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Avermectin nanoliposome and preparation method thereof

A nano-liposome and avermectin technology, applied in the field of animal antiparasitic drugs, can solve the problems of short duration of validity, low bioavailability, and large irritation, so as to increase the duration of drug effect and achieve slow control Release effect, reduce the effect of toxic and side effects

Inactive Publication Date: 2015-07-01
HENAN HUITONGTIANXIA ANIMAL MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The abamectins themselves have poor stability and low drug efficacy, and the reported abamectin dosage forms include powder, tablet, emulsion, microemulsion, capsule and injection, but these dosage forms have certain disadvantages, such as bioavailability Low intensity, high irritation, waste of resources and short duration of validity, etc.

Method used

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  • Avermectin nanoliposome and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] The prescription of abamectin nano liposome is: abamectin 1.0 g, lecithin 10. g, cholesterol 1.1 g, vitamin E 0.036 g.

[0020] The preparation method of Abamectin nano liposome is as follows:

[0021] (1) Weigh the prescribed amount of avermectin, lecithin, cholesterol and vitamin E into a round bottom flask, add ether until fully dissolved, and obtain a solution.

[0022] (2) Under the condition of 40 ℃ water bath, the solution was turned into a uniform film by rotary evaporation.

[0023] (3) Add 100 mL of PBS buffer solution with a pH of 7.0 to wash the membrane until it becomes a milky liquid, then stop washing the membrane.

[0024] (4) Freeze in a low-temperature refrigerator, then take it out to thaw at room temperature, fully shake after thawing, repeat freezing and thawing 3 times, sonicate for 5 minutes, and fill with N 2 Sealed and protected from light, stored in refrigerator at 4°C.

Embodiment 2

[0026] The prescription of abamectin nano liposome is: 5.0 g of avermectin, 50 g of lecithin, 1.1 g of cholesterol, and 0.182 g of vitamin E.

[0027] The preparation method of Abamectin nano liposome is as follows:

[0028] (1) Weigh the prescribed amount of avermectin, lecithin, cholesterol and vitamin E into a round bottom flask, add ether until fully dissolved, and obtain a solution.

[0029] (2) Under the condition of 40 ℃ water bath, the solution was turned into a uniform film by rotary evaporation.

[0030] (3) Add 100 mL of PBS buffer solution with a pH of 7.0 to wash the membrane until it becomes a milky liquid, then stop washing the membrane.

[0031] (4) Freeze in a low-temperature refrigerator, then take it out to thaw at room temperature, fully shake after thawing, repeat freezing and thawing 3 times, sonicate for 5 minutes, and fill with N 2 Sealed and protected from light, stored in refrigerator at 4°C.

Embodiment 3

[0033] The prescription of abamectin nano liposome is: 10 g of abamectin, 100 g of lecithin, 11 g of cholesterol, and 0.364 g of vitamin E.

[0034] The preparation method of Abamectin nano liposome is as follows:

[0035] Weigh the prescribed amount of abamectin, lecithin, cholesterol and vitamin E in a round bottom flask, add ether until it is fully dissolved to obtain a solution.

[0036] (2) Under the condition of 40 ℃ water bath, the solution was turned into a uniform film by rotary evaporation.

[0037] (3) Add 100 mL of PBS buffer solution with a pH of 7.0 to wash the membrane until it becomes a milky liquid, then stop washing the membrane.

[0038] (4) Freeze in a low-temperature refrigerator, then take it out to thaw at room temperature, fully shake after thawing, repeat freezing and thawing 3 times, sonicate for 5 minutes, and fill with N 2 Sealed and protected from light, stored in refrigerator at 4°C.

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Abstract

The invention discloses avermectin nanoliposome and a preparation method thereof. The avermectin nanoliposome is prepared from avermectin, lecithin, cholesterol and vitamin E according to a mass ratio of 1-10: 10-100: 1.1-11: 0.036-0.364. The preparation method comprises the following steps of weighing avermectin, lecithin, cholesterol and vitamin E, putting them in a round-bottom flask, adding diethyl ether into the round-bottom flask so that the above materials are fully dissolved and a solution is obtained, carrying out rotary evaporateion on the solution under the conditions of water bath at a temperature of 40 DEG C to obtain a uniform film, washing the film by a PBS buffer until a milky liquid is obtained, freezing the milky liquid by a cryogenic refrigerator, taking out the milky liquid, carrying out thawing at a room temperature, then carrying out full oscillation, carrying out repeated freezing-thawing three times, carrying out ultrasonic treatment for 5min, carrying out N2 filling sealing, and carrying out light-tight preservation by the refrigerator to obtain the avermectin nanoliposome. The avermectin nanoliposome has long action time, can reduce toxic and side effects, can realize sustained and controlled release and can reduce a cost.

Description

technical field [0001] The invention belongs to the field of antiparasitic drugs for animals, and in particular relates to an avermectin nano liposome, and also relates to a preparation method of the liposome. Background technique [0002] Parasitic diseases are one of the most common diseases in animals. Parasites parasitic in or on the body of livestock such as cattle and sheep can cause organ and tissue loss to the host, rob nutrition or produce toxins. In mild cases, it will lead to slow growth of animals and a decrease in feed utilization; in severe cases, it will lead to animal malnutrition, decline in quality, and even a significant increase in mortality due to low disease resistance of animals. [0003] Abamectin drugs have a high-efficiency killing effect on nematodes and ectoparasites parasitic in animals. Abamectin was first successfully developed by Japanese scientists and American Merck Company. Abamectin is a 16-membered macrolide antibiotic produced by Strept...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/7048A61P33/00
Inventor 张要齐张新蕾李引乾
Owner HENAN HUITONGTIANXIA ANIMAL MEDICINE
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