Novel preparation of tilmicosin and salt of same for livestock and preparation method thereof

A technology of tilmicosin and preparations, which is applied in the field of veterinary antibiotic preparations, can solve the problems of insignificant curative effect, large toxic and side effects, etc., and achieve the effects of significant curative effect, small toxic and side effects, and increased drug concentration

Inactive Publication Date: 2009-12-02
BEIJING DABEINONG ANIMAL HEALTH TECH +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The purpose of the present invention is to provide a novel preparation of tilmicosin and its salts for veterinary use that efficiently treats the lung infection of livestock and poultry. The drug concentration in

Method used

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  • Novel preparation of tilmicosin and salt of same for livestock and preparation method thereof
  • Novel preparation of tilmicosin and salt of same for livestock and preparation method thereof
  • Novel preparation of tilmicosin and salt of same for livestock and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0021] Embodiment 1 Preparation of Veterinary Tilmicosin Lung Targeting Microspheres

[0022] (1) Take 0.4g of gelatin, add 4ml of distilled water, and swell completely in a 60°C water bath to obtain a 10% gelatin solution; add 0.4g of tilmicosin, stir well to mix, and preheat in a 60°C water bath;

[0023] (2) Drop the gelatin solution into a beaker containing 1ml Span-80 and 60ml liquid paraffin, stir in a water bath at 60°C for 15min until milky white, at a speed of 1000r / min;

[0024] (3) Rapidly cool in an ice-water bath to below 5°C, add 3ml of formaldehyde in a thin stream, continue to stir for 30min to cross-link and solidify, dehydrate and stir with 30ml of isopropanol for 10min, and filter with suction;

[0025] (4) Wash with a small amount of isopropanol-ether to remove formaldehyde, wash off the liquid paraffin on the surface of the microspheres with petroleum ether, and dry in vacuum.

Embodiment 2

[0026] Example 2 Preparation of Tilmicosin Lung Targeting Microspheres for Veterinary Use

[0027] (1) Take 0.8g of gelatin, add 4ml of distilled water, and swell completely in a 55°C water bath to obtain a 20% gelatin solution; add 0.1g of tilmicosin, stir well to mix, and preheat in a 55°C water bath;

[0028] (2) Drop the gelatin solution into a beaker containing 1ml Span-60 and 60ml liquid paraffin, stir in a water bath at 55°C for 15min until milky white, at a speed of 1000r / min;

[0029] (3) Rapidly cool in an ice-water bath to below 5°C, add 3ml of glutaraldehyde in a thin stream, continue to stir for 30min to cross-link and solidify, dehydrate with 30ml of isopropanol and stir for 10min, and filter with suction;

[0030] (4) Wash with a small amount of isopropanol-ether to remove the glutaraldehyde, wash off the liquid paraffin on the surface of the microspheres with petroleum ether, and dry in vacuum.

Embodiment 3

[0031] Embodiment 3 preparation of veterinary tilmicosin lung targeting microspheres

[0032] (1) Take 0.4g of gelatin, add 4ml of distilled water, and swell completely in a water bath at 65°C to obtain a 10% gelatin solution. Add 0.1g tilmicosin, stir well to mix, and preheat in a 65°C water bath;

[0033] (2) Drop the gelatin solution into a beaker containing 1ml Span-40 and 60ml liquid paraffin, stir in a water bath at 65°C for 15min until milky white, at a speed of 1000r / min;

[0034] (3) Rapidly cool in an ice-water bath to below 5°C, add 3ml of glutaraldehyde in a thin stream, continue to stir for 30min to cross-link and solidify, dehydrate with 30ml of isopropanol and stir for 10min, and filter with suction;

[0035] (4) Wash with a small amount of isopropanol-ether to remove the glutaraldehyde, wash off the liquid paraffin on the surface of the microspheres with petroleum ether, and dry in vacuum.

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Abstract

The invention belongs to the veterinary antibiotics preparation field and relates to a novel preparation of tilmicosin and salt of same for livestock and a preparation method thereof. The preparation is of lung targeting gelatin microsphere preparation by using tilmicosin or tilmicosin salt as principal components. Clinical drug experiments show that compared with conventional preparations the lung targeting gelatin microsphere of tilmicosin and tilmicosin salt of the invention has better organization selectivity, the drug concentration of lung tissue is higher, the duration is longer, the drug effect is longer and more effective and the side effect is low.

Description

technical field [0001] The invention belongs to the field of veterinary antibiotic preparations, and relates to a novel preparation of tilmicosin for animals and a salt thereof and a preparation method thereof. Background technique [0002] Tilmicosin (Tllmicosin) is a macrolide semi-synthesized by tylosin antibiotics for livestock and poultry. It was successfully developed by the British Elanco Animal Health Products Company in the 1980s and has been approved for clinical use in cattle, goats, Infectious diseases caused by sensitive bacteria in sheep, dairy cows, pigs, chickens and other animals, especially respiratory tract infections of livestock and poultry. Tilmicosin has similar antibacterial activity to tylosin, and has inhibitory effects on gram-positive bacteria and some gram-negative bacteria, mycoplasma, spirochetes, etc. Mycoplasma avium has stronger antibacterial activity than tylosin. [0003] Tilmicosin is used to treat bacterial infections of the respirator...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K9/14A61K31/706A61K47/42A61P31/00A61P11/00
Inventor 田玲莫云刘澜葛冰郭致君张俊儒
Owner BEIJING DABEINONG ANIMAL HEALTH TECH
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