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Preparation method of high-water solubility florfenicol powder

A technology of florfenicol powder and florfenicol, applied in the direction of non-active ingredient medical preparations, active ingredient-containing medical preparations, pharmaceutical formulas, etc., can solve complex preparation methods, inclusion rate and yield Unsatisfactory, low production capacity and other problems, to achieve the effect of increasing solubility and stability, improving bioavailability, and stable product quality

Inactive Publication Date: 2017-12-29
CHINA ANIMAL HUSBANDRY IND
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Currently on the domestic market, the preparation method of florfenicol powder with good water solubility is mainly through the spray drying method. Although the water solubility of the prepared product has been greatly improved, but according to the Calculated, the solubility at room temperature is about 1200-3000ppm, and this method is used to produce, the production capacity is small, and the energy consumption is high
[0005] CN102160854 has introduced a kind of preparation method of florfenicol powder, and the defect of this method is that the one, clathrate is not thorough, and gained product solubility and bioavailability are not perfect, and the solubility of florfenicol has improved 4 times, is about 1200ppm, which is quite different from the existing technology; second, it is prepared by oven drying, which is labor-intensive and energy-consuming; third, this method needs to add glucose for re-mixing
[0008] CN106177983 has introduced a kind of preparation technology of florfenicol powder, the shortcoming of this method one is to add organic solvent ethanol, only applicable to small-scale preparation, during actual production, also must consider the reclaiming and processing of organic solvent; The 2nd, preparation method Complicated, two kinds of solutions A and B need to be formulated first, and then gradually mixed. In addition, in order to obtain the product, it must be refrigerated for 24 hours, and finally washed with ethanol. The preparation method is complicated and the cycle is too long; It is that the inclusion rate and yield of this method are not ideal, and the inclusion is not complete, and the solubility of the product must be affected; the fourth is that this method is not suitable for large-scale production

Method used

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  • Preparation method of high-water solubility florfenicol powder

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] A preparation method of highly water-soluble florfenicol powder, comprising the following steps:

[0039] S1. Add 400 parts by weight of purified water, 200 parts by weight of β-cyclodextrin, and 20 parts by weight of florfenicol into the reaction kettle, stir and heat up to 90°C, keep warm in an environment of 90°C for 2 hours, and keep warm Keep stirring during the process to obtain the first mixed solution;

[0040] S2. Use circulating water to cool the first mixed solution to below 40°C, then use chilled water to cool the first mixed solution to 10°C, keep it warm for 0.5h in an environment of 0°C, and set aside for use, wherein, Keep stirring during the heat preservation process;

[0041] S3. Centrifuge the first mixed solution treated in S2 to obtain a first mixed powder and a first mother liquor, dry and sieve the first mixed powder to obtain a first florfenicol powder.

[0042]S4. Add 400 parts by weight of the first mother liquor, 50 parts by weight of purifi...

Embodiment 2

[0050] A preparation method of highly water-soluble florfenicol powder, comprising the following steps:

[0051] S1. Add 460 parts by weight of deionized water, 224 parts by weight of β-cyclodextrin, and 50 parts by weight of Florfenicol into the reaction kettle, stir and heat up to 90°C, and keep warm in an environment of 92°C for 3h. Keep stirring during the heat preservation process to obtain the first mixed solution;

[0052] S2. Use circulating water to cool the first mixed solution to below 40°C, then use chilled water to cool the first mixed solution to 10°C, keep it warm in an environment of 7°C for 0.5h, and set aside, wherein, Keep stirring during the heat preservation process;

[0053] S3. Centrifuge the first mixed solution treated in S2 to obtain a first mixed powder and a first mother liquor, dry and sieve the first mixed powder to obtain a first florfenicol powder.

[0054] S4. Add 390 parts by weight of the first mother liquor, 80 parts by weight of deionized...

Embodiment 3

[0062] A preparation method of highly water-soluble florfenicol powder, comprising the following steps:

[0063] S1. Add 500 parts by weight of soft water, 250 parts by weight of β-cyclodextrin, and 80 parts by weight of Florfenicol in the reaction kettle, stir and heat up to 90°C, and keep warm for 5 hours in an environment of 95°C. Keep stirring in to obtain the first mixed solution;

[0064] S2. Use circulating water to cool the first mixed solution to below 40°C, then use chilled water to cool the first mixed solution to 10°C, keep it warm at 15°C for 1 hour, and set it aside for later use. stir;

[0065] S3. Centrifuge the first mixed solution treated in S2 to obtain a first mixed powder and a first mother liquor, dry and sieve the first mixed powder to obtain a first florfenicol powder.

[0066] S4. Add 500 parts by weight of the first mother liquor, 100 parts by weight of soft water, 250 parts by weight of β-cyclodextrin, and 80 parts by weight of Florfenicol into the...

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Abstract

The invention discloses a preparation method of high-water solubility florfenicol powder. The preparation method comprises the following steps: S1, adding 400-500 parts by weight of water, 200-250 parts by weight of beta-cyclodextrin and 20-80 parts by weight of florfenicol by weight into a reaction kettle, stirring and heating to 90 DEG C, preserving heat for 2-5 h at 90-95 DEG C, and keeping stirring during heat preservation to obtain a first mixed solution; S2, cooling the first mixed solution to 10 DEG C, preserving heat for 0.5-1 h at 0-15 DEG C for use, and keeping stirring during heat preservation; S3, centrifuging the first mixed solution treated in the step S2 to obtain first mixed powder and a first mother solution, drying the first mixed powder, and sieving to obtain first florfenicol powder. The invention provides the preparation method of the high-water solubility florfenicol powder, by which the solubility of the florfenicol can be effectively improved.

Description

technical field [0001] The invention relates to the field of preparation of florfenicol powder. More specifically, the present invention relates to a preparation method of highly water-soluble florfenicol powder. Background technique [0002] Florfenicol is an antibacterial drug commonly used in animal breeding and production. It is safe, effective and widely used. However, the solubility of florfenicol in water is very small, and it is not suitable for water-soluble administration, which limits its application in the treatment of animal diseases. Cosolvent micronization, β-cyclodextrin inclusion, hydroxypropyl β-cyclodextrin inclusion, PVPK dispersion, PEG6000 dispersion, ultrafine, grinding and other methods generally have unsatisfactory solubilizing effects, and the dissolution rate is slow, The dissolution rate is small, and it is difficult to meet the needs of preparation and concentrated use. [0003] The initial preparation technology of florfenicol powder is simpl...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K31/165A61K47/69A61P31/04
CPCA61K9/146A61K31/165
Inventor 桂亮庞谦程成刘姣张誉赢马宏星
Owner CHINA ANIMAL HUSBANDRY IND
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