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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: 2022-02-15
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, 0.8g of NaCl, and 0.02g of KCl in 100mL of water for injection, dissolve them completely, and prepare the water phase, keep it warm at 60°C, and set aside;

[0055] Step 2: Dissolve 1 g of azithromycin, 8 g of egg yolk lecithin PC-98T, 2 g of cholesterol monosuccinate, 0.1 g of DSPE-PEG2000, 0.05 g of dl-α-tocopherol, and 8.5 g of medium-chain triglycerides 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 azithrom...

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, 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. The azithromycin ion-pair liposome eye drops per 100ml contains: azithromycin 0.5-2g, phospholipids 5-10g, cholesterol derivatives 1-5g, oil phase 5-10g, DSPE-PEG 2000 50-200mg, antiseptic Antioxidant 1‑5mg, antioxidant 30‑80mg. The azithromycin ion-pair liposome eye drops of the present invention adopts ion-pairing technology for drug loading, which improves the solubility and stability of the drug in the preparation, and obviously increases the drug-loading capacity of the drug. And it can be better used in the treatment of dry eye, with high bioavailability.

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 Patents(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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