Water-soluble florfenicol clathrate with high bioavailability and preparation method of water-soluble florfenicol clathrate

A florfenicol and availability technology, which is applied in the directions of drug combinations, medical preparations of inactive ingredients, pharmaceutical formulations, etc., can solve the problem of low oral bioavailability, poor water solubility of florfenicol, and low bioavailability. problems, to achieve the effect of masking bad odor, improving solubility, and improving bioavailability

Inactive Publication Date: 2017-02-15
SHIJIAZHUANG WEIERLI ANIMAL PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The water solubility of florfenicol itself is very poor, and oral bioavailability is very low; To achieve this purpose, such as using methods such as florfenicol phosphate to increase the water solubility of florfenicol, another method is to make florfenicol into PEG solid dispersion, PVP solid dispersion and β-cyclopaste Fine clathrates, etc.; these two methods are to a certain extent more water-soluble than drug suspensions, but the bioavailability is still not high

Method used

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  • Water-soluble florfenicol clathrate with high bioavailability and preparation method of water-soluble florfenicol clathrate
  • Water-soluble florfenicol clathrate with high bioavailability and preparation method of water-soluble florfenicol clathrate
  • Water-soluble florfenicol clathrate with high bioavailability and preparation method of water-soluble florfenicol clathrate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Preparation of florfenicol inclusion compound

[0046]Weigh 2.0kg of hydroxypropyl-sulfobutyl-β-cyclodextrin, 0.05kg of methylcellulose, 0.05kg of hydroxypropylcellulose, 0.05kg of poloxamer, 0.05kg of polyvinylpyrrolidone, and add to 60°C Continue stirring in 5L of water to dissolve it to obtain mixture 1; place mixture 1 in a water bath at 60°C, slowly add 0.5kg of florfenicol, and stir rapidly for 30 minutes until a uniform colorless solution is formed to obtain mixture 2; continue Stir under temperature control and keep warm for 3 hours. After the keep warm is over, prepare the mixture 2 into a powder by freeze-drying to obtain florfenicol inclusion compound 1. The freeze-drying conditions are: put the mixture 3 in batches into the refrigerator to freeze , the freezing time is 24 hours, then placed in a vacuum freeze dryer, vacuumed to about 1.3pa, and continued to dry for 18 hours.

Embodiment 2

[0048] Preparation of florfenicol inclusion compound

[0049] Weigh 1.0kg of hydroxypropyl-sulfobutyl-β-cyclodextrin, 1.0kg of ethylenediamine-β-cyclodextrin, 0.05kg of Tween-800.05kg, 0.05kg of disodium edetate, salicyl Add 0.05kg of sodium p-aminobenzoate and 0.05kg of sodium p-aminobenzoate into 5L of water at 60°C and continue stirring to dissolve to obtain mixture 1; place mixture 1 in a water bath at 60°C, and slowly add 0.5kg of florfenicol sodium succinate , stirred rapidly for 30 minutes, until a uniform colorless solution was formed, and mixture 2 was obtained; continue to control the temperature and stir, keep warm for 3 hours, and when the heat preservation is over, prepare the mixture 2 into powder by spray drying, and obtain the inclusion compound of florfenicol 2. The spray drying conditions are: the inlet air temperature is 160°C, the outlet air temperature is 40°C, the spray pressure is 0.6Mpa, and the vacuum degree is 0-10Kpa.

Embodiment 3

[0051] Preparation of florfenicol inclusion compound

[0052] Weigh 1.0kg of ethylenediamine-β-cyclodextrin, 1.0kg of sulfobutyl-β-cyclodextrin, 0.05kg of methylcellulose, 0.05kg of sodium lauryl sulfate, 0.05kg of polyvinylpyrrolidone, Add 0.05kg of sodium salicylate to 5L of water at 60°C and continue to stir to dissolve it to obtain mixture 1; put mixture 1 in a water bath at 60°C, slowly add 0.5kg of florfenicol sodium phosphate, and stir rapidly for 30 minutes , to form a uniform colorless solution, to obtain mixture 2; continue to control temperature and stir, keep warm for 3 hours, and heat preservation is over, prepare mixture 2 into powder by spray drying, that is, obtain florfenicol inclusion compound 3, spray drying conditions It is: the inlet air temperature is 160°C, the outlet air temperature is 40°C, the spray pressure is 0.6Mpa, and the vacuum degree is 0-10Kpa.

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Abstract

The invention discloses a water-soluble florfenicol clathrate with high bioavailability. The water-soluble florfenicol clathrate is prepared from the following components in parts by weight: 5-15 parts of florfenicol or pharmaceutically acceptable salt of florfenicol, 20-60 parts of a florfenicol adsorption carrier, 1-2 parts of an absorption promoter, and 10-30 parts of a florfenicol cosolvent. For the florfenicol clathrate provided by the invention, the solubility of florfenicol is effectively improved, the bioavailability of florfenicol is improved, the hemolysis property of the medicine is alleviated, the release rate of the medicine is controlled, and the bad smell is masked. The preparation method provided by the invention comprises the following steps: firstly, mixing the florfenicol adsorption carrier, the absorption promoter and the florfenicol cosolvent, adding with florfenicol or the pharmaceutically acceptable salt of florfenicol under the water bath water control condition, carrying out stirring, carrying out heat preservation, and carrying out drying, thus obtaining the florfenicol clathrate. The technological operation is simple, the abundant time and manpower are saved, and during the preparation process, no organic solvents are used, so that the preparation method is safe and reliable and is free of pollution, and the process is simple and easy to realize.

Description

technical field [0001] The invention relates to the technical fields of animal health care and veterinary medicine, in particular to a water-soluble florfenicol inclusion compound with high bioavailability and a preparation method thereof. Background technique [0002] Florfenicol is a new type of chloramphenicol antibiotic specially used in the animal health care market. Its biggest feature is that it has a broad antibacterial spectrum, good absorption, and wide distribution in the body, especially it has no potential aplastic anemia effect on sensitive bacteria. The curative effect on animal diseases is remarkable, and it is the first choice medicine for treating various infections caused by typhoid bacillus, paratyphoid bacillus and salmonella. Because chloramphenicol has severe adverse reactions of aplastic anemia, it has been banned in food animals. Therefore, florfenicol has broad application prospects in the prevention and treatment of food animal diseases. [0003] ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/69A61K47/38A61K47/26A61K47/18A61K47/20A61K47/10A61K47/32A61K47/12A61K31/165A61P31/04A61P1/00
CPCA61K47/38A61K31/165A61K47/10A61K47/12A61K47/18A61K47/183A61K47/20A61K47/26A61K47/32
Inventor 陆安张广智庞鑫郭宽杨春梅刘志杰王慧彬郭永国郭永红
Owner SHIJIAZHUANG WEIERLI ANIMAL PHARMA
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