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A kind of ipremectin transdermal agent and its preparation method and application

A technology of epromectin and transdermal agent, which is applied to the preparation of epramectin transdermal agent, and the field of eprmectin transdermal agent dosage form, can solve the problem of unstable blood drug concentration, increased drug content, and duration of It can achieve the effect of no liver first-pass effect, low distribution coefficient, and small side effects.

Active Publication Date: 2017-02-22
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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  • A kind of ipremectin transdermal agent and its preparation method and application
  • A kind of ipremectin transdermal agent and its preparation method and application
  • A kind of ipremectin transdermal agent and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] A kind of ipremectin transdermal agent, it is made up of the raw material of following parts by weight:

[0043]

[0044] A preparation method of ipremectin transdermal agent, the steps are:

[0045] Step 1: Sample preparation Set five levels for each skin penetration enhancer (as shown in the skin penetration enhancer level table), at 25°C, according to L 25 (5 6 ) Prepare 25 test samples 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 transdermal enhancers respectively, add 0.1 g of ipremectin to each sample, add 95% medical alcohol to make a 5mL sample, and mix the sample evenly.

[0046] Skin penetration enhancer level table

[0047]

[0048] The second step: for in vitro transdermal test, fix the skin of Kunming mice between the diffusion cell and the receiving cell of the YB-P6 intelligent transdermal...

Embodiment 2-6

[0056] A kind of ipremectin transdermal agent, it is made up of the raw material of following weight parts (table 1):

[0057]

[0058] Its preparation steps are identical with embodiment 1.

[0059] An application of an ipremectin transdermal agent in the preparation of medicines for treating or preventing yak gastrointestinal nematodes, the application process is:

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

[0061] Temperature acceleration test Take 3 batches of samples and put them in a closed 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) after 3 months, respectively. No delamination, precipitation, and flocs were found in each sample, and they were all light yellow and transparent liquids.

[0062] Illumination acceleration test Put 3 batches of samples in the light box for irradiation, turn the samples regularly, and place them for 10 days...

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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 the dosage form of ipremectin transdermal agent, more specifically relates to an ipremectin transdermal agent, and also relates to a preparation method of the ipremectin transdermal agent. The invention also relates to the use of an ipremectin transdermal agent, which is mainly suitable for treating various gastrointestinal nematode diseases of yaks and various ectoparasitic diseases such as lice, mites and flies outside the body. Background technique [0002] There is an obvious larval orgasm in yaks in winter and an obvious adult orgasm in spring. Due to the mass reproduction of adults in spring, it brings about a large amount of deprivation of nutrients, mechanical blockage of the intestinal tract, poisoning of parasite metabolites, and insect passages caused by larval migration, which are the main reasons for the death of young yaks due to spring fatigue. reason. There are many anthelmintics...

Claims

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Application Information

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Patent Type & Authority Patents(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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