Artemether nanoliposome, and preparation method and application thereof

A technology of nano-liposome and artemether, applied in the field of medicine, can solve the problems of low bioavailability, staying in the experimental stage, etc., and achieve the effects of improving the distribution in the body, prolonging the circulation time, and improving the safety and curative effect in the body

Active Publication Date: 2017-03-08
KPC PHARM INC +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are many literature reports on artemether for anti-tumor and cancer cells, but most of them stay in the experimental stage, and there are no preparations in this area. Since artemether is a lipophilic drug, its bioavailability into the

Method used

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Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0040] The preparation method of artemether nano liposome of the present invention is prepared by any one of the following methods:

[0041] (1) Film dispersion-ultrasound-membrane filtration method: dissolve artemether, cholesterol and egg yolk lecithin in an organic solvent, and ultrasonically oscillate to make the dissolution uniform. After the dissolution is complete, the organic solvent is evaporated under reduced pressure to form a thin film , then add water for injection to hydrate until the film falls off and dissolves, sonicate for 180s (sonication for 1s, intermittent for 1s), pass through a 0.45μm filter membrane, and then pass through a 0.22μm filter membrane to obtain the target artemether nanoliposome;

[0042] (2) Ethanol injection-ultrasonic method: dissolve artemether, cholesterol and egg yolk lecithin in an organic solvent, and ultrasonically oscillate to make the dissolution uniform. After the dissolution is complete, solution a is obtained, and solution a is...

Embodiment 1

[0053] The artemether nano liposome is mainly made of the following raw materials in parts by weight: 10 mg of artemether, 20 mg of cholesterol, and 80 mg of egg yolk lecithin. Prepared by film dispersion-ultrasonic-membrane filtration method, the specific operation is as follows: put artemether, cholesterol and egg yolk lecithin into an eggplant-shaped bottle, add 5~10ml of absolute ethanol, and ultrasonically oscillate to dissolve evenly and completely Finally, place the eggplant-shaped bottle in a constant temperature water bath at 40°C for decompression and rotary evaporation to remove absolute ethanol, and form a layer of lipid film on the inner wall of the bottle, slowly add 10ml of water for injection to hydrate until the lipid film falls off and dissolves, and the mixed solution After ultrasonic treatment (ultrasonic power 40%, ultrasonic temperature 40°C) for 180 s, ultrasonic 1 s, intermittent 1 s, pass through a 0.45 μm filter membrane, and then pass through a 0.22 μ...

Embodiment 2

[0056]The artemether nano liposome is mainly made of the following raw materials in parts by weight: 10 mg of artemether, 20 mg of cholesterol, and 120 mg of egg yolk lecithin. Prepared by film dispersion-ultrasonic-membrane filtration method, the specific operation is as follows: put artemether, cholesterol and egg yolk lecithin into an eggplant-shaped bottle, add 5~10ml of absolute ethanol, and ultrasonically oscillate to dissolve evenly and completely Finally, place the eggplant-shaped bottle in a constant temperature water bath at 40°C for decompression and rotary evaporation to remove absolute ethanol, and form a layer of lipid film on the inner wall of the bottle, slowly add 10ml of water for injection to hydrate until the lipid film falls off and dissolves, and the mixed solution After ultrasonic treatment (ultrasonic power 40%, ultrasonic temperature 40°C) for 180 s, ultrasonic 1 s, intermittent 1 s, pass through a 0.45 μm filter membrane, and then pass through a 0.22 μ...

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Abstract

The invention discloses an artemether nanoliposome, and a preparation method and an application thereof. The artemether nanoliposome is prepared from the following raw materials in parts by weight: 1 part of artemether, 2 parts of cholesterol and 8-10 parts of egg yolk lecithin. The preparation method comprises a film dispersion-sonication-film filtering method and an ethanol injection-sonication method. The artemether nanoliposome is applied to the preparation of artemether targeting preparation drugs. The encapsulation rate of the artemether nanoliposome is 61.33-63.86%, the average particle size is 161.65-162.73nm, and the poly dispersition index (PDI) is 0.2678-0.4463. The artemether nanoliposome has good stability when being stored at 4 DEG C.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to an artemether nanoliposome and a preparation method and application thereof. Background technique [0002] Artemether is a derivative of artemisinin, which is mainly obtained by semi-synthesis of artemisinin. Artemisinin is an active ingredient extracted and isolated from the annual herb Artemisiaal of Compositae distributed in Guangxi, Yunnan, Sichuan and other places in my country. Artemether synthesized industrially has mature technology and a large amount of synthesis. [0003] The antimalarial effect and effect of artemisinin are internationally recognized. So far, there are many derivatives of artemisinin used for antimalarial, mainly dihydroartemisinin (Dihydroarteminsinin), artether, Derivatives such as artesunate and artemether, among which artemether has better antimalarial effect than other artemisinin derivatives. Artemether developed in China was incl...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/357A61P33/06A61P33/12A61P33/08A61P33/02A61P31/22A61P31/14A61P31/20
Inventor 陈云建周勇军李正蓉杨兆祥
Owner KPC PHARM INC
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