CN1985812A - Lung-targeting florfenicol microsphere for animal and birds and its preparing method - Google Patents
Lung-targeting florfenicol microsphere for animal and birds and its preparing method Download PDFInfo
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- CN1985812A CN1985812A CNA200510122508XA CN200510122508A CN1985812A CN 1985812 A CN1985812 A CN 1985812A CN A200510122508X A CNA200510122508X A CN A200510122508XA CN 200510122508 A CN200510122508 A CN 200510122508A CN 1985812 A CN1985812 A CN 1985812A
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- florfenicol
- microsphere
- gelatin
- isopropyl alcohol
- liquid paraffin
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Abstract
The present invention belongs to the field of veterinary medicine technology, and is especially lung targeting florfenicol microsphere for animal and its preparation process. The florfenicol microsphere is prepared with florfenicol as medicine component and gelatin as carrier in the weight ratio of 1 to 2, and through dissolving florfenicol in gelatin solution and adding Span-80 and liquid paraffin through stirring to obtain emulsion; cooling in icy bath to below 5deg.c and adding glutaraldehyde through stirring for cross-linking and curing; dewatering with isopropyl alcohol and suction filtering; washing with isopropyl alcohol and ethyl ether to eliminate glutaraldehyd, washing with petroleum ether to eliminate liquid paraffin in the surface of microsphere and vacuum drying at room temperature to obtain florfenicol microsphere. The medicine has raised tissue selectivity, delayed release, raised curative effect and lowered toxic side effect.
Description
Technical field
The invention belongs to the technical field of veterinary drug, the present invention relates to the florfenicol is feedstock production lung targeting preparation---florfenicol microsphere and preparation method thereof.
Background technology
Florfenicol is to use a more class antibiotic medicine on veterinary clinic, and the florfenicol chemical name is [R-(R
*, R
*)]-2,2-two chloro-N-[1-(methyl fluoride)-2-hydroxyl-2-[4-(sulfonyloxy methyl) phenyl] ethyl] acetamide.Molecular formula is C
12H
14C
L2FNO
4S.This medicine is white or off-white color crystalline powder, odorless, and slightly soluble in water, very easily dissolving is dissolved in methanol in dimethyl formamide, and is molten in the glacial acetic acid part omitted, soluble,very slightly in water or chloroform.
It is effective to escherichia coli, Salmonella, the klebsiella of anti-chloromycetin that florfenicol is used for the treatment of poultry, post-absorption for oral administration is fast, widely distributed, it is long that the blood medicine is kept the concentration time, to respiratory tract infection, mastitis, the pleuropneumonia of pig, yellow scours, the Hakuri of cattle, the colibacillosis of chicken, Bacillus pasteurii disease etc. have curative effect preferably.
But owing to use widely for a long time clinically, oneself has produced certain drug resistance to florfenicol many pathogen, thereby has caused the reduction of medication effect.For example during pulmonary disease, make medicine reach valid density, certainly will will increase the dosage of medicine, cause easily thus that medicine is residual in other tissue to be increased and produce some to the deleterious toxic and side effects of body in lung tissue in treatment.
Summary of the invention
The objective of the invention is to develop a kind of novel form of florfenicol, improve the tissue selectivity of medicine, delay drug release, heighten the effect of a treatment, reduce toxic and side effects, reach the purpose of slow release, long-acting and targeting.
The present invention provides a kind of veterinary drug florfenicol microsphere for achieving the above object, it is characterized in that, and be raw material with the florfenicol, be carrier is made microsphere with the gelatin, the ratio of florfenicol and gelatin: 1: 2.
Described veterinary drug florfenicol microsphere is characterized in that preparation method is:
A, get gelatin 0.8g, insert in the 8ml purification of aqueous solutions, make the gelatin solution of 10% concentration, 60 ℃ of tepidarium complete swelling;
B, florfenicol 0.4g is dissolved in mix homogeneously in the above-mentioned gelatin solution, slowly be added dropwise to then in the 200ml beaker that fills 1.05ml sorbitan monooleate and 60ml liquid paraffin (1.75% concentration), electromagnetic agitation is even in the uniform temp water-bath, mixing speed is 1000r/min, continue to stir certain hour to milky, emulsification times is 15min; Ice bath is cooled to rapidly below 5 ℃, adds the 6ml glutaraldehyde with the thread shape and continues to stir crosslinking curing 30min; Stir 10min, sucking filtration with isopropyl alcohol 60ml dehydration; Most glutaraldehyde is washed in a little isopropyl alcohol of reuse, ether washing, and with the liquid paraffin of petroleum ether flush away microsphere surface, room temperature vacuum drying 24 hours promptly gets the florfenicol microsphere.The drug loading of making this dosage form of back can reach 22.11%, and envelop rate can reach 42.53%.
Described drug florfenicol microsphere is characterized in that, the florfenicol microspherulite diameter scope of preparation is the lung targeting preparation at 7-30um.
Use has the particle size distribution of the optical microscope measuring florfenicol microsphere of micrometer, its result shows florfenicol microsphere average grain diameter 12.52um, the microsphere of particle size distribution in the 7-30um scope accounts for 91.34%, microsphere form rounding, less sticking, dispersity is good, meets the requirement of lung targeting.
Through the light durability result of the test equal no change almost of outward appearance, form, content, particle diameter of florfenicol microsphere as can be seen; Sterile test is with 1 * 10 of the Co-60 emission
4The Gy radiation dose carries out irradiation sterilization to the florfenicol microsphere that is packaged in the bottle.Florfenicol microsphere behind the irradiation has reached aseptic requirement, and its apparent size, form and content of medicines do not have obvious change yet.
After drug encapsulation is in microsphere, have that obvious control discharges and the effect of prolong drug curative effect, improved the tissue selectivity of medicine, delay drug release, heighten the effect of a treatment, reduce toxic and side effects, reached the purpose of slow release, long-acting and targeting.
The specific embodiment
Embodiment 1: get gelatin 0.8kg, insert (gelatin solution of 10% concentration) among the purification of aqueous solutions 8L, 60 ℃ of tepidarium complete swelling, florfenicol 0.4kg is dissolved in contains mix homogeneously in the gelatin solution, slowly be added dropwise to then in the 200L stirred vessel that fills 1.05L sorbitan monooleate and 60L liquid paraffin (1.75% concentration), even in the uniform temp stirred in water bath, mixing speed is 1000r/min, continue to stir certain hour to milky, emulsification times is 15min.Ice bath is cooled to rapidly below 5 ℃, adds the 6L glutaraldehyde with the thread shape and continues to stir crosslinking curing 30min.Stir 10min, sucking filtration with isopropyl alcohol 60L dehydration.Most glutaraldehyde is washed in a little isopropyl alcohol of reuse, ether washing, and with the liquid paraffin of petroleum ether flush away microsphere surface, room temperature vacuum drying 24 hours promptly gets the florfenicol microsphere.Particle size range is at 7-30um, the general microsphere of good dispersion targeting mainly is a passive target in the water, generally absorbed during less than 7um by the macrophage in liver, the spleen, microsphere between the 7um to 30um is held back in the mechanical filter mode by the minimum capillary bed of lung usually, is entered lung tissue or lung qi bubble by the macrophage picked-up.
Embodiment 2: the florfenicol lung targeting preparation for preparing is used for the treatment of poultry to the escherichia coli of anti-chloromycetin, Salmonella, klebsiella etc., post-absorption for oral administration is fast, widely distributed, it is long that the blood medicine is kept the concentration time, the respiratory tract infection, mastitis, the pleuropneumonia of pig, yellow scours, the Hakuri that are used for the treatment of cattle, the colibacillosis of chicken, Bacillus pasteurii disease etc.Administering mode is the spice administration, feedstuff 228g-456g per ton, and 2 times on the one, 3-5 days is a course of treatment.
Claims (3)
1, a kind of veterinary drug florfenicol microsphere is characterized in that, is raw material with the florfenicol, is that carrier is made microsphere with the gelatin, the ratio of florfenicol and gelatin: 1: 2.
2, veterinary drug florfenicol microsphere according to claim 1 is characterized in that preparation method is:
A, get gelatin 0.8g, insert among the double steaming solution 8ml, make the gelatin solution of 10% concentration, 60 ℃ of tepidarium complete swelling;
B, florfenicol 0.4g is dissolved in mix homogeneously in the above-mentioned gelatin solution, slowly be added dropwise to then in the 200ml beaker of containing 1.05ml sorbitan monooleate and 60ml liquid paraffin (1.75% concentration), electromagnetic agitation is even in the uniform temp water-bath, mixing speed is 1000r/min, continue to stir certain hour to milky, emulsification times is 15min; Ice bath is cooled to rapidly below 5 ℃, adds the 6ml glutaraldehyde with the thread shape and continues to stir crosslinking curing 30min; Stir 10min, sucking filtration with isopropyl alcohol 60ml dehydration; Most glutaraldehyde is washed in a little isopropyl alcohol of reuse, ether washing, and with the liquid paraffin of petroleum ether flush away microsphere surface, room temperature vacuum drying 24 hours promptly gets the florfenicol microsphere.
3, veterinary drug florfenicol microsphere according to claim 2 is characterized in that, the florfenicol microspherulite diameter scope of preparation is the lung targeting preparation at 7-30um.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA200510122508XA CN1985812A (en) | 2005-12-21 | 2005-12-21 | Lung-targeting florfenicol microsphere for animal and birds and its preparing method |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA200510122508XA CN1985812A (en) | 2005-12-21 | 2005-12-21 | Lung-targeting florfenicol microsphere for animal and birds and its preparing method |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1985812A true CN1985812A (en) | 2007-06-27 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA200510122508XA Pending CN1985812A (en) | 2005-12-21 | 2005-12-21 | Lung-targeting florfenicol microsphere for animal and birds and its preparing method |
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| CN (1) | CN1985812A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101849913A (en) * | 2009-03-30 | 2010-10-06 | 北京大北农科技集团股份有限公司 | Method for preparing veterinary florfenicol lung targeting gelatin microsphere |
| CN102106843A (en) * | 2011-02-24 | 2011-06-29 | 河南黑马动物药业有限公司 | Slow-release lung targeted microcapsule preparation of florfenicol and preparation method thereof |
-
2005
- 2005-12-21 CN CNA200510122508XA patent/CN1985812A/en active Pending
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101849913A (en) * | 2009-03-30 | 2010-10-06 | 北京大北农科技集团股份有限公司 | Method for preparing veterinary florfenicol lung targeting gelatin microsphere |
| CN101849913B (en) * | 2009-03-30 | 2013-01-30 | 北京大北农科技集团股份有限公司 | Method for preparing veterinary florfenicol lung targeting gelatin microsphere |
| CN102106843A (en) * | 2011-02-24 | 2011-06-29 | 河南黑马动物药业有限公司 | Slow-release lung targeted microcapsule preparation of florfenicol and preparation method thereof |
| CN102106843B (en) * | 2011-02-24 | 2012-04-04 | 河南黑马动物药业有限公司 | Slow-release lung targeted microcapsule preparation of florfenicol and preparation method thereof |
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| WD01 | Invention patent application deemed withdrawn after publication |