A kind of artemether liposome for injection and its preparation method and application

A technology of artemether and liposomes, which is applied in the field of artemether liposomes for injection and its preparation, and can solve the problems of leakage of contents, easy leakage of contents, short validity period, etc.

Active Publication Date: 2021-11-02
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Yet, although liposome has the above-mentioned advantages, find in long-term practice research, liposome stability is relatively poor, and the liposome that general method prepares is easy to gather and fuse, and valid period is shorter; And because liposome property is not stable enough, its The content is easy to leak. In order to improve the storage stability of liposomes, freeze-drying is often carried out at present, and water is added to reconstitute before use to form a liposome suspension. Liposome vesicles are destroyed, drug leakage occurs, and it is difficult to return to the state before lyophilization after lyophilization, and the contents will leak more or less, so it is necessary to add a lyoprotectant, but adding such substances, It may have an impact on the safety of liposomes. At the same time, different drugs and liposomes prepared by different preparation methods have different bioavailability. For different drugs, the encapsulation efficiency and drug loading of liposomes are very different. Large, resulting in extremely low drug loading of liposomes prepared by certain drugs, making it difficult to exert the effect of drugs

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  • A kind of artemether liposome for injection and its preparation method and application
  • A kind of artemether liposome for injection and its preparation method and application
  • A kind of artemether liposome for injection and its preparation method and application

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preparation example Construction

[0049] In yet another specific embodiment of the present invention, a method for preparing artemether liposomes is disclosed, which specifically includes the following steps:

[0050] Dissolve artemether, soybean lecithin, and cholesterol in absolute ethanol in proportion to ultrasonic dissolution to make a lipid solution, and then inject the lipid solution into phosphate buffered saline (PBS) at 40-45°C. After the injection is completed, Stir to remove ethanol, and then perform ultrasonic treatment to filter the membrane to obtain the artemether liposome liquid preparation.

[0051] In another specific embodiment of the present invention, the mass volume ratio of artemether, soybean lecithin, cholesterol, absolute ethanol and phosphate buffer is 1:6-8:1-2:0.3-0.4:0.8 -1.2(g:g:g:L:L);

[0052] In another specific embodiment of the present invention, the mass volume ratio of the artemether, soybean lecithin, cholesterol, absolute ethanol and phosphate buffer is 1:6:1.5:0.3:1.2...

Embodiment 1

[0059]

[0060] Preparation Process:

[0061] Dissolve the prescribed amount of artemether, soybean lecithin, and cholesterol with 3ml of absolute ethanol 40KHz ultrasound, mix well, slowly inject the mixed solution into 12ml of PBS heated to 45°C with a micro-injector, and use an electronic constant speed The stirrer was stirred at a speed of 800 rpm until the anhydrous ethanol was completely removed, and the resulting suspension was subjected to ultrasound (40KHz) and then passed through a 0.22 μm microporous membrane to obtain artemether liposomes.

Embodiment 2

[0063]

[0064] Preparation Process:

[0065] Dissolve the prescribed amount of artemether, soybean lecithin, and cholesterol with 4ml of absolute ethanol 30KHz ultrasound, mix well, slowly inject the mixed solution into 10ml of PBS heated to 45°C with a micro-injector, and use an electronic constant speed The stirrer was stirred at a speed of 700 rpm until the anhydrous ethanol was completely removed, and the resulting suspension was subjected to ultrasound (40KHz) and then passed through a 0.22 μm microporous membrane to obtain artemether liposomes.

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Abstract

The invention provides an artemether liposome for injection, and the artemether liposome is prepared by an ethanol injection method. The preparation process of the method is simple and can be applied to industrial production. With a suitable preparation process, the prepared artemether liposome has a small particle size (150-200nm), uniform particle size distribution, and an encapsulation efficiency greater than 90%. Artemether liposomes are released slowly in the body to avoid adverse reactions caused by excessive drug concentration at the initial stage of injection. At the same time, the inventors found that the artemether liposome prepared by this method has high stability, high bioavailability, good resolubility, and long storage time, which meets its medication requirements.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to an artemether liposome for injection and a preparation method and application thereof. Background technique [0002] Artemisinin and its derivatives are sesquiterpene lipid compounds extracted from the leaves of Artemisia annua. These drugs are highly effective and fast-acting killers of Plasmodium erythrocytes. At present, they are mainly used for Plasmodium vivax, Symptom control of falciparum malaria and treatment of chloroquine-resistant strains; recent studies have found that artemether has strong anti-tumor activity and has inhibitory and killing effects on a variety of tumor cells. Therefore, the anti-tumor activity of artemether is its new Research hotspots in the discovered pharmacological effects. Artemether is a 10-β-methyldihydro derivative of artemisinin with the molecular formula C 16 h 26 o 5 . Its shape is white crystal or crystalline powd...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K31/357A61K47/24A61K47/28A61P35/00
CPCA61K9/0019A61K9/127A61K31/357A61K47/24A61K47/28
Inventor 黄桂华田柳郝燕云
Owner SHANDONG UNIV
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