CN104706621A - Marbofloxacin micro-capsule and preparation method thereof - Google Patents
Marbofloxacin micro-capsule and preparation method thereof Download PDFInfo
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- CN104706621A CN104706621A CN201510120102.1A CN201510120102A CN104706621A CN 104706621 A CN104706621 A CN 104706621A CN 201510120102 A CN201510120102 A CN 201510120102A CN 104706621 A CN104706621 A CN 104706621A
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Abstract
The invention relates to a marbofloxacin micro-capsule and a preparation method of the marbofloxacin micro-capsule. The preparation method comprises the following steps: (1) preparing a wall material solution, (2) preparing a core material solution, (3) carrying out emulsification and reduced pressure distillation: slowly dropwise adding the core material solution prepared in Step (2) into the wall material solution prepared in Step (1) under a high-speed shearing condition, carrying out the reduced pressure distillation at the same time, recovering a dichloromethane/absolute ethyl alcohol mixed solution, and continuing the reduced pressure distillation after dropwise adding, and (4) carrying out spray drying, wherein the system temperature is 10-40 DEG C; a vacuum degree is 0.01-0.07Mpa; the dropwise adding time is 0.5-2h; and the shearing speed is 5000-10000 r/min. The sensitivity of marbofloxacin to light can be reduced; the drug efficacy is prolonged; an unpleasant odor is covered; the solubility is improved; in addition, various preparations, such as powder, a tablet, a capsule and controlled-release agent can be prepared very conveniently; and animal administration is facilitated.
Description
Technical field
The present invention relates to a kind of marbofloxacin microcapsule and preparation method thereof, belong to field of veterinary medicine preparation.
Background technology
Marbofloxacin is another third generation quinolones animal specific antibacterials after enrofloxacin, danofloxacin, sarafloxacin, difloxacin.Antibacterial mainly through anti-bacteria topoisomerase active.Marbofloxacin is formulated by Roche Holding Ag of Switzerland the earliest, and Vetoquinol company develops further, and in nineteen ninety-five first in Britain's listing, subsequently in succession in France, US and European listing.Marbofloxacin has a broad antifungal spectrum, sterilizing power is strong, all has stronger activity to Gram-negative and positive bacteria, even to some mycete and anaerobe effective.Tissue infiltration power is strong, and its body absorption is complete and widely distributed rapidly, and eliminate long half time, bioavailability is close to 100%; Safe-dosaging limits is wide, antibacterial without cross resistance with other, without obvious reproduction and genetoxic.These all determine it preventing and treating the great potential in poultry respiratory system infection, urinary system infection, digestive system infection, shallow table or deep skin tissue infection, eyes and ear infections etc., are animal specific fluoroquinolone antibacterial agents of new generation.At present, the U.S. and European Union can ratify for house pet, and European Union's approval can be used for domestic animal, and Japan can be used for poultry.
Marbofloxacin structural formula
Marbofloxacin belongs to fluoroquinolones, comparatively responsive to light, dissolubility is poor and there is certain abnormal smells from the patient, is unfavorable for the medication of animal.But this medicine preparation variety is single at present, be mainly injection and the solution oral agents of its lactic acid or hydrochlorate, and application is narrow, is mainly used in house pet.Also there is the technical barrier that cost is high, quality control is difficult simultaneously.
Starch sodium octenyl succinate is as a kind of New Wall Material, be widely used in fatsoluble vitamin embedding, when starch sodium octenyl succinate is as wall material embedding oils and fats, entrapment principle is that the hydrophobic group of sodium octenyl succinate inserts oil phase, sodium carboxylate groups inserts aqueous phase, starch group forms the very large thin film of one deck intensity at oil-water interfaces, reaches embedding effect.But because the solubility property of marbofloxacin is extremely special, its state is solid, and marbofloxacin dissolubility in oils and fats is lower.Limit marbofloxacin formulation development and application.Marbofloxacin dissolves by solvent-applied of the present invention, under high speed shear, solvent is added to aqueous phase, at evaporating solvent simultaneously, marbofloxacin microgranule is separated out, the embedding of marbofloxacin microgranule is formed microcapsule by starch sodium octenyl succinate simultaneously, the sensitivity of marbofloxacin to light can be reduced, extend drug effect, cover bad smell, increase dissolubility, and various preparation can be prepared easily, as powder, tablet, capsule, controlled release agent etc., be conducive to the medication of animal.
Summary of the invention
In order to solve marbofloxacin embedding problem, the invention provides a kind of take starch sodium octenyl succinate as marbofloxacin microcapsule of wall material and preparation method thereof, and by wall material, core are carried out emulsifying, spray is dry, make water solublity microcapsule powder, the sensitivity of marbofloxacin to light can be reduced, extend drug effect, cover bad smell, increase dissolubility, and various preparation can be prepared easily, as powder, tablet, capsule, controlled release agent etc., be conducive to the medication of animal.
For achieving the above object, the present invention is achieved by the following technical solutions:
A kind of marbofloxacin microcapsule, is made up of the component of following mass percent: the starch sodium octenyl succinate 40-99% as wall material and the marbofloxacin 1-60% as core.
A preparation method for marbofloxacin microcapsule, comprises the following steps:
(1) prepare wall material solution: starch sodium octenyl succinate be dissolved in purified water, be mixed with the solution that concentration is 10-30%;
(2) prepare core material solution: be dissolved in by marbofloxacin in dichloromethane/dehydrated alcohol mixed solution, be mixed with the solution that concentration is 20%-50%;
(3) emulsifying and distilling under reduced pressure: under high speed shear condition, the obtained core material solution of step (2) is slowly dripped in the wall material solution that step (1) is obtained, carry out distilling under reduced pressure simultaneously, reclaim dichloromethane/dehydrated alcohol mixed solution, system temperature 10-40 DEG C, vacuum 0.01-0.07Mpa, time for adding is at 0.5-2 hour, shear rate is 5000-10000r/min, dropwises rear continuation distilling under reduced pressure 2 hours;
(4) spraying dry: inlet temperature 180-220 DEG C, carry out spraying dry at leaving air temp 80-120 DEG C.
Dichloromethane in described step (2) and the volume ratio of dehydrated alcohol are 6:4-19:1.
Beneficial effect of the present invention is as follows:
The present invention adopts microencapsulation that microcapsule is made in non-water-soluble marbofloxacin embedding, embedding wall material used is starch sodium octenyl succinate, by adding of auxiliary agent dichloromethane/dehydrated alcohol, marbofloxacin can be embedded, spraying dry after pharmaceutical pack being embedded in wall material, forms instant microcapsule powder.
Present invention process is simple, with low cost, gained marbofloxacin microcapsule powder can reduce the sensitivity of marbofloxacin to light, extend drug effect, cover bad smell, increase dissolubility, and various preparation can be prepared easily, as powder, tablet, capsule, controlled release agent etc., be conducive to the medication of animal.
Detailed description of the invention
Below in conjunction with specific embodiment, the present invention is further illustrated, but protection scope of the present invention is not limited to this.
All raw materials involved in the present invention and auxiliary agent all can adopt mode well known in the art to synthesize, and also can adopt commercially available prod.
embodiment 1
Starch sodium octenyl succinate 40%
Marbofloxacin 60%
Preparation method:
Starch sodium octenyl succinate is dissolved in purified water, the wall material solution of compound concentration 10%.Marbofloxacin is dissolved in dichloromethane/dehydrated alcohol (ratio is 9:1) mixed solution, is mixed with the core material solution that concentration is 20%.Under 5000r/min shear rate, in wall material solution, slowly drip core material solution, carry out distilling under reduced pressure simultaneously, reclaim dichloromethane/dehydrated alcohol mixed solution, system temperature 10 DEG C, vacuum 0.07Mpa, time for adding, at 2 hours, dropwises rear continuation distilling under reduced pressure 2 hours.LS is dry, inlet temperature 180 DEG C, leaving air temp 80 DEG C.
Obtained powdered oil outward appearance is faint yellow, and good fluidity meets water dissolution.
embodiment 2
Starch sodium octenyl succinate 90%
Marbofloxacin 10%
Preparation method:
Starch sodium octenyl succinate is dissolved in purified water, the wall material solution of compound concentration 30%.Marbofloxacin is dissolved in dichloromethane/dehydrated alcohol (ratio is 3:2) mixed solution, is mixed with the core material solution that concentration is 50%.Under 10000r/min shear rate, in wall material solution, slowly drip core material solution, carry out distilling under reduced pressure simultaneously, reclaim dichloromethane/dehydrated alcohol mixed solution, system temperature 40 DEG C, vacuum 0.01Mpa, time for adding, at 0.5 hour, dropwises rear continuation distilling under reduced pressure 2 hours.LS is dry, inlet temperature 220 DEG C, leaving air temp 120 DEG C.
Obtained powdered oil outward appearance is faint yellow, and good fluidity meets water dissolution.
embodiment 3
Starch sodium octenyl succinate 70%
Marbofloxacin 30%
Preparation method:
Starch sodium octenyl succinate is dissolved in purified water, the wall material solution of compound concentration 20%.Marbofloxacin is dissolved in dichloromethane/dehydrated alcohol (ratio is 19:3) mixed solution, is mixed with the core material solution that concentration is 35%.Under 7500r/min shear rate, in wall material solution, slowly drip core material solution, carry out distilling under reduced pressure simultaneously, reclaim dichloromethane/dehydrated alcohol mixed solution, system temperature 25 DEG C, vacuum 0.04Mpa, time for adding, at 1.25 hours, dropwises rear continuation distilling under reduced pressure 2 hours.LS is dry, inlet temperature 200 DEG C, leaving air temp 100 DEG C.
Obtained powdered oil outward appearance is faint yellow, and good fluidity meets water dissolution.
embodiment 4
Starch sodium octenyl succinate 50%
Marbofloxacin 50%
Preparation method:
Starch sodium octenyl succinate is dissolved in purified water, the wall material solution of compound concentration 25%.Marbofloxacin is dissolved in dichloromethane/dehydrated alcohol (ratio is 7:2) mixed solution, is mixed with the core material solution that concentration is 45%.Under 9000r/min shear rate, in wall material solution, slowly drip core material solution, carry out distilling under reduced pressure simultaneously, reclaim dichloromethane/dehydrated alcohol mixed solution, system temperature 15 DEG C, vacuum 0.05Mpa, time for adding, at 1.5 hours, dropwises rear continuation distilling under reduced pressure 2 hours.LS is dry, inlet temperature 190 DEG C, leaving air temp 90 DEG C.
Obtained powdered oil outward appearance is faint yellow, and good fluidity meets water dissolution.
The present invention take starch sodium octenyl succinate as marbofloxacin microcapsule of wall material and preparation method thereof, by wall material, core are carried out emulsifying, spray is dry, makes water solublity microcapsule powder, can reduce the sensitivity of marbofloxacin to light, extend drug effect, cover bad smell, increase dissolubility, and various preparation can be prepared easily, as powder, tablet, capsule, controlled release agent etc., be conducive to the medication of animal.
Above-described embodiment only illustrates inventive concept of the present invention for explaining, but not the restriction to rights protection of the present invention, all changes utilizing this design the present invention to be carried out to unsubstantiality, all should fall into protection scope of the present invention.
Claims (3)
1. a marbofloxacin microcapsule, is characterized in that being made up of the component of following mass percent: the starch sodium octenyl succinate 40-99% as wall material and the marbofloxacin 1-60% as core.
2. a preparation method for marbofloxacin microcapsule, is characterized in that comprising the following steps:
(1) prepare wall material solution: starch sodium octenyl succinate be dissolved in purified water, be mixed with the solution that concentration is 10-30%;
(2) prepare core material solution: be dissolved in by marbofloxacin in dichloromethane/dehydrated alcohol mixed solution, be mixed with the solution that concentration is 20%-50%;
(3) emulsifying and distilling under reduced pressure: under high speed shear condition, the obtained core material solution of step (2) is slowly dripped in the wall material solution that step (1) is obtained, carry out distilling under reduced pressure simultaneously, reclaim dichloromethane/dehydrated alcohol mixed solution, system temperature 10-40 DEG C, vacuum 0.01-0.07Mpa, time for adding is at 0.5-2 hour, shear rate is 5000-10000r/min, dropwises rear continuation distilling under reduced pressure 2 hours;
(4) spraying dry: inlet temperature 180-220 DEG C, carry out spraying dry at leaving air temp 80-120 DEG C.
3. the preparation method of marbofloxacin microcapsule as claimed in claim 1, is characterized in that: the dichloromethane in described step (2) and the volume ratio of dehydrated alcohol are 6:4-19:1.
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| CN201510120102.1A CN104706621B (en) | 2015-03-19 | 2015-03-19 | A kind of marbofloxacin micro-capsule and preparation method thereof |
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| CN104706621B CN104706621B (en) | 2017-08-15 |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110141558A (en) * | 2019-05-29 | 2019-08-20 | 四川农业大学 | A kind of preparation method of marbofloxacin nanoparticle |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101019838A (en) * | 2007-02-12 | 2007-08-22 | 清华大学 | Linseed oil microcapsule powder and its prepn |
| WO2010143186A1 (en) * | 2009-06-08 | 2010-12-16 | Otic Pharma Ltd. | Otic foam formulations |
| CN103271875A (en) * | 2013-07-01 | 2013-09-04 | 浙江华尔成生物药业股份有限公司 | Marbofloxacin freeze-dried powder for injection and preparation method and application thereof |
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2015
- 2015-03-19 CN CN201510120102.1A patent/CN104706621B/en active Active
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101019838A (en) * | 2007-02-12 | 2007-08-22 | 清华大学 | Linseed oil microcapsule powder and its prepn |
| WO2010143186A1 (en) * | 2009-06-08 | 2010-12-16 | Otic Pharma Ltd. | Otic foam formulations |
| CN103271875A (en) * | 2013-07-01 | 2013-09-04 | 浙江华尔成生物药业股份有限公司 | Marbofloxacin freeze-dried powder for injection and preparation method and application thereof |
Non-Patent Citations (3)
| Title |
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| 卢素云，等: "恩诺沙星微囊的制备及急性毒性试验", 《动物医学进展》 * |
| 吴克刚，等: "辛烯基琥珀酸淀粉微胶囊化浓缩鱼油的研究", 《食品研究与开发》 * |
| 张秀荣，等: "诺氟沙星微囊的研制", 《沈阳药科大学学报》 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110141558A (en) * | 2019-05-29 | 2019-08-20 | 四川农业大学 | A kind of preparation method of marbofloxacin nanoparticle |
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Address after: 312500 No. 60, Xingmei Avenue, Xinchang provincial high tech Industrial Park, Shaoxing City, Zhejiang Province Patentee after: Guobang Pharmaceutical Group Co., Ltd Address before: Shaoxing City, Zhejiang Province Dongchang Road 312000 Xinchang County Chengguan Town, No. 2-12 Patentee before: Guobang Pharmaceutical Chemicals Group Co., Ltd. |