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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 topical administration of the eye. Some flexible liposomes can only be used for transdermal drug delivery to improve the transdermal absorption effect, and there is no precedent for eye drug delivery

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

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

Embodiment 2

[0020] Dissolve 15mg of amphotericin B, 150mg of phospholipid, and 50mg of cholesterol in 50ml of ether, and remove the ether by rotary evaporation to obtain a uniformly dispersed film of drug and phospholipid. Add 15mg of dipotassium glycyrrhizinate, dissolve it with 15ml of water for injection, and wash the film thoroughly. Ultrasonic dispersion is uniform to obtain an emulsion, and the emulsion is passed through a high-pressure homogenizer, first crushed with 500bar pressure cycles for 5 times, and then further refined and crushed with 1500bar pressure cycles for 15 times to obtain ophthalmic amphotericin B flexible liposomes .

Embodiment 3

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

[0023] Use the present invention to carry out one example of control experiment as follows:

[0024] Get 56 healthy New Zealand white rabbits and divide them into 2 groups at random. One group is 0.1% amphotericin B liposome eye drops (with amphotericin B liposome for injection), 50 μl eye drops for each rabbit. Aqueous humor was extracted at 5min, 15m...

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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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