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Stable oily avermectin pouring agent and preparation method thereof

A kind of ivermectin pouring agent and ivermectin technology, applied in the field of oily ivermectin pouring agent and preparation thereof, can solve the problem of not reporting cattle as the target animal antiparasitic test, not disclosing formulation stability Data and other issues, to achieve the effects of excellent skin penetration, wide range of insect repellants, and strong adhesion

Inactive Publication Date: 2015-07-01
JINHE ANIMAL PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the invention reported the acute toxicity, allergic reaction, irritation and dog drug efficacy test of skin protection, it did not disclose the stability data of the preparation, and the most important indicators such as transdermal absorption and bioavailability of the transdermal absorption preparation. No reports of antiparasitic trials targeting cattle

Method used

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  • Stable oily avermectin pouring agent and preparation method thereof
  • Stable oily avermectin pouring agent and preparation method thereof
  • Stable oily avermectin pouring agent and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Embodiment 1 The ivermectin pouring agent prescription of the present invention is preferred

[0051] Ivermectin is practically insoluble in water, readily soluble in methanol, ethyl acetate or chloroform, and soluble in ethanol or acetone. In order to release the drug slowly, the effective blood drug concentration can be maintained for a long time, so as to achieve a better therapeutic purpose, the penetration enhancer is selected as isopropyl myristate, the solvent is isopropanol, and the emulsifier is cetearyl Alcohol ethylhexanoate, buffered as triethanolamine; combination of isopropyl myristate and cetearyl ethylhexanoate as emollient. According to the role of each excipient, other components were fixed, and isopropyl myristate and cetearyl ethyl hexanoate were selected for the test with 2 factors and 3 levels. The specific composition of every 100ml ivermectin pour-on is:

[0052] 0.5g of ivermectin, 18-22ml of emollient, 0.05ml of triethanolamine, 0.01g of pate...

Embodiment 2

[0085] Example 2 Optimal selection of influencing factors for skin penetration

[0086] Preliminary experiments found that the amount of emollient used in the pour-on and the pH value of the preparation have a greater impact on the skin penetration of the pour-on. Therefore, based on the formulation 5 screened out in Example 1, the following studies were conducted.

[0087] 1. The effect of the proportion of emollient dosage (different viscosities) in the prescription on the cumulative penetration

[0088] When the emollient accounts for 10%, 20%, 30%, 40%, 50%, 60%, and 70% of the weight percentage of the formula, use the NDJ-5S digital display viscometer to measure the viscosity of the solution, and use the RYJ-6B type Transdermal diffusion meter was used to measure the cumulative permeation amount of the solution at 24H, and the results are shown in Table 7.

[0089] Table 7 Effect of different emollient dosage on penetration

[0090]

[0091] It can be seen from Ta...

Embodiment 3

[0097] Example 3 A kind of ivermectin pouring agent

[0098] Prescription (100L):

[0099]

[0100] The ivermectin pouring agent described in this embodiment is prepared through the following steps:

[0101] 1) Purge the magnetic stirring tank with nitrogen gas of 1 Pa for three times with a tank pressure, then reduce the nitrogen pressure to 0.2 Pa, and continue until the end of the preparation process;

[0102] 2) Rinse the magnetic stirring tank with an appropriate amount of isopropanol, then add about 40L of isopropanol to the beaker, turn on the magnetic stirring tank, and rotate at 130RPM;

[0103] 3) Add 500g of ivermectin into a magnetic stirring tank, stir for 15 minutes to dissolve until clear;

[0104] 4) Add 2L of isopropyl myristate and 18L of cetearyl ethylhexanoate into a magnetic stirring tank, and stir for 15 minutes;

[0105]5) Add 0.05 L of triethanolamine into the magnetic stirring tank, stir for 15 minutes, and measure the pH value to make it betwe...

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Abstract

The invention provides a stable oily avermectin pouring agent and a preparation method thereof. A pH value of the avermectin pouring agent is equal to 5-7, and the viscosity is 40-80 centipoise; the avermectin pouring agent comprises avermectin, an emollient, a pH buffering agent and an oil solvent, wherein the emollient is prepared from isopropyl myristate and cetearyl ethylhexanoate in a volume ratio of (1:1) to (1:11); the buffering agent is triethanolamine; the oil solvent is isopropanol. The avermectin pouring agent has the advantages of good transdermal absorbability, good stability, convenient use, and good effect on control of livestock endoparasites and ectoparasites.

Description

technical field [0001] The invention belongs to the field of veterinary drug preparations, and in particular relates to an oily ivermectin pour-on and a preparation method thereof. Background technique [0002] Ivermectin is the reduction product of Avermectin after chemical hydrogenation. Its anthelmintic and insecticidal mechanism is special, which is different from general anthelmintic drugs: it mainly acts on the nervous system of parasites, blocking the conduction of nerve impulses, leading to paralysis and death of parasites. Ivermectin has a powerful killing effect on worms, nematodes and roundworms of livestock and poultry, and is widely used in the prevention and control of parasites in cattle, sheep, pigs, poultry and pet cats and dogs, such as various gastrointestinal tracts of cattle Nematodes, lungworms, sucking nematodes and ectoparasites psoriasis, itch mites, scabies, lice; sheep various gastrointestinal nematodes and ectoparasites itch mites, scabies, hair ...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/7048A61P33/00A61P33/10A61P33/14
Inventor 李荣顺王文龙路赟
Owner JINHE ANIMAL PHARMA
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