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Eprinomectin transdermal agent, preparation method and application

An ipremectin and ipremectin-containing technology, applied in the field of ipremectin transdermal agents, can solve the problems of unstable blood drug concentration, increased drug content, and decreased milk quality, and achieve no liver first pass Effect, low partition coefficient, small side effects

Active Publication Date: 2014-10-15
HUAZHONG AGRI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are many anthelmintics against gastrointestinal parasites in yaks, but most of them are administered orally and by injection. Oral and injection methods are difficult to implement on yaks that are not docile
Oral and injection administration has liver first-pass effect, blood drug concentration is unstable, short duration, etc. Oral administration often causes diarrhea, etc.
At the same time, many medicines require a long drug withdrawal period. When used on yaks in the milking period, the drug content in milk will increase and the milk quality will decline.

Method used

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  • Eprinomectin transdermal agent, preparation method and application
  • Eprinomectin transdermal agent, preparation method and application
  • Eprinomectin transdermal agent, preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] An eprimectin transdermal agent, which consists of the following parts by weight of raw materials:

[0043]

[0044] A preparation method of eprimectin transdermal agent, its steps are:

[0045] The first step: sample preparation, each penetration enhancer has five levels (as shown in the table of penetration enhancer levels), at 25℃, according to L 25 (5 6 ) 25 test samples were prepared in the first four columns, the first column is azone (a), the second column is oleic acid (b), the third column is propylene glycol (c), and the fourth column is dimethyl sulfoxide (d ), add four kinds of penetration enhancers, add 0.1 g of eprimectin to each sample, add 95% medical alcohol to make a 5mL sample, and mix the samples evenly.

[0046] Penetration enhancer level table

[0047]

[0048] Step 2: Perform an in vitro skin penetration test. Fix the skin of a Kunming mouse between the diffusion pool and the receiving pool of the YB-P6 smart transdermal tester, with the inner skin facing...

Embodiment 2-6

[0056] An eprimectin transdermal agent, which is composed of the following parts by weight of raw materials (Table 1):

[0057]

[0058] The preparation steps are the same as in Example 1.

[0059] The application of an eprimectin transdermal agent in the preparation of a medicine for treating or preventing gastrointestinal nematodes in yak, and the application process is:

[0060] Step 1: Test data and results of stability test

[0061] Temperature acceleration test Take 3 batches of samples and place them in a closed and dark container with a temperature of (40±2)℃ and a relative humidity of (75±5)% for 3 months. The three batches of samples decreased by 1.85%, 1.62%, and 2.63% (n=3) respectively after 3 months. There was no layering, precipitation or flocculation in each sample, and they were all slightly yellow and transparent liquids.

[0062] Light acceleration test Place 3 batches of samples in a light box, turn the samples regularly, and place them for 10 days at a temperature ...

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Abstract

The invention discloses an eprinomectin transdermal agent, a preparation method and application. The eprinomectin transdermal agent is composed of azone, oleic acid, propylene glycol, dimethyl sulfoxide and alcohole with a certain weight amount. The preparation method comprises: A, performing sample preparation, namely, setting five levels for each transdermal promoting agent, and adding alcohol for preparing samples; B, performing in-vitro transdermal experiments, fixedly disposing skin of a white mouse between a dispersion pool and a receiving pool of a YB-P6 intelligent transdermal tester, enabling the inner layer surface of skin to face to the receiving pool, enabling the whole dispersion pool to be full with the eprinomectin transdermal-agent formula sample, and adding acetonitrile to fill the receiving pool as a receiving solution; C, detecting the receiving solution obtained in the step B by using high performance liquid chromatographic instrument, and selecting a formula through visual analysis and variance analysis on an orthogonal experiment result; D, preparing the formula and verifying according to the front steps; and E, preparing a final product, and preparing a transdermal agent containing 0.025-0.1 g of eprinomectin. The formula is reasonable, convenient to use and capable of continuously expelling parasites without needing withdrawal time, and has the expelling rate of 90% or more on nematode and ectoparasites.

Description

Technical field [0001] The present invention relates to the technical field of eplamectin transdermal dosage forms, and more specifically to an eplamectin transdermal agent, and also relates to a preparation method of eplamectin transdermal agent. It also relates to the use of an eprimectin transdermal agent, which is mainly suitable for treating various gastrointestinal nematode diseases of yak and various ectoparasitic diseases such as lice, mites and flies in vitro. Background technique [0002] The yak has an obvious larval climax in winter and an obvious adult climax in spring. Due to the large number of adult worms in spring, problems such as a large number of nutrient capture, mechanical blockage of the intestines, toxic effects of parasite metabolites, and insect pathways caused by larval migration are the main causes of death of young yaks. the reason. There are many anthelmintics against gastrointestinal parasites in yak, but most of them are administered by oral or i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7048A61K9/00A61P33/14A61P1/00
Inventor 李家奎张可荣张鼎高建峰旦巴次仁韩照清刘梦媛
Owner HUAZHONG AGRI UNIV
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