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Ivermectin emulsion for injection and preparation method thereof

A technology of ivermectin emulsion and ivermectin, which is applied in the field of animal health care and animal medicine, can solve the problems of increased breeding costs for farmers, long-term redness and swelling, and high cost of injections, so as to improve bioavailability and reproducibility Good and safe effect

Inactive Publication Date: 2009-12-02
烟台爱士津动物保健品有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Commercially available ivermectin injections are common solution type injections. Since ivermectin is insoluble in water, when preparing common solution type injections, a large amount of organic solvent (glycerol formal) is needed to dissolve the drug. The proportion of the formula is 40%, and the toxic and side effects are obvious; after injection of ordinary solution injection, local pain, lump formation, redness and swelling will not disappear for a long time, causing additional damage to animals; ordinary solution injection is due to the use of a large amount of organic solvent , the high cost of injections indirectly increases the breeding cost of farmers
Traditional powders, common solution injections, premixes and other dosage forms are difficult to meet the development and needs of the current animal husbandry. Therefore, a safe, effective, quality-controllable, and low-toxic ivermectin preparation is required.

Method used

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  • Ivermectin emulsion for injection and preparation method thereof
  • Ivermectin emulsion for injection and preparation method thereof

Examples

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Effect test

example 1

[0016] Example 1: Preparation of Ivermectin Emulsion for Injection

[0017] Ivermectin 1.0g

[0018] Refined soybean oil 20g

[0019] Poloxamer 3.0g

[0020] Benzyl Benzoate 10g

[0021] Distilled water to 100ml

[0022] Preparation:

[0023] Dissolve ivermectin with benzyl benzoate and add it to refined soybean oil, mix to obtain a refined soybean oil solution containing 33 mg / ml ivermectin, as the oil phase, disperse poloxamer in distilled water, Dissolved in water to form a dispersed phase, as the water phase, under high-speed stirring conditions, slowly drop the oil solution containing ivermectin into the water phase to make a coarse emulsion, add distilled water to the full amount, and dilute the obtained emulsion Under the condition of a pressure of 100Mpa, it is further emulsified by a milk homogenizer. After the emulsification is completed, it is packaged and sterilized at 115°C for 30 minutes.

example 2

[0024] Example 2: Preparation of Ivermectin Emulsion for Injection

[0025] Ivermectin 1.0g

[0026] Refined corn oil 15g

[0027] Poloxamer 2.5g

[0028] Benzyl Benzoate 10g

[0029] Distilled water to 100ml

[0030] Preparation:

[0031] Dissolve ivermectin with benzyl benzoate and add it to refined corn oil, mix to obtain a refined corn oil solution containing 33 mg / ml ivermectin, as the oil phase, disperse poloxamer in distilled water, Dissolved in water to form a dispersed phase, as the water phase, under high-speed stirring conditions, slowly drop the oil solution containing ivermectin into the water phase to make a coarse emulsion, add distilled water to the full amount, and dilute the obtained emulsion Under the condition of a pressure of 100Mpa, it is further emulsified by a milk homogenizer. After the emulsification is completed, it is packaged and sterilized at 115°C for 30 minutes.

example 3

[0032] Example 3: Preparation of Ivermectin Emulsion for Injection

[0033] Ivermectin 500mg

[0034] Refined sunflower oil 15g

[0035] Tween 80 2.5g

[0036] Benzyl Benzoate 5g

[0037] Distilled water to 100ml

[0038] Preparation:

[0039] Dissolve ivermectin in benzyl benzoate and add it to refined sunflower oil, mix to obtain a refined sunflower oil solution containing 25 mg / ml ivermectin, as the oil phase, disperse Tween 80 in distilled water, dissolve Finally form the dispersed phase, as the water phase, under the condition of high-speed stirring, slowly drop the oil solution containing ivermectin in the water phase to make a coarse emulsion, add distilled water to the full amount, and put the obtained emulsion under pressure Under the condition of 100Mpa, it is further emulsified by a milk homogenizer. After the emulsification is completed, it is packaged and sterilized at 115°C for 30 minutes.

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Abstract

The invention relates to an emulsion for injection, which is used for controlling parasites in vitro and in vivo. The emulsion for injection comprises the following components: 0.5 percent to 1 percent (w / v) of ivermectin, 5 percent to 10 percent (w / v) of benzyl benzoate, 2.5 percent to 5 percent (w / v) of poloxamer, 5 percent to 20 percent (w / v) of refined soybean oil, and the balance of distilled water. In the formula, v is volume unit ml, and w is weight unit g. The ivermectin emulsion for injection is an oil-in-water emulsion, wherein the ivermectin is a macrolide medicine with the antiparasitic activity, the poloxamer is an emulsifier, the benzyl benzoate is a medicine dissolving agent, the refined soybean oil is an oil-phase diluent, and the distilled water is a water-phase diluent. The emulsion for the injection has favorable repelling and killing action to the parasites both insides and outsides the animal body, has wide use range, and can be used for various animals including big animals such as cattle, sheep, pigs and the like, small animals such as dogs, cats, pets and the like as well as economical animals such as foxes, martens, racoon dogs and the like.

Description

technical field [0001] The invention relates to an ivermectin emulsion for injection and a preparation method thereof, and relates to the fields of animal medicine, animal health care and the like. Background technique [0002] At present, the management of my country's breeding industry is becoming more and more mature, and the epidemic prevention measures are relatively in place. However, whether it is domestic or intensively raised animals, due to the limitation of hygienic conditions, they are often susceptible to various internal and external parasites. Parasites often cause mechanical damage to animals during the process of invading animals or migrating and parasitizing in the body. Animals suffer from malnutrition, emaciation, anemia, stunted growth and even death. [0003] Ivermectin is a class of macrolide antibiotics with antiparasitic activity. It is an antiparasitic drug and has a good killing effect on internal and external parasites, especially nematodes and a...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/7048A61K47/44A61P33/00
Inventor 梁玉王永军
Owner 烟台爱士津动物保健品有限公司
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