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Abamectin transdermal solution and preparation method thereof

A technology of abamectin and solution, applied in the field of abamectin transdermal solution and its preparation, can solve the problem of strong skin irritation, large first-pass effect, inability to satisfy parasitic diseases and secondary infection of bacteria and fungi at the same time To meet the needs of treatment of sexual skin diseases and other issues, to achieve good stability, improve drug efficacy, reduce drug residues and side effects

Inactive Publication Date: 2021-08-06
WEIDA HUNAN TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The above two avermectin transdermal agents still have limitations in clinical use, such as large first-pass effect and strong skin irritation, which cannot meet the treatment needs for parasitic diseases and secondary infection bacterial and fungal skin diseases at the same time

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] An avermectin transdermal solution, in parts by weight, comprising 5 parts of avermectin, 20 parts of azone, 10 parts of sec-butyl acetate, 20 parts of ethyl acetate, N,N-dimethylethyl acetate 5 parts of amide, 5 parts of glycerol methylal, 5 parts of methylpyrrolidone.

[0024] The preparation method of described Abamectin transdermal solution, comprises the steps:

[0025] 1) After mixing ethyl acetate, sec-butyl acetate, and methylpyrrolidone, heat to 40-50° C. for 30 minutes, and add abamectin to dissolve;

[0026] 2) Add glycerol methylal and N,N-dimethylacetamide to the solution described in step 1) in turn, and after mixing uniformly into a clear solution, add azone ultrasonic stirring and mixing; wherein the ultrasonic treatment frequency is 50 kHz, Vacuum sterilized packaging.

Embodiment 2

[0028] An avermectin transdermal solution, in parts by weight, comprising 1 part of avermectin, 5 parts of azone, 5 parts of sec-butyl acetate, 5 parts of ethyl acetate, N,N-dimethylethyl acetate 15 parts of amides, 15 parts of glycerol methylal, and 15 parts of methylpyrrolidone.

[0029] The preparation method of described Abamectin transdermal solution, comprises the steps:

[0030] 1) After mixing ethyl acetate, sec-butyl acetate, and methylpyrrolidone, heat to 40-50° C. for 10 minutes, and add abamectin to dissolve;

[0031] 2) adding glycerol methylal and N,N-dimethylacetamide to the solution described in step 1) in turn, and after mixing uniformly into a clear solution, adding azone ultrasonic stirring and mixing, wherein the ultrasonic treatment frequency is 50kHz; Vacuum sterilized packaging.

Embodiment 3

[0033] An avermectin transdermal solution, in parts by weight, comprising 3 parts of avermectin, 10 parts of azone, 8 parts of sec-butyl acetate, 10 parts of ethyl acetate, N,N-dimethylethyl acetate 15 parts of amides, 9 parts of glycerol methylal, 7 parts of methylpyrrolidone, 3 parts of sucrose acetate isobutyrate, and 10 parts of benzyl alcohol.

[0034] The preparation method of described Abamectin transdermal solution, comprises the steps:

[0035] 1) After mixing ethyl acetate, sec-butyl acetate, and methylpyrrolidone, heat to 40-50° C. for 20 minutes, add benzyl alcohol to mix, and add abamectin to dissolve;

[0036] 2) Add glycerol methylal and N,N-dimethylacetamide to the solution described in step 1) in turn, and after mixing uniformly into a clear solution, add azone, ultrasonically stir and mix well, add sucrose acetate isobutyrate Mix well; the ultrasonic treatment frequency is 60 kHz, and it is obtained by vacuum sterilization and packaging.

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PUM

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Abstract

The invention provides an abamectin transdermal solution and a preparation method thereof. The abamectin transdermal solution comprises abamectin, azone, sec-butyl acetate, ethyl acetate, N, N-dimethylacetamide, glycerol methylal and methyl pyrrolidone. The azone and the methyl pyrrolidone are used as composite penetrating agents, and sucrose acetate isobutyrate and benzyl alcohol are used as sustained-release transdermal enhancers, so that the treatment effect is prolonged under the action of the sustained-release transdermal enhancers while the rapid penetration treatment of the abamectin transdermal solution is ensured. The sec-butyl acetate, the ethyl acetate, the N, N-dimethylacetamide and the glycerol methylal are used as a mixed solvent, so that the stability of veterinary drugs can be improved, the viscosity can be reduced, drug residues and toxic and side effects can be reduced, and a synergistic effect can be achieved.

Description

technical field [0001] The invention relates to the technical field of veterinary drugs, in particular to an abamectin transdermal solution and a preparation method thereof. Background technique [0002] Abamectin is a class of 16-membered macrolide compounds with insecticidal, acaricidal and nematicidal activities first developed by Kitasato University, Japan, and Merck Company. It is fermented by Streptomyces avermitilis. produce. Natural Abamectin contains 8 components, mainly including 4 kinds, namely A1a, A2a, B1a and B2a, the total content of which is ≥ 80%; the corresponding 4 homologues with smaller proportions are A1b, A2b, B1b and B2b , its total content ≤ 20%. Avermectin pesticides currently available in the market use abamectin as the main insecticidal component (Avermectin B1a+B1b, where B1a is not less than 90% and B1b is not more than 5%), and is calibrated by the content of B1a. Abamectin has the characteristics of novel structure, high efficiency, broad s...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K47/26A61K47/10A61K47/22A61K47/14A61K47/18A61K31/7048A61P31/10A61P31/04A61P31/02A61P17/00A61P33/14
CPCA61K9/08A61K9/0014A61K47/26A61K47/10A61K47/22A61K47/14A61K47/18A61K31/7048A61P31/10A61P31/04A61P31/02A61P17/00A61P33/14
Inventor 刘云福王兹舜陈国英李蔚徐楚维
Owner WEIDA HUNAN TECH
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