CN104546735A - Pediatric tosufloxacin tosilate granule and preparation method thereof - Google Patents
Pediatric tosufloxacin tosilate granule and preparation method thereof Download PDFInfo
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- CN104546735A CN104546735A CN201410798002.XA CN201410798002A CN104546735A CN 104546735 A CN104546735 A CN 104546735A CN 201410798002 A CN201410798002 A CN 201410798002A CN 104546735 A CN104546735 A CN 104546735A
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Abstract
The invention provides a pediatric tosufloxacin tosilate granule and a preparation method thereof. For the prepared pediatric tosufloxacin tosilate granule, the main drug is tosufloxacin tosilate, and excipients include saccharose, aspartame, hydroxypropyl cellulose SSL, silicon dioxide and the like, wherein the saccharose is a diluent and sweetener, aspartame is a sweetener, hydroxypropyl cellulose SSL is a binder, fresh orange powder essence is a correctant, silicon dioxide is a flow aid, and carmine is a coloring agent, so that the formula is formed. According to the prepared pediatric tosufloxacin tosilate granule, the problems of color dullness, tone, corrosion and the like can be solved by replacing ferric oxide with the carmine as the coloring agent; and by taking the fresh orange powder essence as the correctant, the granules are good in mouth feeling and taste. For the formula, the preparation technology is simple, the reproducibility is good, and the pediatric tosufloxacin tosilate granule is stable and reliable in quality, and safe and effective.
Description
Technical field
The present invention relates to children's with tosufloxacin tosilate granule and preparation method thereof.
Background technology
Tosufloxacin tosilate is developed by Japan folic hill chemical industry Co., Ltd., nineteen ninety is at first at Japan's listing oral tablet, specification: 75mg, 150mg, be applicable to treat the infection disease of adult patients because of the responsive microbial multiple system of tosufloxacin, as the secondary infection, osteomyelitis, arthritis, acute bronchitis, pneumonia, pyelonephritis, prostatitis, urethritis etc. of shallow and deep skin infection, wound or thermal burn and operation wound etc.In August, 2009, Toyama Chemical Co., Ltd. development tosufloxacin tosilate children's with granula subtilis in the granted listing of Japan, specification 0.5g:75mg, 100g:15g, be applicable to treatment child patient because of tosufloxacin responsive microbial pneumonia, otitis media, cholera, anthrax, it incorporates bacterial pneumonia and the acute bacterial otitis media child patient of 1 ~ 15 years old at the III clinical trial phase of Japan.
Children Streptococcus and otitis media are the common infectious disease of China's department of pediatrics, and China's existing 2004 versions " Antibiotic susceptibility test " and up-to-date documents and materials investigation display two kinds of disease Main Pathogenic Bacterias are streptococcus pneumoniae, hemophilus influenza and moraxelle catarrhalis.In recent years along with antibiotic extensive use, fastbacteria such as PISP, PRSP, BLNAR etc. of these antibacterials increase year by year, the antibiotic (mainly beta-lactam, Macrolide antibacterials) that domestic existing applicable child uses demonstrates limitation, clinical in the urgent need to new effectively and safe drugs as alternative medication.
Tosufloxacin in Development of Fluoroquinolone Antibacterials, cross resistance is not had with beta-lactam and Macrolide antibacterials, to the Main Pathogenic Bacteria of children Streptococcus and otitis media---comprise the streptococcus pneumoniae of the fastbacteria such as PRSP, BLNAR, hemophilus influenza and moraxelle catarrhalis, demonstrate than other Development of Fluoroquinolone Antibacterials and the stronger antibacterial activity of beta-lactam antibacterials.Japan Clinic test also shows that tosufloxacin tosilate children's has excellent clinical efficacy and bacteria clearance with granula subtilis for children Streptococcus and otitis media, and for drug resistance streptococcus pneumoniae (PISP, PRSP) and the caused infected patient of drug resistance hemophilus influenza (BLNAR, BLPAR, BLPACR) and previously use the patient of other antibacterial drug therapy all to have the clinical efficacy of excellence.
It is current that to affect the principal element that tosufloxacin and other Development of Fluoroquinolone Antibacterials be used for child be that this kind of medicine can bring out joint toxicity to growing animal, China so far non-official approval fluoroquinolones is used for child, but domestic existed the situation that fluoroquinolones treatment Pediatrics applied outward by label.Compared with domestic, external existing 4 kinds of fluoroquinolones (ciprofloxacin, levofloxacin, norfloxacin, tosufloxacin) specify that child adjustment disease and usage and dosage, meet the Treatment need of Among Children bacterial infection patient first, second avoid clinician's exploration and apply the abuse caused.
In addition, better, compare although use during tosufloxacin tosilate sheet with adult, child uses adverse reaction rate during granula subtilis higher than adult for the overall security of this product and toleration, but untoward reaction type and adult do not have difference, and most of untoward reaction is light, moderate.Tosufloxacin tosilate granula subtilis is easy to use, and child easily takes, and is conducive to the compliance improving child patient.
In sum, the exploitation of this product is conducive to optimizing existing child and uses antibacterials breed structure, better medication can be provided to select for department of pediatrics pneumonia and the otitis media patient patient that especially other Perorally administrable antimicrobial medicine is failed to respond to any medical treatment.
Summary of the invention
The object of the invention is to provide a kind of children's with tosufloxacin tosilate granule and preparation method thereof, replaces ferrum oxide to make coloring agent, solve the problems such as color dimness degree, tone and corrosivity with carmine; Using orange powdered flavor as correctives, made granule mouthfeel and taste are all better, and this formula preparation technique is simple, favorable reproducibility, stable and reliable product quality, safe and effective.
The technical solution used in the present invention:
Children's provided by the invention uses tosufloxacin tosilate granule, containing, for example lower component in every 1000 bags: principal agent tosufloxacin tosilate 75g, adjuvant contains diluent, sweeting agent, adhesive, fluidizer, correctives, wherein: sucrose 411.5g ~ 413.5g, aspartame 2g ~ 4g, hydroxypropyl cellulose SSL 1.5g ~ 5g, orange powdered flavor 2g ~ 4g, silicon dioxide 0.25g, purified water 37g, described coloring agent is carmine or ferrum oxide.The preferred coloring agent of the present invention is carmine.
Preferred prescription is: principal agent tosufloxacin tosilate 75g, adjuvant: sucrose 412.5g, aspartame 4g, hydroxypropyl cellulose SSL 2g, orange powdered flavor 4g, silicon dioxide 2.5g, carmine 0.009mg(0.0018%), purified water 37g.
Present invention also offers the preparation method of a kind of children's with tosufloxacin tosilate granule, comprise the steps:
Tosufloxacin tosilate pulverized 100 mesh sieves, and sucrose, aspartame, hydroxypropyl cellulose SSL cross 100 mesh sieves, and orange powdered flavor, silicon dioxide cross 60 mesh sieves.Take the tosufloxacin tosilate of recipe quantity, sucrose, aspartame, hydroxypropyl cellulose SSL, add in high-speed mixing granulating machine, 5 minutes are mixed with the speed of 200 revs/min, add carmine aqueous solution soft material, 24 mesh sieves are granulated, wet granular is in 60 DEG C of forced air dryings to moisture content < 2%, dry granule crosses 20 mesh sieve granulate, fine powder is removed with 80 mesh sieve sieves, add in material bin mixer, finally add the orange powdered flavor of recipe quantity, silicon dioxide, 3 minutes are mixed with the speed of 18 revs/min, obtain children's and use tosufloxacin tosilate granule.
Detailed description of the invention
Embodiment 1
Prescription 1
Tosufloxacin tosilate 75g
Sucrose 413.5g
Aspartame 2g
Hydroxypropyl cellulose SSL 5g
Carmine 0.009g
Orange powdered flavor 2g
Silicon dioxide 2.5g
Preparation technology: raw mill crosses 100 mesh sieves (D50=8.74 μm, D90=45.56 μm), sucrose, hydroxypropyl cellulose SSL, aspartame cross 100 mesh sieves, and silicon dioxide, orange powdered flavor cross 60 mesh sieves, for subsequent use.Carmine is added water and is made into 0.025% solution, stir and make wetting agent, for subsequent use.Take the tosufloxacin tosilate of recipe quantity, sucrose, aspartame, hydroxypropyl cellulose SSL, abundant mix homogeneously, add appropriate carmine aqueous solution soft material, 24 mesh sieves are granulated, wet granular is in 60 DEG C of forced air dryings to moisture content < 2%, and dry granule crosses 20 mesh sieve granulate, removes fine powder with 80 mesh sieve sieves, finally add orange powdered flavor, the silicon dioxide of recipe quantity, mixing.
Embodiment 2
Prescription 2
Tosufloxacin tosilate 75g
Sucrose 411.5g
Aspartame 4g
Hydroxypropyl cellulose SSL 3g
Carmine 0.009g
Orange powdered flavor 4g
Silicon dioxide 2.5g
Preparation technology: raw mill crosses 100 mesh sieves (D50=8.74 μm, D90=45.56 μm), sucrose, hydroxypropyl cellulose SSL, aspartame cross 100 mesh sieves, and silicon dioxide, orange powdered flavor cross 60 mesh sieves, for subsequent use.Carmine is added water and is made into 0.025% solution, stir and make wetting agent, for subsequent use.Take the tosufloxacin tosilate of recipe quantity, sucrose, aspartame, hydroxypropyl cellulose SSL, abundant mix homogeneously, add appropriate carmine aqueous solution soft material, 24 mesh sieves are granulated, wet granular is in 60 DEG C of forced air dryings to moisture content < 2%, and dry granule crosses 20 mesh sieve granulate, removes fine powder with 80 mesh sieve sieves, finally add orange powdered flavor, the silicon dioxide of recipe quantity, mixing.
Embodiment 3
Prescription 3
Tosufloxacin tosilate 75g
Sucrose 412.5g
Aspartame 4g
Hydroxypropyl cellulose SSL 2g
Carmine 0.009g
Orange powdered flavor 4g
Silicon dioxide 2.5g
Preparation technology: raw material pulverizing crosses 100 mesh sieves (D50=4.73 μm, D90=16.11 μm), sucrose, hydroxypropyl cellulose SSL, aspartame cross 100 mesh sieves, and silicon dioxide, orange powdered flavor cross 60 mesh sieves, for subsequent use.Carmine is added water and is made into 0.025% solution, stir and make wetting agent, for subsequent use.Take the tosufloxacin tosilate of recipe quantity, sucrose, aspartame, hydroxypropyl cellulose SSL, abundant mix homogeneously, add appropriate carmine aqueous solution soft material, 24 mesh sieves are granulated, wet granular is in 60 DEG C of forced air dryings to moisture content < 2%, and dry granule crosses 20 mesh sieve granulate, removes fine powder with 80 mesh sieve sieves, finally add orange powdered flavor, the silicon dioxide of recipe quantity, mixing.
Embodiment 4
Prescription 4
Tosufloxacin tosilate 75g
Sucrose 413g
Aspartame 4g
Hydroxypropyl cellulose SSL 1.5g
Carmine 0. 009g
Orange powdered flavor 4g
Silicon dioxide 2.5g
Preparation technology: raw material pulverizing crosses 100 mesh sieves (D50=4.73 μm, D90=16.11 μm), sucrose, hydroxypropyl cellulose SSL, aspartame cross 100 mesh sieves, and silicon dioxide, orange powdered flavor cross 60 mesh sieves, for subsequent use.Carmine is added water and is made into 0.025% solution, stir and make wetting agent, for subsequent use.Take the tosufloxacin tosilate of recipe quantity, sucrose, aspartame, hydroxypropyl cellulose SSL, abundant mix homogeneously, add appropriate carmine aqueous solution soft material, 24 mesh sieves are granulated, wet granular is in 60 DEG C of forced air dryings to moisture content < 2%, and dry granule crosses 20 mesh sieve granulate, removes fine powder with 80 mesh sieve sieves, finally add orange powdered flavor, the silicon dioxide of recipe quantity, mixing.
Result shows: mobility of particle, the granularity of 4 prescriptions are all better.Wherein the mouthfeel of prescription 1 is slightly poor, and after increasing aspartame and orange powdered flavor consumption, the mouthfeel of prescription 2 ~ 4 is all better.The stripping of prescription 1 is comparatively slow, and after prescription 2 reduces the consumption of adhesive hydroxypropyl cellulose SSL, stripping is still slower; Prescription 3 reduces the particle diameter of raw material while reducing adhesive consumption, obtains the stripping curve basically identical with control formulation of going on the market; Prescription 4 reduces the consumption of adhesive further on the basis of prescription 3, causes mobility of particle and granularity to be deteriorated.Therefore determine that prescription 3 is the best prescription of this product.
Experimental example 1 study on the stability
Children's's tosufloxacin tosilate granule is prepared by the above-mentioned best prescription technique determined, removing inner packing, put in clean plate, spread out into the thin layer of below 5mm, place 10 days under high light (4500lx), high temperature (60 DEG C), high humidity (RH92.5%, RH75%) condition respectively, respectively at sampling in the 0th, 5,10 day, measure every quality index, the results are shown in following table.
Separately get children's's tosufloxacin tosilate granule, adopt composite membrane for packaging medicine bag packaging, place 10 days under high light (4500lx), high humidity (RH92.5%) condition respectively, respectively at sampling in the 0th, 5,10 day, detect every quality index.The results are shown in following table.
Influence factor's result of the test
After children's's tosufloxacin tosilate granule removing inner packing, put in clean plate, spread out into the thin layer of below 5mm, place 10 days under high light (4500lx), high temperature (60 DEG C), high humidity (RH75%, RH92.5%) condition, except moisture absorption weightening finish under high humidity (RH92.5%) condition is obvious, have deliquescence phenomenon, outside under high light (4500lx) condition, related substance increases, other every quality index compared with 0 day, have no significant change, illustrate that this product answers lucifuge, sealing is preserved.
After children's's tosufloxacin tosilate granule adopts pharmaceutical packaging composite membrane bag packaging, place 10 days under high light (4500lx) and high humidity (RH92.5%) condition, every quality index compared with 0 day, had no significant change.Illustrate that these packaging material can play lucifuge, moistureproof effect.
Result shows: this formula preparation technique is simple, repeatability good, and quality research result shows, by the obtained stable and reliable product quality of this formulation and technology, can meet the requirement of industrialized great production.
Claims (5)
1. a children's uses tosufloxacin tosilate granule, it is characterized in that children's described in every 1000 bags with in tosufloxacin tosilate granule containing, for example lower component: principal agent tosufloxacin tosilate 75g, adjuvant contains diluent, sweeting agent, adhesive, fluidizer, correctives, wherein: sucrose 411.5g-413.5g, aspartame 2g-4g, hydroxypropyl cellulose SSL 1.5g-5g, orange powdered flavor 2g-4g, silicon dioxide 0.25g, purified water 37g, described coloring agent is carmine or ferrum oxide.
2. the children's according to claims 1 uses tosufloxacin tosilate granule, it is characterized in that described coloring agent is carmine or ferrum oxide.
3. the children's according to claims 2 uses tosufloxacin tosilate granule, it is characterized in that described coloring agent is carmine.
4. the children's according to claims 3 uses tosufloxacin tosilate granule, it is characterized in that described carmine, and addition is 0.009mg(0.0018%).
5. the children's according to claims 1 uses tosufloxacin tosilate granule, it is characterized in that described adjuvant: sucrose 412.5g, aspartame 4g, hydroxypropyl cellulose SSL 2g, orange powdered flavor 4g, silicon dioxide 2.5g, carmine 0.009mg(0.0018%), purified water 37g.
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| Application Number | Priority Date | Filing Date | Title |
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| CN201410798002.XA CN104546735A (en) | 2014-12-22 | 2014-12-22 | Pediatric tosufloxacin tosilate granule and preparation method thereof |
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| CN201410798002.XA CN104546735A (en) | 2014-12-22 | 2014-12-22 | Pediatric tosufloxacin tosilate granule and preparation method thereof |
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| CN104546735A true CN104546735A (en) | 2015-04-29 |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106176646A (en) * | 2016-08-19 | 2016-12-07 | 珠海同源药业有限公司 | A kind of tosufloxacin tosilate dispersible tablet and preparation method thereof |
| CN106310286A (en) * | 2016-08-19 | 2017-01-11 | 珠海同源药业有限公司 | Tosufloxacin tosylate composition |
| CN107519145A (en) * | 2017-08-24 | 2017-12-29 | 青岛正大海尔制药有限公司 | A kind of tosufloxacin tosilate children effervescent tablet and preparation method thereof |
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| JP2007269783A (en) * | 2006-03-06 | 2007-10-18 | Toyama Chem Co Ltd | Tosufloxacin tosylate-containing granular solid preparation |
| JP2013231090A (en) * | 2013-08-23 | 2013-11-14 | Toyama Chem Co Ltd | Granular solid preparation containing tosufloxacin and polyvinylpyrrolidone |
| JP2013231091A (en) * | 2013-08-23 | 2013-11-14 | Toyama Chem Co Ltd | Granular solid preparation containing tosufloxacin |
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2014
- 2014-12-22 CN CN201410798002.XA patent/CN104546735A/en active Pending
Patent Citations (3)
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| JP2007269783A (en) * | 2006-03-06 | 2007-10-18 | Toyama Chem Co Ltd | Tosufloxacin tosylate-containing granular solid preparation |
| JP2013231090A (en) * | 2013-08-23 | 2013-11-14 | Toyama Chem Co Ltd | Granular solid preparation containing tosufloxacin and polyvinylpyrrolidone |
| JP2013231091A (en) * | 2013-08-23 | 2013-11-14 | Toyama Chem Co Ltd | Granular solid preparation containing tosufloxacin |
Non-Patent Citations (1)
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| 袁国平，等: "甲苯磺酸托氟沙星胶囊的UV测定", 《中国医药工业杂志》 * |
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106176646A (en) * | 2016-08-19 | 2016-12-07 | 珠海同源药业有限公司 | A kind of tosufloxacin tosilate dispersible tablet and preparation method thereof |
| CN106310286A (en) * | 2016-08-19 | 2017-01-11 | 珠海同源药业有限公司 | Tosufloxacin tosylate composition |
| CN106176646B (en) * | 2016-08-19 | 2020-08-11 | 珠海同源药业有限公司 | Tosufloxacin tosylate dispersible tablets and preparation method thereof |
| CN107519145A (en) * | 2017-08-24 | 2017-12-29 | 青岛正大海尔制药有限公司 | A kind of tosufloxacin tosilate children effervescent tablet and preparation method thereof |
| CN107519145B (en) * | 2017-08-24 | 2021-04-30 | 正大制药（青岛）有限公司 | Tosufloxacin tosylate effervescent tablet for children and preparation method thereof |
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Application publication date: 20150429 |