CN104706621B - A kind of marbofloxacin micro-capsule and preparation method thereof - Google Patents
A kind of marbofloxacin micro-capsule and preparation method thereof Download PDFInfo
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- CN104706621B CN104706621B CN201510120102.1A CN201510120102A CN104706621B CN 104706621 B CN104706621 B CN 104706621B CN 201510120102 A CN201510120102 A CN 201510120102A CN 104706621 B CN104706621 B CN 104706621B
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Abstract
The present invention relates to a kind of marbofloxacin micro-capsule and preparation method thereof, comprise the following steps：（1）Prepare wall material solution（2）Prepare core material solution（3）Emulsification and vacuum distillation：Under the conditions of high speed shear, to step（1）Step is slowly added dropwise in obtained wall material solution（2）Obtained core material solution, while carrying out vacuum distillation, reclaims dichloromethane/absolute ethyl alcohol mixed solution, 10 40 DEG C of system temperature, the 0.07Mpa of vacuum 0.01, time for adding was at 0.5 2 hours, shear rate is 5000 10000r/min, continues vacuum distillation 2 hours after completion of dropping；（4）Spray drying.The present invention can reduce sensitivity of the marbofloxacin to light, extend drug effect, cover bad smell, increase solubility, and can easily prepare various preparations, and such as powder, tablet, capsule, controlled release agent are conducive to the medication of animal.
Description
Technical field
The present invention relates to a kind of marbofloxacin micro-capsule and preparation method thereof, belong to field of veterinary medicine preparation.
Background technology
Marbofloxacin is another third generation quinoline promise after Enrofloxacin, Danofloxacin, sarafloxacin, Difloxacin
Ketone animal specific antibacterials.It is main by suppressing bacterial topoisomerase activity and antibacterial.Marbofloxacin is earliest by Switzerland
Roche Holding Ag formulates, and Vetoquinol companies further develop, and is listed first in Britain in nineteen ninety-five, then in succession in method
State, US and European listing.Marbofloxacin has a broad antifungal spectrum, sterilizing power is strong, has stronger work to Gram-negative and positive bacteria
Property, or even it is effective to some moulds and anaerobic bacteria.Tissue infiltration power is strong, and its body absorption is rapid complete and widely distributed, disappears
Except long half time, bioavilability is close to 100%；Safe-dosaging limits are wide, with other antibacterials without cross resistance, without substantially raw
Grow and genetoxic.These all determine its preventing and treating livestock and poultry infection in respiratory system, urinary system infection contamination, digestive system infection,
Great potential in terms of superficial or deep skin tissue infection, eyes and ear infections, is animal specific fluorine quinoline promise of new generation
Ketone antimicrobial.At present, USA and EU can be ratified to be used for 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 FQNS, to light is more sensitive, dissolubility is poor and there is certain smell, no
Beneficial to the medication of animal.But the current medicine preparation variety is single, and the injection and solution of predominantly its lactic acid or hydrochloride are oral
Agent, and application field is narrow, is mainly used in pet.Also there is the technical barrier that cost is high, quality control is difficult simultaneously.
Starch Sodium Octenyl Succinate has been widely used for liposoluble vitamin embedding as a kind of New Wall Material, pungent
When starch alkenyl succinate sodium embeds grease as wall material, entrapment principle is the hydrophobic grouping insertion oil of sodium octenyl succinate
Phase, sodium carboxylate groups' insertion aqueous phase, starch group reaches embedding effect in one layer of intensity of oil-water interfaces formation very big film.
But because marbofloxacin solubility property it is extremely special, its state be solid, and marbofloxacin in grease solubility compared with
It is low.Limit marbofloxacin formulation development and application.Solvent-applied of the present invention dissolves marbofloxacin, by solvent under high speed shear
Aqueous phase is added to, in evaporation solvent simultaneously, separates out marbofloxacin particulate, while starch Sodium Octenyl Succinate is by marbofloxacin
Particulate embeds to form micro-capsule, can reduce sensitivity of the marbofloxacin to light, extends drug effect, covers bad smell, increases solubility,
And various preparations can be easily prepared, such as powder, tablet, capsule, controlled release agent are conducive to the medication of animal.
The content of the invention
In order to solve marbofloxacin embedding problem, the invention provides a kind of using starch Sodium Octenyl Succinate as wall material
Marbofloxacin micro-capsule and preparation method thereof, by the way that wall material, core are emulsified, water-soluble micro-capsule powder is made in spray drying, can be with
Sensitivity of the marbofloxacin to light is reduced, extends drug effect, bad smell is covered, increases solubility, and can easily prepare
Various preparations, such as powder, tablet, capsule, controlled release agent, are conducive to the medication of animal.
To reach above-mentioned purpose, the present invention is achieved by the following technical solutions：
A kind of marbofloxacin micro-capsule, is made up of the component of following mass percent：Formed sediment as the ocentyl succinic of wall material
The powder sodium 40-99% and marbofloxacin 1-60% as core.
A kind of preparation method of marbofloxacin micro-capsule, comprises the following steps：
（1）Prepare wall material solution：Starch Sodium Octenyl Succinate is dissolved in purified water, concentration is configured to for 10-30%
Solution；
（2）Prepare core material solution：Marbofloxacin is dissolved in dichloromethane/absolute ethyl alcohol mixed solution, is configured to dense
Spend the solution for 20%-50%；
（3）Emulsification and vacuum distillation：Under the conditions of high speed shear, to step（1）It is slowly added dropwise in obtained wall material solution
Step（2）Obtained core material solution, while carrying out vacuum distillation, reclaims dichloromethane/absolute ethyl alcohol mixed solution, system temperature
10-40 DEG C, vacuum 0.01-0.07Mpa, time for adding was at 0.5-2 hours, and shear rate is 5000-10000r/min, was added dropwise
Continue vacuum distillation 2 hours after finishing；
（4）Spray drying：It is spray-dried at 180-220 DEG C of EAT, 80-120 DEG C of leaving air temp.
The step（2）In dichloromethane and absolute ethyl alcohol volume ratio be 6:4-19:1.
Beneficial effects of the present invention are as follows：
Using microencapsulation micro-capsule is made in water-insoluble marbofloxacin embedding by the present invention, and embedding wall material used is pungent
Starch alkenyl succinate sodium, by the addition of auxiliary agent dichloromethane/absolute ethyl alcohol, allows marbofloxacin to be embedded, by medicine
Spray drying after wall material is embedded in, instant micro-capsule powder is formed.
Present invention process is simple, and with low cost, gained marbofloxacin micro-capsule powder can reduce marbofloxacin to the quick of light
Sense, extends drug effect, covers bad smell, increases solubility, and can easily prepare various preparations, such as powder, tablet, glue
Wafer, controlled release agent etc., are conducive to the medication of animal.
Embodiment
With reference to specific embodiment, the present invention is further illustrated, but protection scope of the present invention is not limited to
This.
Involved all raw materials and auxiliary agent can be synthesized using mode well known in the art in the present invention, can also be adopted
Use 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 molten
Solution is in dichloromethane/absolute ethyl alcohol（Ratio is 9：1）In mixed solution, the core material solution that concentration is 20% is configured to.In 5000r/
Under min shear rates, core material solution is slowly added dropwise into wall material solution, while vacuum distillation is carried out, recovery dichloromethane/anhydrous
Alcohol mixed solution, 10 DEG C of system temperature, vacuum 0.07Mpa, time for adding continues to depressurize at 2 hours, after completion of dropping to be steamed
Evaporate 2 hours.LS is dried, 180 DEG C of EAT, 80 DEG C of leaving air temp.
It is faint yellow, good fluidity that powdered oil outward appearance, which is made, meets water dissolving.
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 molten
Solution is in dichloromethane/absolute ethyl alcohol（Ratio is 3：2）In mixed solution, the core material solution that concentration is 50% is configured to.
Under 10000r/min shear rates, core material solution is slowly added dropwise into wall material solution, while carrying out vacuum distillation, dichloromethane is reclaimed
Alkane/absolute ethyl alcohol mixed solution, 40 DEG C of system temperature, vacuum 0.01Mpa, time for adding was at 0.5 hour, and completion of dropping is follow-up
Continuous vacuum distillation 2 hours.LS is dried, 220 DEG C of EAT, 120 DEG C of leaving air temp.
It is faint yellow, good fluidity that powdered oil outward appearance, which is made, meets water dissolving.
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 molten
Solution is in dichloromethane/absolute ethyl alcohol（Ratio is 19：3）In mixed solution, the core material solution that concentration is 35% is configured to.
Under 7500r/min shear rates, core material solution is slowly added dropwise into wall material solution, while carrying out vacuum distillation, dichloromethane is reclaimed
Alkane/absolute ethyl alcohol mixed solution, 25 DEG C of system temperature, vacuum 0.04Mpa, time for adding was at 1.25 hours, after completion of dropping
Continue vacuum distillation 2 hours.LS is dried, 200 DEG C of EAT, 100 DEG C of leaving air temp.
It is faint yellow, good fluidity that powdered oil outward appearance, which is made, meets water dissolving.
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 molten
Solution is in dichloromethane/absolute ethyl alcohol（Ratio is 7：2）In mixed solution, the core material solution that concentration is 45% is configured to.In 9000r/
Under min shear rates, core material solution is slowly added dropwise into wall material solution, while vacuum distillation is carried out, recovery dichloromethane/anhydrous
Alcohol mixed solution, 15 DEG C of system temperature, vacuum 0.05Mpa, time for adding continues to depressurize at 1.5 hours, after completion of dropping
Distillation 2 hours.LS is dried, 190 DEG C of EAT, 90 DEG C of leaving air temp.
It is faint yellow, good fluidity that powdered oil outward appearance, which is made, meets water dissolving.
Marbofloxacin micro-capsule by wall material of starch Sodium Octenyl Succinate of the present invention and preparation method thereof, by by wall
Material, core are emulsified, spray drying, and water-soluble micro-capsule powder is made, and can reduce sensitivity of the marbofloxacin to light, extend drug effect,
Bad smell is covered, increases solubility, and can easily prepare various preparations, such as powder, tablet, capsule, slow control
Agent etc. is released, is conducive to the medication of animal.
Above-described embodiment is only used for illustrating the inventive concept of the present invention, rather than the restriction to rights protection of the present invention,
All changes for carrying out unsubstantiality to the present invention using this design, all should fall into protection scope of the present invention.
Claims (2)
1. a kind of marbofloxacin micro-capsule, it is characterised in that be made up of the component of following mass percent：It is used as the octenyl of wall material
The succinic acid starch sodium 40-99% and marbofloxacin 1-60% as core；
The preparation method of the marbofloxacin micro-capsule comprises the following steps：
（1）Prepare wall material solution：Starch Sodium Octenyl Succinate is dissolved in purified water, it is the molten of 10-30% to be configured to concentration
Liquid；
（2）Prepare core material solution：Marbofloxacin is dissolved in dichloromethane/absolute ethyl alcohol mixed solution, being configured to concentration is
20%-50% solution；
（3）Emulsification and vacuum distillation：Under the conditions of high speed shear, to step（1）Step is slowly added dropwise in obtained wall material solution
（2）Obtained core material solution, while carrying out vacuum distillation, reclaims dichloromethane/absolute ethyl alcohol mixed solution, system temperature 10-
40 DEG C, vacuum 0.01-0.07Mpa, time for adding was at 0.5-2 hours, and shear rate is 5000-10000r/min, is dripped
Continue vacuum distillation 2 hours after finishing；
（4）Spray drying：It is spray-dried at 180-220 DEG C of EAT, 80-120 DEG C of leaving air temp.
2. marbofloxacin micro-capsule as claimed in claim 1, it is characterised in that：The step（2）In dichloromethane and anhydrous second
The volume ratio of alcohol is 6:4-19:1.
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| Application Number | Priority Date | Filing Date | Title |
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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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| CN201510120102.1A CN104706621B (en) | 2015-03-19 | 2015-03-19 | A kind of marbofloxacin micro-capsule and preparation method thereof |
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| CN104706621A CN104706621A (en) | 2015-06-17 |
| CN104706621B true CN104706621B (en) | 2017-08-15 |
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Families Citing this family (1)
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| CN110141558A (en) * | 2019-05-29 | 2019-08-20 | 四川农业大学 | A kind of preparation method of marbofloxacin nanoparticle |
Citations (2)
| 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 |
| 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 |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2010143186A1 (en) * | 2009-06-08 | 2010-12-16 | Otic Pharma Ltd. | Otic foam formulations |
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2015
- 2015-03-19 CN CN201510120102.1A patent/CN104706621B/en active Active
Patent Citations (2)
| 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 |
| 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 |
|---|
| 恩诺沙星微囊的制备及急性毒性试验;卢素云，等;《动物医学进展》;20141231;第35卷(第12期);第99-103页 * |
| 诺氟沙星微囊的研制;张秀荣，等;《沈阳药科大学学报》;20000731;第17卷(第4期);第247-249页 * |
| 辛烯基琥珀酸淀粉微胶囊化浓缩鱼油的研究;吴克刚，等;《食品研究与开发》;20060331;第27卷(第3期);第4-6页 * |
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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. |
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