CN104042562A - Novel solid preparation of roxithromycin - Google Patents
Novel solid preparation of roxithromycin Download PDFInfo
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- CN104042562A CN104042562A CN201410222516.0A CN201410222516A CN104042562A CN 104042562 A CN104042562 A CN 104042562A CN 201410222516 A CN201410222516 A CN 201410222516A CN 104042562 A CN104042562 A CN 104042562A
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- roxithromycin
- micronization
- oral formulations
- micronized
- microcrystalline cellulose
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Abstract
The invention provides an oral roxithromycin preparation, which is prepared from micronized roxithromycin and non-micronized roxithromycin in the weight ratio of 1:2 as active ingredients.
Description
Technical field
The present invention relates to medicine and preparation method thereof, particularly relate to a kind of Roxithromycin oral formulations and preparation method thereof.
Background technology
Roxithromycin (Roxithromycin) CAS:80214-83-1, structural formula is:
Roxithromycin is one of three current most widely used large antibiotic, and the eighties appears on the market first in France.Roxithromycin preparation at home market mainly contains four kinds of dosage forms at present: capsule, granule, dry suspension and tablet, be used for the treatment of respiratory tract infection, otorhinolaryngology infection, reproductive tract infection, skin soft-tissue infection and dentistry infection and mycoplasma pneumonia, chlamydia trachomatis infection and legionnaires disease etc.
Roxithromycin is the derivant of Erythromycin A, it is a relatively new semi-synthetic macrolide antibiotics, it has retained the original antibacterial activity of erythromycin and bactericidal mechanism, and chemical stability and lipotropy are improved, since coming out, be the antibacterials of wide spectrum clinically always, to gram positive bacteria, comprise that staphylococcus aureus, streptococcus pyogenes, staphylococcus epidermidis, streptococcus pneumoniae and part gram negative bacteria and anaerobe, mycoplasma, chlamydia, legionella all have stronger antibacterial activity.Roxithromycin has the features such as consumption is little, absorption is fast, long action time, its untoward reaction be common feel sick, the digestive tract reaction such as stomachache, diarrhoea, also can have a headache, dizzy, erythra and pruritus etc., particularly to liver, the bad person of renal function, anemia of pregnant woman, women breast-feeding their children will be cautious use of.
Roxithromycin ordinary tablet or conventional capsule description regulation: should be oral on an empty stomach; Should take with water is same at 1 hour before the meal or 3～4 hours after the meal; Feed can make the about half of declined bioavailability of oral administration.This may be relevant with the dissolubility pH dependency of Roxithromycin.After feed, gastric pH is increased to 4 left and right from 1 rapidly, and dissolubility and the rate of dissolution of Roxithromycin reduce rapidly, has a strong impact in body and absorbs.
Summary of the invention
The invention provides and can discharge a kind of Roxithromycin oral formulations more stably.
The present invention solves the problems of the technologies described above adopted technical scheme: a kind of Roxithromycin oral formulations, this oral formulations be by micronization and not the Roxithromycin of 2 kinds of forms of micronization form as active fraction preparation;
Described micronization Roxithromycin is mixed with by Roxithromycin and microcrystalline Cellulose;
The preparation method of described micronization Roxithromycin is: get Roxithromycin and microcrystalline Cellulose according to mass ratio 5: 1, mix homogeneously, grinds, and crosses sieve aperture internal diameter 75 μ m sieves.
In described Roxithromycin oral formulations, micronization and not micronized Roxithromycin part by weight are 1: 2.
Described Roxithromycin oral formulations is Roxithromycin Tablets, roxithromycin capsules, Roxithromycin oral latex emulsion.
Described Roxithromycin Tablets is roxithromycin dispersing tablet, roxithromycin sustained release tablets, Roxithromycin conventional tablet.
In described Roxithromycin oral formulations, also comprise filling machine, surfactant, pH adjusting agent, binding agent.
Described filler is one or more the mixing in microcrystalline Cellulose, polyethylene glycol 6000, lactose, calcium hydrogen phosphate, sucrose, Icing Sugar, dextrin, mannitol, sorbitol, xylitol;
Described surfactant is one or more the mixing in tween, sodium lauryl sulphate, dodecyl sodium sulfate, perfluorooctane sulfonate.
Described pH adjusting agent is one or more the combination in citric acid, tartaric acid, fumaric acid, malic acid, succinic acid, maleic acid, glutamic acid, mandelic acid.
Described binding agent is one or more the mixing in polyvidone, hydroxypropyl methylcellulose, starch, hydroxypropyl cellulose, hydroxy ethyl cellulose.
In described Roxithromycin oral formulations, also comprise sealing coat coating material, release controlling coating material, porogen, protective layer coating material, antiplastering aid.
Described sealing coat coating material is one or more the mixing in hydroxypropyl emthylcellulose, hydroxypropyl cellulose, polyvidone;
Described release controlling coating material is one or more mixing in polyacrylic resin, ethyl cellulose, cellulose acetate, ethylene-vinyl acetate copolymer;
Described porogen is one or more mixing in lactose, Polyethylene Glycol, polyvidone, hydroxypropyl cellulose;
Described protective layer coating material is one or more mixing in hydroxypropyl emthylcellulose, hydroxypropyl cellulose, polyvidone;
Described antiplastering aid is one or more mixing in Pulvis Talci, magnesium stearate, glyceryl monostearate.
Detailed description of the invention
Below in conjunction with embodiment, the present invention will be further described.
Embodiment 1 micronization
Get 75g Roxithromycin and 15g grinding agent, mix homogeneously, inserts in horizontal planetary ball mill ball grinder, places agate ball in tank,, self-timing rotating respectively moves processing, takes out sieve aperture internal diameter 75 μ m sieves, obtains Roxithromycin-grinding agent micronization mixture.Calculate Roxithromycin-grinding agent micronization mixture weight, calculate recovery rate.Grinding agent is selected from lactose, sucrose, microcrystalline Cellulose and xylitol.
The response rate=micronization mixture weight/(Roxithromycin raw material weight+grinding agent weight)
Result demonstration, when grinding agent is microcrystalline Cellulose, micronization yield is the highest, therefore select microcrystalline Cellulose as grinding agent.
The mixed proportion of embodiment 2 micronizations and micronized Roxithromycin
Get micronization and micronized Roxithromycin mixture 100g, polyvinylpolypyrrolidone 8g, hyprolose 25g, malic acid 2g, microcrystalline Cellulose 30g, perfluorooctane sulfonate 0.5g, 1% PVP K30 alcoholic solution (70%) is appropriate, makes altogether 1000.
Roxithromycin-lactose micropowder mixture is mixed homogeneously with the microcrystalline Cellulose of recipe quantity, partial cross-linked polyvidone, hyprolose, malic acid respectively, cross sieve aperture internal diameter (180 ± 7.6) m sieve, do binding agent soft material processed with 1% PVP K30 alcoholic solution (70%), cross sieve aperture internal diameter (850 ± 29) m sieve series grain, 60 DEG C of oven dry, cross sieve aperture internal diameter 840m sieve granulate, add remainder polyvinylpolypyrrolidone and perfluorooctane sulfonate to mix, tabletting.
The mixed proportion of micronization and micronized Roxithromycin is respectively 3: 1,2: 1,1: 1,1: 2,1: 3.
According to two annex IVA of Pharmacopoeia of the People's Republic of China version in 2000, measure absorbance at the wavelength place of 482nm respectively, by the stripping quantity of every of ratio calculation, limit is 80%.
Result shows that the mixed proportion of micronization and micronized Roxithromycin is at 1: 2 o'clock, and stripping is the most steady.
Embodiment 3 roxithromycin sustained release tablets
Get micronization and micronized Roxithromycin mixture 100g (ratio is 1: 2), polyvinylpolypyrrolidone 8g, hyprolose 25g, malic acid 2g, microcrystalline Cellulose 30g, perfluorooctane sulfonate 0.5g, 1% PVP K30 alcoholic solution (70%) is appropriate, makes altogether 1000.
Roxithromycin-lactose micropowder mixture is mixed homogeneously with the microcrystalline Cellulose of recipe quantity, partial cross-linked polyvidone, hyprolose, malic acid respectively, cross sieve aperture internal diameter (180 ± 7.6) m sieve, do binding agent soft material processed with 1% PVP K30 alcoholic solution (70%), cross sieve aperture internal diameter (850 ± 29) m sieve series grain, 60 DEG C of oven dry, cross sieve aperture internal diameter 840m sieve granulate, add remainder polyvinylpolypyrrolidone and perfluorooctane sulfonate to mix, tabletting.
Get HPMC E58g, Pulvis Talci 2g is prepared into sealing coat; Eudragit NE30D70g, PVP K30 2.1g and Pulvis Talci 21g prepare controlled release layer; Get HPMC E512g, Pulvis Talci 3g prepares protective layer.Prepare slow releasing tablet.
Claims (2)
1. a Roxithromycin oral formulations, this oral formulations be by micronization and not the Roxithromycin of 2 kinds of forms of micronization form as active fraction preparation, described micronization and not micronized Roxithromycin part by weight are 1: 2.
2. Roxithromycin oral formulations as claimed in claim 1, is characterized in that micronization Roxithromycin is mixed with by Roxithromycin and microcrystalline Cellulose.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410222516.0A CN104042562A (en) | 2014-05-21 | 2014-05-21 | Novel solid preparation of roxithromycin |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410222516.0A CN104042562A (en) | 2014-05-21 | 2014-05-21 | Novel solid preparation of roxithromycin |
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| CN104042562A true CN104042562A (en) | 2014-09-17 |
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| CN201410222516.0A Pending CN104042562A (en) | 2014-05-21 | 2014-05-21 | Novel solid preparation of roxithromycin |
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Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20030124191A1 (en) * | 2001-12-27 | 2003-07-03 | Jerome Besse | Use of an immediate-release powder in pharmaceutical and nutraceutical compositions |
| CN102406939A (en) * | 2010-09-26 | 2012-04-11 | 上海复星普适医药科技有限公司 | Method for improving solubility of slightly soluble medicine to improve bioavailability |
| CN102552172A (en) * | 2012-03-21 | 2012-07-11 | 广州共禾医药科技有限公司 | Roxithromycin controlled-release preparation and preparation method thereof |
| CN103083278A (en) * | 2011-11-04 | 2013-05-08 | 四川科伦药物研究有限公司 | Roxithromycin capsule and preparation method thereof |
-
2014
- 2014-05-21 CN CN201410222516.0A patent/CN104042562A/en active Pending
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20030124191A1 (en) * | 2001-12-27 | 2003-07-03 | Jerome Besse | Use of an immediate-release powder in pharmaceutical and nutraceutical compositions |
| CN102406939A (en) * | 2010-09-26 | 2012-04-11 | 上海复星普适医药科技有限公司 | Method for improving solubility of slightly soluble medicine to improve bioavailability |
| CN103083278A (en) * | 2011-11-04 | 2013-05-08 | 四川科伦药物研究有限公司 | Roxithromycin capsule and preparation method thereof |
| CN102552172A (en) * | 2012-03-21 | 2012-07-11 | 广州共禾医药科技有限公司 | Roxithromycin controlled-release preparation and preparation method thereof |
Non-Patent Citations (5)
| Title |
|---|
| 张兆旺: "《中药药剂学》", 31 January 2003, 中国中医药出版社 * |
| 张劲: "《药物制剂技术》", 31 August 2005, 化学工业出版社 * |
| 徐成等: "罗红霉素微粉化分散片的制备与溶出度测定", 《医药导报》 * |
| 朱照静: "《药剂学》", 30 June 2010, 科学出版社 * |
| 李津明: "《现代制药技术》", 30 April 2005, 中国医药科技出版社 * |
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