machine, adjustment granulator temperature is 50-90 DEG C, using potassium clavulanate lysate as adhesive, carries out spraying granulation, will prepare
Particle 24-40 mesh screen whole grain, suitable lubricant is added and carries out total mix, packaging to get.
8. amoxicillin and clavulanate potassium preparation and preparation method thereof according to claim 7, it is characterised in that the carat
It ties up sour potassium to be dissolved with suitable water, water is distilled water or purified water.
9. amoxicillin and clavulanate potassium preparation and preparation method thereof according to claim 7, it is characterised in that the auxiliary material
Refer to disintegrating agent, diluent, lubricant and corrigent.
10. amoxicillin and clavulanate potassium preparation and preparation method thereof according to claim 9, it is characterised in that the disintegration
Agent includes but is not limited to soluble starch, silica, carboxyrnethyl starch sodium, sodium carboxymethylcellulose, one in crospovidone
Kind, two or more mixture；By weight be 3-8%, preferably with silica, dosage 3-8%.
11. amoxicillin and clavulanate potassium preparation and preparation method thereof according to claim 9, it is characterised in that the dilution
Agent includes but is not limited to one of Icing Sugar, lactose, microcrystalline cellulose and pre-paying starch, two or more combination
Object, by weight be 1-10%, preferably with microcrystalline cellulose, dosage 10-90%.
12. amoxicillin and clavulanate potassium preparation and preparation method thereof according to claim 9, it is characterised in that the lubrication
Agent includes but is not limited to silica, talcum powder or magnesium stearate, and by weight being 3-8%, preferably with magnesium stearate, dosage is
3-8%.
13. amoxicillin and clavulanate potassium preparation and preparation method thereof according to claim 9, it is characterised in that the flavoring
Agent includes but is not limited to one of Icing Sugar, lactose, orange essence, flavoring apple essence, hawthorn essence, or two kinds or more mixtures,
It is preferred that the mixture with Icing Sugar and orange essence, dosage is 0.05%~1.0%.
14. amoxicillin and clavulanate potassium preparation and preparation method thereof according to claim 9, it is characterised in that the adjustment
Granulator temperature be 50-90 DEG C, preferably with 50-60 DEG C.
15. amoxicillin and clavulanate potassium preparation and preparation method thereof according to claim 9, it is characterised in that described to make
The particle got ready 24-40 mesh screen whole grain, preferably and with 24 mesh screen whole grains.
16. according to amoxicillin and clavulanate potassium preparation and preparation method thereof described in claim 7-14, it is characterised in that preparation
Method preferably with: take a small amount of water of potassium clavulanate 31.25g to dissolve, after filtering, obtain potassium clavulanate lysate, it is spare；Take Ah
Amdinocillin 125g, microcrystalline cellulose 31.25g, 5% carboxyrnethyl starch sodium 5% of silica, Icing Sugar 1.5kg and orange essence
It after 0.05% carries out super prestige crushing respectively, is uniformly mixed, sets in spray granulator, adjustment granulator temperature is 55 DEG C, with carat
Tieing up sour potassium lysate is adhesive, carries out spraying granulation for 24 mesh screen whole grains of the particle prepared and suitable tristearin is added
Sour magnesium 3% carries out total mix, packaging to get.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201910422568.5A CN110051637A (en) | 2019-05-21 | 2019-05-21 | Amoxicillin and clavulanate potassium preparation and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201910422568.5A CN110051637A (en) | 2019-05-21 | 2019-05-21 | Amoxicillin and clavulanate potassium preparation and preparation method thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN110051637A true CN110051637A (en) | 2019-07-26 |
Family
ID=67323882
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201910422568.5A Pending CN110051637A (en) | 2019-05-21 | 2019-05-21 | Amoxicillin and clavulanate potassium preparation and preparation method thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN110051637A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN112190561A (en) * | 2020-10-30 | 2021-01-08 | 四川制药制剂有限公司 | Preparation method of amoxicillin and clavulanate potassium tablets |
Citations (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1242705A (en) * | 1997-11-17 | 2000-01-26 | 吉斯特-布罗卡迪斯有限公司 | Granules comprising clavulanate and one or more excipients |
| EP1044680A1 (en) * | 1999-04-13 | 2000-10-18 | Beecham Pharmaceuticals (Pte) Limited | Novel method of treatment using a high dosage regimen of amoxycillin and potassium clavulanate |
| CN1939267A (en) * | 2005-09-26 | 2007-04-04 | 刘凤鸣 | Oral preparation containing amoxicillin clatrenoin and its making method |
| CN101269069A (en) * | 2007-03-22 | 2008-09-24 | 刘凤鸣 | Oral preparation containing amoxicillin and clavulanic acid, preparation method and application thereof |
| CN101897701A (en) * | 2009-05-27 | 2010-12-01 | 华北制药集团制剂有限公司 | Preparation method of amoxicillin and clavulanate potassium tablets |
| CN102600141A (en) * | 2012-02-24 | 2012-07-25 | 南京臣功制药股份有限公司 | Dispersible tablet containing amoxicillin and potassium clavulanate |
| CN109248150A (en) * | 2017-07-13 | 2019-01-22 | 鲁南制药集团股份有限公司 | A kind of amoxicillin and clavulanate potassium preparation and preparation method thereof |
-
2019
- 2019-05-21 CN CN201910422568.5A patent/CN110051637A/en active Pending
Patent Citations (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1242705A (en) * | 1997-11-17 | 2000-01-26 | 吉斯特-布罗卡迪斯有限公司 | Granules comprising clavulanate and one or more excipients |
| EP1044680A1 (en) * | 1999-04-13 | 2000-10-18 | Beecham Pharmaceuticals (Pte) Limited | Novel method of treatment using a high dosage regimen of amoxycillin and potassium clavulanate |
| CN1939267A (en) * | 2005-09-26 | 2007-04-04 | 刘凤鸣 | Oral preparation containing amoxicillin clatrenoin and its making method |
| CN101269069A (en) * | 2007-03-22 | 2008-09-24 | 刘凤鸣 | Oral preparation containing amoxicillin and clavulanic acid, preparation method and application thereof |
| CN101897701A (en) * | 2009-05-27 | 2010-12-01 | 华北制药集团制剂有限公司 | Preparation method of amoxicillin and clavulanate potassium tablets |
| CN102600141A (en) * | 2012-02-24 | 2012-07-25 | 南京臣功制药股份有限公司 | Dispersible tablet containing amoxicillin and potassium clavulanate |
| CN109248150A (en) * | 2017-07-13 | 2019-01-22 | 鲁南制药集团股份有限公司 | A kind of amoxicillin and clavulanate potassium preparation and preparation method thereof |
Non-Patent Citations (3)
| Title |
|---|
| MOHIUDDIN HUSSAIN KHAN等: ""Effects of packaging and storage conditions on the quality of amoxicillin-clavulanic acid - an analysis of Cambodian samples"", 《BMC PHARMACOLOGY & TOXICOLOGY》 * |
| 奚念朱主编: "《药剂学》", 30 April 1996, 人民卫生出版社 * |
| 黄国军等: ""阿莫西林克拉维酸钾分散片制备工艺与溶出度考察"", 《医药导报》 * |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN112190561A (en) * | 2020-10-30 | 2021-01-08 | 四川制药制剂有限公司 | Preparation method of amoxicillin and clavulanate potassium tablets |
| CN112190561B (en) * | 2020-10-30 | 2022-02-01 | 四川制药制剂有限公司 | Preparation method of amoxicillin and clavulanate potassium tablets |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN104434809B (en) | A kind of olaparib solid dispersion preparation and preparation method thereof | |
| KR20180104125A (en) | A dosage form composition comprising an inhibitor of bruton tyrosine kinase | |
| CN104650091A (en) | Micronization and crystal form of ticagrelor and preparation method and pharmaceutical application of crystal form of ticagrelor | |
| US20190117647A1 (en) | Granule Formulation for Oral Administration | |
| CN106265581B (en) | Tranexamic acid tablet and preparation method thereof | |
| CN104887633B (en) | A kind of razaxaban tablet and preparation method thereof | |
| CN109157522A (en) | Pharmaceutical composition and its preparation method and application comprising Xi Gelieting or its officinal salt | |
| CN110051637A (en) | Amoxicillin and clavulanate potassium preparation and preparation method thereof | |
| CN107595782A (en) | A kind of Linezolid dry suspensoid agent and preparation method thereof | |
| CN117562900A (en) | New apixaban preparation composition with obvious clinical advantage and preparation method thereof | |
| CN105030781B (en) | A kind of compound Zinc, Iron, Calcium particle and preparation method thereof | |
| CN108743554B (en) | A kind of toluenesulfonic acid Yi Dushaban tablet and preparation method thereof | |
| CN108420798A (en) | A kind of immediate release drug formulations of anti-coagulants and preparation method thereof | |
| CN114288259B (en) | Quick-release preparation of vitamin B2 and preparation method thereof | |
| CN104523627B (en) | Clopidogrel hydrogen sulfate tablet medicine composition and preparation method thereof | |
| CN102311452A (en) | Cefixime crystal, preparation method thereof and tablet composition containing same | |
| CN104173307A (en) | Preparation method of ezetimibe tablet | |
| CN104961751B (en) | A kind of Cefobutazine sodium compound and the pharmaceutical preparation containing the compound | |
| CN106176655A (en) | A kind of penicillin V potassium and preparation technology thereof | |
| CN102204910B (en) | Pharmaceutical composition of moxifloxacin hydrochloride, and preparation method thereof | |
| CN110237097A (en) | A kind of Fufang Anfenwanan capsules pellet and preparation method thereof | |
| CN107875137B (en) | Traditional Chinese medicine moisture-proof coating agent | |
| CN105663054B (en) | A kind of Sitafloxacin hydrate granules agent and preparation method thereof | |
| CN113057944A (en) | Preparation method of tablets with improved performance | |
| CN105640908A (en) | Milnacipran hydrochloride sustained-release tablets and preparing method thereof |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PB01 | Publication | ||
| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| WD01 | Invention patent application deemed withdrawn after publication | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20190726 |