Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

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
View PDF1 Cites 6 Cited by
  • 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 dihydroartemisinin, the duration of action is relatively short.
Although there is a patent application for the preparation method (patent application number: 200410023737.1) of the emulsion of artemisinin and its fat-soluble derivatives, the patent of this application is a microemulsion, and its formula and preparation method break away from the common sense of pharmacy. It is also difficult to prepare the emulsion or microemulsion described in the patent.

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

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...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): A61K9/107A61K31/357A61P35/00
CPCY02A50/30
Inventor 裴蕾李启燕
Owner 裴蕾
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com