CN103768025B - Florfenicol sodium succinate soluble powder and its preparation method and application - Google Patents
Florfenicol sodium succinate soluble powder and its preparation method and application Download PDFInfo
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- CN103768025B CN103768025B CN201410046428.XA CN201410046428A CN103768025B CN 103768025 B CN103768025 B CN 103768025B CN 201410046428 A CN201410046428 A CN 201410046428A CN 103768025 B CN103768025 B CN 103768025B
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- sodium succinate
- soluble powder
- florfenicol
- florfenicol sodium
- polyethylene glycol
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Abstract
The invention provides a kind of florfenicol sodium succinate soluble powder and its preparation method and application, technical scheme: a kind of florfenicol sodium succinate soluble powder, this soluble powder comprises the component of following mass percent, florfenicol sodium succinate 5%-30%, stabilizing agent 1%-10%, Polyethylene Glycol 10%-50%, all the other are correctives.This soluble powder improves stability and the bioavailability of florfenicol sodium succinate, is convenient to clinical administration.Present invention also offers preparation method, solve and still do not have suitable florfenicol sodium succinate form of medication clinically, be difficult to give full play to drug effect, Clinical practice is inconvenient, is difficult to the problem promoted the use of.
Description
Technical field
The invention belongs to veterinary drug technical field, specifically, relate to a kind of florfenicol sodium succinate soluble powder and its preparation method and application.
Background technology
Florfenicol (Florfenicol) has another name called fluprofen, Florfenicol, it is the broad spectrum antibiotic of a kind of new special chloromycetin of veterinary successfully developed in the late nineteen eighties in last century, nineteen ninety goes on the market in Japan first, Norway in 1993 ratifies the furunculosis of this medicine treatment salmon, nineteen ninety-five France, Britain, Austria, Mexico and Spain ratifies to be used for the treatment of cattle respiratory system bacterial disease.Also ratify in Japan and Mexico the feed additive being used as pig, the bacterial disease (Qiu Yinsheng etc., 1996) of prevention and therapy pig, China have passed the examination & approval of this medicine at present, is approved for pig, cattle, chicken, the bacterial infection of fish.
The dosage form of florfenicol has powder, pre-mixing agent, solution, and injection.But florfenicol dissolubility in water is very low, limits drinking water administration, solution is poured into water easily to separate out blocks pipeline.Cannot solve medicine by common formulation method is insoluble in water problem at present, now domesticly at present develop florfenicol sodium succinate, water solublity is fine, through experimental study, florfenicol sodium succinate dissolubility in water is greater than 50g, antibacterial activity is more weak in vitro, change into florfenicol more rapidly in vivo, in rat body, carry out experiment find, florfenicol sodium succinate to staphylococcus aureus, bacillus subtilis, Bacillus proteus, dust Xi Shi escherichia coli have good inhibition, have played good antibacterial action.
The structure formula I of florfenicol sodium succinate is as follows:
（Ⅰ）
At present, florfenicol sodium succinate is in initial conceptual phase, does not still have suitable form of medication clinically, is difficult to give full play to drug effect, and Clinical practice is inconvenient, is difficult to promote the use of.So need the novel form developing florfenicol sodium succinate, be convenient to Clinical practice, storage and transport.
Summary of the invention
The invention provides a kind of florfenicol sodium succinate soluble powder and its preparation method and application, current florfenicol sodium succinate Clinical practice can be solved inconvenient, be difficult to the problem promoted the use of.This soluble powder improves stability and the bioavailability of florfenicol sodium succinate, is convenient to clinical administration.
For solving the problems of the technologies described above, the present invention is achieved by the following technical solutions:
A kind of florfenicol sodium succinate soluble powder, this soluble powder comprises the component of following mass percent, florfenicol sodium succinate 5%-30%, stabilizing agent 1%-10%, Polyethylene Glycol 10%-50%, and all the other are correctives.
Florfenicol sodium succinate soluble powder described above, described Polyethylene Glycol adopt in Macrogol 4000, polyethylene glycol 6000, PEG 8000, Polyethylene Glycol 12000 one or more.
Florfenicol sodium succinate soluble powder described above, described stabilizing agent is selected from: one or more in anhydrous calcium chloride, anhydrous sodium sulfate, anhydrous magnesium sulfate.
Florfenicol sodium succinate soluble powder described above, described correctives is selected from: glucose, sucrose, lactose, one or more in fructose.
The preparation method additionally providing florfenicol sodium succinate (having another name called florfenicol sodium succinate) soluble powder of the present invention, adopt following steps: each component of getting formula ratio, by florfenicol sodium succinate and Polyethylene Glycol Hybrid Heating until Polyethylene Glycol melts, then cooling curing, upper step gained solid, stabilizing agent, correctives pulverize and sieve respectively, then mix, subpackage can obtain florfenicol sodium succinate soluble powder.
Optimum condition is florfenicol sodium succinate and Polyethylene Glycol mixing post-heating to 60 ~ 100 DEG C, crosses grit number at 65 order to 150 orders.
Preparation method of the present invention, improves stability and the bioavailability of florfenicol sodium succinate, is convenient to clinical administration.
Florfenicol sodium succinate soluble powder of the present invention is used for the treatment of the bacteriological infection that sensitive organism causes.The clinical trial carried out in Qingdao, Shandong Province Laixi City plant shows that florfenicol sodium succinate of the present invention is good to chicken colibacillosis therapeutic effect.
The present invention compared with prior art, has following advantage:
(1) florfenicol sodium succinate soluble powder quality of the present invention is high, and soluble powder prepared by single impurity or the same commonsense method of total impurities (florfenicol sodium succinate+glucose) is compared much lower, and therefore drug effect is high, and adverse reaction rate is low.
(2), not easily there is the moisture absorption during storage in florfenicol sodium succinate soluble powder good stability of the present invention, and caking and metachromatism, substantially increase stability, outward appearance is good.
Therefore, prescription of the present invention and preparation method advanced person.
Detailed description of the invention
Below by specific embodiment, the present invention is described further, but embodiment is not used in the scope limiting the present invention and protect.
Embodiment 1
5% florfenicol sodium succinate soluble powder, by florfenicol sodium succinate, anhydrous calcium chloride, polyethylene glycol 6000, glucose forms, and each constituent mass percentage ratio is as follows:
Florfenicol sodium succinate 5%, anhydrous calcium chloride 1%, polyethylene glycol 6000 accounts for 10%, glucose 84%.
Preparation technology: by weight portion be 5 florfenicol sodium succinate and weight portion be 10 polyethylene glycol 6000 Hybrid Heating, be heated to 60 ~ 65 DEG C, cooling curing after melting, then upper step gained solid, the anhydrous calcium chloride of 1 weight portion, the glucose of 84 weight portions were pulverized 65 mesh sieves respectively, mixing, then subpackage and get final product.
Embodiment 2
10% florfenicol sodium succinate soluble powder, by florfenicol sodium succinate, anhydrous sodium sulfate, PEG 8000, sucrose forms, and each constituent mass percentage ratio is as follows:
Florfenicol sodium succinate 10%, anhydrous sodium sulfate 10%, PEG 8000 accounts for 50%, sucrose 30%.
Preparation technology: by weight portion be 10 florfenicol sodium succinate and weight portion be 50 PEG 8000 Hybrid Heating, be heated to 70 ~ 80 DEG C, cooling curing after melting, then upper step gained solid, the anhydrous sodium sulfate of 10 weight portions, the sucrose of 30 weight portions were pulverized 80 mesh sieves respectively, mixing, then subpackage and get final product.
Embodiment 3.
30% florfenicol sodium succinate soluble powder, by florfenicol sodium succinate, anhydrous magnesium sulfate, Polyethylene Glycol 12000, fructose forms, and each constituent mass percentage ratio is as follows:
Florfenicol sodium succinate 30%, anhydrous magnesium sulfate 5%, Polyethylene Glycol 12000 accounts for 50%, fructose 15%.
Preparation technology: by weight portion be 30 florfenicol sodium succinate and weight portion be 50 Polyethylene Glycol 12000 Hybrid Heating, be heated to 90 ~ 100 DEG C, cooling curing after melting, then upper step gained solid, the anhydrous magnesium sulfate of 5 weight portions, the fructose of 15 weight portions were pulverized 150 mesh sieves respectively, mixing, then subpackage and get final product.
Embodiment 4.
10% florfenicol sodium succinate soluble powder, by florfenicol sodium succinate, anhydrous calcium chloride, Macrogol 4000, lactose forms, and each constituent mass percentage ratio is as follows:
Florfenicol sodium succinate 10%, anhydrous calcium chloride 5%, Macrogol 4000 accounts for 30%, lactose 55%.
Preparation technology: by weight portion be 10 florfenicol sodium succinate and weight portion be 30 Macrogol 4000 Hybrid Heating, be heated to 60 ~ 70 DEG C, cooling curing after melting, then upper step gained solid, the anhydrous calcium chloride of 5 weight portions, the lactose of 55 weight portions were pulverized 100 mesh sieves respectively, mixing, then subpackage and get final product.
Florfenicol sodium succinate powder (5% florfenicol sodium succinate+95% glucose prepared by the florfenicol sodium succinate soluble powder (lot number 20120801) of Example 1 and commonsense method, lot number 20120804) carry out accelerated test, experiment condition is temperature 40 DEG C+2 DEG C, humidity 75%+5 DEG C, result is as following table:
Florfenicol sodium succinate soluble powder of the present invention, stability improves greatly, by florfenicol sodium succinate soluble powder of the present invention with only comprise glucose and compare with the common powder of florfenicol sodium succinate, find through accelerated test, its color of florfenicol sodium succinate soluble powder of the present invention is substantially constant, do not have caking phenomenon, and the powder only comprising glucose and florfenicol sodium succinate has obvious caking phenomenon in accelerated test, and darken, caking.In the accelerated test of 6 months, the maximum single impurity of florfenicol sodium succinate soluble powder of the present invention is increased to 0.3% by 0.1%, total impurities is increased to 0.9% by 0.5%, the maximum single impurity of common powder only containing florfenicol sodium succinate and glucose is increased to 2.6% by 0.1%, and total impurities is increased to 5.2% by 0.5%.Florfenicol sodium succinate soluble powder of the present invention is significantly better than the common powder only containing florfenicol sodium succinate and glucose.
Laixi City, Qingdao plant 8000 chickens occur that spirit is depressed, cough, the symptoms such as feces is thin, and diagnosis pathogenic bacterium are escherichia coli, are divided into by chicken group mean two groups to carry out treatment process:
5% florfenicol sodium succinate soluble powder of experimental group embodiment 1, mixed drink: in florfenicol sodium succinate, every 10 grams are watered 100-200kg, are used in conjunction 3.
Drug control group 5% florfenicol powder, mixed feeding: in florfenicol, every 1g spice 10-20kg, 1 day twice, is used in conjunction 3.
Experimental result is as follows:
Florfenicol sodium succinate soluble powder is to chicken colibacillosis therapeutic effect
| Group | Chicken number | Recovery from illness number | Cure rate |
| Experimental group | 4000 | 3928 | 98.2% |
| Drug control group | 4000 | 3892 | 97.3% |
Test above illustrates that florfenicol sodium succinate soluble powder cure rate is higher than florfenicol, effective, thus demonstrates succeeding in developing of a kind of new preparation type.
The above is only preferred embodiment of the present invention, and be not restriction the present invention being made to other form, any those skilled in the art may utilize the technology contents of above-mentioned announcement to be changed or be modified as the Equivalent embodiments of equivalent variations.But everyly do not depart from technical solution of the present invention content, any simple modification, equivalent variations and the remodeling done above embodiment according to technical spirit of the present invention, still belong to the protection domain of technical solution of the present invention.
Claims (4)
1. a florfenicol sodium succinate soluble powder, is characterized in that: this soluble powder comprises the component of following mass percent, florfenicol sodium succinate 5%-30%, stabilizing agent 1%-10%, Polyethylene Glycol 10%-50%, and all the other are correctives; Described stabilizing agent is selected from: one or more in anhydrous calcium chloride, anhydrous sodium sulfate, anhydrous magnesium sulfate; Described Polyethylene Glycol adopt in Macrogol 4000, polyethylene glycol 6000, PEG 8000, Polyethylene Glycol 12000 one or more.
2. florfenicol sodium succinate soluble powder according to claim 1, is characterized in that: described correctives is selected from: glucose, sucrose, lactose, one or more in fructose.
3. the preparation method of florfenicol sodium succinate soluble powder described in a claim 1, it is characterized in that adopting following steps: each component of getting formula ratio, by florfenicol sodium succinate and Polyethylene Glycol Hybrid Heating until Polyethylene Glycol melts, then cooling curing, upper step gained solid, stabilizing agent, correctives pulverize and sieve respectively, then mix, subpackage can obtain florfenicol sodium succinate soluble powder.
4. the preparation method of florfenicol sodium succinate soluble powder according to claim 3, is characterized in that florfenicol sodium succinate and Polyethylene Glycol mixing post-heating to 60 ~ 100 DEG C, crosses grit number at 65 order to 150 orders.
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| CN106420628A (en) * | 2016-09-26 | 2017-02-22 | 保定冀中药业有限公司 | Florfenicol sodium succinate water-soluble granule and preparation method thereof |
| CN113416304B (en) * | 2021-06-22 | 2022-07-29 | 四川永诺生物科技有限公司 | Preparation method and application of four-arm polyethylene glycol succinic acid florfenicol compound |
| CN113749020B (en) * | 2021-10-12 | 2022-05-13 | 中国水产科学研究院黄海水产研究所 | Method for breeding parent of sepia duchensis |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101289416A (en) * | 2008-03-03 | 2008-10-22 | 西南大学 | High-water-solubility florfenicol prodrug quickly released in vivo |
| CN101406456A (en) * | 2007-10-12 | 2009-04-15 | 河南农业大学 | Technique for preparing florfenicol soluble powder |
| CN102872014A (en) * | 2012-08-03 | 2013-01-16 | 九江大成制药有限公司 | Compound florfenicol composition and preparation process and application thereof |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101406456A (en) * | 2007-10-12 | 2009-04-15 | 河南农业大学 | Technique for preparing florfenicol soluble powder |
| CN101289416A (en) * | 2008-03-03 | 2008-10-22 | 西南大学 | High-water-solubility florfenicol prodrug quickly released in vivo |
| CN102872014A (en) * | 2012-08-03 | 2013-01-16 | 九江大成制药有限公司 | Compound florfenicol composition and preparation process and application thereof |
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