Preparation method of azithromycin for injection

A technology for azithromycin and injection, which is applied in the field of medicine, can solve the problems of high waste rate and low yield of azithromycin, and achieve the effects of reduced waste rate, good stability and reconstitution rate, and simple preparation method

Inactive Publication Date: 2020-08-18
福州华为医药技术开发有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

But the azithromycin for injection prepared by current prepara

Method used

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  • Preparation method of azithromycin for injection

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[0014] The invention provides a preparation method of azithromycin for injection, comprising the following steps:

[0015] Step 1, adding co-solvent and azithromycin in sequence to the water for injection, adding a pH regulator until the pH is 6.5-6.8, constant volume, filtering and sterilizing to obtain a sterile azithromycin solution;

[0016] Step 2, filling and half-stoppering the sterile azithromycin solution, and pre-freezing at -70°C for 2 hours;

[0017] Step 3. After pre-freezing in step 2, carry out five-stage sublimation drying, first-level: temperature -20--10°C, vacuum degree 10-100mbar, keep for 3h; second-level: temperature-10-0°C, vacuum degree 10- 100mbar, keep for 5h; level 3: temperature 0℃, vacuum 100-200mbar, keep 5h; level 4: temperature 5-15℃, vacuum 150-200mbar, keep 6h; level 5: temperature 10-25℃, vacuum 50-150mbar, keep for 3h;

[0018] Among them, during the sublimation drying process, the temperature showed an upward trend, and the vacuum degree ...

Embodiment 1

[0031] The preparation method of azithromycin for injection specifically comprises the following steps:

[0032] Step 1. Add 4g glutamic acid and 1.024g citric acid to 800mL water for injection at 20°C to dissolve, then add 12.5g azithromycin and stir until dissolved, add sodium bicarbonate to pH 6.8, dilute to 1000mL, then add 0.1 % (g / ml) of activated carbon, stirred and decolorized, then decarbonized and filtered with a 0.45 μm filter membrane, and then sterilized and filtered with a 0.22 μm filter membrane to obtain a sterile azithromycin solution;

[0033] Step 2. Cool the sterile azithromycin solution to 10°C, perform filling and semi-stoppering, and pre-freeze at -70°C for 2 hours under normal pressure, and the cooling rate to the pre-freezing temperature is 28°C / h;

[0034] Step 3. After the pre-freezing in step 2, carry out five-stage sublimation drying. The first stage: temperature -20°C, vacuum degree 100mbar, keep for 3h; the second stage: temperature 0°C, vacuum d...

Embodiment 2

[0037] The preparation method of azithromycin for injection specifically comprises the following steps:

[0038] Step 1. Add 2.75g of glutamic acid and 1.125g of citric acid to 750mL of water for injection at 30°C to dissolve, then add 12.5g of azithromycin and stir until dissolved, add sodium bicarbonate until the pH is 6.8, set the volume to 1000mL, and then add 0.1% (g / ml) of activated carbon, stirred and decolorized, then decarbonized and filtered with a 0.45 μm filter membrane, and then sterilized and filtered with a 0.22 μm filter membrane to obtain a sterile azithromycin solution;

[0039] Step 2. Cool the sterile azithromycin solution to 4°C, perform filling and half stoppering, and pre-freeze at -70°C for 2 hours under normal pressure, and the cooling rate to the pre-freezing temperature is 35°C / h;

[0040] Step 3. After the pre-freezing in step 2, carry out five-stage sublimation drying. The first stage: temperature -20°C, vacuum degree 100mbar, keep for 3h; the seco...

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Abstract

The invention discloses a preparation method of azithromycin for injection and belongs to the technical field of medicines. By mixing and dissolving water for injection, a cosolvent and azithromycin,and performing pre-freezing, five-stage sublimation drying and desorption drying, azithromycin freeze-dried powder for injection is obtained. In the sublimation drying process, the temperature is in arising trend, and the vacuum degree is in a rising-falling trend. The preparation method is simple, the original equipment does not need to be replaced or improved; in the preparation process, the pre-freezing temperature is reduced, five-stage sublimation drying is adopted, and the specific temperature and vacuum degree of sublimation drying are improved, so that rejection rate is reduced, yieldis increased, and production costs are further effectively saved in comparison with the traditional process; and the obtained product is easily dissolved in water for injection and has good stabilityand redissolution rate.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a preparation method of azithromycin for injection. Background technique [0002] Azithromycin (Azithromycin, AM) is the first 15-membered macrolide antibiotic developed by Priva Pharmaceutical Company in Croatia. The structure of azithromycin is similar to that of erythromycin, and its antibacterial mechanism is also similar to that of erythromycin. It mainly binds to the 50S subunit of bacterial ribosomes, inhibits protein synthesis dependent on RNA, and thus plays an antibacterial role. However, the antibacterial spectrum of azithromycin is relatively low. Wide, especially the antibacterial spectrum against Gram-negative bacteria is wider than erythromycin. Azithromycin is effective against Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus viridans, Bordetella pertussis, Haemophilus ducretii, Neisseria meningitidis, Campylobacter pylori, Peptostrept...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K31/7052A61P31/04
CPCA61K9/0019A61K9/19A61K31/7052A61P31/04
Inventor 林健勇符友伟张婷谢治平叶燕军张会会张娜蔡燕峰
Owner 福州华为医药技术开发有限公司
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