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Oral ivermectin microemulsion concentrate and preparation method and application thereof

A technology of microemulsion concentrate and ivermectin, which is applied in the directions of emulsion delivery, pharmaceutical formulations, and medical preparations containing active ingredients, etc. question

Inactive Publication Date: 2015-06-17
天津迈迪瑞康生物医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

As is well known to those skilled in the art, the appearance of this type of preparation is milky white liquid, which cannot form a transparent solution when added to water, which affects the feeding of poultry and animals; and the product must be strictly avoided from freezing, and the breeding areas in my country are mostly distributed in the north, which poses a problem for transportation and storage in winter. bring inconvenience

Method used

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  • Oral ivermectin microemulsion concentrate and preparation method and application thereof
  • Oral ivermectin microemulsion concentrate and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0125] Example 1: Preparation of Oral Ivermectin Microemulsion Concentrate Sample 1

[0126] Its composition is as follows:

[0127] Ivermectin 10g

[0128] Medium-chain fatty acid glycerides (Capmul MCM, Abitec) 52g

[0129] 1,2-Propanediol 11.7 g

[0130] PEG400 6.8 g

[0131] Soy Lecithin 9.3g

[0132] Polyethylene glycol lauryl hydroxystearate (Solutol HS 15, BASF) 6.8 g

[0133] Tween 80 2.9 g

[0134] Oleic acid 0.3 g

[0135] Vitamin E 0.2g

[0136] The preparation method of the oral ivermectin microemulsion concentrate is as follows:

[0137] 1) At 20°C, add the above-mentioned weight of soybean lecithin to medium-chain fatty acid glycerides, and stir at 8000 rpm to form a clear and clear solution;

[0138] 2) Add the above weight of ivermectin, 1,2-propylene glycol, PEG400, polyethylene glycol lauryl hydroxystearate, Tween 80, oleic acid, and vitamin E to step 1) at 45°C The product is continuously stirred under stirring conditions of 1000 rpm until the entire system is transparent an...

Embodiment 2

[0140] Example 2: Preparation of Oral Ivermectin Microemulsion Concentrate Sample 2

[0141] Its composition is as follows:

[0142] Ivermectin 6.8g

[0143] Medium-chain fatty acid glycerides (Capmul MCM, Abitec) 61 g

[0144] 1, 2-propanediol 10.6 g

[0145] Soy Lecithin 6.8g

[0146] Polyglycerol oleate 4.8g

[0147] Polyethylene glycol lauryl hydroxystearate (Solutol HS 15, BASF) 6.3 g

[0148] Tween 80 3.5g

[0149] 0.2 grams of oleic acid;

[0150] The preparation method of the oral ivermectin microemulsion concentrate is as follows:

[0151] 1) At 25°C, add the above-mentioned weight of soybean lecithin and polyglyceryl oleate to medium-chain fatty acid glyceride, and stir at 1000 rpm until a transparent and clear solution is formed;

[0152] 2) Add the above weight of ivermectin, 1, 2-propanediol, polyethylene glycol lauryl stearate, Tween 80, and oleic acid to the product of step 1) at 25°C, and Stirring was continued under 200rpm stirring conditions until the entire system was trans...

Embodiment 3

[0154] Example 3: Preparation of Oral Ivermectin Microemulsion Concentrate Sample 3

[0155] Its composition is as follows:

[0156] Ivermectin 8.1 g

[0157] Medium-chain fatty acid glycerides (Capmul MCM, Abitec) 53g

[0158] 1,2-Propanediol 11.9 g

[0159] PEG400 7.2 g

[0160] Soy Lecithin 9.5g

[0161] Polyethylene glycol lauryl hydroxystearate (Solutol HS 15, BASF) 6.9 g

[0162] Tween 80 2.9 g

[0163] Sodium oleate 0.3 g

[0164] Vitamin E 0.2g

[0165] The preparation method of the oral ivermectin microemulsion concentrate is as follows:

[0166] 1) At 25°C, add the above-mentioned weight of soybean lecithin to medium-chain fatty acid glycerides, and stir at 3000 rpm until a clear and clear solution is formed;

[0167] 2) Add the above weight of ivermectin, 1,2-propylene glycol, PEG400, polyethylene glycol lauryl stearate, Tween 80, sodium oleate, and vitamin E to step 1 under the condition of 25°C ) The product is continuously stirred under 200 rpm stirring conditions until the entir...

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Abstract

The invention discloses an oral ivermectin microemulsion concentrate and a preparation method and application thereof, and belongs to the field of medicine and pharmacy. The oral ivermectin microemulsion concentrate product uses auxiliary materials mainly comprising natural ingredients and pharmaceutical grade auxiliary materials, is high in safety and environment friendly, and overcomes the problems of the existing product environmental pollution. The oral ivermectin microemulsion concentrate has simple preparation process, and is only related to the ordinary mixing process. The oral ivermectin microemulsion concentrate product can spontaneously emulsify by diluting with tap water and other water solution and slight oscillation, and under the optimum conditions, the emulsified average particle size is 0.05 to 0.2 mum. The oral ivermectin microemulsion concentrate product has good liquidity, and may not be hung on the wall, the appearance is single-phase, transparent and clear, and after repeated freezing and thawing, preparation stratification phenomenon may not occur, and preparations emulsification effect may not be affected. The oral ivermectin microemulsion concentrate product is used for controlling livestock gastrointestinal nematodiasis, bovine myiasis, hypoderma lineatum, sheep nasal myiasis, goat scab mite, swine sarcoptic mange and other parasitic insects diseases.

Description

technical field [0001] The invention belongs to the field of pharmacy and pharmacy, and relates to an oral ivermectin microemulsion concentrate, its preparation method and application. Background technique [0002] Ivermectin (Ivermectin, IVM) is the first avermectin drug derivative developed by U.S. Merck Company. Compared with avermectin, IVM is less toxic and more stable. Abroad, IVM has been widely used It is used in various economic animals such as pigs, cattle, sheep, rabbits, horses, camels, deer, and foxes, as well as pets such as dogs and cats. In 1996, among the global sales of veterinary drug raw materials and preparations, IVM raw materials and their main preparations accounted for one In 1996, the number of people who used IVM in the world Reached more than 600,000.In China, IVM has been widely used in domestic animals and pets as a veterinary drug. [0003] Ivermectin has poor water solubility (4μg / ml), and the required dose is low (0.3mg / kg body weight). It ...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/7048A61P33/02A61P33/14A61P33/10
Inventor 杨杰其他发明人请求不公开姓名
Owner 天津迈迪瑞康生物医药科技有限公司
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