CN104055727A - Florfenicol solid dispersion and preparation method thereof - Google Patents
Florfenicol solid dispersion and preparation method thereof Download PDFInfo
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- CN104055727A CN104055727A CN201410274957.5A CN201410274957A CN104055727A CN 104055727 A CN104055727 A CN 104055727A CN 201410274957 A CN201410274957 A CN 201410274957A CN 104055727 A CN104055727 A CN 104055727A
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Abstract
The invention belongs to the technical field of veterinary medicines and relates to florfenicol solid dispersion and a preparation method thereof. Every 1kg of the solid dispersion is prepared from the following raw materials by weight: 0.1-0.3kg of florfenicol, 0.58-0.78kg of PEG (polyethylene glycol)-6000, 60-100g of poloxamer and 20-100g of solid acid. The florfenicol solid dispersion disclosed by the invention is suitable for being orally taken, great in solubility, quick in oral absorbability, quick to act, safe and non-toxic, and free of organic solvent residue; the preparation process is simple, and the product is stable, effective and safe, low in cost, suitable for industrial large-scale production, and wide in market prospect.
Description
technical field
The invention belongs to veterinary medicine technical field, be specifically related to a kind of florfenicol solid dispersion and preparation method thereof.
background technology
Florfenicol (Florfenicol) is animal specific antibiotic, has the advantages such as has a broad antifungal spectrum, antibacterial activity is strong, pharmaco-kinetic properties is good, untoward reaction is little, in world many countries and China's approved, is used for food animal.Florfenicol all has effect to multiple gram positive bacteria and gram negative bacteria and mycoplasma etc., but florfenicol is insoluble in water, dissolubility is low, causes onset slow.
Solid dispersion is a kind of new dosage form, and solid dispersion Chinese medicine can molecule, colloidal state, amorphous, microcrystalline state are dispersed in carrier material, and the solid dispersion dissolution rate that wherein disperses with molecularity is the highest, effect is best.At present, the existing technology that florfenicol is made into solid dispersion, but current florfenicol solid dispersion generally adopts Microcrystalline to make, and its solute effect is also not fully up to expectations, is further improved.
summary of the invention
The object of the present invention is to provide florfenicol solid dispersion that a kind of dissolubility is good and preparation method thereof.
For achieving the above object, the present invention is by the following technical solutions:
A veterinary florfenicol solid dispersion, this solid dispersion of every 1kg is raw materials used as follows: florfenicol 0.1-0.3kg, PEG-6000 0.58-0.78kg, poloxamer 60-100g, solid acid 20-100g.
Described solid acid is ethylenediaminetetraacetic acid, tartaric acid, citric acid.
The method of preparing veterinary florfenicol solid dispersion, comprises the following steps: a, get each raw material in proportion, by PEG-6000 and poloxamer, heating and melting, adds solid acid, continues heating and melting, add florfenicol to dissolve after insulated and stirred obtain mixed solution;
B, mixed solution is freezing, solidifies rear sealing, places rear pulverizing in 3-5 days and obtain florfenicol solid dispersion under normal temperature environment.
The temperature of heating and melting is 90-110 ℃.
Temperature when freezing is-5--20 ℃.
Temperature retention time is 10-20min.
Florfenicol solid dispersion of the present invention has added a kind of special carrier-solid acid of specified quantitative in the preparation, can greatly improve dissolubility, dissolution velocity and the clinical effectiveness of florfenicol solid dispersion, meets the demand of the medication of drinking water on market completely; Adopt in the preparation solid solution technology to make the florfenicol solid dispersion making have a new breakthrough than general product, and filled up the blank of high-load florfenicol solid dispersion on market.
The florfenicol solid dispersion that the present invention makes is used for the treatment of due to pig, chicken and fish sensitive organism and infects, as actinomyces suis pleuropneumonia, Bacillus pasteurii disease, typhoid fever, paratyphoid fever, Hakuri etc.; Be suitable for orally, dissolubility is large, oral absorption is fast, effect rapidly; Adopt PEG6000 and poloxamer to do adjuvant, safety non-toxic, and organic solvent-free is residual; Preparation technology is simple, and product is stable, effective, safety, with low cost, is applicable to large-scale industrialization and produces, and market prospect is wide.
the specific embodiment
Embodiment 1
1, in veterinary florfenicol solid dispersion, the preparation prescription of every 1kg florfenicol solid dispersion is as follows: florfenicol 0.1kg, PEG-6000 0.78kg, poloxamer 60g, ethylenediaminetetraacetic acid 70g.
2, the preparation method of described veterinary florfenicol solid dispersion, comprises the following steps:
A, get PEG6000 and poloxamer, after heating and melting (95 ℃), then add ethylenediaminetetraacetic acid, continue heating and makes it dissolve (110 ℃), then add florfenicol and dissolve after insulated and stirred 10 minutes.
B, solution is poured in plate ,-10 ℃ are carried out freezingly, and sample path length 1-3cm is thick.After solidifying, put into plastic bag sealing, place after pulverizing after 3-5 days and obtain florfenicol solid dispersion.
3, quality inspection: the dissolubility of gained florfenicol solid dispersion is 5.25mg/ml.
Embodiment 2
1, in veterinary florfenicol solid dispersion, the preparation prescription of every 1kg florfenicol solid dispersion is as follows: florfenicol 0.2kg, PEG-6000 0.65kg, poloxamer 80g, citric acid 0g.
2, the preparation method of described veterinary florfenicol solid dispersion, comprises the following steps:
A, get PEG6000 and poloxamer, after heating and melting (100 ℃), then add citric acid, continue heating and makes it dissolve (110 ℃), then add florfenicol and dissolve after insulated and stirred 10 minutes.
B, solution is poured in plate ,-20 ℃ are carried out freezingly, and sample path length 1-3cm is thick.After solidifying, put into plastic bag sealing, place after pulverizing after 3-5 days and obtain florfenicol solid dispersion.
3, quality inspection: the dissolubility of gained florfenicol solid dispersion is 5.07mg/ml.
Embodiment 3
1, in veterinary florfenicol solid dispersion, the preparation prescription of every 1kg florfenicol solid dispersion is as follows: florfenicol 0.3kg, PEG-6000 0.58kg, poloxamer 100g, tartaric acid 100g.
2, the preparation method of described veterinary florfenicol solid dispersion, comprises the following steps:
A, get PEG6000 and poloxamer, after heating and melting (110 ℃), then add tartaric acid, continue heating and makes it dissolve (110 ℃), then add florfenicol and dissolve after insulated and stirred 10 minutes.
B, solution is poured in plate ,-5 ℃ are carried out freezingly, and sample path length 1-3cm is thick.After solidifying, put into plastic bag sealing, place after pulverizing after 3-5 days and obtain florfenicol solid dispersion.
3, quality inspection: the dissolubility of gained florfenicol solid dispersion is 4.81mg/ml.
Effect experiment
Experimental subject: pig, suffers from pleuropneumonia, totally 76.
Experimental design: adopt the former powder of florfenicol (Zhangjiagang Heng Sheng pharmaceutcal corporation, Ltd), florfenicol powder (Hai Tian bio tech ltd, Henan), florfenicol solid dispersion (Shandong Qilu Animal Health Products Co., Ltd.) carries out Contrast on effect with the florfenicol solid dispersion of embodiment 3 in contrast, the former powder of florfenicol, florfenicol powder, Shandong, Shandong florfenicol solid dispersion, the florfenicol solid dispersion of embodiment 3 is labeled as respectively 1, 2, 3, 4 groups, dissolubility, clinical trial result, drug sensitive test (two parallel laboratory tests, adopt antibiotic-microbial assays to survey inhibition zone size).
Comparing result is as follows:
Table 1 dissolubility correction data
Table 2 Comparison of clinical effect data
The standard of curing is transference cure.
Table 3 drug sensitive test correction data
By above result, found out, the dissolubility of veterinary florfenicol solid dispersion of the present invention is good; Mortality rate is lower than matched group, and cure rate is higher than matched group, and therapeutic effect is desirable; For staphylococcus and colibacillary fungistatic effect, be better than the former powder of florfenicol.
Claims (6)
1. a veterinary florfenicol solid dispersion, is characterized in that, this solid dispersion of every 1kg is raw materials used as follows: florfenicol 0.1-0.3kg, PEG-6000 0.58-0.78kg, poloxamer 60-100g, solid acid 20-100g.
2. veterinary florfenicol solid dispersion as claimed in claim 1, is characterized in that, described solid acid is ethylenediaminetetraacetic acid, tartaric acid or citric acid.
3. the method for preparing veterinary florfenicol solid dispersion described in claim 1, it is characterized in that, comprise the following steps: a, get each raw material in proportion, by PEG-6000 and poloxamer, heating and melting, add solid acid, continue heating and melting, add florfenicol to dissolve rear insulated and stirred and obtain mixed solution;
B, mixed solution is freezing, solidifies rear sealing, places rear pulverizing in 3-5 days and obtain florfenicol solid dispersion under normal temperature environment.
4. the method for preparing veterinary florfenicol solid dispersion as claimed in claim 3, is characterized in that, the temperature of heating and melting is 90-110 ℃.
5. the method for preparing veterinary florfenicol solid dispersion as claimed in claim 3, is characterized in that, temperature when freezing is-5--20 ℃.
6. the method for preparing veterinary florfenicol solid dispersion as claimed in claim 3, is characterized in that, temperature retention time is 10-20min.
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| CN201410274957.5A CN104055727B (en) | 2014-06-19 | 2014-06-19 | A kind of florfenicol solid dispersoid and preparation method thereof |
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| CN201410274957.5A CN104055727B (en) | 2014-06-19 | 2014-06-19 | A kind of florfenicol solid dispersoid and preparation method thereof |
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| CN104055727B CN104055727B (en) | 2017-10-20 |
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Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104642256A (en) * | 2015-02-10 | 2015-05-27 | 河南普尼尔生物制药有限公司 | Fifty-fifty pig-raising method |
| CN104800167A (en) * | 2015-04-22 | 2015-07-29 | 河南牧翔动物药业有限公司 | Florfenicol soluble powder and preparation method thereof |
| CN105560189A (en) * | 2016-01-22 | 2016-05-11 | 山东畜牧兽医职业学院 | Florfenicol slow-release dispersoid and preparation method thereof |
| CN105902497A (en) * | 2016-06-01 | 2016-08-31 | 洛阳瑞华动物保健品有限公司 | Preparation method of water-soluble florfenicol veterinary preparation |
| CN106913537A (en) * | 2015-12-25 | 2017-07-04 | 山东新时代药业有限公司 | A kind of Abiraterone acetate sublingual tablets 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 |
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| CN102657614A (en) * | 2012-05-03 | 2012-09-12 | 青岛绿曼生物工程有限公司 | Method for preparing solid florfenicol dispersion |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN102657614A (en) * | 2012-05-03 | 2012-09-12 | 青岛绿曼生物工程有限公司 | Method for preparing solid florfenicol dispersion |
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| 刘洋等: ""氟苯尼考PEG6000固体分散体的无溶剂熔融法制备与分析"", 《中国兽药杂志》 * |
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Cited By (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104642256A (en) * | 2015-02-10 | 2015-05-27 | 河南普尼尔生物制药有限公司 | Fifty-fifty pig-raising method |
| CN104800167A (en) * | 2015-04-22 | 2015-07-29 | 河南牧翔动物药业有限公司 | Florfenicol soluble powder and preparation method thereof |
| CN106913537A (en) * | 2015-12-25 | 2017-07-04 | 山东新时代药业有限公司 | A kind of Abiraterone acetate sublingual tablets and preparation method thereof |
| CN106913537B (en) * | 2015-12-25 | 2021-02-09 | 山东新时代药业有限公司 | Abiraterone acetate sublingual tablet and preparation method thereof |
| CN105560189A (en) * | 2016-01-22 | 2016-05-11 | 山东畜牧兽医职业学院 | Florfenicol slow-release dispersoid and preparation method thereof |
| CN105902497A (en) * | 2016-06-01 | 2016-08-31 | 洛阳瑞华动物保健品有限公司 | Preparation method of water-soluble florfenicol veterinary preparation |
| CN105902497B (en) * | 2016-06-01 | 2019-06-11 | 洛阳瑞华动物保健品有限公司 | A kind of preparation method of water-solubility florfenicol veterinary drug preparation |
| CN112791056A (en) * | 2021-01-22 | 2021-05-14 | 河北农业大学 | Florfenicol solid dispersion and preparation method thereof |
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| CN104055727B (en) | 2017-10-20 |
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Effective date of registration: 20200313 Address after: 454950 Gongye West Road, Zhandian New District, Wuzhi County, Jiaozuo City, Henan Province Patentee after: THE DIYI BIOLOGICAL PHARMACEUTICAL Co. Address before: 450000, No. 35, No. 1, Jinshui District, Henan, Zhengzhou Patentee before: Ma Gaiyun |
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