Slow-release azithromycin ion exchange resin compound and application thereof

A technology of ion exchange resin and slow-release azithromycin, which is applied in the field of medicine and can solve the problems of small capacity and low drug loading of ion exchange resin

Active Publication Date: 2017-03-22
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, it still has many deficiencies at present, such as the small capacity of ion exchange resins, and is only suitable for water-soluble ionic drugs (water-insoluble drugs can be added with ionizing agents to form dissociable salt solutions, but due to ionizing agents inhibiting The dissociation of the active groups of the ion exchange resin leads to a very low drug loading), etc.

Method used

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  • Slow-release azithromycin ion exchange resin compound and application thereof
  • Slow-release azithromycin ion exchange resin compound and application thereof
  • Slow-release azithromycin ion exchange resin compound and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Example 1: Dissolve 20 g of azithromycin in a mixed solvent of 1000 mL of ethanol-water (3:2 in volume ratio), add 40 g of methacrylic acid-based weakly acidic cation exchange resin (Amberlite IRP64), continue to stir for 4 hours, let stand, Filter and dry to obtain azithromycin ion exchange resin complex. After determination, the content of azithromycin in the azithromycin ion exchange resin complex is 32.1%. The dissolution amounts at 0.5 hour, 1 hour and 3 hours were 86.48%, 92.59% and 98.78%, respectively.

Embodiment 2

[0053] Example 2: Dissolve 10g of azithromycin and 25g of acrylic resin (Eudragit RL 100) in a mixed solvent of 1000mL of ethanol-water (2:3 by volume), and then dissolve 20g of methacrylic acid weakly acidic cation exchange resin (Amberlite IRP64) column packing, the above-mentioned solution containing medicine and retardation material is sampled from the top of the ion-exchange resin column, and the outflow solution circulates through the ion-exchange resin column, and the ion-exchange resin in the column is taken out and dried to obtain a slow-release azithromycin ion-exchange resin Complex. It is determined that the content of azithromycin in the slow-release azithromycin ion exchange resin complex is 28%. The dissolution amounts at 0.5 hour, 1 hour and 3 hours were 2.02%, 8.66% and 20.56%, respectively.

Embodiment 3

[0054] Example 3: Dissolve 20g of azithromycin and 5g of acrylic resin (Eudragit RL 100) in a mixed solvent of 1000mL of ethanol-water (3:2 by volume), and add 40g of methacrylic acid weakly acidic cation exchange resin (Amberlite IRP64 ), continuously stirred for 8 hours, allowed to stand, filtered, and dried to obtain a sustained-release azithromycin ion-exchange resin complex. After determination, the content of azithromycin in the slow-release azithromycin ion exchange resin complex is 29.6%. The dissolution amounts at 0.5 hour, 1 hour and 3 hours were 60.63%, 72.37% and 86.91%, respectively.

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PUM

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Abstract

The invention belongs to the technical field of medicines, and relates to a slow-release azithromycin ion exchange resin compound and a preparation method and application thereof. The slow-release azithromycin ion exchange resin compound comprises the following components: azithromycin, ion exchange resin and a retardant, wherein the content of the azithromycin is equivalent to 5-50% of the amount of the dry azithromycin ion exchange resin compound; the content of the ion exchange resin is equivalent to 30-80% of the amount of the dry azithromycin ion exchange resin compound; and the content of the retardant is equivalent to 0.05-5% of the amount of the dry azithromycin ion exchange resin compound. The prepared azithromycin ion exchange resin compound has good slow-release effect.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a sustained-release azithromycin ion-exchange resin complex and a preparation method and application thereof. Background technique [0002] Azithromycin is a semi-synthetic 15-membered ring azalide antibiotic. Its mechanism of action is to interfere with bacterial protein synthesis by binding to the subunit of the bacterial 50s ribosome. Azithromycin has a long half-life and is a time-dependent antibiotic. Compared with erythromycin, azithromycin has stronger antibacterial effect, and it is mainly used clinically to treat acute pharyngitis, sinusitis, otitis media, pneumonia caused by Haemophilus influenzae and Mycoplasma pneumoniae, urethritis, cervicitis and sensitive bacteria. skin and soft tissue infections. [0003] Adverse reactions of azithromycin, such as abdominal pain, nausea, and vomiting, are relatively common in clinical practice. The occurrence of these adverse re...

Claims

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Application Information

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IPC IPC(8): A61K31/7052A61K47/32A61K47/38A61K47/34A61P31/04
CPCA61K31/7052A61K47/32A61K47/34A61K47/38
Inventor 徐晖赵美慧王绍宁陈慧琳张欣茹
Owner SHENYANG PHARMA UNIVERSITY
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