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Nystatin flexible liposome as well as gel and preparation method of nystatin flexible liposome

A flexible liposome and nystatin technology, which is applied in liposome delivery, antifungal agents, pharmaceutical formulations, etc., can solve the problems of non-absorption, difficult storage, and sensitivity of nystatin, and achieve enhanced residence time and cost Low, easy-to-use effect

Inactive Publication Date: 2012-07-25
JILIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The invention discloses a flexible liposome of nystatin, which solves the problem that nystatin is not absorbed through the skin and is not easy to store, has the effect of treating skin surface and deep layer infections, and can be used to treat systemic fungal infections, and Susceptible to multidrug-resistant fungi

Method used

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  • Nystatin flexible liposome as well as gel and preparation method of nystatin flexible liposome
  • Nystatin flexible liposome as well as gel and preparation method of nystatin flexible liposome
  • Nystatin flexible liposome as well as gel and preparation method of nystatin flexible liposome

Examples

Experimental program
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Embodiment 1

[0029] Weigh 4g of hydrogenated soybean lecithin, add 2g of cholesterol, dissolve in 150ml of chloroform; weigh another 1g of nystatin, dissolve in 500mL of methanol. The two solutions were mixed and ultrasonicated for 5 min. Evaporate to dryness under reduced pressure at 48°C, blow nitrogen for 6h, and remove residual organic solvent. Add a hydration solution containing 67.5 g of sucrose, 150 g of ethanol, 600 g of water, and 10 g of sodium cholate, hydrate at 65° C. for 2 h, pass through a 100 nm carbonate membrane twice, and obtain flexible nystatin liposomes.

Embodiment 2

[0031] Weigh 20g of soybean lecithin, add 1g of cholesterol, dissolve in 630ml of chloroform; weigh another 10g of nystatin, dissolve in 2000mL of methanol. The two solutions were mixed and sonicated for 10 min. Evaporate to dryness under reduced pressure at 48°C, blow nitrogen for 8 hours, remove residual organic solvents, add a hydration solution containing 90g of sucrose, 300g of ethanol, 700g of water, and 50g of sodium deoxycholate, hydrate at 60°C for 1 hour, pass through a 100nm carbonate membrane 3 times to obtain nystatin flexible liposomes.

Embodiment 3

[0033] Weigh 15g of hydrogenated soybean lecithin, add 3g of cholesterol, dissolve in 360ml of chloroform; weigh another 8g of nystatin, dissolve in 4000mL of methanol. The two solutions were mixed and sonicated for 10 min. Evaporate to dryness under reduced pressure at 48°C, blow nitrogen for 6 hours, remove residual organic solvents, add a hydration solution containing 135g of sucrose, 500g of ethanol, 1000g of water, and 30g of sodium deoxycholate, hydrate at 65°C for 2.5h, and form a 100nm carbonate film. Membrane 5 times to obtain flexible liposomes of nystatin.

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Abstract

The invention provides a nystatin flexible liposome and external preparation gel and simultaneously discloses a preparation method of the nystatin flexible liposome. Through the nanometer liposome technology, nystatin is covered and sealed in the liposome, the solubility of the nystatin is enhanced, the liposome recipe is improved, sodium cholate or sodium deoxycholate is added, the flexible liposome is prepared, the liposome pereutaoeous permeation is enhanced, in addition, the nystatin stability can be improved, a nystatin cutaneous penetration path is developed, and the treatment effect is realized in aspects of skin superficial layer or deep infection and systemic fungal infection. The nystatin flexible liposome is prepared into the gel, the detention time of the nystatin flexible liposome on the skin is prolonged, the use is simple and convenient, the cost is low, in addition, the compliance of users is improved, the toxicity is reduced, medicine storage bases can be formed on the skin, medicine is continuously released, and the medicine acting time is prolonged.

Description

technical field [0001] The invention relates to the field of novel preparations of antibacterial drugs, in particular provides a flexible liposome of nystatin and a gel for external use, and discloses a preparation method thereof. Background technique [0002] In 1950, it was discovered that the soil microorganism Streptomyces noursei could secrete an anti-mold substance, thus discovering the first anti-mold antibiotic. Nystatin has a conjugated polyene macrolide structure, which can inhibit the activity of fungi and dermatophytes, but has no inhibitory effect on bacteria. Nystatin is a membrane permeability enhancer. It has a strong inhibitory effect on a variety of fungi such as yeast, Candida albicans, and Blastomyces dermatitis. Nystatin is not absorbed by the gastrointestinal tract after oral administration, and the blood concentration is extremely low after oral administration, so it has no therapeutic effect on systemic fungal infections. Almost the entire dose is ...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K9/00A61K31/7048A61K47/28A61K47/32A61P31/10
Inventor 滕利荣尹秀菊孟庆繁权宇彤赵敏汤海峰姜丹王贞佐逯家辉
Owner JILIN UNIV
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