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

Netilmicin liposome and technique of preparing the same

A preparation process, the technology of netilmicin, is applied in the directions of liposome delivery, medical preparations containing active ingredients, antibacterial drugs, etc. The time of action in the astral body and the increase in reports of side effects have achieved the effect of reducing nephrotoxicity, reducing drug dosage and improving permeability.

Inactive Publication Date: 2008-05-14
谢开智
View PDF0 Cites 3 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Although the nephrotoxicity and ototoxicity of netilmicin are the lowest among the aminoglycoside antibiotics, reports on its side effects have increased in recent years, and adverse reactions such as nephrotoxicity and ototoxicity cannot be ignored
In addition, the biological half-life of netilmicin is only 2-2.5 hours, making netilmicin into liposomes can solve ear and kidney toxicity to a certain extent, and appropriately prolong the in vivo action time of netilmicin, and this study Not yet reported in the literature, does not involve intellectual property issues

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

[0063] Dissolve 0.04g of netilmicin in 5ml of pH7.0 phosphate buffer solution as the water phase, dissolve 0.1g of cholesterol and 0.4g of egg yolk lecithin in 10ml of ether as the organic phase; take the prepared water phase and place it in a water bath Heat to 55°C, add 10ml of the organic phase above to the water phase at a constant speed, stir while adding, control the dropping speed to 2ml / 9min, after the addition, ultrasonicate in a 250Hz water bath for 8 minutes to form a uniform emulsion, that is Obtain liposomes with an average particle diameter of 150 nm.

Embodiment 2

[0065] Dissolve 0.04g of netilmicin in 2ml of pH7.0 phosphate buffer solution as the water phase, dissolve 0.1g of cholesterol and 0.4g of egg yolk lecithin in 10ml of ether as the organic phase, and mix 0.3ml of the water phase with the above 10ml of the organic phase , 250Hz short-term water bath ultrasonication for 5min to make it evenly mixed to form a uniform liquid of a large amount of organic phase and a small amount of water phase. Use a rotary evaporator to evaporate and dry the organic solvent in the organic phase under reduced pressure. Add the remaining 1.7ml of water phase, 250Hz short-time water bath ultrasonic 5min to mix evenly, form a uniform emulsion, cooling and stirring, probe ultrasonic 5min, to obtain liposomes with an average particle size of 150nm.

Embodiment 3

[0067] Dissolve 0.04g of netilmicin in 5ml of pH7.0 phosphate buffer solution as the water phase, dissolve 0.2g of cholesterol and 0.6g of egg yolk lecithin in 10ml of ether as the organic phase; take the prepared water phase and place it in a water bath Heat to 60°C, add the above 10ml organic phase to the water phase at a constant speed, stir while adding, control the dropping speed to 2ml / 10min, after the addition, ultrasonicate in a 250Hz water bath for 9 minutes to form a uniform emulsion, that is Obtain liposomes with an average particle diameter of 170 nm.

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 invention discloses a Netilmicin liposome and the preparation technique. The Netilmicin liposome is composed by the following materials in weight ratio: one share of Netilmicin, two to seven shares of cholesterol and four to eighteen shares of lecithin. The preparation technique includes the infusing and ultrasonic method and the multiple emulsion and ultrasonic method, with the following steps: firstly, dissolve a matched proportion of Netilmicin medicine into a neutral-pH buffer solution of phosphate as an aqueous phase; secondly, dissolve a matched proportion of the cholesterol and the lecithin into a proper proportion of Ethyl ether as an organic phase; thirdly, drop the organic phase into the aqueous phase uniformly and stir simultaneously; and finally with the water ultrasonic extraction method, an uniform emulsion, the Netilmicin liposome with a particle diameter of one hundred to two hundreds nanometers, is formed with renal toxicity decreased greatly. The invention has the advantages that due to simplified operation of processing, the liposome with less particle diameter and better stability can be formed; the particle diameter is notably reduced while the uniformity is improved; additionally, the envelope rate rises to fifty percents or above.

Description

Technical field: [0001] The invention relates to a netilmicin liposome and a preparation process thereof. Background technique: [0002] The development of aminoglycoside antibiotics has gone through more than half a century. Up to now, more than 300 new compounds have been obtained through various channels, of which more than 70 have clinical value, and more than 50 have been clinically applied. Some varieties are used in agricultural production. With the long-term and widespread use of some aminoglycoside antibiotics, various researches on bacterial resistance and the different degrees of ear and kidney toxicity of these antibiotics have achieved certain results. [0003] In recent years, some new varieties of aminoglycoside antibiotics with high efficiency and low toxicity against drug-resistant bacteria have been released one after another. Netimicin is a semi-synthetic broad-spectrum aminoglycoside antibiotic produced by Micromonospora. Its mechanism of action is to ...

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
Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/7036A61P31/04
Inventor 谢开智
Owner 谢开智
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