CN101843586A - Water-soluble micro powder containing florfenicol and preparation method thereof - Google Patents
Water-soluble micro powder containing florfenicol and preparation method thereof Download PDFInfo
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- CN101843586A CN101843586A CN 201010160013 CN201010160013A CN101843586A CN 101843586 A CN101843586 A CN 101843586A CN 201010160013 CN201010160013 CN 201010160013 CN 201010160013 A CN201010160013 A CN 201010160013A CN 101843586 A CN101843586 A CN 101843586A
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Abstract
The invention discloses a water-soluble micro powder containing florfenicol and a preparation method thereof. The micro powder is prepared from the following raw materials in percentage by weight: 5 to 10 percent of florfenicol, 2.5 to 2.75 percent of PVPK30, 2.5 to 2.75 percent of SDS and the balance anhydrous glucose. PVPK30, SDS and florfenicol are mixed uniformly, crushed, pass through a 150mesh screen, and then are added with the anhydrous glucose to be mixed uniformly. The micro powder also can be combined with other medicines to prepare water-soluble compound florfenicol micro powder. The grain size of the florfenicol through micro powder treatment is finer and more uniform, so the surface area is increased, the porosity is increased, the absorbability and the solubility are improved, the medicines can be well dispersed and dissolved in gastric juice, the contact area with gastric mucosa is enlarged, so that the medicines can be absorbed by the gastrointestinal tract more easily, thereby greatly improving the bioavailability. The preparation method is more convenient than a coating process, and is more applicable to large-scale production.
Description
Technical field
The present invention relates to a kind of water-soluble micropowder that contains florfenicol and preparation method thereof, belong to the veterinary drug technical field.
Background technology
Florfenicol (Florfenicol) Chinese: fluprofen, florfenicol, Florfenicol, it is the broad spectrum antibiotic of the special-purpose chloromycetin of a kind of new veterinary successfully developed in the late nineteen eighties, nineteen ninety goes on the market in Japan first, Norway in 1993 ratify the furunculosis of this medicine treatment salmon, nineteen ninety-five France, Britain, Austria, Mexico and Spain's approval be used for the treatment of cattle respiratory system bacterial disease.Also ratify feed additive as pig in Japan and Mexico, prevention and the bacterial disease (Qiu Yinsheng etc., 1996) for the treatment of pig, China has passed through examining of this medicine at present.Florfenicol all has the excellent antibiotic effect to poultry gram positive bacteria and gram negative bacteria, is the choice drug of bacterial diseases such as treatment avian typhoid, paratyphoid fever.The prodrug chloromycetin of florfenicol bans use of in food animal at present owing to can cause very serious aplastic anemia.As for animals special-purpose antibacterials few in number, florfenicol has a wide range of applications, but because its poorly water-soluble, this uses inconvenience medicine in the large-scale cultivation field, its use is had very big restriction.
The present hydrotropy method that adopts; owing to adopt very complicated production technology; cause use cost to increase; be not suitable for the large-scale cultivation field; and present hydrotropy method causes this rate of release in intestinal of florfenicol slack-off, because the birds digestive system is short, medicine is shorter through the used time ratio of whole system; the absorption and the effect of medicine are reduced, cause the waste of medicine.
Summary of the invention
The present invention's first purpose provides a kind of water-soluble micropowder that contains florfenicol, improves absorption and the blood drug level of florfenicol at digestive system, strengthens the therapeutic effect of florfenicol.Its granularity of florfenicol behind micropowder is trickleer, even, therefore surface area increases, porosity increases, adsorptivity and dissolubility strengthen, medicine can disperse preferably, be dissolved in the gastric juice, the contact area of increase and gastric mucosa, thus easier in gastrointestinal absorption, improved bioavailability greatly.Another object of the present invention provides a kind of water-soluble micropowder preparing process that contains florfenicol, and the method is more convenient by technology than bag, is more suitable in large-scale production.
Technical scheme of the present invention is: a kind of water-soluble micropowder that contains florfenicol, it is characterized in that, and make by following raw material by weight percentage, florfenicol 5-10%, PVPK30 2.5-2.75%, SDS2.5-2.75%, all the other are anhydrous glucose.
The further technical scheme of the present invention is: a kind of water-soluble micropowder that contains florfenicol, it is characterized in that, and make by following raw material by weight percentage, florfenicol 5%, PVPK30 2.5%, and SDS 2.5%, anhydrous glucose 90%.
The PVPK30 chemical name is polyvinylpyrrolidone K30, and white is to off-white powder; Odorless or have special smellyly, tasteless slightly has hygroscopicity.This product is dissolved in water, ethanol, isopropyl alcohol or chloroform, and is insoluble in acetone or ether, and the solution viscosity below 10% is identical with water base.This product has characteristic and effects such as bonding, thickening, suspending, dispersion, complexation, film forming, is used as thickening agent, suspending agent, dispersant, chelating agent etc. in medicament.
The SDS chemical name is a sodium lauryl sulphate, is white or yellowish crystallization thin slice or powder, have slight special smelly, similar fat, bitter in the mouth, soluble in water.Be partially soluble in ethanol, be insoluble to chloroform, ether and petroleum ether.Critical micelle concentration (20 ℃) is 8.2 * 10
-3Mol/L.Relative density is 1.07, and HLB is 40, and interfacial tension is 11.8mN/m.This product is an anion surfactant, has effects such as emulsifying, de-sludging, dispersion, moistening, foaming, and is all effective in acid, alkaline solution and hard water.
PVPK30, SDS all play solubilising and hydrotropy effect in the present invention.
The above-mentioned water-soluble micropowder preparation method that contains florfenicol is: with PVPK30, SDS, florfenicol mix homogeneously, pulverize, cross 150 mesh sieves, and then add anhydrous glucose, mix homogeneously.
The present invention also provides a kind of water solublity compound florfenicol micropowder, it is characterized in that, is mainly made by florfenicol, PVPK30, SDS and anhydrous glucose.
The further technical scheme of the present invention is: a kind of water solublity compound florfenicol micropowder, it is characterized in that, and make by following raw material by weight percentage, florfenicol 5%, PVPK30 2.5%, and SDS 2.5%, quinolones 5%, anhydrous glucose 85%.With florfenicol, PVPK30, SDS and quinolones mix homogeneously, pulverize, cross 150 mesh sieves, add the anhydrous glucose mix homogeneously.Described quinolones can be norfloxacin, ofloxacin, levofloxacin, pefloxacin, enoxacin, cinoxacin etc.This compound recipe adds quinolones on the basis of the highly dissoluble of the water-soluble micropowder that keeps containing florfenicol and rate of release, play the effect of Synergistic, and the antibacterial activity of two kinds of medicines is strengthened.
Technical scheme of the present invention is: a kind of water solublity compound florfenicol micropowder, it is characterized in that, and make by following raw material by weight percentage, florfenicol 5%, PVPK30 2.5%, and SDS 2.5%, Bisolvon 5%, enrofloxacin sodium 7%, anhydrous glucose 78%.With florfenicol, PVPK30, SDS, Bisolvon, enrofloxacin sodium mix homogeneously, pulverize, cross 150 mesh sieves, add the anhydrous glucose mix homogeneously.This compound recipe is on the basis of the highly dissoluble of the water-soluble micropowder that keeps containing florfenicol and rate of release, add Bisolvon and enrofloxacin sodium, make it not only have antibacterial functions, and have function of relieving cough and calming asthma, quicken the rehabilitation of respiratory tract infection.
Technical scheme of the present invention is: a kind of water solublity compound florfenicol micropowder, it is characterized in that, and make by following raw material by weight percentage, florfenicol 5%, PVPK30 2.5%, and SDS 2.5%, sulfamonomethoxine sodium 10%, doxycycline pulverizes 5%, anhydrous glucose 75%.With florfenicol, PVPK30, SDS, sulfamonomethoxine sodium, doxycycline mix homogeneously, pulverize, cross 150 mesh sieves, add the anhydrous glucose mix homogeneously.This compound recipe adds sulfamonomethoxine sodium and doxycycline on the basis of the highly dissoluble of the water-soluble micropowder that keeps containing florfenicol and rate of release, make it not only have antibacterial functions, and Eperythrozoon and the toxoplasma that can treat pig infect.
Technical scheme of the present invention is: a kind of water solublity compound florfenicol micropowder, it is characterized in that, and make by following raw material by weight percentage, florfenicol 5%, PVPK30 2.5%, and SDS 2.5%, methanesulfonic acid Gatifloxacin 5%, ambroxol hydrochloride 5%, anhydrous glucose 80%.With florfenicol, PVPK30, SDS, methanesulfonic acid Gatifloxacin, ambroxol hydrochloride mix homogeneously, pulverize, cross 150 mesh sieves, add the anhydrous glucose mix homogeneously.This compound recipe adds methanesulfonic acid Gatifloxacin and ambroxol hydrochloride on the basis of the highly dissoluble of the water-soluble micropowder that keeps containing florfenicol and rate of release, strengthened the antibacterial action of florfenicol and the effect of treatment respiratory tract infection.
The further technical scheme of the present invention is: a kind of water solublity compound florfenicol micropowder, it is characterized in that, and make by following raw material by weight percentage, florfenicol 5%, PVPK30 2.5%, and SDS 2.5%, berberine hydrochloride 10%, anhydrous glucose 80%.With florfenicol, PVPK30, SDS and berberine hydrochloride mix homogeneously, pulverize, cross 150 mesh sieves, add anhydrous glucose and be mixed and made into.This compound recipe adds berberine hydrochloride on the basis of the highly dissoluble of the water-soluble micropowder that keeps containing florfenicol and rate of release, strengthened the therapeutic effect of florfenicol to intestinal infection.
Beneficial effect of the present invention: present technique adopts PVPK30, SDS as surfactant, superfine grinding method makes the water-soluble micropowder that contains florfenicol, make the florfenicol granularity be reduced to 90um by original 250um, dissolubility is increased to 5% by original 0.01%, and rate of release is 99.12% to be florfenicol powder (rate of release 30.25%) and former powder (rate of release 2.3%) 3.27 times and 43.1 times.This preparation method is that a kind of method is simple, cost is low and can improves the hydrotropy method of the rate of release of medicine own.
The specific embodiment
The present invention will be further described below in conjunction with specific embodiment.
Embodiment 1:
As produce water-soluble micropowder that 100kg contains florfenicol, and the 5kg florfenicol, 2.5kgPVPK30,2.5kg SDS, mix homogeneously is pulverized, and crosses 150 mesh sieves, and the anhydrous glucose that adds 90kg mixes, and equivalent increases progressively mix homogeneously and makes.This water-soluble micropowder that contains florfenicol is as follows to the influence of broiler:
1, experimental animal:
Picked at random is suffered from 90 of colibacillosis broiler, is divided into 3 groups at random, and 30 every group, body weight is at 1～2kg.
2, experiment medicine:
The water-soluble micropowder that contains florfenicol of the embodiment of the invention 1 preparation;
5% florfenicol powder: the quality percentage composition is 5% florfenicol, the quality percentage composition be 95% starch mix homogeneously promptly.
3, experimental technique:
1 group is the blank group, without medicine.
2 group of 5% florfenicol powder treated usage: 100g florfenicol powder (5%) spice 50kg, once-a-day, concentrate to use up logotype 4 days in 3 hours.
3 groups contain water-soluble micropowder of florfenicol with the present invention, and usage: 100g converts water 100kg, once-a-day, concentrates to use up logotype 4 days in 3 hours.
After the treatment beginning, write down disease fowl mental condition and dead the distribution every day, treat and add up therapeutic effect after 4 days, wherein.
Invalid: after referring to 4 days, sick fowl symptom has the situation of increasing the weight of or death.
Effectively: after referring to 4 days, sick fowl symptom changes, and symptom is controlled or with respect to having obviously and alleviate before the treatment.
Cure: after referring to 4 days, transference cure, the sick fowl mental status and feed intake are recovered normal condition.Its digital packets is contained in the significant digits.
Symptom is arranged during end: after referring to treat 4 days, sick fowl still has certain symptom, and the performance of its symptom is better than before the treatment or does not have change, and sick fowl is cured fully, and its numeral has been included in the numeral of invalid number of elements and effective number of elements.
Result of the test is as shown in table 1:
Table 1: each organizes therapeutic effect
| Numbering | Group | Invalid number of elements | Effective number of elements | Cure number of elements | The symptom number of elements is arranged during end |
| 1 group | Matched group | ??30 | ??0 | ??0 | ??30 |
| Numbering | Group | Invalid number of elements | Effective number of elements | Cure number of elements | The symptom number of elements is arranged during end |
| 2 groups | 5% florfenicol powder | ??8 | ??22 | ??12 | ??18 |
| 3 groups | The water-soluble micropowder that contains florfenicol | ??2 | ??28 | ??27 | ??3 |
4, conclusion:
Analyze by statistics from the result of the test of table 1, water-soluble micropowder, 5% florfenicol treated powder group and the matched group difference that contains florfenicol is (P＜0.01) extremely significantly.Treatment of the present invention is better than existing powder.
Embodiment 2:
As produce 100kg water solublity compound florfenicol micropowder, and the 5kg florfenicol, 2.5kg PVPK30,2.5kgSDS, 5kg quinolones (norfloxacin), mix homogeneously is pulverized, and crosses 150 mesh sieves, and the anhydrous glucose that adds 85kg is mixed and made into.
Embodiment 3:
As produce water-soluble micropowder that 100kg contains florfenicol, and the 10kg florfenicol, 2.6kgPVPK30,2.6kg SDS, mix homogeneously is pulverized, and crosses 150 mesh sieves, and the anhydrous glucose that adds 84.8kg mixes, and equivalent increases progressively mix homogeneously and makes.
Embodiment 4:
As produce water-soluble micropowder that 100kg contains florfenicol, and the 8kg florfenicol, 2.75kgPVPK30,2.75kg SDS, mix homogeneously is pulverized, and crosses 150 mesh sieves, and the anhydrous glucose that adds 86.5kg mixes, and equivalent increases progressively mix homogeneously and makes.
Embodiment 5:
As produce 100kg water solublity compound florfenicol micropowder, and the 5kg florfenicol, 2.5kg PVPK30,2.5kgSDS, the 5kg Bisolvon, 7kg enrofloxacin sodium mix homogeneously is pulverized, and crosses 150 mesh sieves, and the anhydrous glucose that adds 78kg is mixed and made into.
Embodiment 6:
As produce 100kg water solublity compound florfenicol micropowder, and the 5kg florfenicol, 2.5kg PVPK30,2.5kgSDS, the 10kg sulfamonomethoxine sodium, 5kg doxycycline mix homogeneously is pulverized, and crosses 150 mesh sieves, and the anhydrous glucose that adds 75kg is mixed and made into.
Embodiment 7:
As produce 100kg water solublity compound florfenicol micropowder, and the 5kg florfenicol, 2.5kg PVPK30,2.5kgSDS, 5kg methanesulfonic acid Gatifloxacin, 5kg ambroxol hydrochloride mix homogeneously is pulverized, and crosses 150 mesh sieves, and the anhydrous glucose that adds 80kg is mixed and made into.
Embodiment 8:
As produce 100kg water solublity compound florfenicol micropowder, and the 5kg florfenicol, 2.5kg PVPK30,2.5kgSDS, 10kg berberine hydrochloride mix homogeneously is pulverized, and crosses 150 mesh sieves, and the anhydrous glucose that adds 80kg is mixed and made into.
Claims (9)
1. a water-soluble micropowder that contains florfenicol is characterized in that, make by following raw material by weight percentage, and florfenicol 5-10%, PVPK30 2.5-2.75%, SDS 2.5-2.75%, all the other are anhydrous glucose.
2. a kind of water-soluble micropowder that contains florfenicol as claimed in claim 1 is characterized in that, makes by following raw material by weight percentage, and florfenicol 5%, PVPK30 2.5%, and SDS 2.5%, anhydrous glucose 90%.
3. claim 1 or the 2 described water-soluble micropowder preparation methoies that contain florfenicol is characterized in that, with PVPK30, SDS, florfenicol mix homogeneously, pulverize, and cross 150 mesh sieves, and then add anhydrous glucose, mix homogeneously.
4. a water solublity compound florfenicol micropowder is characterized in that, is mainly made by florfenicol, PVPK30, SDS and anhydrous glucose.
5. a kind of water solublity compound florfenicol micropowder as claimed in claim 4 is characterized in that, makes by following raw material by weight percentage, and florfenicol 5%, PVPK30 2.5%, and SDS 2.5%, quinolones 5%, anhydrous glucose 85%.
6. a kind of water solublity compound florfenicol micropowder as claimed in claim 4 is characterized in that, is made by following raw material by weight percentage, florfenicol 5%, PVPK30 2.5%, and SDS 2.5%, Bisolvon 5%, enrofloxacin sodium 7%, anhydrous glucose 78%.
7. a kind of water solublity compound florfenicol micropowder as claimed in claim 4 is characterized in that, is made by following raw material by weight percentage, florfenicol 5%, PVPK30 2.5%, and SDS 2.5%, sulfamonomethoxine sodium 10%, doxycycline pulverizes 5%, anhydrous glucose 75%.
8. a kind of water solublity compound florfenicol micropowder as claimed in claim 4 is characterized in that, is made by following raw material by weight percentage, florfenicol 5%, PVPK30 2.5%, and SDS 2.5%, methanesulfonic acid Gatifloxacin 5%, ambroxol hydrochloride 5%, anhydrous glucose 80%.
9. a kind of water solublity compound florfenicol micropowder as claimed in claim 4 is characterized in that, makes by following raw material by weight percentage, and florfenicol 5%, PVPK30 2.5%, and SDS 2.5%, berberine hydrochloride 10%, anhydrous glucose 80%.
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| CN102429918A (en) * | 2011-11-02 | 2012-05-02 | 南京威泰珐玛兽药研究所有限公司 | Medicinal composition containing florfenicol and tea saponin and preparation method thereof |
| CN102697730A (en) * | 2012-05-07 | 2012-10-03 | 郑州后羿制药有限公司 | Florfenicol soluble power and preparation method thereof |
| CN102885777A (en) * | 2012-10-25 | 2013-01-23 | 上海邦森生物科技有限公司 | Efficient florfenicol powder composition and preparation method thereof |
| CN103127019A (en) * | 2013-03-22 | 2013-06-05 | 成都乾坤动物药业有限公司 | Florfenicol dispersible tablet as well as preparation method and application thereof |
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| CN105213315A (en) * | 2015-10-12 | 2016-01-06 | 河南新正好生物工程有限公司 | A kind of florfenicol soluble powder and preparation method thereof |
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| CN108524451A (en) * | 2018-05-02 | 2018-09-14 | 安徽安丰堂动物药业有限公司 | A kind of environment-friendly high-efficiency technique of veterinary drug Florfenicol |
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| CN105343882B (en) * | 2015-11-19 | 2019-01-25 | 河北普德动物药业有限公司 | A kind of Florfenicol synergy wettable powder and preparation method thereof |
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| CN106176615A (en) * | 2016-08-30 | 2016-12-07 | 天津市中升挑战生物科技有限公司 | A kind of Bisolvon soluble powder and preparation method and application |
| CN108658817A (en) * | 2018-03-14 | 2018-10-16 | 广东润华药业有限公司 | A kind of preparation method of Florfenicol nanocrystal |
| CN108524451A (en) * | 2018-05-02 | 2018-09-14 | 安徽安丰堂动物药业有限公司 | A kind of environment-friendly high-efficiency technique of veterinary drug Florfenicol |
| CN109172528A (en) * | 2018-10-30 | 2019-01-11 | 河南后羿实业集团有限公司 | A kind of florfenicol soluble powder and preparation method thereof |
| CN109553556A (en) * | 2018-12-31 | 2019-04-02 | 京山瑞生制药有限公司 | A kind of novel processing step preparing Florfenicol crystal |
| CN109851536A (en) * | 2018-12-31 | 2019-06-07 | 京山瑞生制药有限公司 | A method of preparing Florfenicol |
| CN110279663A (en) * | 2019-08-02 | 2019-09-27 | 四川恒通动物制药有限公司 | A kind of adhesion type Florfenicol pre-mixing agent and preparation method thereof |
| CN112076160A (en) * | 2020-10-29 | 2020-12-15 | 四川欧邦生物科技有限公司 | Preparation method of florfenicol soluble powder |
| CN114272213A (en) * | 2021-12-28 | 2022-04-05 | 厦门惠盈动物药业有限公司 | Florfenicol powder and preparation method thereof |
| CN114272213B (en) * | 2021-12-28 | 2023-10-10 | 厦门惠盈动物药业有限公司 | Florfenicol powder and preparation method thereof |
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