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Closantel or its sodium salt long-acting sustained-release injection and preparation thereof

A technology of iodoclosamide and sustained-release injections, which is applied in the direction of pharmaceutical formulations, nitrile/isonitrile active ingredients, oil/fat/wax non-active ingredients, etc., and can solve the problem of lack of long-term anti-parasitic activity and drug effect time Short and other problems, to achieve the effect of convenient storage and transportation, good stability and stable release

Inactive Publication Date: 2010-06-16
NORTHWEST A & F UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In view of the defects and deficiencies in the prior art, the object of the present invention is to provide a long-acting sustained-release injection of closantamide or its sodium salt suitable for veterinary clinical application, which solves the problem of closantamide or its sodium salt. The traditional preparations of sodium salt have the problems of short drug effect time and no long-term antiparasitic activity

Method used

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  • Closantel or its sodium salt long-acting sustained-release injection and preparation thereof
  • Closantel or its sodium salt long-acting sustained-release injection and preparation thereof
  • Closantel or its sodium salt long-acting sustained-release injection and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] 1) Put 80 parts of castor oil for injection into a beaker and heat it to 50°C; then weigh 2 parts of aluminum monostearate into the castor oil, stir to form a white uniform paste, and swell for 10 hours. Heat the swollen white pasty mixture to 130°C while stirring to make it completely transparent, let it cool to 50°C, and filter through a vertical melting funnel to obtain light yellow transparent aluminum monostearate castor oil gel.

[0020] 2) Weigh 10 parts of iodosamide crude drug, add 40 parts of absolute ethanol, fully shake to dissolve, and filter with a 0.45 μm microporous membrane. Under sterile conditions, slowly add the filtrate to 80 parts of aluminum monostearate castor oil gelatin at 50°C, and stir while adding to form a light yellow transparent liquid, then heat up to 60°C to evaporate 20 parts of absolute ethanol , and subpackage after cooling to obtain a 10% closantamide long-acting sustained-release injection.

Embodiment 2

[0022] 1) Put 50 parts of castor oil for injection into a beaker and heat it to 50°C; then weigh 2 parts of aluminum stearate into the castor oil, stir to form a white uniform paste, and swell for 10 hours. Heat the swollen white pasty mixture to 130°C while stirring to make it completely transparent, let it cool to 50°C, and filter through a vertical melting funnel to obtain light yellow transparent aluminum stearate castor oil gel.

[0023] 2) Weigh 15 parts of iodosamide crude drug, add 60 parts of absolute ethanol, fully shake to dissolve, and filter with a 0.45 μm microporous membrane. Under sterile conditions, slowly add the filtrate to 50 parts of aluminum stearate castor oil gelatin at 50°C, and stir while adding to form a light yellow transparent liquid, heat up to 60°C to evaporate 10 parts of absolute ethanol, After cooling, sub-package to obtain 15% closantamide long-acting sustained-release injection.

Embodiment 3

[0025] 1) Put 50 parts of castor oil for injection into a beaker and heat it to 50°C; then weigh 1 part of aluminum monostearate into the castor oil, stir to form a white uniform paste, and swell for 10 hours. Heat the swollen white pasty mixture to 140°C while stirring to make it completely transparent, let it cool to 50°C, and filter through a vertical melting funnel to obtain light yellow transparent aluminum monostearate castor oil gel.

[0026] 2) Weigh 10 parts of iodosamide sodium crude drug, add 40 parts of dimethyl sulfoxide and 10 parts of absolute ethanol, fully shake to dissolve, and filter with a 0.45 μm microporous membrane. Under sterile conditions, slowly add the filtrate to 50 parts of aluminum monostearate castor oil gelatin at 50°C, and stir while adding to form a light yellow transparent liquid. % Closantamide Sodium Long-acting Sustained Release Injection.

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Abstract

The present invention discloses a closantel or closantel sodium long effect sustained-release injection which consists of 1 to 20 portions of the closantel or closantel sodium, 4 to 60 portions of organic solvent, 0.2 to 4 portions of aluminum stearate or aluminum monostearate and 50 to 100 portions of castor oil for injection. A preparation method is that: firstly, aluminum stearate or aluminum monostearate castor oil factice is prepared; then the organic solvent of the closantel or closantel sodium is slowly added into the aluminum stearate or aluminum monostearate castor oil factice with the temperature of 50 DEG C to be stirred completely to form light yellow transparent liquid, the temperature is risen to 60 to 70 DEG C, the solvent with proper quantity is vaporized, and the present invention is obtained after being cooled and packed. The present invention has the simple preparation method and stable storage, which not only keeps the advantages of the traditional preparation typeof the closantel or closantel sodium of wide anti-insect spectrum, strong activity, etc. but the present invention can also be released inside the animal body slowly and stably for a long time, and the preventive and curative effect of one time of medication can act for three to four months.

Description

technical field [0001] The invention relates to the field of veterinary medicine, in particular to a broad-spectrum antiparasitic drug-closantamide or its sodium salt long-acting sustained-release injection and a preparation method thereof. Background technique [0002] Closantel or Closantel Sodium (Closantel or Closantel Sodium) is a new synthetic drug in the sulphamide compounds, and is a broad-spectrum anthelmintic used for the treatment and prevention of parasitic infections in cattle and sheep. Oral or parenteral and other forms of administration, but its oral bioavailability is only 50% of subcutaneous or intramuscular injection. The drug is safe for clinical use and has no toxic and side effects. In 1993, it was approved as a second-class new veterinary drug by the Ministry of Agriculture. [0003] Closantamide or its sodium salt is a strong oxidative phosphorylation uncoupling agent, which can inhibit the phosphorylation process of mitochondria in worms, thereby p...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/08A61K31/275A61K47/12A61K47/44A61P33/00
Inventor 欧阳五庆张文娟
Owner NORTHWEST A & F UNIV
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