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Preparation method of tiamulin/tiamulin salt micro-capsule

A tiamulin and formaldehyde technology, applied in microcapsules, capsule delivery, antibacterial drugs, etc., can solve the problems of strong respiratory tract irritation, obvious side effects, low bioavailability, etc., to reduce irritation, improve stability and bioavailability The effect of utilization and reduction of incompatibility

Inactive Publication Date: 2012-10-24
宁夏泰瑞制药股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Tiamulin salts are all in powder state, with small specific gravity, strong respiratory irritation to humans and animals, obvious side effects, and low bioavailability

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] The preparation method of tiamulin microcapsules:

[0021] (1) Add zein aqueous solution with a mass concentration of 2% to 8% to tiamulin, and the volume of the zein aqueous solution added is 3 times the mass of tiamulin. Stir well, mix well, heat slowly to 50°C, and keep warm for 0.5~1h.

[0022] (2) Slowly add 0.5 times the volume of the above mixed solution of formaldehyde, stir for 0.5~1h until the cross-linking solidifies, and wash with 2~3 times the volume of isopropanol.

[0023] (3) Suction filtration, wash with 5~6 times of isopropanol-petroleum ether mixture with a volume ratio of 1:1, until formaldehyde is removed.

[0024] (4) Vacuum dry at 50~60°C until the loss on drying is less than 1%.

Embodiment 2

[0026] The preparation method of tiamulin microcapsules:

[0027] (1) Add 2% to 8% gelatin protein aqueous solution to tiamulin, and the volume of gelatin protein aqueous solution added is 3 times the mass of tiamulin. Stir well, mix well, heat slowly to 50°C, and keep warm for 0.5~1h.

[0028] (2) Slowly add 1 times the volume of the above mixed solution of formaldehyde, stir for 0.5~1h until the cross-linking is solidified, and wash with 2~3 times the volume of isopropanol.

[0029] (3) Suction filtration, wash with 5~6 times of isopropanol-petroleum ether mixture with a volume ratio of 1:1, until formaldehyde is removed.

[0030] (4) Vacuum dry at 50~60°C until the loss on drying is less than 1%.

Embodiment 3

[0032] The preparation method of tiamulin microcapsules:

[0033] (1) Add 2%~8% serum protein aqueous solution to tiamulin, and the volume of gelatin protein aqueous solution is 4 times the mass of tiamulin. Stir well, mix well, heat slowly to 60°C, and keep warm for 0.5~1h.

[0034] (2) Slowly add 1 times the volume of the above mixed solution of formaldehyde, stir for 0.5~1h until the cross-linking is solidified, and wash with 2~3 times the volume of isopropanol.

[0035] (3) Suction filtration, wash with 5~6 times of isopropanol-petroleum ether mixture with a volume ratio of 1:1, until formaldehyde is removed.

[0036] (4) Vacuum dry at 50~60°C until the loss on drying is less than 1%.

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Abstract

The invention provides a preparation method of a tiamulin / tiamulin salt micro-capsule. The preparation method is characterized by comprising the following steps: adding corn protein aqueous solution or glutin aqueous solution in tiamulin / tiamulin salt, completely stirring to obtain uniform mixed solution; slowly heating to 50-60 DEG C, preserving the heat for 0.5-1h, and then crosslinking and curing with formaldehyde serving as a crosslinking agent; washing with isopropanol, carrying out suction filtering, washing a filter cake with isopropanol-petroleum ether till formaldehyde is completely washed away; drying till the drying loss is less than 1%, thus obtaining the tiamulin / tiamulin salt micro-capsule. The preparation method can be used for preparing the tiamulin / tiamulin salt micro-capsule which can be directly applied to animal feed; and the prepared tiamulin / tiamulin salt micro-capsule has the advantages that irritation to respiratory tracts of people and animals can be reduced and the stability and the medicinal bioavailability of medicinal preparations can be improved. The preparation method is simple.

Description

technical field [0001] The invention belongs to the field of veterinary antibiotic preparations, in particular to a method for preparing tiamulin or tiamulin salt microcapsules. Background technique [0002] Tiamulin is a diterpene antibiotic produced by semi-synthesis after obtaining pleuromutilin by fermenting and cultivating the higher fungus Basidiomycete Pleurotus mutilus. Tiamulin belongs to a relatively new antibiotic, which is a special antibiotic for animals. It has special effects on many Gram-positive bacteria and mycoplasma. Reproductive respiratory tract maintains higher concentrations. In particular, it has a strong effect on Staphylococcus aureus, Streptococcus, various mycoplasma and some spirochetes. [0003] Tiamulin has been used to prevent pig diseases since 1978. It can effectively prevent and treat endemic pneumonia (asthma), mycoplasma arthritis, actinobacillus pleurisy, swine dysentery, ileitis and edema in pigs. This product is only used as a vete...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/50A61K31/22A61P31/04
Inventor 王义王彬任勇周丽娜
Owner 宁夏泰瑞制药股份有限公司
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