Fatty artemisinin emulsion and its prepn and application

A technology of fat emulsion and artemisinin, which is applied in the direction of pharmaceutical formula, emulsion delivery, and medical preparations containing active ingredients, etc. It can solve the problems of difficult preparation of emulsion or microemulsion, short action time and allergic reaction of patients, etc. problems, to avoid the first-pass effect, increase stability, and reduce toxic and side effects

Inactive Publication Date: 2006-05-17
裴蕾
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Since artemisinin and its fat-soluble derivatives are insoluble in water, polyoxyethylene castor oil and absolute ethanol (50:50) should be used as solubilizing carriers when they are used as injection preparations clinically, which will easily lead to the release of histamine and make patients suffer from Severe allergic reactions and toxic side effects
In addition, due to the short half-life in the body after artemisinin is converted into dihy

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Put 20g of soybean oil for injection and 160mg of artemisinin into a container, place the container in a water bath, heat to 50°C, stir until the drug is dispersed and dissolved, cool to 40°C, put in 2.5g of lecithin and stir until the phospholipid is dissolved, Mix well; place 170ml of water for injection in another container, stir and dissolve 2.5g of glycerin at 50℃ to form an aqueous phase; mix the mixture containing artemisinin, soybean oil and lecithin with glycerin at 40℃ under mechanical stirring Mix the water phase with water for injection to 200ml, and continue to stir at 40℃ for 1 hour at high speed to prepare colostrum, adjust the pH to 6; transfer the prepared colostrum to a high-pressure homogenizer, and homogenize to the droplets Until the particle size inspection is qualified; the emulsion is filled, nitrogen is passed, and capped; sterilized under the conditions of 121°C and F0 of 20 with a rotary autoclave. That is, 80mg. / 100ml artemisinin fat emulsion int...

Embodiment 2

[0034] Put 150g of soybean oil for injection and 1200mg of artemisinin into a container, place the container in a water bath, heat to 55°C, stir until the drug is dispersed and clear, cool to 50°C, add 25g of lecithin, stir until the phospholipid is dissolved, and mix Evenly. Place 750 ml of water for injection in another container with 15 g of polyethylene glycol and 25 g of glycerol at 50° C. and stir to dissolve to form an aqueous phase. Mix the mixture containing artemisinin, soybean oil and lecithin with water containing glycerol and polyethylene glycol at 50°C under mechanical stirring, add water for injection to 1000ml and continue stirring at 50°C at high speed for 1 hour Make colostrum. The prepared colostrum is transferred into a high-pressure homogenizer, and homogenized until the droplet size is qualified; then the emulsion is filled, nitrogen is passed, and sealed; and sterilized with a rotary autoclave. That is, 120mg / 100ml artemisinin fat emulsion intravenous inject...

Embodiment 3

[0036] Put 200g of soybean oil for injection and 1600mg of artemisinin into a container, place the container in a water bath, heat to 60°C, stir until the drug is dispersed and clear, cool to 50°C, add 25g of lecithin and stir until the phospholipid is dissolved and formed uniformly Mixed phase. Put 700 ml of water for injection in another container, 30 g of hydroxypropyl β-cyclodextrin, and 25 g of glycerol at 60° C. and stir to dissolve to form an aqueous phase. Mix the mixture containing artemisinin, soybean oil and lecithin with water containing glycerol and hydroxypropyl β-cyclodextrin at 60°C under mechanical stirring, add water for injection to 1000ml, and continue at 55°C Colostrum is made by mechanical stirring for 1 hour. Move the prepared colostrum into a high-pressure homogenizer and homogenize it until the droplet size is qualified; then fill the emulsion with nitrogen and fuse it; use a rotary autoclave to perform 121°C, F0=20 conditions Sterilize under. That is, a 1...

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Abstract

The present invention discloses one kind of fatty artemisinin emulsion and its preparation and application. The fatty artemisinin emulsion includes oil for injection, smulsifier, solubilizer and isotonizer, and has artemisinin or dihydroartemisinin well dissolved in oil and coated in emulsified oil phase, so that it has high stability, strengthened medicinal effect, slow releasing and targeting administration effect, prolonged medicine residence time in blood and raised bioavailability.

Description

Technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a fat emulsion of anticancer drug artemisinin and its derivative dihydroartemisinin. technical background [0002] Artemisinin and its derivatives are used as antimalarial drugs. The currently marketed varieties are mainly taken as tablets. They are widely used because of their definite curative effect and low side effects. With the in-depth research on artemisinin and its derivatives, the miraculous anti-cancer effect of artemisinin and its derivatives has been discovered. A large number of experimental studies at home and abroad have shown that artemisinin and its derivatives can affect a variety of animals and humans. Tumor cells have a definite anti-cancer effect. In 1991, Deng Ding’an, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, first reported that artemisinic acid derivatives had killing activity on mouse leukemia P388 cells, and found that in ad...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/357A61P35/00
CPCY02A50/30
Inventor 裴蕾李启燕
Owner 裴蕾
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