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Moxidectin pour sprinkling preparation and preparation method thereof

A technology of moxictine pour-on and pour-on, which is applied in the field of preparation of moxictine pour-on and its industrialization, which can solve the problems of toxicity of aromatic hydrocarbons that are difficult to dissolve, toxicity of users and target animals, and easy volatilization. To achieve the effect of improving the tendency to cause explosion, good transdermal absorption effect, and improving toxicity

Active Publication Date: 2011-07-27
ZHEJIANG HISUN ANIMAL HEALTH PROD CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The strong solubility of aromatic hydrocarbons is Pour On increases the ease of operation of the preparation process, but aromatic hydrocarbons have disadvantages such as high toxicity, strong odor, low flash point (about 40°C), volatile, and easy to cause explosions.
Toxic and safety hazards for production personnel, users and target animals
In addition, the use of aromatic hydrocarbon solvents in my country is seldom used in medicine, so that the purity and quality of aromatic hydrocarbon solvents in my country still need to be improved compared with foreign countries. Therefore, it is not only uneconomical but also not environmentally friendly to use aromatic hydrocarbons to prepare moxictine pour-on formulations. unsafe
[0006] In view of the above shortcomings, in order to overcome the disadvantages of difficult dissolution of process configuration, toxicity of aromatic hydrocarbons and easy explosion

Method used

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  • Moxidectin pour sprinkling preparation and preparation method thereof
  • Moxidectin pour sprinkling preparation and preparation method thereof
  • Moxidectin pour sprinkling preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Embodiment 1: prepare moxictine pour-on

[0041] Raw materials

Dosage

Moxidectin

5g

tert-butyl hydroquinone

0.5g

anhydrous citric acid

0.5g

Isopropyl myristate

50.0g

Polyisobutylene (molecular weight 2400)

15.0g

Oil soluble purple

0.06g

medium chain triglycerides

Add to 100ml

[0042] Prepare the moxictine pouring agent with the method of the present invention, and specific method comprises the following steps:

[0043] 1) After weighing 5g of antiparasitic active substance moxictine, 0.5g of tert-butyl hydroquinone and 0.5g of anhydrous citric acid and mixing them uniformly, add them to 10ml of medium-chain triglycerides while stirring to make them dissolve;

[0044] 2) Weigh 15.0g of polyisobutylene and add it to 10ml of medium-chain triglyceride, add it while stirring, stir and dissolve until it becomes clear and transparent;

[0045] 3) Then weigh 0.06g of oil-so...

Embodiment 2

[0048] Embodiment 2: Preparation of moxictine pour-on

[0049] Raw materials

Dosage

Moxidectin

0.1g

tert-butyl hydroxyanisole

0.02g

Isopropyl myristate

30.0g

Polybutene (molecular weight 1900)

8.0g

Oil soluble purple

0.01g

liquid paraffin

Add to 100ml

[0050] Prepare the moxictine pouring agent with the method of the present invention, and specific method comprises the following steps:

[0051] 1) Weigh 0.1g of anti-parasitic active substance moxictine and 0.02g of tert-butyl hydroxyanisole and mix evenly, then add it into 10ml of liquid paraffin while stirring to dissolve it;

[0052] 2) Weigh 8.0g of polybutene and add it to 10ml of liquid paraffin, add it while stirring, stir and dissolve until it becomes clear and transparent;

[0053] 3) Then weigh 0.01g of oil-soluble purple, and add to 3ml of liquid paraffin while stirring to dissolve completely;

[0054] 4) Add the solution prep...

Embodiment 3

[0056] Embodiment 3: prepare moxictine pour-on

[0057] Raw materials

Dosage

Moxidectin

2.0g

tert-butyl hydroquinone

0.1g

Isopropyl myristate

20.0g

Polyisobutylene (molecular weight 1300)

20.0g

cottonseed oil

Add to 100ml

[0058] Prepare the moxictine pouring agent with the method of the present invention, and specific method comprises the following steps:

[0059] 1) Weigh 2.0 g of anti-parasitic active substance moxictin and 0.1 g of tert-butyl hydroquinone and mix evenly, then add it to 8 ml of cottonseed oil while stirring to dissolve it;

[0060] 2) Weigh 20.0g of polyisobutylene and add it to 15ml of cottonseed oil, add it while stirring, stir and dissolve until it becomes clear and transparent;

[0061] 3) Add the solution prepared in step 1) to the solution in step 2), stir for 0.5 hours and mix well;

[0062] 4) Weigh 20.0 g of isopropyl myristate and add it to the solution prepared in s...

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Abstract

The invention provides a novel and environmental-friendly Moxidectin pour sprinkling preparation and an industrialized preparation method thereof. The pour sprinkling preparation developed in the invention is prepared by taking Moxidectin as an active ingredient for resisting parasites inside and out of animals and adding an appropriate amount of auxiliaries, such as an antioxidant, a trandermal absorbent, an adhesive, an oil solvent and the like; and the formulation of the preparation is the oily pour sprinkling preparation and belongs to the field of novel veterinary medicinal antiparasitic preparations. The pour sprinkling preparation does not contain an aromatic compound with a low flash point and the potential safety hazard in industrial production. In order to improve medicinal effect, the trandermal absorbent is selected through an in-vitro trandermal absorption test so as to improve the bioavailability of the Moxidectin pour sprinkling preparation in the animals. The environmental-friendly Moxidectin pour sprinkling preparation which has a long-term effect, and is safe and easy to industrially produce is prepared finally.

Description

technical field [0001] The invention relates to a preparation for treating and preventing internal and external parasitic diseases of animals. Specifically, the invention relates to a novel environment-friendly moxictine pour-on agent and an industrialized preparation method thereof. Background technique [0002] Moxidectin, like Ivermetin and Avermectin, is a broad-spectrum, high-efficiency, new macrolide anthelmintic antibiotic widely used in veterinary clinics. It is a member of the Milbemycin family. The structural formula is as follows: [0003] [0004] Moxidectin differs from other macrolide antiparasitic drugs ivermetin and avermectin in that it is a single component with higher anthelmintic activity and Long-acting, safe and other characteristics, and it has strong anti-nematode and arthropod and other internal and external parasite activity at very low doses. Moxictine has a broad-spectrum anti-anthelmintic activity and is highly active against nematodes and ...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/365A61K47/32A61P33/14
Inventor 谢等龙邵伍军陈金凤王以跃陈国庆
Owner ZHEJIANG HISUN ANIMAL HEALTH PROD CO LTD
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