CN104523596A - Soluble enrofloxacin solid dispersion and preparation method thereof - Google Patents
Soluble enrofloxacin solid dispersion and preparation method thereof Download PDFInfo
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- CN104523596A CN104523596A CN201410760427.1A CN201410760427A CN104523596A CN 104523596 A CN104523596 A CN 104523596A CN 201410760427 A CN201410760427 A CN 201410760427A CN 104523596 A CN104523596 A CN 104523596A
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- enrofloxacin
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Abstract
The invention relates to a soluble enrofloxacin solid dispersion and a preparation method thereof. The soluble enrofloxacin solid dispersion comprises enrofloxacin, carbonate, EDTA2Na and glycerin monostearate. The soluble enrofloxacin solid dispersion prepared by the method has the characteristics of being convenient to administrate, good in water solubility, high in dissolution rate, high in bioavailability, good in palatability and the like.
Description
Technical field
the invention belongs to field of veterinary medicine preparation, be specifically related to a kind of solubility Enrofloxacin solid dispersion and preparation method thereof.
Background technology
Enrofloxacin was the third generation carbostyril family antibacterial drugs of animal specific, and this medicine, first by first being succeeded in developing in 1987 by German Bayer company, obtained U.S. FDA approval in 1996.Enrofloxacin has another name called ENR, enrofloxacin, is light yellow crystalline powder, is slightly soluble in water, odorless, bitter in the mouth.This product has good antibacterial action to multiple gram negative bacilli and coccus, comprises bacillus pyocyaneus, klebsiella, escherichia coli, Enterobacter, campylobacter, Shigella, Salmonella, Aeromonas, haemophilus, yersinia's genus, Serratia, vibrio, Proteus etc.Also effective to Brucella, pasteurella, Erysipelothrix, Bordetella, staphylococcus (comprise and produce penicillium sp enzyme and methicillin resistance bacterial strain), Mycoplasma and chlamydia.But variant to most of streptococcic effect, faint to most of anaerobe effect.Because the water solublity of enrofloxacin is very poor, cause poor bioavailability, so improve enrofloxacin water solublity to seem extremely important, and enrofloxacin has bitterness, and palatability is very poor, and oral administration poultry does not like absorption, have impact on therapeutic effect further.And enrofloxacin injection is comparatively strong due to alkalescence, cause animal body uncomfortable.Poultry drug administration by injection is restricted, and not easily applies.There are some researches show, utilize enrofloxacin and Polyethylene Glycol (PEG 6000) or polyvinylpyrrolidone to form solid dispersion by fusion method or spray drying method and also can improve its water solubility problems, but need in fusion method preparation process to put into flat board sub-cooled by after enrofloxacin and Polyethylene Glycol heating for dissolving, due to solidification process mixture poor thermal conductivity, so the cooling procedure time is longer, and thawing of being easily heated in follow-up crushing process, and production capacity receives the restriction of film-cooled heat, be difficult to realize large-scale production; The powder size that employing spray drying method obtains is little, and easily glues wall or produce product thawing caking due to cooling effect difference.So lack a kind of applicable suitability for industrialized production solubility Enrofloxacin solid dispersion technology of preparing at present.
Summary of the invention
the object of the invention is to overcome the deficiencies in the prior art, for treatment animal bacterial infection provides a kind of convenient drug administration, good water solubility, dissolution is high, and bioavailability is high, is easy to solubility Enrofloxacin solid dispersion realizing suitability for industrialized production and preparation method thereof.
A kind of Enrofloxacin solid dispersion of the present invention and preparation method thereof, described Enrofloxacin solid dispersion comprises the enrofloxacin that mass percent is 5%-20%, mass percent is sodium carbonate or the potassium carbonate of 20%-50%, mass percent is the EDTA2Na of 5%-10%, is the glyceryl monostearate of 20%-70% with mass percent.
A kind of Enrofloxacin solid dispersion of the present invention and preparation method thereof, is characterized in that, its preparation, by after glyceryl monostearate heating and melting, adds enrofloxacin, carbonate, EDTA2Na respectively, then homogenous disperse, pulverized 24 mesh sieves and get final product after cooling.
Solid dispersion prepared by the present invention, can apply for enrofloxacin soluble powder lot number, direct Clinical practice.
Enrofloxacin solid dispersion prepared by the present invention has good water solubility, facilitates the feature of Clinical practice, effectively reduces the bitter of preparation simultaneously, improves the palatability of enrofloxacin oral formulations.
detailed description of the invention:
Following detailed description of the invention for illustration of the present invention, but is not used in and limits the scope of the invention.
Embodiment 10% solubility Enrofloxacin solid dispersion and preparation method thereof
Prescription: enrofloxacin mass percent 10%, sodium carbonate mass percent is 20%, EDTA2Na mass percent is 5%, glyceryl monostearate mass percent 65%.Technique: after glyceryl monostearate heating and melting, adds enrofloxacin, carbonate, EDTA2Na, then homogenous disperse respectively, pulverized 24 mesh sieves and get final product after cooling.
Claims (2)
1. the present invention relates to a kind of Enrofloxacin solid dispersion and preparation method thereof, described Enrofloxacin solid dispersion comprises the enrofloxacin that mass percent is 5%-20%, mass percent is sodium carbonate or the potassium carbonate of 20%-50%, mass percent is the EDTA2Na of 5%-10%, is the glyceryl monostearate of 20%-70% with mass percent.
2. the present invention relates to a kind of Enrofloxacin solid dispersion and preparation method thereof, it is characterized in that, its preparation, by after glyceryl monostearate heating and melting, adds enrofloxacin, carbonate, EDTA2Na respectively, then homogenous disperse, pulverized 24 mesh sieves and get final product after cooling.
Priority Applications (1)
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CN201410760427.1A CN104523596A (en) | 2014-12-12 | 2014-12-12 | Soluble enrofloxacin solid dispersion and preparation method thereof |
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CN201410760427.1A CN104523596A (en) | 2014-12-12 | 2014-12-12 | Soluble enrofloxacin solid dispersion and preparation method thereof |
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CN104523596A true CN104523596A (en) | 2015-04-22 |
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CN201410760427.1A Pending CN104523596A (en) | 2014-12-12 | 2014-12-12 | Soluble enrofloxacin solid dispersion and preparation method thereof |
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Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN105078899A (en) * | 2015-08-26 | 2015-11-25 | 四川农业大学 | Enrofloxacin stratified high molecular taste mashing skeleton particle and preparation method thereof |
-
2014
- 2014-12-12 CN CN201410760427.1A patent/CN104523596A/en active Pending
Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN105078899A (en) * | 2015-08-26 | 2015-11-25 | 四川农业大学 | Enrofloxacin stratified high molecular taste mashing skeleton particle and preparation method thereof |
CN105078899B (en) * | 2015-08-26 | 2018-06-29 | 四川农业大学 | A kind of Enrofloxacin cladding macromolecule flavoring skeleton particle and preparation method thereof |
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WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20150422 |
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WD01 | Invention patent application deemed withdrawn after publication |