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 low solubility of azithromycin and prolong residence time, and achieve the effect of improving bioavailability, prolonging residence time and reducing the chance of pollution

Inactive Publication Date: 2011-06-29
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] 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

[0026] 0.5%of Achithromycin ultra -fine powder (calculated with the actual content of Akithromycin)

[0027] 5% alginic acid

[0028] NaCl 0.9%

[0029] 0.02% citric acid

[0030] 0.03% of Nepalese ethyl ester

[0031] NaOH AQ is dissolved in an appropriate amount to sea alginic acid

[0032] Add ion water to 10ml of injection.

[0033] The specific process is:

[0034] A polymer solution: Take an injection of 8ml of de -ion water, add the prescribed alginic acid, slowly add a 5%NAOH solution under the condition of the room temperature, until it is all dissolved, at this time the pH of the solution should be close to 7.Then perform 0.22 μm microporous filter membrane pressure filtration.

[0035] B preparation of Achicidin ultra -fine powder: Applied chemical ultrasound method.A certain amount of Akithromycin ingredients are dissolved in the hydrochloric acid solution of 20ml 0.06 mol / L to make Akithromycin hydrochloride.Take a certain amount of sixteen alkyl trisidium bromide and...

Embodiment 2

[0039] Achicillin ultra -fine powder 1%(measured with the actual content of Akithromycin)

[0040] 10% alginic acid

[0041] 0.5% mannitol 0.5%

[0042] Sodium sodium sodium 0.01%

[0043] 0.01% of sulfate mercury

[0044] NaOH AQ is dissolved in an appropriate amount to sea alginic acid

[0045] Add ion water to 10ml of injection.

[0046] The specific process is:

[0047] A polymer solution: Take an injection of 8ml of de -ion water, add the prescribed alginic acid, slowly add a 5%NAOH solution under the condition of the room temperature, until it is all dissolved, at this time the pH of the solution should be close to 7.Then perform 0.22 μm microporous filter membrane pressure filtration.

[0048] B preparation of Achicidin ultra -fine powder: Apply ultrasound emulsified solvents evaporation method.A certain amount of Akithromycin was dissolved in a 100ml cup with a 10ml pyrine, and then the Achicterin solution was mixed with a certain concentration of polyethylene pyrirol.Put ...

Embodiment 3

[0052] 1.5%of Achithromycin ultra -fine powder (calculated with the actual content of Akithromycin)

[0053] 15% sea alginic acid

[0054] KCL 1%

[0055] Sodium sulfate 0.08%

[0056] 0.03% of benzobenbenblyzide

[0057] NaOH AQ is dissolved in an appropriate amount to sea alginic acid

[0058] Add ion water to 10ml of injection.

[0059] The specific process is:

[0060] A polymer solution: Take an injection of 8ml of de -ion water, add the prescribed alginic acid, slowly add a 5%NAOH solution under the condition of the room temperature, until it is all dissolved, at this time the pH of the solution should be close to 7.Then perform 0.22 μm microporous filter membrane pressure filtration.

[0061] B Preparation of Achicidin ultra -fine powder: Application reaction precipitation method.Accurately referred to as Achicillin ingredients dissolved in a sparse HCL of 0.05 mol / L, and prepared Azithromycin HCL solution with a concentration of 0.02 mol / L, and filtered with a filter of 0....

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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

[0001] Technical field [0002] The present invention is a pharmaceutical technology field involving an in original gel eye drops and preparation methods for Achicterin ultra -fine powder ion. Background technique [0003] Due to other types of antibiotics such as ninosone antibiotics such as antibiotics, macrolactone drugs for the treatment of bacterial conjunctivitis and trachoma have caused widespread attention.Azithromycin (AZI) is a large -ring dectind drug. Compared with the erythromycin of the maternal material, Azithromycin has a stable acidity, high concentration in the body tissue, long effect duration, wide antibacterial spectrum, good bacteriostatic effectThe advantages of low side effects.Achicillin has strong antibacterial activity for Gram -positive bacteria in common pathogenic bacteria.MIC ≤ 0.06mf / L is similar or slightly stronger to the role of Luo erythromycin and erythromycin.For Gram -negative bacteria in the Gram -negative bacteria, germ bacon, germine and ...

Claims

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Application Information

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