CN1985820A - Lung-targeting amoxicillin microsphere for animal and birds and its preparing method - Google Patents
Lung-targeting amoxicillin microsphere for animal and birds and its preparing method Download PDFInfo
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- CN1985820A CN1985820A CNA2005101225107A CN200510122510A CN1985820A CN 1985820 A CN1985820 A CN 1985820A CN A2005101225107 A CNA2005101225107 A CN A2005101225107A CN 200510122510 A CN200510122510 A CN 200510122510A CN 1985820 A CN1985820 A CN 1985820A
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- amoxicillin
- 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 amoxicillin microsphere for animal and its preparation process. The amoxicillin microsphere is prepared with amoxicillin as medicine component and gelatin as carrier in the weight ratio of 1 to 2, and through dissolving amoxicillin 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 amoxicillin 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 amoxicillin is feedstock production lung targeting preparation---amoxicillin microsphere and preparation method thereof.
Background technology
Penicillin antibiotics is to use more class antibacterials modern age clinically, known amoxicillin chemical name is (2S, 5R, 6R)-3,3-dimethyl-6-[(R)-(-)-2-amino-2-(4-carboxyl phenyl) acetylamino]-7-oxo-4-thia-1-azabicyclo [3.2.0] heptane-2-formic acid trihydrate.Molecular formula is C
16H
19N
3O
5S, molecular weight are 419.46.The character of this medicine is white or off-white color crystalline powder, mildly bitter flavor, and slightly soluble in water, almost insoluble in ethanol.
The antimicrobial spectrum of amoxicillin is identical with the ampicillin, and oral absorption is good, the medicine of sumat talem, this medicine with the serum concentration higher about one times than the ampicillin.Be usually used in respiratory tract, urinary tract and biliary tract infection and typhoid fever etc. due to the sensitive organism clinically.
But owing to use widely for a long time, oneself has produced certain drug resistance to the amoxicillin many pathogen, thereby causes 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 amoxicillin, 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 amoxicillin microsphere for achieving the above object, it is characterized in that, and be raw material with the amoxicillin, be carrier is made microsphere with the gelatin, the ratio of amoxicillin and gelatin: 1: 2.
Described veterinary drug amoxicillin 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, amoxicillin 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 amoxicillin microsphere.The drug loading of making this dosage form of back can reach 22.41%, and envelop rate can reach 44.32%.
Described medicine amoxicillin microsphere is characterized in that, the amoxicillin microspherulite diameter scope of preparation is the lung targeting preparation at 7-30um.
Use has the particle size distribution of the optical microscope measuring amoxicillin microsphere of micrometer, its result shows amoxicillin microsphere average grain diameter 12.54um, the microsphere of particle size distribution in the 7-30um scope accounts for 92.15%, 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 amoxicillin 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 amoxicillin microsphere that is packaged in the bottle.Amoxicillin 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, amoxicillin 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 amoxicillin 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 amoxicillin preparation for preparing is used for the treatment of infection such as respiratory tract that poultry cause because of some gram positive bacteria, urinary tract, biliary tract, intestinal.Administering mode is spice or drinking-water administration, poultry 0.04-0.08g/kg body weight, and domestic animal 0.01-0.05g/kg body weight, 2 times on the one, 3-5 days is a course of treatment.
Claims (3)
1, a kind of veterinary drug amoxicillin microsphere is characterized in that, is raw material with the amoxicillin, is that carrier is made microsphere with the gelatin, the ratio of amoxicillin and gelatin: 1: 2.
2, veterinary drug according to claim 1 amoxicillin microsphere 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, amoxicillin 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 amoxicillin microsphere.
3, veterinary drug according to claim 2 amoxicillin microsphere is characterized in that the amoxicillin microspherulite diameter scope of preparation is the lung targeting preparation at 7-30um.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2005101225107A CN1985820A (en) | 2005-12-21 | 2005-12-21 | Lung-targeting amoxicillin microsphere for animal and birds and its preparing method |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2005101225107A CN1985820A (en) | 2005-12-21 | 2005-12-21 | Lung-targeting amoxicillin microsphere for animal and birds and its preparing method |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1985820A true CN1985820A (en) | 2007-06-27 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA2005101225107A Pending CN1985820A (en) | 2005-12-21 | 2005-12-21 | Lung-targeting amoxicillin microsphere for animal and birds and its preparing method |
Country Status (1)
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| CN (1) | CN1985820A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108272756A (en) * | 2018-04-09 | 2018-07-13 | 四川恒通动保生物科技有限公司 | A kind of amoxicillin soluble powder and preparation method thereof |
| CN115414522A (en) * | 2022-09-23 | 2022-12-02 | 上海纳米技术及应用国家工程研究中心有限公司 | Preparation method of gelatin drug-loaded microspheres with controllable particle size and single distribution, product and application thereof |
-
2005
- 2005-12-21 CN CNA2005101225107A patent/CN1985820A/en active Pending
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108272756A (en) * | 2018-04-09 | 2018-07-13 | 四川恒通动保生物科技有限公司 | A kind of amoxicillin soluble powder and preparation method thereof |
| CN115414522A (en) * | 2022-09-23 | 2022-12-02 | 上海纳米技术及应用国家工程研究中心有限公司 | Preparation method of gelatin drug-loaded microspheres with controllable particle size and single distribution, product and application thereof |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Open date: 20070627 |