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Ultrahigh-water-solubility and high-bioavailability aureomycin hydrochloride

A chlortetracycline hydrochloride and water-soluble technology, which is applied in the field of veterinary drugs, can solve the problems of low bioavailability and low solubility of chlortetracycline hydrochloride, and achieve the goals of increasing the dissolution rate, increasing the contact area, and increasing the biological activity Effect

Pending Publication Date: 2022-04-05
PUCHENG CHIA TAI BIOCHEM
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The purpose of the present invention is to provide a kind of ultra-high water-solubility and high bioavailability aureomycin hydrochloride for the problem of low solubility and low bioavailability of aureomycin hydrochloride in the prior art

Method used

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  • Ultrahigh-water-solubility and high-bioavailability aureomycin hydrochloride
  • Ultrahigh-water-solubility and high-bioavailability aureomycin hydrochloride

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0063] A kind of aureomycin hydrochloride with ultra-high water solubility and high bioavailability is obtained by the following preparation method, comprising the steps of:

[0064] Cool the chlortetracycline fermentation broth to 2°C, and add purified water equivalent to 1.0 times the volume of the chlortetracycline fermentation broth;

[0065] Then add oxalic acid at a ratio of 2.0 g per 100 mL of aureomycin fermentation broth, and adjust the pH to 1.3 with hydrochloric acid;

[0066] Then add yellow blood salt sodium in a ratio of 0.15g per 100mL aureomycin fermentation broth, and stir for 25min;

[0067] Then add zinc sulfate at a ratio of 0.2 g per 100 mL of aureomycin fermentation broth, and stir for 25 min;

[0068] The obtained acidified solution is subjected to plate and frame pressure filtration, the filtrate is collected, the mycelia residue is washed with acid water having a pH of 1.5, the filtrate and the lotion are combined, the plate and frame re-filtration is...

Embodiment 2

[0086] A kind of aureomycin hydrochloride with ultra-high water solubility and high bioavailability is obtained by the following preparation method, comprising the steps of:

[0087] 1) Acidification of fermentation broth:

[0088] Cool the chlortetracycline fermentation broth to 0°C, and add purified water equivalent to 1.2 times the volume of the chlortetracycline fermentation broth;

[0089] Then add oxalic acid at a rate of 1.5 g per 100 mL of aureomycin fermentation broth, and adjust the pH to 1.4 with hydrochloric acid;

[0090] Add yellow blood salt sodium at a ratio of 0.1 g per 100 mL of aureomycin fermentation liquid, and stir for 20 min;

[0091] Then add zinc sulfate at a ratio of 0.1 g per 100 mL of aureomycin fermentation broth, and stir for 20 min;

[0092] The obtained acidified solution is subjected to plate and frame pressure filtration, the filtrate is collected, the mycelia residue is washed with acid water having a pH of 1.5, the filtrate and the lotion ...

Embodiment 3

[0110] A kind of aureomycin hydrochloride with ultra-high water solubility and high bioavailability is obtained by the following preparation method, comprising the steps of:

[0111] 1) Acidification of fermentation broth:

[0112] Cool the chlortetracycline fermentation broth to 5°C, and add purified water equivalent to 0.5 times the volume of the chlortetracycline fermentation broth;

[0113] Then add oxalic acid at a ratio of 2.5 g per 100 mL of aureomycin fermentation liquid, and adjust the pH to 1.2 with hydrochloric acid;

[0114] Then add yellow blood salt sodium in a ratio of 0.2 g per 100 mL of aureomycin fermentation broth, and stir for 30 min;

[0115] Then add zinc sulfate at a rate of 0.3 g per 100 mL of aureomycin fermentation broth, and stir for 30 min;

[0116] The obtained acidified solution is subjected to plate and frame pressure filtration, the filtrate is collected, the mycelia residue is washed with acid water having a pH of 1.5, the filtrate and the lo...

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Abstract

The invention discloses chlortetracycline hydrochloride with ultrahigh water solubility and high bioavailability, the apparent solubility of the chlortetracycline hydrochloride is greater than or equal to 0.9 g / 100ml, and when the concentration is gt; when the weight is 0.9 g / 100ml, the emulsion is in an emulsified state and is not layered or precipitated after being placed for a long time; the preparation method comprises the following steps: (1) acidifying fermentation liquor; 2) double salt; 3) coarse crystallization; (4) recrystallizing; 5) performing high-pressure homogenization: performing high-pressure homogenization treatment on the material obtained in the step 2) by taking purified water as a dispersion medium according to a water-material ratio of 1: (1-1.5) for 10-12 times; and 6) spray drying: carrying out spray drying treatment on the material obtained in the previous step, controlling the feeding frequency to be 20Hz and the air inlet temperature to be 175-180 DEG C to obtain the ultrahigh water-soluble chlortetracycline hydrochloride.

Description

technical field [0001] The invention belongs to the technical field of veterinary drugs, in particular to aureomycin hydrochloride with ultrahigh water solubility and high bioavailability. Background technique [0002] Chlortetracycline hydrochloride, also known as chlortetracycline hydrochloride, has the same antibacterial spectrum as tetracycline, and its curative effect on penicillin-resistant Staphylococcus aureus is slightly stronger than tetracycline. Chlortetracycline hydrochloride is prepared by acidifying, separating, double salting, crystallization, recrystallization and other processes from the fermentation broth of aureomycin. [0003] Chlortetracycline hydrochloride is used to treat conjunctivitis, trachoma, etc., but it is mainly used to prevent and treat diseases such as colibacillosis and mycoplasma synovialis in chickens; There are problems such as low solubility and low bioavailability. The solubility of chlortetracycline hydrochloride in water at room te...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C231/24C07C237/26
Inventor 张君启宁富豪黄小毛陈浩然吴新芝杨占英李书至朱正江
Owner PUCHENG CHIA TAI BIOCHEM
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