Ivermectin fat emulsion concentrated solution, preparation method and application thereof

A technology of ivermectin and fat emulsion, which is applied in the direction of emulsion delivery, pharmaceutical formula, medical preparations containing active ingredients, etc., and can solve the problems of inconvenient transportation and storage

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

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Problems solved by technology

In addition, existing fat emulsions require specialized equipment to sterilize under high pressure
As is well known to those skilled in the art, fat milk products need to be stored a...

Method used

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  • Ivermectin fat emulsion concentrated solution, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0125] Example 1: Preparation of Ivermectin Fat Emulsion Concentrate Sample 1

[0126] Its composition is as follows:

[0127] Ivermectin 7.6g

[0128] Medium-chain fatty acid glycerides (Capmul MCM, Abitec) 26.6 g

[0129] Soybean oil 26.6g

[0130] 1,2-Propanediol 8.3g

[0131] Soy Lecithin 9.4g

[0132] Polyglycerol oleate 3.1 g

[0133] Polyethylene glycol lauryl hydroxystearate (Solutol HS 15, BASF) 10 grams

[0134] Tween 80 8.2g

[0135] Oleic acid 0.1 g

[0136] Vitamin E 0.1 g

[0137] The preparation method of the ivermectin fat emulsion concentrate is as follows:

[0138] 1) At 20°C, add the above-mentioned weight of soybean lecithin and polyglyceryl oleate to medium-chain fatty acid glycerides and soybean oil, and stir at 8000 rpm until a clear and clear solution is formed;

[0139] 2) Add the above weight of ivermectin, 1,2-propylene glycol, polyethylene glycol lauryl stearate, Tween 80, oleic acid, and vitamin E to the product of step 1) at 45°C, Stirring was continued under stirr...

Embodiment 2

[0141] Example 2: Preparation of Ivermectin Fat Emulsion Concentrate Sample 2

[0142] Its composition is as follows:

[0143] Ivermectin 10.8g

[0144] Medium-chain fatty acid glycerides (Capmul MCM, Abitec) 60g

[0145] 1,2-Propanediol 7.5g

[0146] Soy Lecithin 6.7g

[0147] Polyglycerol oleate 3.7g

[0148] Polyethylene glycol lauryl hydroxystearate (Solutol HS 15, BASF) 7.4 g

[0149] Tween 80 3.7 g

[0150] Oleic acid 0.1 g

[0151] Vitamin E 0.1 g

[0152] The preparation method of the ivermectin fat emulsion concentrate is as follows:

[0153] 1) At 45°C, add the above-mentioned weight of soybean lecithin and polyglyceryl oleate to medium-chain fatty acid glyceride, and stir at 10000rpm until a clear and clear solution is formed;

[0154] 2) Add the above weight of ivermectin, 1,2-propylene glycol, polyethylene glycol lauryl stearate, Tween 80, oleic acid, and vitamin E to the product of step 1) under the condition of 20°C, Stirring was continued under stirring conditions at 2000 rpm u...

Embodiment 3

[0156] Example 3: Preparation of Ivermectin Fat Emulsion Concentrate Sample 3

[0157] Its composition is as follows:

[0158] Ivermectin 11.7g

[0159] Medium-chain fatty acid glycerides (Capmul MCM, Abitec) 59.7g

[0160] 1,2-Propanediol 9.4 g

[0161] Soy lecithin 10.5 g

[0162] Polyoxyethylene ether (35) castor oil (Cremophor EL, BASF) 8.7g

[0163] The preparation method of the ivermectin fat emulsion concentrate is as follows:

[0164] 1) At 25°C, add the above-mentioned weight of soybean lecithin to medium-chain fatty acid glycerides, and stir at 1000 rpm until a clear and clear solution is formed;

[0165] 2) Add the above weight of ivermectin, 1,2-propylene glycol, and polyoxyethylene ether (35) castor oil to the product of step 1) at 25°C, and continue stirring under 200rpm stirring conditions until the whole The system was transparent and clear. After sterilization by 0.22μm microporous membrane, the ivermectin fat emulsion concentrate was finally obtained.

[0166]

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Abstract

An ivermectin fat emulsion concentrated solution, a preparation method and an application thereof belong to the field of pharmacology and pharmaceutics. According to the invention, the defect that a traditional fat emulsion preparation technology is complex and stability is poor is overcome. The preparation technology provided by the invention is simple; the general physical stirring process is only needed; and no homogenization technology is required. A product prepared in the invention can be sterilized through a 0.22-micron microfiltration membrane; and in clinical use, the product can be spontaneously emulsified into a fat emulsion system after diluted by the use of an aqueous solution such as normal saline, etc. and slightly oscillated. The product has good fluidity, will not be retained on the wall, is single-phase, transparent and clear in appearance, can undergo clarification detection, will not cause preparation stratification after multigelation and is applied in controlling gastrointestinal nematodiasis, hypodermosis, Hypoberma Iineata maggot, oestriasis, Psoroptes ovis and swine sarcoptic acariasis of livestock and other parasitic insect diseases.

Description

technical field [0001] The invention belongs to the field of pharmacy and pharmacy, and relates to an ivermectin fat emulsion concentrate, a preparation method and application thereof. Background technique [0002] Ivermectin (Ivermectin, IVM) is the first avermectin drug derivative developed by Merck Company in the United States. Compared with avermectin, IVM is less toxic and more stable. Abroad, IVM has been widely used in various economic animals such as pigs, cattle, sheep, rabbits, horses, camels, deer, foxes and pets such as dogs and cats. In 1996, among the global sales of veterinary drug raw materials and preparations, the sales of IVM raw materials and its main preparations were the first, reaching 750 million US dollars and 735 million US dollars respectively. In addition, IVM is also used to control human filarial and human acariasis. In 1996, more than 600,000 people worldwide had used IVM. In China, IVM has been widely used as a veterinary drug in domestic a...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/7048A61P33/02A61P33/10A61P33/14
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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