CN106511317A - Preparing method for taste masking clarithromycin granules - Google Patents
Preparing method for taste masking clarithromycin granules Download PDFInfo
- Publication number
- CN106511317A CN106511317A CN201611146983.5A CN201611146983A CN106511317A CN 106511317 A CN106511317 A CN 106511317A CN 201611146983 A CN201611146983 A CN 201611146983A CN 106511317 A CN106511317 A CN 106511317A
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- Prior art keywords
- clarithromycin
- taste masking
- granule
- preparation
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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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
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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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/5005—Wall or coating material
- A61K9/5021—Organic macromolecular compounds
- A61K9/5026—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
-
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/5005—Wall or coating material
- A61K9/5021—Organic macromolecular compounds
- A61K9/5031—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poly(lactide-co-glycolide)
-
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/5005—Wall or coating material
- A61K9/5021—Organic macromolecular compounds
- A61K9/5036—Polysaccharides, e.g. gums, alginate; Cyclodextrin
- A61K9/5042—Cellulose; Cellulose derivatives, e.g. phthalate or acetate succinate esters of hydroxypropyl methylcellulose
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/5005—Wall or coating material
- A61K9/5021—Organic macromolecular compounds
- A61K9/5036—Polysaccharides, e.g. gums, alginate; Cyclodextrin
- A61K9/5042—Cellulose; Cellulose derivatives, e.g. phthalate or acetate succinate esters of hydroxypropyl methylcellulose
- A61K9/5047—Cellulose ethers containing no ester groups, e.g. hydroxypropyl methylcellulose
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Molecular Biology (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention discloses a preparing method for taste masking clarithromycin granules. Clarithromycin and saturated fatty acid are heated to prepare the granules, solubility of the clarithromycin in water is reduced to mask the bitter taste of the clarithromycin, and then the granules with the proper granular size are screened out to be coated with an insoluble or enteric coating material in a fluidized bed or a non-hole coating boiler, and the taste masking clarithromycin granules can be obtained after the granules reach the proper coating weighing. The obvious bitter taste of the clarithromycin can be masked, the taste of the preparation granules is improved, in addition, the beneficial effects that the preparing process is simple, few auxiliary materials are used, and production operation is facilitated are achieved, and the quality of the product is well controlled.
Description
【Technical field】
The present invention relates to a kind of antibiotic medicine, and in particular to a kind of preparation method of taste masking clarithromycin granule.
【Background technology】
Clarithromycin is second filial generation macrolide antibiotics, and Antibacterial Mechanism is to act on the core egg in antibacterial 70S systems
Lean type 50S subunit, hinders the synthesis of bacterioprotein.Clarithromycin has to gram positive bacteria, various gram negative bacterias
Antibacterial action, in addition to anaerobe and other pathogens, such as mycoplasma, chlamydia and legionella still have stronger antibacterial to make
With.The characteristics of this product is that antibacterial activity in vitro is not significantly better than erythromycin, in vivo to golden yellow staphylococcus, Diplococcus pneumoniae,
Micrococcus scarlatinae, Haemophilus influenzae antibacterial activity it is but strong compared with erythromycin 2-10 times.Clarithromycin to morazella catarrhalis,
Multocida, campylobacter jejuni and campylobacter fetuses, Diplococcus gonorrhoeae, Salmonella, legionella pneumophilia and detest
The antibacterial action of oxygen coccus is strong compared with erythromycin, is this to the antibacterial action of helicobacter pylori, chlamydia trachomatiss, mycoplasma pulmonises
It is most strong in class antibiotic, in addition clarithromycin be treat HIV sufferers mycobacteria infections choice drug, clarithromycin
There is obviously bitterness, product patient is difficult to swallow made by ordinary preparation technology, for the solid preparation medicine that can be taken after mixing it with water
For, the quality of mouthfeel directly determines submissiveness of the patient to doctor's advice, therefore proposes a kind of system of taste masking clarithromycin granule
Preparation Method.
【The content of the invention】
The purpose of the present invention is exactly to solve the problems of the prior art, proposes a kind of preparation side of taste masking clarithromycin granule
Method, covers the bitterness of clarithromycin granule agent by hot melt, coating, granulation, simple with operating process, adjuvant using less,
The characteristics of being easy to production operation, controls product quality well.
For achieving the above object, the present invention proposes a kind of preparation method of taste masking clarithromycin granule, including following step
Suddenly:
(1) heating granulation
Clarithromycin reduces clarithromycin dissolving in water by the method for heating granulation with appropriate satisfied fatty acid
The bitterness for spending to cover clarithromycin, is extruded by hot-melt extruded equipment after clarithromycin is mixed in proportion with stearic acid
Cooling, clarithromycin are 1 with the proportion of satisfied fatty acid:10 to 10:1.
(2) sieving and grading
20 mesh of selection are crushed and screened after the extrusion cooling of hot-melt extruded equipment to 120 mesh clarithromycin granules.
(3) coating drying
The clarithromycin that the insoluble or enteric-coating material used in fluid bed or non-porous coating pan is chosen to screening
Grain is coated, and further covers the bitterness of clarithromycin, and coating weight gain is no less than 20%.
Preferably, the proportion preferably 1 of clarithromycin described in step (1) and satisfied fatty acid:3 to 3:1.
Preferably, method of granulating is heated described in step (1) hot melt granulation, spray congealing and hot-melt extruded granulation,
It is preferred that spray congealing and hot melt granulation.
Preferably, clarithromycin granule described in step (2) screening preferred scope be 40 mesh to 80 mesh.
Preferably, coating material described in step (3) be ethyl cellulose, Hydroxypropyl methyl cellulose phtalate,
Among hypromellose succinate, polyvinyl acetate phthalate, methacrylic acid and ethylacylic acid copolymer
One or more.
Preferably, coating weight gain preferably 25% to 120% described in step (3).
Preferably, the clarithromycin with the mass ratio of satisfied fatty acid is:30 parts of clarithromycin, satisfied fatty acid
50 parts;The coating material each component mass ratio is:10 parts of ethyl cellulose, 1.8 parts of Oleum Ricini, 12 parts of Pulvis Talci, hydroxypropyl
5 parts of methylcellulose phthalic acid ester, 85% 300 parts of ethanol solution.
Beneficial effects of the present invention:The present invention is closed by clarithromycin and satisfied fatty acid are carried out screening after heating granulation
The granule of suitable particle diameter insoluble or enteric-coating material used in fluid bed or non-porous coating pan is coated, and reaches in granule
The clarithromycin granule of taste masking is obtained after suitable coating weight gain, simple with operating process, adjuvant is easy to using less
The characteristics of production operation, product quality is controlled well.
【Specific embodiment】
The present invention proposes a kind of preparation method of taste masking clarithromycin granule, comprises the following steps:
(1) heating granulation
Clarithromycin reduces clarithromycin dissolving in water by the method for heating granulation with appropriate satisfied fatty acid
The bitterness for spending to cover clarithromycin, is extruded by hot-melt extruded equipment after clarithromycin is mixed in proportion with stearic acid
Cooling, clarithromycin are 1 with the proportion of satisfied fatty acid:10 to 10:1.
(2) sieving and grading
20 mesh of selection are crushed and screened after the extrusion cooling of hot-melt extruded equipment to 120 mesh clarithromycin granules.
(3) coating drying
The clarithromycin that the insoluble or enteric-coating material used in fluid bed or non-porous coating pan is chosen to screening
Grain is coated, and further covers the bitterness of clarithromycin, and coating weight gain is no less than 20%.
The proportion preferably 1 of clarithromycin described in step (1) and satisfied fatty acid:3 to 3:1;The heating granulation
Method has hot melt granulation, spray congealing and hot-melt extruded granulation, preferred spray congealing and hot melt granulation.Described in step (2) gram
Drawing mycin particle screening preferred scope is 40 mesh to 80 mesh.Coating material described in step (3) is ethyl cellulose, hydroxypropyl first fibre
The plain phthalic acid ester of dimension, hypromellose succinate, polyvinyl acetate phthalate, methacrylic acid and ethyl
One or more among acrylic copolymer;The coating weight gain preferably 25% to 120%.
The present invention specific embodiment be:
Clarithromycin with the mass ratio of satisfied fatty acid is:30 parts of clarithromycin, 50 parts of satisfied fatty acid;The coating
Material each component mass ratio is:10 parts of ethyl cellulose, 1.8 parts of Oleum Ricini, 12 parts of Pulvis Talci, hypromellose neighbour's benzene two
5 parts of formic acid esters, 85% 300 parts of ethanol solution.
Crushed and screened after the extrusion cooling of hot-melt extruded equipment after clarithromycin is mixed in proportion with stearic acid
Choose 30 to 100 mesh granules stand-by;Ethyl cellulose, Hydroxypropyl methyl cellulose phtalate and Oleum Ricini are dissolved in into 300
In gram 85% ethanol water and then superfine talcum powder is uniformly dispersed in the solution ethyl cellulose ethanol solution is stand-by,
The ethyl cellulose ethanol solution prepared used in clarithromycin is uncoated granule input fluid bed carries out bottom spray coating.
Above-described embodiment is the description of the invention, is not limitation of the invention, it is any to simple transformation of the present invention after
Scheme belong to protection scope of the present invention.
Claims (7)
1. a kind of preparation method of taste masking clarithromycin granule, it is characterised in that comprise the following steps:
(1) heating granulation
Clarithromycin and appropriate satisfied fatty acid by the method for heating granulation reduce dissolubility of the clarithromycin in water come
The bitterness of clarithromycin is covered, is extruded by hot-melt extruded equipment after clarithromycin is mixed in proportion with stearic acid cold
But, clarithromycin and the proportion of satisfied fatty acid are 1:10 to 10:1.
(2) sieving and grading
20 mesh of selection are crushed and screened after the extrusion cooling of hot-melt extruded equipment to 120 mesh clarithromycin granules.
(3) coating drying
The insoluble or enteric-coating material used in fluid bed or non-porous coating pan enters to the clarithromycin granule that screening is chosen
Row coating, further covers the bitterness of clarithromycin, and coating weight gain is no less than 20%.
2. a kind of preparation method of taste masking clarithromycin granule as claimed in claim 1, it is characterised in that:Institute in step (1)
State the proportion preferably 1 of clarithromycin and satisfied fatty acid:3 to 3:1.
3. a kind of preparation method of taste masking clarithromycin granule as claimed in claim 1, it is characterised in that:Institute in step (1)
Stating heating method of granulating has hot melt granulation, spray congealing and hot-melt extruded granulation, preferred spray congealing and hot melt granulation.
4. a kind of preparation method of taste masking clarithromycin granule as claimed in claim 1, it is characterised in that:Institute in step (2)
State clarithromycin granule screening preferred scope be 40 mesh to 80 mesh.
5. a kind of preparation method of taste masking clarithromycin granule as claimed in claim 1, it is characterised in that:Institute in step (3)
Coating material is stated for ethyl cellulose, Hydroxypropyl methyl cellulose phtalate, hypromellose succinate, poly-vinegar acid second
One or more among alkene phthalic acid ester, methacrylic acid and ethylacylic acid copolymer.
6. a kind of preparation method of taste masking clarithromycin granule as claimed in claim 1, it is characterised in that:Institute in step (3)
State coating weight gain preferably 25% to 120%.
7. a kind of preparation method of taste masking clarithromycin granule as claimed in claim 1, it is characterised in that:The clarithromycin
Mass ratio with satisfied fatty acid is:30 parts of clarithromycin, 50 parts of satisfied fatty acid;The coating material each component mass ratio
Example be:10 parts of ethyl cellulose, 1.8 parts of Oleum Ricini, 12 parts of Pulvis Talci, 5 parts of Hydroxypropyl methyl cellulose phtalate, 85% second
300 parts of alcoholic solution.
Priority Applications (1)
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CN201611146983.5A CN106511317A (en) | 2016-12-13 | 2016-12-13 | Preparing method for taste masking clarithromycin granules |
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CN201611146983.5A CN106511317A (en) | 2016-12-13 | 2016-12-13 | Preparing method for taste masking clarithromycin granules |
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CN201611146983.5A Pending CN106511317A (en) | 2016-12-13 | 2016-12-13 | Preparing method for taste masking clarithromycin granules |
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Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP3624840A4 (en) * | 2017-05-19 | 2021-03-10 | Lunella Biotech, Inc. | Antimitoscins: targeted inhibitors of mitochondrial biogenesis for eradicating cancer stem cells |
US11497759B2 (en) | 2017-12-01 | 2022-11-15 | Lunella Biotech, Inc. | Repurposcins: targeted inhibitors of mitochondrial biogenesis for eradicating cancer stem cells |
Citations (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPH05255075A (en) * | 1991-12-04 | 1993-10-05 | Taisho Pharmaceut Co Ltd | Production of taste-modifying peroral composition |
WO2000018372A1 (en) * | 1998-09-30 | 2000-04-06 | Taisho Pharmaceutical Co., Ltd. | Grains for oral preparations |
JP2002087966A (en) * | 2000-09-13 | 2002-03-27 | Taisho Pharmaceut Co Ltd | Elution-regulated particle for medicinal preparation |
CN1960716A (en) * | 2004-06-03 | 2007-05-09 | 大正制药株式会社 | Oral preparations and process for production thereof |
CN103239406A (en) * | 2012-02-01 | 2013-08-14 | 杭州赛利药物研究所有限公司 | Clarithromycin enteric preparation and preparation method thereof |
CN103315964A (en) * | 2013-06-21 | 2013-09-25 | 新华制药(高密)有限公司 | Method for preparing sweet clarithromycin granules |
-
2016
- 2016-12-13 CN CN201611146983.5A patent/CN106511317A/en active Pending
Patent Citations (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPH05255075A (en) * | 1991-12-04 | 1993-10-05 | Taisho Pharmaceut Co Ltd | Production of taste-modifying peroral composition |
WO2000018372A1 (en) * | 1998-09-30 | 2000-04-06 | Taisho Pharmaceutical Co., Ltd. | Grains for oral preparations |
JP2002087966A (en) * | 2000-09-13 | 2002-03-27 | Taisho Pharmaceut Co Ltd | Elution-regulated particle for medicinal preparation |
CN1960716A (en) * | 2004-06-03 | 2007-05-09 | 大正制药株式会社 | Oral preparations and process for production thereof |
CN103239406A (en) * | 2012-02-01 | 2013-08-14 | 杭州赛利药物研究所有限公司 | Clarithromycin enteric preparation and preparation method thereof |
CN103315964A (en) * | 2013-06-21 | 2013-09-25 | 新华制药(高密)有限公司 | Method for preparing sweet clarithromycin granules |
Non-Patent Citations (1)
Title |
---|
罗明生等: "《药剂辅料大全》", 31 January 2006 * |
Cited By (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP3624840A4 (en) * | 2017-05-19 | 2021-03-10 | Lunella Biotech, Inc. | Antimitoscins: targeted inhibitors of mitochondrial biogenesis for eradicating cancer stem cells |
US11160821B2 (en) | 2017-05-19 | 2021-11-02 | Lunella Biotech, Inc. | Antimitoscins: targeted inhibitors of mitochondrial biogenesis for eradicating cancer stem cells |
US11865130B2 (en) | 2017-05-19 | 2024-01-09 | Lunella Biotech, Inc. | Antimitoscins: targeted inhibitors of mitochondrial biogenesis for eradicating cancer stem cells |
US11497759B2 (en) | 2017-12-01 | 2022-11-15 | Lunella Biotech, Inc. | Repurposcins: targeted inhibitors of mitochondrial biogenesis for eradicating cancer stem cells |
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