CN107582538A - Azithromycin capsule and preparation method thereof - Google Patents
Azithromycin capsule and preparation method thereof Download PDFInfo
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- CN107582538A CN107582538A CN201710404607.XA CN201710404607A CN107582538A CN 107582538 A CN107582538 A CN 107582538A CN 201710404607 A CN201710404607 A CN 201710404607A CN 107582538 A CN107582538 A CN 107582538A
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Abstract
A kind of azithromycin capsule and preparation method thereof.It is made up of capsule filling and capsule shells, and capsule filling is made up of the raw material of following mass fraction：245~255 parts of azithromycin dihydrate (in terms of Afatinib), 45~50 parts of microcrystalline cellulose, 0.6~1.0 part of lauryl sodium sulfate, 12~15 parts of PVPP, 5~6 parts of magnesium stearate.The present invention utilizes the crystallization water in material, and powder directly is made into particle, can carry out continuous production, has that compaction profile is uniform than other facility for granulating, granule stability, good fluidity, cross crush it is few, the advantages that high yield rate, convenient large-scale production.
Description
Technical field
The invention belongs to field of pharmaceutical preparations.Specifically, the present invention relates to a kind of azithromycin capsule and its preparation side
Method.
Background technology
Azithromycin, its chemical name are：(2R, 3S, 4R, 5R, 8R, 10R, 11R, 12S, 13S, 14R) -13- [(2,6-
The pyranose of dideoxy -3-C- methyl -3-O- methyl-α-L- cores -) oxygen] -2- ethyls -3,4,10- trihydroxies -3,5,6,8,
10,12,14- seven methyl isophthalic acid 1- [[3,4,6- tri- deoxidation -3- (dimethylamino)-β-D- wood-pyranose] oxygen] -1- oxa-s -
6- azepine cyclopentadecane -15- ketone, its chemical structural formula are：Molecular formula：C38H72N2O12, molecular weight：749.00.Chemical constitution
Formula is：
Azithromycin is that macrolide antibiotics is applied to acpuei pharyngitis, acute flat caused by treatment micrococcus scarlatinae
Acute bronchitis, AECB caused by peach body inflammation and sensitive bacterial, streptococcus pneumonia, Bacillus influenzae
And the pneumonia caused by mycoplasma pneumoniae.Suitable for the urethritis and NUS (uterine neck caused by treatment Chlamydia
It is scorching), the skin soft-tissue infection caused by sensitive bacteria.Pure genital infection (syphilis spiral shell caused by non-multidrug resistant gonococcus
Revolve body concurrent infection except), urogenital infections.Its preparation method is the wet granulation using wet granule compression tablet as principle
Technology is the method being most widely used in medical industry, but technique is complex, uncomfortable for the material such as thermal sensitivity, moisture-sensitive
Close and tabletting is carried out using the method.The corresponding concept of wet granule compression tablet is dry granulation tabletting and direct powder compression, both
It is respectively provided with the advantages of being applied to wet, thermally labile medicine.Dry granulation tabletting refers to mix drug powder and necessary auxiliary material
After closing uniformly, solid (block, sheet or graininess) is pressed into suitable equipment, is then ground into appropriately sized do again
Particle, finally it is pressed into tablet.Direct powder compression is compared with wet granulation technique, the step of eliminating wet granulation, and it is saved
Shi Jieneng, simple process, technique are few, accelerate the dissolution of medicine, and these advantages make direct powder compression have larger development
Space.But direct compression method be faced with much challenge 1. pairs of active components, auxiliary material species and dosage it is very fastidious；2.
The poor fluidity of powder；3. it is big to lay particular stress on difference；4. easily cause sliver.
The content of the invention
It is an object of the invention to provide a kind of azithromycin capsule and preparation method thereof, using the crystallization water in material, directly
Particle is made in powder, continuous production can be carried out, has that compaction profile is uniform than other facility for granulating, granule stability, stream
Dynamic property is good, cross crush it is few, the advantages that high yield rate, convenient large-scale production.
To achieve the above object, the present invention uses following technical scheme：
A kind of azithromycin capsule, it is made up of capsule filling and capsule shells, and capsule filling is by following mass fraction
Raw material be made：245~255 parts of azithromycin dihydrate (in terms of Afatinib), 45~50 parts of microcrystalline cellulose, dodecane
0.6~1.0 part of base sodium sulphate, 12~15 parts of PVPP, 5~6 parts of magnesium stearate.
Preferably, the microcrystalline cellulose is PH302.
Preferably, the capsule shells are No. 1 capsule of gelatin.
Present invention also offers a kind of azithromycin capsule preparation method, comprise the following steps：
Each supplementary material is accurately taken according to mass fraction, first by azithromycin dihydrate and microcrystalline cellulose, the poly- dimension of crosslinking
Ketone is mixed and adds magnesium stearate, is pelletized using dry granulating machine, and lauryl sodium sulfate mixing is added after obtaining particle,
Progress No. 1 capsule of gelatin is filling, and it is 340mg to control loading amount.
The present invention prepares azithromycin capsule using dry granulation process, using the crystallization water in material, directly by powder system
Into particle, the advantages of preparation method is respectively provided with suitable for wet, thermally labile medicine compared to wet granulation, directly by dry powder
It is de-gassed, compression molding, crushing, two level pelletize, cross sieve classification, and dry granulating machine is electromechanical integrated product, can be carried out
Continuous production, has that compaction profile is uniform than other facility for granulating, granule stability, good fluidity, crosses and crushes few, high yield rate
The advantages that, avoid the stability problem that azithromycin dihydrate is brought using wet granulation and disturb, and be prepared by dry granulation
Process is relatively simple, convenient large-scale production.
Embodiment
In order to which the present invention is apparent to understand, with reference to specific embodiment, the invention will be further described, to help
Understand present disclosure.
Embodiment one：
Weigh Azithromycin Raw Material 1.309kg, microcrystalline cellulose 0.266kg, PVPP 0.079kg, magnesium stearate
0.029kg with three-dimensional mixing machine mix 5min, pelletized with dry granulating machine, weigh 0.0045kg lauryl sodium sulfate with
Particle mixes 3min, and prepared by filler completes, and crosses 20 mesh sieves and obtains particle, and mobility of particle is good, and it is bright to carry out gelatin 1
The progress of glue capsule is filling, and it is 340mg to control loading amount.
| Title | Prescription (Kg) | Prescription (Kg) |
| Azithromycin | 1.309 | 1.311 |
| Crystallite 302 | 0.266 | 0.265 |
| Lauryl sodium sulfate | 0.0045 | 0.005 |
| Magnesium stearate | 0.029 | 0.029 |
| PVPP | 0.079 | 0.077 |
| Amount to | 1.687.5 | 1.687 |
Embodiment two：
Weigh Azithromycin Raw Material 1.311kg, microcrystalline cellulose 0.265kg, PVPP 0.077kg, magnesium stearate
0.029kg with three-dimensional mixing machine mix 5min, pelletized with dry granulating machine, weigh 0.005kg lauryl sodium sulfate with
Particle mixes 3min, and prepared by filler completes, and crosses 20 mesh sieves and obtains particle, and mobility of particle is good, and it is bright to carry out gelatin 1
The progress of glue capsule is filling, and it is 340mg to control loading amount.
Embodiment three：
Weigh Azithromycin Raw Material 1.309kg, microcrystalline cellulose 0.267kg, PVPP 0.074kg, magnesium stearate
0.029kg with three-dimensional mixing machine mix 5min, pelletized with dry granulating machine, weigh 0.0042kg lauryl sodium sulfate with
Particle mixes 3min, and prepared by filler completes, and crosses 20 mesh sieves and obtains particle, and mobility of particle is good, and it is bright to carry out gelatin 1
The progress of glue capsule is filling, and it is 340mg to control loading amount.
The microcrystalline cellulose can use PH-101, PH-102, PH-103, PH-105, PH-F20, PH-301, PH-302,
Any in KG-801, preferably PH302, microcrystalline cellulose 302 is free flowable imperceptible corynebacterium or powdered
Grain, color is odorless, tasteless for white or near-white, has the characteristics that good fluidity, fater disintegration are fast and dissolution, above-mentioned crystallite are fine
It is excellent filler new material to tie up plain PH-302, has good compressibility but also can improve inherent " dissolution " performance, special
Other to have the function that to promote vivo biodistribution availability to insoluble drug, the PVPP is capsule endoparticle disintegrant,
Concentration is 2%~5% in direct tablet compressing and dry granulation tablet forming technique, can show rapidly high capillary activity and
Excellent hydration capability, almost without the tendency of gel, there is the cross-linked structure of height, not soluble in water, organic solvent and strong
Acid, highly basic；With extremely strong water imbibition, rapid water absorption and swelling, volume 150%~200% can be increased in a short time, nothing
It is malicious, nonirritant, do not absorbed by alimentary canal, outward appearance is larger cellular particle, meet water after water can be made to quickly enter particle
In, promote its disintegration, the big PVPP of particle it is smaller than particle can play faster calving disaggregation, the PVPP
Grain is larger, exceedes 200mg tablet again suitable for piece.The magnesium stearate in tablet manufacturing mainly as lubricant, generally
Think oral, non-toxic, dosage is generally 0.25%~5.0%, and magnesium stearate is in hydrophobicity, and can blocking medicine from solid dosage forms
Middle dissolution, therefore, use minimum concentration as far as possible in prescription while mobility of particle is ensured, mixed with tablet and powder
During conjunction, the coefficient of variation increase of mixing, dissolution rate reduces, and incorporation time increase, the dissolution rate and degree of fragmentation of tablet reduce,
Magnesium stearate may also increase the friability of tablet, therefore the incorporation time of magnesium stearate answers Cautious control.
The supplementary material part by weight of azithromycin of the present invention is by a large amount of strict screening tests, process certification, surely
Just obtain after qualitative research, directly obtained not by preparation teaching material or other reference cans, tried by screening
Test, process certification, stability study confirms that supplementary material ratio of the present invention is reasonable, and stable preparation process, finished product preparation is stable, meets
The preparation guideline requirement of galenic pharmacy and State Food and Drug Administration for tablet.
Claims (4)
- A kind of 1. azithromycin capsule, it is characterised in that：It is made up of capsule filling and capsule shells, and capsule filling is by following The raw material of mass fraction is made：245~255 parts of azithromycin dihydrate (in terms of Afatinib), microcrystalline cellulose 45~50 Part, 0.6~1.0 part of lauryl sodium sulfate, 12~15 parts of PVPP, 5~6 parts of magnesium stearate.
- 2. capsule according to claim 1, it is characterised in that：The microcrystalline cellulose is PH302.
- 3. capsule according to claim 1, it is characterised in that：The capsule shells are No. 1 capsule of gelatin.
- 4. a kind of azithromycin capsule preparation method, it is characterised in that comprise the following steps：Each supplementary material is accurately taken according to mass fraction, first mixes azithromycin dihydrate and microcrystalline cellulose, PVPP It is even to add magnesium stearate, pelletized using dry granulating machine, add lauryl sodium sulfate mixing after obtaining particle, carry out No. 1 capsule of gelatin is filling, and it is 340mg to control loading amount.
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|---|---|---|---|
| CN201710404607.XA CN107582538A (en) | 2017-06-01 | 2017-06-01 | Azithromycin capsule and preparation method thereof |
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| CN201710404607.XA CN107582538A (en) | 2017-06-01 | 2017-06-01 | Azithromycin capsule and preparation method thereof |
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| CN107582538A true CN107582538A (en) | 2018-01-16 |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110292567A (en) * | 2019-05-17 | 2019-10-01 | 北京悦康科创医药科技股份有限公司 | A kind of preparation method of azithromycin capsule |
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| CN1602888A (en) * | 2004-07-30 | 2005-04-06 | 浙江大德药业集团有限公司 | Azithromycin enteric casing preparation and its preparing process |
| CN1813783A (en) * | 2005-12-07 | 2006-08-09 | 范敏华 | Azithromycin micro-pill capsule and its preparing method |
| CN101579327A (en) * | 2008-05-12 | 2009-11-18 | 长治市三宝生化药业有限公司 | Azithromycin enteric capsule and preparation method thereof |
| CN102423306A (en) * | 2011-12-12 | 2012-04-25 | 珠海润都制药股份有限公司 | Azithromycin enteric capsules |
| CN102429889A (en) * | 2011-11-30 | 2012-05-02 | 无锡福祈制药有限公司 | Large ring lactone type medicament capsule and preparation method thereof |
| CN103040787A (en) * | 2012-12-24 | 2013-04-17 | 蚌埠丰原涂山制药有限公司 | Azithromycin capsule and preparation method thereof |
| CN103156814A (en) * | 2011-12-09 | 2013-06-19 | 四川科伦药物研究有限公司 | Azithromycin enteric composition and preparation method |
| CN106074427A (en) * | 2016-07-31 | 2016-11-09 | 合肥远志医药科技开发有限公司 | A kind of maleic acid Afatinib tablet and preparation method thereof |
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2017
- 2017-06-01 CN CN201710404607.XA patent/CN107582538A/en active Pending
Patent Citations (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1602888A (en) * | 2004-07-30 | 2005-04-06 | 浙江大德药业集团有限公司 | Azithromycin enteric casing preparation and its preparing process |
| CN1813783A (en) * | 2005-12-07 | 2006-08-09 | 范敏华 | Azithromycin micro-pill capsule and its preparing method |
| CN101579327A (en) * | 2008-05-12 | 2009-11-18 | 长治市三宝生化药业有限公司 | Azithromycin enteric capsule and preparation method thereof |
| CN102429889A (en) * | 2011-11-30 | 2012-05-02 | 无锡福祈制药有限公司 | Large ring lactone type medicament capsule and preparation method thereof |
| CN103156814A (en) * | 2011-12-09 | 2013-06-19 | 四川科伦药物研究有限公司 | Azithromycin enteric composition and preparation method |
| CN102423306A (en) * | 2011-12-12 | 2012-04-25 | 珠海润都制药股份有限公司 | Azithromycin enteric capsules |
| CN103040787A (en) * | 2012-12-24 | 2013-04-17 | 蚌埠丰原涂山制药有限公司 | Azithromycin capsule and preparation method thereof |
| CN106074427A (en) * | 2016-07-31 | 2016-11-09 | 合肥远志医药科技开发有限公司 | A kind of maleic acid Afatinib tablet and preparation method thereof |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110292567A (en) * | 2019-05-17 | 2019-10-01 | 北京悦康科创医药科技股份有限公司 | A kind of preparation method of azithromycin capsule |
| CN110292567B (en) * | 2019-05-17 | 2022-02-18 | 北京悦康科创医药科技股份有限公司 | Preparation method of azithromycin capsule |
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Application publication date: 20180116 |