Eye amphotericin B flexible liposome

A technology of flexible liposome and amphotericin, which is applied in the direction of liposome delivery, organic active ingredients, and medical preparations containing active ingredients, etc. To achieve the effect of good drug stability, definite curative effect and high bioavailability

Inactive Publication Date: 2009-03-25
SHANDONG EYE INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The flexible modifiers used in flexible liposomes are such as sodium cholate, sodium deoxycholate, Tween and Spans, etc. These flexible modifiers have corneal toxicity and cannot be used in topic

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Example Embodiment

[0017] Example 1

[0018] Dissolve 15mg amphotericin B, 150mg phospholipid, and 50mg cholesterol in 50ml ether. Rotary evaporation to fully remove the ether to obtain a uniformly dispersed film of the drug and phospholipids. Add 1.5mg dipotassium glycyrrhizinate, dissolve it with 15ml water for injection, and wash the membrane thoroughly , The emulsion is obtained after uniform ultrasonic dispersion, and the emulsion is passed through a high-pressure homogenizer, first pulverized with 500bar pressure cycle 5 times, and then 1500bar pressure cycle 15 times for further refinement and pulverization, to obtain ophthalmic amphotericin B flexible lipid body. Adjust the osmotic pressure of the ophthalmic amphotericin B flexible liposome with sodium chloride to isotonic, and adjust the pH value to 6.5 with dilute boric acid to obtain the amphotericin B flexible liposome eye drops. The laser particle size potential analyzer measured the particle size of the flexible liposome to be 10nm-100...

Example Embodiment

[0019] Example 2

[0020] Dissolve 15mg amphotericin B, 150mg phospholipid, and 50mg cholesterol in 50ml ether. Rotary evaporation to fully remove the ether to obtain a uniformly dispersed film of drug and phospholipid. Add 15mg dipotassium glycyrrhizinate, dissolve it with 15ml water for injection, and wash the membrane thoroughly. The emulsion is uniformly dispersed by ultrasonic, and the emulsion is passed through a high-pressure homogenizer, first pulverized with 500 bar pressure cycle 5 times, and then 1500 bar pressure cycle 15 times for further refinement and pulverization, to obtain ophthalmic amphotericin B flexible liposomes .

Example Embodiment

[0021] Example 3

[0022] Dissolve 1g of amphotericin B and 20g of phospholipids in 1000ml of dichloromethane. Rotary evaporation to fully remove the dichloromethane to obtain a uniformly dispersed film of the drug and phospholipids. Add 4g of dipotassium glycyrrhizinate, dissolve it with 1000ml of water for injection, and wash the film thoroughly. , The emulsion is obtained after uniform ultrasonic dispersion, and the emulsion is passed through a high-pressure homogenizer, first pulverized with 500bar pressure cycle 5 times, and then 1500bar pressure cycle 15 times for further refinement and pulverization, to obtain ophthalmic amphotericin B flexible lipid body.

[0023] An example of a control experiment using the present invention is as follows:

[0024] Fifty-six healthy New Zealand white rabbits were randomly divided into 2 groups, one group was 0.1% amphotericin B liposome eye drops (injection amphotericin B liposome), each rabbit 50μl eye drops, The aqueous humor was extrac...

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PUM

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Abstract

The invention discloses an eye amphotericin B flexible liposome which contains amphotericin B, phospholipids, cholesterol, flexible modifier of flexible liposome, osmotic pressure regulator and PH regulator which regulate the PH value to 5.5-8.0; wherein, the dosage of the amphotericin B is 1%-20% of phospholipid by mass percentage in flexible liposome. The eye amphotericin B flexible liposome is characterized in that the flexible modifier of flexible liposome is dipotassium glycyrrhizinate; wherein, dipotassium glycyrrhizinate is 1%-20% of phospholipid by mass percentage; the phospholipid can be soybean phospholipid or egg yolk lecithin which is in the pharmaceutical auxiliary material level. The invention adopts flexible modifier without corneal toxicity to prepare flexible liposome which is firstly applied to the ocular medicine delivery such as eye drop; excellent deformation performance of the flexible liposome is sufficiently utilized to reduce the resistance of medicine entering eye through corneal epithelial cell membrane, so as to improve the absorption and treatment effect of the ocular medicine so that the local ocular irritation and toxic side effects are avoided; the medicine stability and treatment effect are good.

Description

technical field [0001] The invention relates to an ophthalmic amphotericin B flexible liposome. Background technique [0002] In recent years, with the gradual increase in the application of antibiotics, glucocorticoids, immunosuppressants, corneal contact lenses, and vegetative trauma, the incidence of ocular fungal infections is on the rise, and it has become a difficult disease to treat and has a high rate of blindness. Infectious eye disease. The main pathogenic bacteria are Fusarium and Aspergillus, and the pathogenic genera present diversity. The most common fungal infections of the eye are fungal keratitis and fungal endophthalmitis. [0003] Fungal keratitis (fungal keratitis) is a common blinding eye disease worldwide, and it is more common in developing countries dominated by agricultural populations. In recent years, fungal keratitis has been increasing year by year in China, and has become the leading cause of corneal blindness in some areas. At present, due ...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/7048A61P27/02
Inventor 谢立信吴祥根
Owner SHANDONG EYE INST
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