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Daptomycin ethosome preparation

A technology of daptomycin alcohol and daptomycin, which is applied in the field of new pharmaceutical preparations, can solve problems such as inconvenience in use, poor patient compliance, and pain in injection, and achieve the effects of convenient use, high encapsulation rate and good stability

Inactive Publication Date: 2013-04-03
SOUTHWEST UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The preparation of daptomycin is currently only a sterile powder for injection, which has disadvantages such as inconvenient use, painful injection, and poor patient compliance.

Method used

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  • Daptomycin ethosome preparation
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  • Daptomycin ethosome preparation

Examples

Experimental program
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Effect test

Embodiment 1

[0033] Prescription: Daptomycin 1mg, lecithin 15mg, absolute ethanol 0.7ml, water 1.3ml, make 2ml daptomycin ethosome preparation.

[0034] Preparation method: dissolve the prescribed amount of daptomycin in the prescribed amount of water to obtain the daptomycin aqueous solution; dissolve the prescribed amount of lecithin in the prescribed amount of absolute ethanol to obtain the lecithin ethanol solution; The daptomycin aqueous solution and the lecithin ethanol solution were mixed at room temperature, and the ultrasonic power was 800W with an ice-bath probe for 20 minutes, and then passed through a homogenizer with a pore size of 200nm, 100nm, and 50nm in sequence in a homogenizer. film, so that the ethosomes are uniformly dispersed to obtain the daptomycin ethosome preparation.

[0035] Quality evaluation: The obtained daptomycin ethosome preparation was a stable translucent dispersion system with light blue opalescence by visual observation. Observed under a transmission ...

Embodiment 2

[0040] Prescription: Daptomycin 1mg, lecithin 15mg, absolute ethanol 0.8ml, water 1.2ml, make 2ml daptomycin ethosome preparation.

[0041] Preparation method: dissolve the prescribed amount of daptomycin in the prescribed amount of water to obtain the daptomycin aqueous solution; dissolve the prescribed amount of lecithin in the prescribed amount of absolute ethanol to obtain the lecithin ethanol solution; The daptomycin aqueous solution and the lecithin ethanol solution were mixed at room temperature, and the ultrasonic power was 800W with an ice-bath probe for 40 minutes, and then passed through a microporous homogeneous membrane with a pore size of 200 nm and 100 nm in a homogenizer, The ethosomes are uniformly dispersed to obtain the daptomycin ethosome preparation.

[0042] Quality evaluation: The average particle size of the obtained daptomycin ethosome was 150.6nm, and the encapsulation efficiency was 93.7%.

Embodiment 3

[0044] Prescription: Daptomycin 1mg, lecithin 10mg, absolute ethanol 0.6ml, water 1.4ml, make 2ml daptomycin ethosome preparation.

[0045] Preparation method: dissolve the prescribed amount of daptomycin in the prescribed amount of water to obtain the daptomycin aqueous solution; dissolve the prescribed amount of lecithin in the prescribed amount of absolute ethanol to obtain the lecithin ethanol solution; The daptomycin aqueous solution and the lecithin ethanol solution were mixed at room temperature, and the ultrasonic power was 800W with an ice-bath probe for 20 minutes, and then passed through a microporous homogeneous membrane with a pore size of 200 nm and 100 nm in a homogenizer, The ethosomes are uniformly dispersed to obtain the daptomycin ethosome preparation.

[0046] Quality evaluation: The obtained daptomycin ethosome had an average particle size of 126.7nm and an encapsulation efficiency of 85.7%.

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Abstract

The invention discloses a daptomycin ethosome preparation. The prescription comprises 1mg of prescription, 10-20mg of lecithin, 0.6-0.8ml of ethanol and the balance water which are prepared into 2ml of the daptomycin ethosome preparation. A preparation method includes: dissolving the daptomycin in water to prepare daptomycin water solution; dissolving the lecithin in anhydrous ethanol to prepare lecithin ethanol solution; and uniformly mixing the daptomycin water solution and lecithin ethanol solution at the room temperature, performing ice-bath probe ultrasonography with the ultrasonic power of 800W for 20-40minutes, and then enabling the mixture to pass through a microporous homogeneous membrane with the pore diameter of 50-20nm in a homogenizing instrument to enable ethosomes to be dispersed uniformly so that the daptomycin ethosome preparation is prepared. The daptomycin ethosome preparation is a stable translucent dispersion system with light blue opalescence, small and uniform in particle size, high in entrapment efficiency and excellent in transdermal performance and drug release and has certain slow-release effect, and the preparation method is simple and convenient, low in cost and good in stability.

Description

technical field [0001] The invention belongs to the field of pharmacy and relates to a new drug preparation. Background technique [0002] In September 2003, daptomycin (Cubicin) was listed in the United States for the first time as a new structural class of antibiotics. This antibiotic is a cyclic lipopeptide substance extracted from the fermented liquid of streptomyces reseosporus. Its mechanism of action is different from other antibiotics on the market, so it will not be affected by cross-resistance caused by other antibiotics. In addition to rapidly killing most clinically relevant Gram-positive bacteria in vitro, more importantly, daptomycin is effective against isolates that have shown resistance to methicillin, vancomycin, and linezolid in vitro. Has strong activity. At present, it is mainly used for Gram-positive bacterial infections that do not respond to current therapies, including infections caused by methicillin-resistant Staphylococcus aureus, vancomycin-res...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K38/10A61P31/04
Inventor 李翀刘厦殷齐坤王晓颖陈章宝
Owner SOUTHWEST UNIV
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