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Method for preparing azithromycin superfine powder by ultrasound homogenization dissolvent diffusion method

A technology of azithromycin and phacoemulsification, which is applied in powder delivery, pharmaceutical formulations, medical preparations containing active ingredients, etc. It can solve the problems of unstable absorption and low bioavailability of azithromycin, and achieve the effect of inhibiting crystal growth and easy operation

Inactive Publication Date: 2005-07-06
CHINA UNIV OF GEOSCIENCES (WUHAN)
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Typical problems with azithromycin, like other poorly soluble drugs, are low bioavailability and erratic absorption

Method used

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  • Method for preparing azithromycin superfine powder by ultrasound homogenization dissolvent diffusion method
  • Method for preparing azithromycin superfine powder by ultrasound homogenization dissolvent diffusion method
  • Method for preparing azithromycin superfine powder by ultrasound homogenization dissolvent diffusion method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Embodiment 1: be the preferred example of the present invention.

[0025] Raw material of azithromycin, average particle size 20μm (Shanghai Modern Pudong Pharmaceutical Co., Ltd.), SEM photo see figure 2 ; Polyethylene glycol, A.R grade (Tianjin Damao Chemical Instrument Supply Station); absolute ethanol, A.R grade (Tianjin Benchmark Chemical Reagent Co., Ltd.):

[0026] Other reagents were of analytical grade, and the experimental water was distilled water.

[0027] Add 100ml of polyethylene glycol stabilizer aqueous solution with a concentration of (1%, w / v) into a 250ml Erlenmeyer flask, place it in an ice-water bath at 5°C, and under ultrasonic conditions (50K-Hz), add 1ml Slowly add 25ml of azithromycin ethanol solution (the concentration of azithromycin is 0.03mol / L) dropwise at a speed of 1 / min until the solution system becomes turbid. After standing still for 2 hours, centrifuge at high speed until the separation is complete to obtain a solid sample. Then t...

Embodiment 2

[0029] The operating parameters are the same as those in Example 1, except that the diffusion crystallization temperature is at room temperature of 25° C., and the samples obtained by SEM detection show serious agglomeration and agglomeration. And because the crystallization speed is accelerated, the particle size of the sample tends to increase, and at least 90% of the particles have a particle size above 1.0um.

[0030] Effect of temperature on particle size and morphology (comparison of embodiment 1 and embodiment 2):

[0031] The main factors affecting the crystal size are the nucleation rate and the crystallization rate of the crystal, and the crystallization rate is greatly affected by the temperature. When the temperature rises, because the crystallization speed of the product is accelerated, the phenomenon of product agglomeration and agglomeration is more serious. However, in an ice-water bath at 0-5°C, the nucleation rate of the product is much faster than the cryst...

Embodiment 3

[0033] Operating parameter is identical with embodiment 1, and only difference is that the concentration of azithromycin ethanol solution is 0.1mol / L, detects by SEM, as Figure 4 As shown, the chances of the particles colliding with each other increase due to the increase of the concentration, so that the particles become larger and agglomerate. At least 80% of the particles have a particle size above 1.0um.

[0034] The impact of azithromycin concentration on particle size and morphology (comparison of embodiment 1 and embodiment 3):

[0035] The concentration of azithromycin in the solution system has a great influence on the formation and morphology of particles.

[0036] Characterized by scanning electron microscopy, the results are shown in image 3 , Figure 4 , it can be seen from the figure that at a lower concentration (≤0.03mol / L), the obtained particles are mainly spherical, with a uniform particle size. As the concentration increases, the chance of particle siz...

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Abstract

The invention relates to a method for preparing azithromycin superfine powder by ultrasound homogenization dissolvent diffusion method which comprises the steps of, (1) loading water solution of 0.2-2% (w / v) of hydrophilic polyelectrolyte stabilizer into 0-25 deg. C water-bath, (2) under the ultrasonic condition, dropping ethanol solution of Azithromycin into water solution of hydrophilic polyelectrolyte stabilizer, (3) subjecting the opacity solution system to ageing 2-24 hours, high speed centrifugalizing until the complete separation of solid body, (4) centrifugally washing the obtained solid body with distilled water 2-8 times, drying in 40-60 deg. C vacuum drying oven.

Description

technical field [0001] The invention relates to a method for preparing azithromycin ultrafine powder from raw materials of azithromycin, in particular to preparing uniformly dispersed and controllable particle size azithromycin ultrafine powder by using an emulsified solvent diffusion method in the presence of ultrasound and a hydrophilic stabilizer. Background technique [0002] Azithromycin is a macrolide antibiotic mainly used to treat diseases caused by sensitive microorganisms. Typical problems with azithromycin, like other poorly soluble drugs, are low bioavailability and erratic absorption. To solve such problems, the micronization processing method is often used to increase the dispersion and solubility of azithromycin powder. After micronization, the particle size is small and the specific surface area is large, which can greatly improve the drug dissolution rate and solubility, and can also increase its adhesion, which is conducive to increasing the drug retention...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K31/7052A61P31/00
Inventor 皮振邦田熙科杨超龙涛罗东岳
Owner CHINA UNIV OF GEOSCIENCES (WUHAN)
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