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Acyclovir ethosome and preparation method thereof

A technology of ethosomes and systems, which is applied in the direction of liposome delivery, antiviral agents, active ingredients of heterocyclic compounds, etc., can solve the lack of research on the stability of ethosomes, affect the stability of ethosome preparations, and encapsulation The efficiency is not high, to achieve the effect of improving bioavailability, improving stability, and good affinity

Inactive Publication Date: 2012-02-29
XIANGTAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The encapsulation efficiency of hydrophilic drugs in ethosomes is generally not high, and they are prone to aggregation, degradation, sedimentation, fusion and other changes and leakage, thus affecting the stability of ethosome preparations
At present, research on ethosomes at home and abroad is mainly focused on the preparation of ethosomes and their transdermal absorption properties, and there is a lack of systematic research on the stability of ethosomes.

Method used

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  • Acyclovir ethosome and preparation method thereof
  • Acyclovir ethosome and preparation method thereof
  • Acyclovir ethosome and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] prescription for

[0020]

[0021] Preparation method: Dissolve the prescribed amount of acyclovir, phospholipids and cholesterol in absolute ethanol, dissolve PEG6000 in water for injection, mix and stir at room temperature, then slowly add water for injection under airtight conditions, and continue stirring for 30 minutes. After standing still for 1 hour, ultrasonication was performed for 8 minutes, and acyclovir ethosomes were obtained by grading with a 0.45 μm microporous filter membrane. The ethosome particle size was 223.5 nm and the scattering intensity was 69.6 Kcps as measured by a laser scattering instrument. It was 0.249; the encapsulation efficiency was 71.2%.

Embodiment 2

[0023] prescription for

[0024]

[0025] Preparation method: Dissolve the phospholipids, cholesterol and acyclovir in the prescription amount in absolute ethanol, slowly add 1% 6-O-quaternary ammonium salt chitosan aqueous solution under room temperature and stirring under airtight conditions, and then slowly Add water for injection, continue to stir for 30 minutes, after standing for 1 hour, ultrasonic for 10 minutes, use a 0.45 μm microporous filter membrane to granulate to obtain acyclovir ethosome, and the ethosome particle size measured on the laser scattering instrument is 165.9 nm, the scattering intensity is 62.9Kcps, the distribution is 0.205; the encapsulation efficiency is 65.3%.

Embodiment 3

[0027] prescription for

[0028]

[0029] Preparation method: Weigh the prescribed amount of phospholipids, cholesterol, acyclovir sodium and acyclovir and dissolve them in absolute ethanol, slowly add water for injection under room temperature and stirring under airtight conditions, continue to stir for 30 minutes, and let stand After 1 hour, ultrasound for 10 minutes, and a 0.45 μm microporous filter membrane was used to granulate the aciclovir ethosome. The ethosome particle size was 80.2 nm, the scattering intensity was 47.8 Kcps, and the distribution was 0.268 ; The encapsulation efficiency was 58.3%.

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Abstract

The invention discloses an acyclovir ethosome preparation with improved stability and a preparation method thereof. In the invention, polyethylene glycol (PEG) or chitosan (CS) derivatives are added to the percutaneous administration carrier ethosome to improve the stability of the ethosome. The preparation process of the preparation disclosed by the invention is simple, and the prepared acyclovir ethosome has high stability and narrow particle size distribution.

Description

technical field [0001] The invention relates to a novel preparation of acyclovir ethosome for treating viral skin diseases, a preparation process and a preparation method for improving stability. Background technique [0002] Acyclovir is a second-generation nucleoside antiviral drug widely used at home and abroad with high efficiency, broad-spectrum and low toxicity. It is the drug of choice for the treatment of viral skin diseases such as chickenpox and herpes zoster clinically. Due to the poor skin penetration of acyclovir itself, it is difficult to carry the drug into the deep layer of the skin, which greatly limits the clinical use of topical application. The high concentration of ethanol in the ethosome can not only increase the solubility of the drug in the stratum corneum, change the phase transition temperature of the stratum corneum lipid, enhance its fluidity and flexibility; The preparation of ciclovir into ethosome can improve transdermal absorption performance...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K31/522A61K47/34A61K47/36A61P31/20A61P31/22A61K47/10
Inventor 吴学文熊艳
Owner XIANGTAN UNIV
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