Azithromycin ion pair liposome eye drops and preparation method thereof

A technology of azithromycin and liposome, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., and can solve problems such as insoluble azithromycin oil

Active Publication Date: 2019-02-26
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0017] Azithromycin is a Lewis base and tends to combine with Lewis acidic auxiliary materials (cholesterol succinate monoester, etc.) to form ion pairs. The present invention uses hydrophobic ion pair technology to solve the problem that azithromycin is insoluble in both oil and water

Method used

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  • Azithromycin ion pair liposome eye drops and preparation method thereof
  • Azithromycin ion pair liposome eye drops and preparation method thereof
  • Azithromycin ion pair liposome eye drops and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Example 1 Formula 1 Azithromycin content 1g: 100ml

[0051] Based on 100ml eye drops

[0052]

[0053] The preparation steps of azithromycin ion-pair liposome eye drops are as follows:

[0054] Step 1: Na 2 HPO 4 12H 2 O 0.29g, NaH 2 PO 4 2H 2 O 0.13g, KH 2 PO 4 Disperse 0.02g, NaCl0.8g, KCl0.02g in 100mL water for injection, dissolve them all, and prepare the water phase, keep it warm at 60°C, and set aside;

[0055] Step 2: Dissolve azithromycin 1g, egg yolk lecithin PC-98T 8g, cholesterol succinate monoester 2g, DSPE-PEG 20000.1g, dl-α-tocopherol 0.05g, medium chain triglyceride 8.5g in chloroform and transfer into a round-bottomed flask, and chloroform was removed by rotary evaporation to obtain a yellow oily liquid. Continue drying the obtained oily substance under nitrogen flow for 1 h; hydrate the obtained oily substance with the aqueous phase prepared in step 1 at 60° C. for 30 minutes to obtain azithromycin liposome coarse dispersion system, which...

Embodiment 2

[0060] Example 2 formula 2 azithromycin content 2g: 100ml

[0061] Based on 100ml eye drops

[0062]

[0063] The preparation steps of azithromycin ion-pair liposome eye drops are the same as in Example 1.

[0064] Among them, the liposome has no oil droplets, no insoluble components or massive aggregates under the naked eye observation, no azithromycin precipitation under the microscope, the particle size is 137.0nm, the Zeta potential is -28.36mv, the pH value is 7.79, and the content is 93.4%. The encapsulation rate is 92.7%, and the osmotic pressure is in the range of 280-310 mosm / kg.

Embodiment 3

[0065] Example 3 Formula 3 Azithromycin content 0.5g: 100ml

[0066] Based on 100ml eye drops

[0067]

[0068] The preparation steps of azithromycin ion-pair liposome eye drops are the same as in Example 1.

[0069] Among them, the liposome has no oil droplets, no insoluble components or massive aggregates under the naked eye observation, no azithromycin precipitation under the microscope, the particle size is 29.8nm, the Zeta potential is -19.64mv, the pH value is 7.88, and the content is 99.6%. The encapsulation rate is 98.3%, and the osmotic pressure is in the range of 280-310 mosm / kg.

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Abstract

The invention belongs to the field of pharmaceutical preparations, and relates to azithromycin ion pair liposome eye drops and a preparation method thereof, particularly to a method for preparing azithromycin ion pair liposome eye drops from a cholesterol derivative by using azithromycin as an active component, and new uses of the azithromycin ion pair liposome eye drops in preparation of xerophthalmia treating drugs, wherein per 100 ml of the azithromycin ion pair liposome eye drops comprise 0.5-2 g of azithromycin, 5-10 g of phospholipid, 1-5 g of a cholesterol derivative, 5-10 g of an oil phase, 50-200 mg of DSPE-PEG, 1-5 mg of a preservative, and 30-80 mg of an antioxidant. According to the present invention, the azithromycin ion pair liposome eye drops load the drug by using the ion pair technology, such that the solubility and the stability of the drug in the preparation are improved, the drug loading amount is significantly increased, the azithromycin ion pair liposome eye dropscan be well used for the treatment of xerophthalmia, and the bioavailability is high.

Description

Technical field: [0001] The invention belongs to the field of pharmaceutical preparations, and relates to azithromycin ion-pair liposome eye drops and a preparation method thereof, in particular to a method for preparing azithromycin ion-pair liposome eye drops with azithromycin as an active ingredient and cholesterol derivatives The method and its new application in the preparation of medicine for treating dry eye syndrome. Background technique: [0002] Dry eye, also known as keratoconjunctival sicca, is a type of disease that causes ocular surface damage due to insufficient tear secretion due to unstable lacrimal gland secretion, causing various symptoms in the eye, such as inflammation, pain, redness, and itching. Dry eye can also cause some complications, making the condition more complicated. Because of its complexity and diversity, it is easy to be misdiagnosed as keratitis, conjunctivitis and other diseases. Meibomian gland dysfunction (meibomian gland dysfuction, ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/69A61K47/54A61K31/7052A61P27/02
CPCA61K9/0048A61K31/7052
Inventor 唐星林小杨张宇何海冰尹湉黄成龙
Owner SHENYANG PHARMA UNIVERSITY
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