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Azithromycin syrup and preparation method thereof

A technology of azithromycin and syrup, which is applied in the field of azithromycin syrup and its preparation, can solve the problems of poor stability and poor compliance of clinical medication, and achieve the effects of increasing stability, rapid drug onset, and preventing microbial contamination

Active Publication Date: 2014-12-17
GUANGDONG SHUNFENG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Based on this, it is necessary to address the problems of poor stability and poor compliance of clinical medication in the existing oral preparations of azithromycin, and provide an azithromycin syrup with good stability, good bioavailability, convenient medication and good taste

Method used

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  • Azithromycin syrup and preparation method thereof
  • Azithromycin syrup and preparation method thereof
  • Azithromycin syrup and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Embodiment one: the selection of azithromycin salt-forming agent

[0031] Azithromycin is insoluble in water and cannot be directly made into a syrup. Since the molecular structure of azithromycin has two amino groups, it is considered to react with an acid to prepare a water-soluble salt of azithromycin. However, among the clinically acceptable acids, the acid that can form a salt with sufficient water solubility with azithromycin, the pH value of the resulting aqueous solution can meet the requirements of oral preparations (pH value is 5.0-6.0), and the acid with little toxic and side effects in clinical application is not suitable. In addition, because azithromycin is sensitive to acid, its chemical structure is easily destroyed when it forms a salt with acid.

[0032] After a lot of tests and analysis, this application selected glutamic acid as the salt-forming agent, which can significantly improve the solubility of azithromycin in water without destroying the stru...

Embodiment 2

[0056] Embodiment two: the selection of the oxidizing agent in the azithromycin syrup

[0057] Azithromycin has poor stability and is easy to degrade. The azithromycin syrup of the present invention uses antioxidants, metal chelating agents and cyclodextrin in combination to exert a synergistic antioxidant effect and can effectively improve the stability of azithromycin.

[0058] Take the azithromycin glutamate solution, add the antioxidants shown in Table 5 respectively, carry out the accelerated damage stability test, place it at 40°C ± 2°C, and take samples on the 10th day, the 20th day, and the 30th day respectively. The content of azithromycin was determined, and the test results are shown in Table 5.

[0059] Table 5 Effect of antioxidants on the stability of azithromycin glutamate solution

[0060]

[0061] The experimental results showed that β-cyclodextrin combined with thiourea and EDTA-2Na formed inclusion antioxidants and improved the stability of azithromycin ...

Embodiment 3

[0064] Embodiment three: the preparation of azithromycin syrup of the present invention

[0065] Follow the steps below to prepare azithromycin syrup:

[0066] 1) Weigh each component according to the following formula:

[0067] components

Dosage

Azithromycin

20g

glutamic acid

8.0g

β-cyclodextrin

35g

Thiourea

1.0g

EDTA-2Na

0.3g

Benzoic acid

2.0g

Ethylparaben

0.5g

strawberry flavor

1.0g

Amaranth

0.005g

sucrose

650g

purified water

1000mL

[0068] 2) Add sucrose to 300 ml of purified water, stir and heat until boiling, so that the sucrose is completely dissolved into syrup, cool down to below 60°C, and filter;

[0069] 3) Add amaranth into 1 ml of purified water and stir until completely dissolved;

[0070] 4) Heat 230ml of purified water to boiling, add β-cyclodextrin, thiourea, EDTA-2Na, benzoic acid and ethylparaben, stir until comple...

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Abstract

The invention discloses azithromycin syrup which comprises the following components by weight in every 100ml of purified water: 1-2.5g of azithromycin, 0.5-1.5g of glutamic acid, 0.5-5g of cyclodextrin, 35-65g of cane sugar, 0.05-0.5g of antioxidant and 0.02-0.05g of metal chelating agent. The azithromycin syrup prepared by the invention has the advantages of high stability, high bioavailability, convenience in administration and good taste.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to azithromycin syrup and a preparation method thereof. Background technique [0002] In recent years, due to the rise of β-lactamase strains produced by common respiratory pathogens such as influenza bacillus, pneumococcus, and Moraxella catarrhalis, the increase of other pathogenic microorganisms such as mycoplasma, chlamydia, and Legionella infections, as well as the increase in immunodeficiency patients Mycobacterium avium, The emergence of Toxoplasma infection has brought attention to the clinical application of macrolide antibiotics. [0003] Azithromycin is one of the modified macrolide derivatives. It mainly binds to the bacterial 50S ribosomal subunit, blocks the translocation of peptides, and prevents the synthesis of bacterial polypeptides to achieve antibacterial effects. Azithromycin has the advantages of wide antibacterial activity, strong tissue p...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61P15/00A61P13/00A61K31/7052A61P11/00A61P31/04A61K9/00A61P17/00A61K47/16
Inventor 余良钟潘红炬梁勇坤潘欢云洪淑华王北明
Owner GUANGDONG SHUNFENG PHARMA