CN102657614A - Method for preparing solid florfenicol dispersion - Google Patents
Method for preparing solid florfenicol dispersion Download PDFInfo
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- CN102657614A CN102657614A CN2012101337155A CN201210133715A CN102657614A CN 102657614 A CN102657614 A CN 102657614A CN 2012101337155 A CN2012101337155 A CN 2012101337155A CN 201210133715 A CN201210133715 A CN 201210133715A CN 102657614 A CN102657614 A CN 102657614A
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- florfenicol
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Abstract
The invention discloses a method for preparing solid florfenicol dispersion, and relates to the field of animal medicine. The solid florfenicol dispersion is uniformly and sequentially prepared from the following components in parts by weight: 15 to 25 parts of florfenicol (sieved with a sieve of 80 meshes), 15 to 25 parts of poloxamer, and 50 to 70 parts of polyethylene glycol-4000. The preparation method comprises the following steps of: (1) weighing 15 to 25 parts of florfenicol (sieved with the sieve of 80 meshes), 15 to 25 parts of poloxamer and 50 to 70 parts of polyethylene glycol-4000 by weight; (2) heating and melting the poloxamer and the polyethylene glycol-4000, stirring for 3 to 5 minutes till the mixture is uniform, adding the florfenicol, and stirring uniformly; and (3) quickly cooling the mixture obtained in the (2) to the temperature of 10 DEG C below zero, crushing, and thus obtaining the solid florfenicol dispersion. The preparation process is simple, and the dissolubility of the florfenicol is remarkably improved and is about 2 times that of a common florfenicol preparation (soluble powder or oral liquid).
Description
Technical field
The present invention relates to a kind of method for preparing of florfenicol solid dispersion, belong to the animal field of medicaments, particularly a kind of method for preparing of florfenicol solid dispersion.
Background technology
Florfenicol is the broad spectrum antibiotic of the special-purpose chloromycetin of a kind of new veterinary successfully developed in the late nineteen eighties, and these article are white or off-white color crystalline powder, odorless, bitter in the mouth.These article are very easily dissolving in dimethyl formamide, in methanol, dissolves, and dissolves micro dissolution in water or chloroform in the glacial acetic acid part omitted.Be mainly used in the bacterial disease of pig, chicken and fish due to the sensitive bacterial, especially evident in efficacy to respiratory system infection and intestinal infection.
Because the florfenicol water solublity is relatively poor, has brought the deuce to pay to clinical practice, has influenced promoting the use of of it.Therefore researching and developing the above-mentioned shortcoming deficiency that a new technique overcomes florfenicol is one of this field scientific research technical staff new problem anxious to be solved.
Summary of the invention
The objective of the invention is to overcome above-mentioned weak point, provide that a kind of technology is simple, the method for preparing of the florfenicol solid dispersion of steady quality, good water solubility.
Following for realizing the embodiment that above-mentioned purpose the present invention adopted: a kind of method for preparing of florfenicol solid dispersion, formulated in regular turn by following components in weight portion number: 15～25 parts of florfenicols (mistake 80 mesh sieves), 15～25 parts of poloxamers, Polyethylene Glycol-400050～70 part than evenly.
On the basis of such scheme, said various component optimum ratio amounts are: 20 parts of florfenicols (cross 80 mesh sieves), 20 parts of poloxamers, Polyethylene Glycol-400060 part.
A kind of method for preparing of florfenicol solid dispersion, carry out as follows:
(1) takes by weighing 15～25 parts of florfenicols (cross 80 mesh sieves), 15～25 parts of poloxamers, Polyethylene Glycol-400050～70 part by weight;
(2) with said poloxamer, Polyethylene Glycol-4000 heating and melting, stir 3～5 minutes to evenly, add florfenicol, stir;
(3) (2) gained mixture is cooled to-10 ℃ rapidly, pulverizes and promptly get the florfenicol solid dispersion.
The medicinal property of each component is following:
Florfenicol: be the broad spectrum antibiotic of the special-purpose chloromycetin of a kind of new veterinary successfully developed in the late nineteen eighties, these article are white or off-white color crystalline powder, odorless, bitter in the mouth.These article are very easily dissolving in dimethyl formamide, in methanol, dissolves, and dissolves micro dissolution in water or chloroform in the glacial acetic acid part omitted.Be mainly used in the bacterial disease of pig, chicken and fish due to the sensitive bacterial, especially evident in efficacy to respiratory system infection and intestinal infection.
Poloxamer: being polyoxyethylene, polyoxypropylene ether block copolymers, is one type of novel macromolecule non-ionic surface active agent.Can be used as emulsifying agent, stabilizing agent, solubilizing agent, absorption enhancer, slow-release material and solid dispersion, can improve the dissolubility of medicine greatly, promote the absorption of medicine.
Polyethylene Glycol-4000: the mixture that forms for oxirane and water polycondensation; In water or ethanol, be prone to dissolve; It has the extensive compatibility with all kinds of solvents, is good solvent and solubilizing agent, for being difficult for dissolved drug in the water; These article can be made the carrier of solid dispersion, to reach the solid dispersion purpose.
The invention has the beneficial effects as follows: preparation technology is simple, has significantly improved the dissolubility of florfenicol, and its dissolution is about 2 times of common florfenicol.
The specific embodiment
Below in conjunction with preferred embodiment, to details are as follows according to the specific embodiment provided by the invention:
Embodiment 1
A kind of method for preparing of florfenicol solid dispersion is carried out: (every part by 10g) as follows
(1) takes by weighing 150 parts of florfenicols (cross 80 mesh sieves), 150 parts of poloxamers, Polyethylene Glycol-4000500 part by weight;
(2) with said poloxamer, Polyethylene Glycol-4000 heating and melting, stir 3～5 minutes to evenly, add florfenicol, stir;
(3) (2) gained mixture is cooled to-10 ℃ rapidly, pulverizes and promptly get the florfenicol solid dispersion.
Embodiment 2
A kind of method for preparing of florfenicol solid dispersion is carried out: (every part by 10g) as follows
(1) takes by weighing 200 parts of florfenicols (cross 80 mesh sieves), 200 parts of poloxamers, Polyethylene Glycol-4000600 part by weight;
(2) with said poloxamer, Polyethylene Glycol-4000 heating and melting, stir 3～5 minutes to evenly, add florfenicol, stir;
(3) (2) gained mixture is cooled to-10 ℃ rapidly, pulverizes and promptly get the florfenicol solid dispersion.
Embodiment 3
A kind of method for preparing of florfenicol solid dispersion is carried out: (every part by 10g) as follows
(1) takes by weighing 250 parts of florfenicols (cross 80 mesh sieves), 250 parts of poloxamers, Polyethylene Glycol-4000700 part by weight;
(2) with said poloxamer, Polyethylene Glycol-4000 heating and melting, stir 3～5 minutes to evenly, add florfenicol, stir;
(3) (2) gained mixture is cooled to-10 ℃ rapidly, pulverizes and promptly get the florfenicol solid dispersion.
Solubility experiment: in accordance with the law measure according to VII page or leaf " solubility test method " in " People's Republic of China's veterinary drug allusion quotation " one one (version in 2010) " note on the use ".Former powder 1 gram of fluorobenzene Buddhist nun and thing of the present invention 5.0 grams (being equivalent to crude drug 1 gram approximately) respectively are ground into fine powder; Place 25 ℃, 30 milliliters, 100 milliliters, 1000 milliliters, 10000 milliliters distilled water respectively; Every at a distance from 5 minutes 30 seconds of powerful jolting; Observe the dissolving situation in 30 minutes, as do not have visual visible particles of solute and promptly be regarded as dissolving fully.
According to the criterion of " People's Republic of China's veterinary drug allusion quotation " (version in 2010) note on the use part VII page or leaf " dissolubility ", can know that by this experiment the former powder of florfenicol does not have solid particle in 100 ml waters, be judged to be and be slightly soluble in water; And the florfenicol solid dispersion does not have visible solid particle in 10 ml waters, is judged as to be dissolved in water.Former powder is compared with thing of the present invention, and dissolubility significantly improves.
Dissolution experiment: in accordance with the law measure according to " first method (basket method) " in " appendix " in " People's Republic of China's veterinary drug allusion quotation " one one (version in 2010) " rules of preparations " the 114th page " dissolution method ".
This experimental result is through statistical analysis, and thing of the present invention is compared aspect the dissolution with the florfenicol oral liquid, and the former is about 2 times of the latter, and difference is (P＜0.01) extremely significantly.
Above-mentioned detailed description of a kind of method for preparing of florfenicol solid dispersion being carried out with reference to embodiment; Be illustrative rather than determinate; Can enumerate out several embodiment according to institute's limited range; Therefore in the variation and the modification that do not break away under the general plotting of the present invention, should belong within protection scope of the present invention.
Claims (3)
1. the method for preparing of a florfenicol solid dispersion is characterized in that by following components in weight portion number more formulated in regular turn than evenly: 15～25 parts of florfenicols (crossing 80 mesh sieves), 15～25 parts of poloxamers, Polyethylene Glycol-400050～70 part.
2. the method for preparing of a kind of florfenicol solid dispersion according to claim 1 is characterized in that by following components in weight portion number more formulated in regular turn than evenly: 20 parts of florfenicols (cross 80 mesh sieves), 20 parts of poloxamers, Polyethylene Glycol-400060 part.
3. the method for preparing of a florfenicol solid dispersion according to claim 1 and 2 is characterized in that carrying out as follows:
(1) takes by weighing 15～25 parts of florfenicols (cross 80 mesh sieves), 15～25 parts of poloxamers, Polyethylene Glycol-400050～70 part by weight;
(2) with said poloxamer, Polyethylene Glycol-4000 heating and melting, stir 3～5 minutes to evenly, add florfenicol, stir;
(3) (2) gained mixture is cooled to-10 ℃ rapidly, pulverizes and promptly get the florfenicol solid dispersion.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2012101337155A CN102657614A (en) | 2012-05-03 | 2012-05-03 | Method for preparing solid florfenicol dispersion |
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| CN2012101337155A CN102657614A (en) | 2012-05-03 | 2012-05-03 | Method for preparing solid florfenicol dispersion |
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| CN102657614A true CN102657614A (en) | 2012-09-12 |
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| CN2012101337155A Pending CN102657614A (en) | 2012-05-03 | 2012-05-03 | Method for preparing solid florfenicol dispersion |
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Cited By (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102973489A (en) * | 2012-12-11 | 2013-03-20 | 江西新世纪民星动物保健品有限公司 | Florfenicol solid dispersoid 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 |
| CN103330942A (en) * | 2013-06-19 | 2013-10-02 | 山东鲁抗舍里乐药业有限公司 | Florfenicol smell masking preparation and preparation method thereof |
| CN104003917A (en) * | 2014-03-14 | 2014-08-27 | 河北润普兽药有限公司 | Preparing method of florfenicol sodium succinate microcrystals |
| CN104055727A (en) * | 2014-06-19 | 2014-09-24 | 马改云 | Florfenicol solid dispersion and preparation method thereof |
| CN105640889A (en) * | 2014-11-11 | 2016-06-08 | 天津嘉创生物科技有限公司 | Florfenicol soluble powder and preparation method thereof |
| CN106344516A (en) * | 2016-10-17 | 2017-01-25 | 安庆市柯旷动物药业有限公司 | Florfenicol powder |
| CN106727342A (en) * | 2017-01-04 | 2017-05-31 | 广东紫金正天药业有限公司 | A kind of high content florfenicol powder and its preparation method and application |
| CN107233315A (en) * | 2017-05-10 | 2017-10-10 | 刘淑鹤 | Florfenicol soluble powder, Florfenicol liquid and preparation method thereof |
| CN109568273A (en) * | 2019-01-25 | 2019-04-05 | 四川农业大学 | A kind of Florfenicol instant capacity particle and preparation method thereof |
| CN112791056A (en) * | 2021-01-22 | 2021-05-14 | 河北农业大学 | Florfenicol solid dispersion and preparation method thereof |
| CN113230233A (en) * | 2021-05-14 | 2021-08-10 | 中国农业科学院兰州畜牧与兽药研究所 | Florfenicol solid dispersion inclusion microcapsule and preparation method and application thereof |
| CN113750050A (en) * | 2021-10-13 | 2021-12-07 | 杭州艾贝德生命科技研究院有限公司 | Method for preparing florfenicol solid dispersion through hot-melt extrusion |
Citations (2)
| 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 |
| CN101909600A (en) * | 2007-11-09 | 2010-12-08 | 英特维特国际股份有限公司 | Fast release solid formulation, preparation and use thereof |
-
2012
- 2012-05-03 CN CN2012101337155A patent/CN102657614A/en active Pending
Patent Citations (2)
| 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 |
| CN101909600A (en) * | 2007-11-09 | 2010-12-08 | 英特维特国际股份有限公司 | Fast release solid formulation, preparation and use thereof |
Cited By (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102973489A (en) * | 2012-12-11 | 2013-03-20 | 江西新世纪民星动物保健品有限公司 | Florfenicol solid dispersoid and preparation method thereof |
| CN102973489B (en) * | 2012-12-11 | 2014-04-30 | 江西新世纪民星动物保健品有限公司 | Florfenicol solid dispersoid 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 |
| CN103127019B (en) * | 2013-03-22 | 2015-04-22 | 成都乾坤动物药业有限公司 | Florfenicol dispersible tablet as well as preparation method and application thereof |
| CN103330942A (en) * | 2013-06-19 | 2013-10-02 | 山东鲁抗舍里乐药业有限公司 | Florfenicol smell masking preparation and preparation method thereof |
| CN104003917A (en) * | 2014-03-14 | 2014-08-27 | 河北润普兽药有限公司 | Preparing method of florfenicol sodium succinate microcrystals |
| CN104055727A (en) * | 2014-06-19 | 2014-09-24 | 马改云 | Florfenicol solid dispersion and preparation method thereof |
| CN105640889A (en) * | 2014-11-11 | 2016-06-08 | 天津嘉创生物科技有限公司 | Florfenicol soluble powder and preparation method thereof |
| CN106344516A (en) * | 2016-10-17 | 2017-01-25 | 安庆市柯旷动物药业有限公司 | Florfenicol powder |
| CN106727342A (en) * | 2017-01-04 | 2017-05-31 | 广东紫金正天药业有限公司 | A kind of high content florfenicol powder and its preparation method and application |
| CN107233315A (en) * | 2017-05-10 | 2017-10-10 | 刘淑鹤 | Florfenicol soluble powder, Florfenicol liquid and preparation method thereof |
| CN109568273A (en) * | 2019-01-25 | 2019-04-05 | 四川农业大学 | A kind of Florfenicol instant capacity particle and preparation method thereof |
| CN109568273B (en) * | 2019-01-25 | 2021-09-03 | 四川农业大学 | Florfenicol instant particles and preparation method thereof |
| CN112791056A (en) * | 2021-01-22 | 2021-05-14 | 河北农业大学 | Florfenicol solid dispersion and preparation method thereof |
| CN113230233A (en) * | 2021-05-14 | 2021-08-10 | 中国农业科学院兰州畜牧与兽药研究所 | Florfenicol solid dispersion inclusion microcapsule and preparation method and application thereof |
| CN113750050A (en) * | 2021-10-13 | 2021-12-07 | 杭州艾贝德生命科技研究院有限公司 | Method for preparing florfenicol solid dispersion through hot-melt extrusion |
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Application publication date: 20120912 |