CN1985831A - Lung-targeting cefradine microsphere for animal and birds and its preparing method - Google Patents
Lung-targeting cefradine microsphere for animal and birds and its preparing method Download PDFInfo
- Publication number
- CN1985831A CN1985831A CNA2005101225018A CN200510122501A CN1985831A CN 1985831 A CN1985831 A CN 1985831A CN A2005101225018 A CNA2005101225018 A CN A2005101225018A CN 200510122501 A CN200510122501 A CN 200510122501A CN 1985831 A CN1985831 A CN 1985831A
- Authority
- CN
- China
- Prior art keywords
- cefradine
- microsphere
- gelatin
- isopropyl alcohol
- liquid paraffin
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The present invention belongs to the field of veterinary medicine technology, and is especially lung targeting cefradine microsphere for animal and its preparation process. The cefradine microsphere is prepared with cefradine as medicine component and gelatin as carrier in the weight ratio of 1 to 2, and through dissolving cefradine in gelatin solution and adding Span-80 and liquid paraffin through stirring to obtain emulsion; cooling in icy bath to below 5 deg.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 cefradine 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 cefradine is feedstock production lung targeting preparation---cefradine microsphere and preparation method thereof.
Background technology
Cephalosporins is to use maximum class antibacterials modern age clinically, chemical name this product of cefradine is (6R, 7R)-7-[(R)-2-amino-2-(1, the 4-cyclohexenyl group) acetylamino]-3-methyl-8-oxo-5-thia-1-azabicyclo [4.2.0] oct-2-ene-2-carboxylic acid.Press anhydride and calculate, contain C
16H
19N
3O
4S must not be less than 90.0%.
This medicine character is white or off-white color crystalline powder; Little smelly.Molten in the water part omitted, almost insoluble in ethanol, chloroform or ether.
Its antibacterial action is strong than cefalexin, and bacterium such as staphylococcus, escherichia coli, hemophilus influenza are had bactericidal action.Range of application and cefmetazole are approximate.But this product is invalid to bacillus pyocyaneus.
Cefradine is a broad spectrum antibiotic, and this medicine has has a broad antifungal spectrum, bactericidal activity is strong, body is interior widely distributed, does not have characteristics such as cross resistance with other antimicrobial drugs, is used to prevent and treat the fowl bacterial disease, and significant curative effect is arranged.
But owing to use widely for a long time, many pathogen oneself draw fixed output quota to give birth to certain drug resistance to cephalo, thereby cause 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 cefradine, 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 cefradine microsphere for achieving the above object, it is characterized in that, and be raw material with the cefradine, be carrier is made microsphere with the gelatin, the ratio of cefradine and gelatin: 1: 2.
Described veterinary drug cefradine 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, cefradine 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 cefradine microsphere.The drug loading of making this dosage form of back can reach 20.84%, and envelop rate can reach 42.37%.
Described medicine cefradine microsphere is characterized in that, the cefradine microspherulite diameter scope of preparation is the lung targeting preparation at 7-30um.
Use has the particle size distribution of the optical microscope measuring cefradine microsphere of micrometer, its result shows cefradine microsphere average grain diameter 11.87um, the microsphere of particle size distribution in the 7-30um scope accounts for 90.13%, 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 cefradine 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 cefradine microsphere that is packaged in the bottle.Cefradine 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, cefradine 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 cefradine 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 lung-targeting cefradine preparation for preparing is used for the treatment of poultry because of microbial bacterial infections such as staphylococcus, escherichia coli, hemophilus influenzas.Administering mode is spice or drinking-water administration, poultry 0.02-0.04g/kg body weight, and domestic animal 0.01-0.03g/kg body weight, 2 times on the one, 3-5 days is a course of treatment.
Claims (3)
1, a kind of veterinary drug cefradine microsphere is characterized in that, is raw material with the cefradine, is that carrier is made microsphere with the gelatin, the ratio of cefradine and gelatin: 1: 2.
2, veterinary drug cefradine 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, cefradine 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 cefradine microsphere.
3, veterinary drug cefradine microsphere according to claim 2 is characterized in that, the cefradine microspherulite diameter scope of preparation is the lung targeting preparation at 7-30um.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2005101225018A CN1985831A (en) | 2005-12-21 | 2005-12-21 | Lung-targeting cefradine microsphere for animal and birds and its preparing method |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2005101225018A CN1985831A (en) | 2005-12-21 | 2005-12-21 | Lung-targeting cefradine microsphere for animal and birds and its preparing method |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1985831A true CN1985831A (en) | 2007-06-27 |
Family
ID=38182858
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA2005101225018A Pending CN1985831A (en) | 2005-12-21 | 2005-12-21 | Lung-targeting cefradine microsphere for animal and birds and its preparing method |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1985831A (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101829063A (en) * | 2010-03-18 | 2010-09-15 | 青岛康地恩药业有限公司 | Lung targeting microsphere of veterinary ceftiofur hydrochloride and preparation method |
| CN101564798B (en) * | 2008-04-23 | 2011-12-28 | 深超光电（深圳）有限公司 | Full-inspection type double-track laser short loop circuit cutting machine and cutting and detecting method thereof |
| CN110693888A (en) * | 2019-11-05 | 2020-01-17 | 山东省农业科学院奶牛研究中心 | Application of cefradine as bovine enterovirus inhibitor |
-
2005
- 2005-12-21 CN CNA2005101225018A patent/CN1985831A/en active Pending
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101564798B (en) * | 2008-04-23 | 2011-12-28 | 深超光电（深圳）有限公司 | Full-inspection type double-track laser short loop circuit cutting machine and cutting and detecting method thereof |
| CN101829063A (en) * | 2010-03-18 | 2010-09-15 | 青岛康地恩药业有限公司 | Lung targeting microsphere of veterinary ceftiofur hydrochloride and preparation method |
| CN110693888A (en) * | 2019-11-05 | 2020-01-17 | 山东省农业科学院奶牛研究中心 | Application of cefradine as bovine enterovirus inhibitor |
| CN110693888B (en) * | 2019-11-05 | 2022-12-06 | 山东省农业科学院奶牛研究中心 | Application of cefradine as bovine enterovirus inhibitor |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN1985831A (en) | Lung-targeting cefradine microsphere for animal and birds and its preparing method | |
| CN101536985A (en) | Livestock cefquinome lung-targeted microspheres and preparation method thereof | |
| CN101756910B (en) | Lung targeting ceftiofur microsphere and preparation method | |
| CN101829082A (en) | Method for preparing veterinary injection of spectinomycin hydrochloride and lincomycin hydrochloride | |
| CN117379378A (en) | Compound amoxicillin soluble powder for livestock and preparation process thereof | |
| CN104688713A (en) | Cefradine capsule and preparation method thereof | |
| CN1985838A (en) | Lung-targeting tylan microsphere for animal and birds and its preparing method | |
| CN1985832A (en) | Lung-targeting cefoperazone microsphere for animal and birds and its preparing method | |
| CN101756909B (en) | Lung-targeting ceftiofur microsphere and preparation method thereof | |
| CN1985820A (en) | Lung-targeting amoxicillin microsphere for animal and birds and its preparing method | |
| CN101829129B (en) | Veterinary compound gentamycin sulfate injection and preparation method thereof | |
| CN102813623B (en) | Method for preparing ceftiofur hydrochloride suspension injection | |
| CN1985839A (en) | Lung-targeting roxithromycin microsphere for animal and birds and its preparing method | |
| CN1985805A (en) | Lung targeting clarithromycin microsphere for animal and birds and its preparing method | |
| CN108670957A (en) | One kind acidification amoxicillin soluble powder for animals and preparation method thereof | |
| CN1985812A (en) | Lung-targeting florfenicol microsphere for animal and birds and its preparing method | |
| CN1985830A (en) | Lung-targeting ofloxacin microsphere for animal and birds and its preparing method | |
| CN104800229B (en) | A kind of compound sulfadiazine suspension and preparation method thereof | |
| CN102526121A (en) | Wound repair composition and preparation method and application thereof | |
| CN1985825A (en) | Lung-targeting fleroxacin microsphere for animal and birds and its preparing method | |
| CN1985841A (en) | Lung-targeting azithromycin microsphere for animal and birds and its preparing method | |
| CN101829063B (en) | Lung targeting microsphere of veterinary ceftiofur hydrochloride and preparation method | |
| CN103432087B (en) | Clindamycin hydrochloride preparation for injection and preparation method thereof | |
| CN1985824A (en) | Lung-targeting sparfloxacin microsphere for animal and birds and its preparing method | |
| CN102772790A (en) | Compound echinacea purpurea preparation and preparation method and application thereof |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |