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Method for preparing florfenicol-beta-cyclodextrin inclusion compound through ultrasonic-centrifugal drying

A technology of cyclodextrin inclusion compound and centrifugal drying, which is applied in the direction of pharmaceutical formula, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc. Identify problems such as clathrates, achieve high yield and clathrate rate, and improve solubility

Active Publication Date: 2018-02-16
HENAN SOAR VETERINARY PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The patent with publication number CN105477642A discloses a highly bioavailable Florfenicol composition and its preparation method, wherein β-cyclodextrin is used as a carrier with high bioavailability of Florfenicol, rather than as an inclusion carrier , also does not involve inclusion parameters such as the ratio of guest molecule and host molecule, inclusion method and other parameters, and does not identify the inclusion compound of the product

Method used

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  • Method for preparing florfenicol-beta-cyclodextrin inclusion compound through ultrasonic-centrifugal drying
  • Method for preparing florfenicol-beta-cyclodextrin inclusion compound through ultrasonic-centrifugal drying
  • Method for preparing florfenicol-beta-cyclodextrin inclusion compound through ultrasonic-centrifugal drying

Examples

Experimental program
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Effect test

Embodiment 1

[0030] A method for preparing florfenicol-beta-cyclodextrin inclusion compound by ultrasonic-centrifugal drying method, the steps are as follows:

[0031] (a) Weigh 66.7 kg of florfenicol and 133.3 kg of β-cyclodextrin into the reaction kettle, add 800 kg of purified water, heat and dissolve at a constant temperature of 110 ℃, and obtain the feed liquid A;

[0032] (b) Use an ultrasonic instrument to ultrasonicate the material liquid A at a frequency of 60 HZ for 2 hours to obtain the material liquid B;

[0033] (c) Use an LPG high-speed centrifugal dryer to centrifugally dry the feed liquid B, and the dried product is florfenicol-β-cyclodextrin inclusion compound. The drying parameters of the LPG high-speed centrifugal dryer: centrifugal disc speed 24000 r / min, the inlet air temperature is 140 ℃, and the feed rate is 400 kg / h.

[0034] It was determined that the yield of the inclusion complex of Florfenicol-β-cyclodextrin prepared in this example was 98.5%, and the inclusion...

Embodiment 2

[0036] A method for preparing florfenicol-beta-cyclodextrin inclusion compound by ultrasonic-centrifugal drying method, the steps are as follows:

[0037] (a) Weigh 20 kg of florfenicol and 180 kg of β-cyclodextrin into the reaction kettle, add 400 kg of purified water, heat and dissolve at a constant temperature of 90°C, and obtain material liquid A;

[0038] (b) Use an ultrasonic instrument to ultrasonicate the material liquid A at a frequency of 40 HZ for 4 hours to obtain the material liquid B;

[0039] (c) Use an LPG high-speed centrifugal dryer to centrifugally dry the feed liquid B. The dried product is florfenicol-β-cyclodextrin inclusion compound. Drying parameters of the LPG high-speed centrifugal dryer: centrifugal disc speed 20000 r / min, the inlet air temperature is 160 ℃, and the feed rate is 200 kg / h.

[0040] It was determined that the yield of the inclusion complex of Florfenicol-β-cyclodextrin prepared in this example was 98.7%, and the inclusion rate was 95....

Embodiment 3

[0042] A method for preparing florfenicol-beta-cyclodextrin inclusion compound by ultrasonic-centrifugal drying method, the steps are as follows:

[0043] (a) Weigh 40 kg of florfenicol and 160 kg of β-cyclodextrin into the reaction kettle, add 600 kg of purified water, heat and dissolve at a constant temperature of 100°C, and obtain material liquid A;

[0044] (b) Use an ultrasonic instrument to ultrasonicate the material liquid A at a frequency of 50 HZ for 4 hours to obtain the material liquid B;

[0045] (c) Use an LPG high-speed centrifugal dryer to centrifugally dry the liquid B, and the dried product is the inclusion compound of florfenicol-β-cyclodextrin. The drying parameters of the LPG high-speed centrifugal dryer: centrifugal disc speed 22000 r / min, the inlet air temperature is 150 ℃, and the feed rate is 300 kg / h.

[0046] It was determined that the yield of the inclusion complex of Florfenicol-β-cyclodextrin prepared in this example was 98.2%, and the inclusion r...

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Abstract

The invention belongs to the field of veterinary drugs and discloses a method for preparing a florfenicol-beta-cyclodextrin inclusion compound through ultrasonic-centrifugal drying. The method comprises the following steps: florfenicol and beta-cyclodextrin are taken, water is added, the solution is heated and dissolved at the constant temperature of 90-110 DEG C, and a feed liquid A is obtained,wherein the mass ratio of florfenicol to beta-cyclodextrin is 1:(2-9), and the ratio of the mass of the water to the total mass of florfenicol and beta-cyclodextrin is (2-4):1; the feed liquid A is ultrasonically treated with the ultrasonic frequency being 40-60 HZ, and a feed liquid B is obtained; the feed liquid B is centrifugally dried, and a dried product is the florfenicol-beta-cyclodextrin inclusion compound; in terms of centrifugal drying parameters, the rotating rate of a centrifugal pan is 20,000-24,000 rpm, the air intake temperature is 140-160 DEG C, and the feeding amount is 200-400 kg / h. The water solubility of the florfenicol-beta-cyclodextrin inclusion compound is as high as 5,000 ppm at the water temperature of 25 DEG C, so that the water solubility of the florfenicol is improved substantially; the yield of the florfenicol-beta-cyclodextrin inclusion compound is 98% or higher, and the inclusion rate is 95% or higher.

Description

technical field [0001] The invention belongs to the field of veterinary medicine, and in particular relates to a method for preparing florfenicol-beta-cyclodextrin inclusion compound by an ultrasonic-centrifugal drying method. Background technique [0002] Florfenicol (florfenicol) is a new generation of broad-spectrum antibiotics for amide alcohol animals. Its antibacterial activity is significantly better than that of chloramphenicol and thiamphenicol. It is effective against Actinobacillus pleuropneumoniae, Pasteurella multocida, Gram-positive and negative bacteria such as Bordetella septica, Streptococcus, Haemophilus parasuis, Salmonella, Escherichia coli and mycoplasma have strong lethality. At present, the drug is widely used in veterinary clinics, but the drug is almost insoluble in water, and its oral bioavailability is very low. Therefore, how to improve the solubility and dissolution rate of the drug through preparation technology is of great significance for the...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K31/165A61P31/04
CPCA61K31/165
Inventor 胡帅李灵娟李凌峰李登云袁富威
Owner HENAN SOAR VETERINARY PHARMA
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