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Azithromycin ultrafine powder in-situ gel eye drops and preparation method thereof

A technology of azithromycin and ultrafine powder, which is applied in the field of medicine, can solve the problems of prolonged residence time and low solubility of azithromycin, and achieve the effects of prolonging residence time, improving bioavailability and stable storage

Inactive Publication Date: 2012-11-07
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] The purpose of the present invention is to solve the problem of low solubility of azithromycin, another purpose is to prolong the residence time of the preparation in the eye, aiming at the characteristics of azithromycin as a time-dependent antibiotic, improve the local bioavailability of the drug, and provide a clinical A Practical, Reliable and Convenient Azithromycin Ophthalmic Preparation for Treating Eye Infections

Method used

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  • Azithromycin ultrafine powder in-situ gel eye drops and preparation method thereof
  • Azithromycin ultrafine powder in-situ gel eye drops and preparation method thereof
  • Azithromycin ultrafine powder in-situ gel eye drops and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Using alginic acid as the base material, (1mL deionized water for injection: 0.005g main drug)

[0026] Azithromycin superfine powder 0.5% (based on the actual content of azithromycin)

[0027] Alginic Acid 5%

[0028] NaCl 0.9%

[0029] Citric acid 0.02%

[0030] Ethylparaben 0.03%

[0031] Appropriate amount of NaOH aq to dissolve alginic acid

[0032] Add deionized water for injection to 10mL.

[0033] The specific process is:

[0034] A Polymer solution: Take 8ml of deionized water for injection, add the prescribed amount of alginic acid, and slowly add 5% NaOH solution under stirring at room temperature until it is completely dissolved. At this time, the pH of the solution should be close to 7. Then perform pressure filtration with a 0.22 μm microporous membrane.

[0035] B Preparation of ultrafine powder of azithromycin: application of chemical ultrasonic method. A certain amount of azithromycin bulk drug is dissolved in the hyd...

Embodiment 2

[0038] Using alginic acid as the base material, (1mL deionized water for injection: 0.01g main drug)

[0039] Azithromycin superfine powder 1% (based on the actual content of azithromycin)

[0040] Alginic Acid 10%

[0041] Mannitol 0.5%

[0042] Sodium sulfite 0.01%

[0043] Thimerosal 0.01%

[0044] Appropriate amount of NaOH aq to dissolve alginic acid

[0045] Add deionized water for injection to 10mL.

[0046] The specific process is:

[0047] A Polymer solution: Take 8ml of deionized water for injection, add the prescribed amount of alginic acid, and slowly add 5% NaOH solution under stirring at room temperature until it is completely dissolved. At this time, the pH of the solution should be close to 7. Then perform pressure filtration with a 0.22 μm microporous membrane.

[0048] B Preparation of ultrafine powder of azithromycin: application of ultrasonic emulsification solvent evaporation method. A certain amount of azithromycin is d...

Embodiment 3

[0051] Using alginic acid as the base material, (1mL deionized water for injection: 0.015g main drug)

[0052] Azithromycin superfine powder 1.5% (based on the actual content of azithromycin)

[0053] Alginic Acid 15%

[0054] KCl 1%

[0055] Sodium thiosulfate 0.08%

[0056] Benzalkonium Bromide 0.03%

[0057] Appropriate amount of NaOH aq to dissolve alginic acid

[0058] Add deionized water for injection to 10mL.

[0059] The specific process is:

[0060] A Polymer solution: Take 8ml of deionized water for injection, add the prescribed amount of alginic acid, and slowly add 5% NaOH solution under stirring at room temperature until it is completely dissolved. At this time, the pH of the solution should be close to 7. Then perform pressure filtration with a 0.22 μm microporous membrane.

[0061] B Preparation of ultrafine powder of azithromycin: application of reaction precipitation method. Accurately weigh the azithromycin raw material and...

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Abstract

The invention provides azithromycin ultrafine powder in-situ gel eye drops and a preparation method thereof. The method comprises the following steps of: firstly, micronizing a medicament by using a proper method to remarkably improve the dissolution rate and solubility of the medicament; and secondly, preparing an ophthalmic preparation which is in a liquid state in vitro and is in a gel state when dripped into eyes by adopting sodium alginate as an ion-sensitive gel matrix or adopting poloxamer 407 and poloxamer 188 as thermosensitive gel matrixes. The eye drops are steady in storage at 4 DEG C and uniform in content, and are not required for secondary preparation so as to reduce contamination. In the method, azithromycin ultrafine powder and in-situ gel are combined for the treatment of bacterial keratitis and trachoma; and by the dual effects of the ultrafine powder and the gel, the sustained release effect is achieved when the retention time of the preparation in the eyes is prolonged, so that the local bioavailability of the medicament and the compliance of patients are improved, and the medicament absorption of the cornea is increased to reduce the toxic or side effect caused by the systemic absorption of ophthalmic medicaments.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to azithromycin ultrafine powder ion in-situ gel eye drops and a preparation method thereof. Background technique [0002] Due to resistance to other classes of antibiotics such as quinolones, macrolides have attracted widespread attention in the treatment of bacterial conjunctivitis and trachoma. Azithromycin (AZI) is a macrocyclic lactone drug. Compared with the parent raw material erythromycin, azithromycin is relatively stable to acid, has a high concentration in the body tissue, a long duration of action, a broad antibacterial spectrum, and good antibacterial effect. , low side effects and other advantages. Azithromycin has strong antibacterial activity against Gram-positive cocci among common pathogenic bacteria, and has strong antibacterial activity against Staphylococcus aureus, hemolytic streptococcus, Streptococcus pneumoniae, Streptococcus viridans, Streptococcus Neisseri...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/00A61K31/7052A61K47/34A61K47/36A61P27/02A61P31/04A61K47/10
Inventor 王东凯
Owner SHENYANG PHARMA UNIVERSITY
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