Freeze drying method of azithromycin for injection

A technology of azithromycin and drying method, which is applied in the direction of freeze-drying transportation, drying solid materials, and drying solid materials without heating, etc. It can solve the problems of large difference in moisture content of azithromycin freeze-dried agent, poor uniformity of formed powder, low solubility of azithromycin, etc. , to achieve the effects of promoting conduction and heat conduction, fast forming speed, accelerated sublimation rate and stability

Active Publication Date: 2021-06-01
HAINAN HULUWA PHARMA GRP CO LTD
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] But in the process of drying the azithromycin intermediate solution by the existing freeze-drying process, on the one hand, it is limited by the low solubility and poor stability of azithromycin; When freeze-drying is carried out to control the freezing conditions at different stages, it is easy to cause broken bottles, incomplete drying, and increased waste rate, and the forming speed of the freeze-dried powder is slow, resulting in a large difference in the moisture content of the obtained azithromycin freeze-dried agent, and the formation of the powder. Poor uniformity, reduced resolubility, poor stability, etc.

Method used

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  • Freeze drying method of azithromycin for injection

Examples

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Comparison scheme
Effect test

Embodiment 1

[0023] Embodiment 1-a kind of freeze-drying method of azithromycin for injection comprises the steps:

[0024] Step 1: Prepare the solution of azithromycin before lyophilization: mix azithromycin with 25% citric acid solution and 73% citric acid-sodium hydroxide mixed solution in turn, stir until clear, and use the remaining amount of citric acid solution. The citric acid solution is used as a pH regulator to adjust the pH to 6.60, and the rest is supplemented with water for injection to obtain the solution of azithromycin before lyophilization;

[0025] Among them, the prescription volume ratio of azithromycin, anhydrous citric acid, sodium hydroxide and water for injection is: 500:394:190:5548;

[0026] The citric acid-sodium hydroxide mixed solution is to add 700rmp / min of sodium hydroxide to 700rmp / min stirring and dissolving at room temperature 26 ℃ by the water for injection of prescription quantity 20%, drop to 8 ℃, add the anhydrous citric acid of prescription quantity...

Embodiment 2

[0030] Embodiment 2-a kind of freeze-drying method of azithromycin for injection comprises the steps:

[0031] Step 1: Prepare the solution of azithromycin before lyophilization: mix the azithromycin with 24.5% citric acid solution and 73.5% citric acid-sodium hydroxide mixed solution in turn, stir until clear, and use the remaining amount of citric acid solution. The citric acid solution is used as a pH regulator to adjust the pH to 6.60, and the rest is supplemented with water for injection to obtain the solution of azithromycin before lyophilization;

[0032] Among them, the prescription volume ratio of azithromycin, anhydrous citric acid, sodium hydroxide and water for injection is: 540:426:190:5548;

[0033]The citric acid-sodium hydroxide mixed solution is to add 700rmp / min of sodium hydroxide at room temperature 26 ℃ to the water for injection of 20% of the prescription quantity, stir and dissolve, then drop to 16 ℃, add anhydrous citric acid of 73.5% of the prescriptio...

Embodiment 3

[0037] Embodiment 3-a kind of freeze-drying method of azithromycin for injection comprises the steps:

[0038] Step 1: Prepare the solution of azithromycin before freeze-drying: mix the azithromycin with 24.8% citric acid solution and 73.2% citric acid-sodium hydroxide mixed solution successively, stir until clear, and use the remaining amount of citric acid solution. The citric acid solution is used as a pH regulator to adjust the pH to 6.60, and the rest is supplemented with water for injection to obtain the solution of azithromycin before lyophilization;

[0039] Among them, the prescription volume ratio of azithromycin, anhydrous citric acid, sodium hydroxide and water for injection is: 520:410:197.5:5769.5;

[0040] The citric acid-sodium hydroxide mixed solution is to add 700rmp / min of sodium hydroxide to 700rmp / min stirring and dissolving at room temperature 26 ℃ by the water for injection of prescription quantity 20%, drop to 12 ℃, add the anhydrous citric acid of pres...

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Abstract

The invention provides a freeze-drying method of azithromycin for injection, which comprises the following steps: (1) mixing azithromycin with a citric acid solution and a citric acid-sodium hydroxide mixed solution in sequence, stirring for clarification, and adjusting the pH value to obtain an azithromycin solution before freeze-drying; (2) after low-temperature water is sprayed outside the filled liquid medicine, pre-freezing; (3) heating the temperature to -10 DEG C from -45 DEG C within 110-130 min at the vacuum degree of 18-22 Pa, keeping the temperature, increasing the vacuum degree to 28-30 Pa, keeping the temperature, recovering the vacuum degree to 20-25 Pa, and continously keeping the temperature; gradually raising the temperature from -10 DEG C to 0 DEG C within 50-70 minutes, and keeping the temperature; and (4) analyzing and drying to obtain the azithromycin freeze-dried powder injection for injection. According to the method, the high-stability azithromycin solution before freeze-drying is combined with a new freeze-drying process curve, so that the method has the characteristics of high freeze-drying powder forming speed, more uniform powder particles, thorough drying and low rejection rate.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical processing technology, in particular to a freeze-drying method of azithromycin for injection. Background technique [0002] Azithromycin (Azithromycin) is a second-generation macrolide semi-synthetic broad-spectrum antibiotic, a derivative of azaerythromycin, which has broad antibacterial spectrum, acid stability, wide distribution in the body, short course of treatment, low toxicity and Good tolerance and other characteristics, it can be suitable for all kinds of people, especially children and the elderly, and it can be used in the treatment of diseases such as upper and lower respiratory tract, skin soft tissue and genitourinary system infections caused by sensitive bacteria, and the curative effect is remarkable. Azithromycin lyophilized preparation for injection is very popular in clinic because of its advantages of fast onset of action and high bioavailability. [0003] However, in t...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K47/12A61K47/02A61K31/7052A61P31/04F26B5/06
CPCA61K9/19A61K9/0019A61K47/12A61K47/02A61K31/7052A61P31/04F26B5/06Y02A50/30
Inventor 刘景萍刘全国陈克领麦发任韩玉燕陈俞竹吴玉涵纪子珍吴伟贞
Owner HAINAN HULUWA PHARMA GRP CO LTD
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