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Natamycin cationic liposome eye drop and preparation method thereof

A cationic liposome and natamycin technology, which is applied in liposome delivery, medical preparations containing active ingredients, organic active ingredients, etc., can solve the problem of eye discomfort in patients with increased preparation costs, complex preparation process, and drug Large dosage and other problems, to achieve the effects of reducing drug leakage, good permeability, and high transcorneal transfer rate

Inactive Publication Date: 2015-06-10
THE AFFILIATED HOSPITAL OF QINGDAO UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the above patents partially solve the problems in the prior art, the invention still has the disadvantages of large drug dosage, high cost and complicated preparation process.
The content of natamycin contained in this invention is relatively high, and the concentration of natamycin is low when it acts on the eye, which increases the cost of preparation and the potential eye discomfort of patients to a certain extent
In addition, the invention demonstrated the corneal permeability and eye action time of its eye drops through controlled experiments, and did not evaluate its curative effect

Method used

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  • Natamycin cationic liposome eye drop and preparation method thereof
  • Natamycin cationic liposome eye drop and preparation method thereof
  • Natamycin cationic liposome eye drop and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] A kind of natamycin cationic liposome eye drop, comprises natamycin and phosphate buffer saline, and described eye drop also comprises lecithin, cholesterol and octadecylamine, and concrete component quantity is as follows:

[0028]

[0029]

[0030] The preparation technology of above-mentioned natamycin cationic liposome eye drops, comprises the steps:

[0031] Step 1: Dissolve natamycin in an appropriate amount of methanol, lecithin, cholesterol and octadecylamine in an appropriate amount of chloroform, mix them in a water bath at 48°C, rotate at 110 rpm, and evaporate at a reduced pressure of 0.08-0.09 MPa until a thin film is formed;

[0032] Step 2: Add PBS pH=7.0, 40°C water bath, rotate 140rpm for elution;

[0033] Step 3: Stir the obtained suspension magnetically for 30 minutes, and sonicate in an ultrasonic cleaner for 10 minutes to obtain the natamycin cationic liposome suspension.

Embodiment 2

[0035] A kind of natamycin cationic liposome eye drop, comprises natamycin and phosphate buffer saline, and described eye drop also comprises lecithin, cholesterol and octadecylamine, and concrete component quantity is as follows:

[0036]

[0037] The preparation technology of above-mentioned natamycin cationic liposome eye drops, comprises the steps:

[0038] Step 1: Dissolve natamycin in an appropriate amount of methanol, lecithin, cholesterol and octadecylamine in an appropriate amount of chloroform, mix them in a water bath at 48°C, rotate at 110 rpm, and evaporate at a reduced pressure of 0.08-0.09 MPa until a thin film is formed;

[0039] Step 2: Add PBS pH=7.0, 40°C water bath, rotate 140rpm for elution;

[0040] Step 3: Stir the obtained suspension magnetically for 30 minutes, and sonicate in an ultrasonic cleaner for 10 minutes to obtain the natamycin cationic liposome suspension.

Embodiment 3

[0042] A kind of natamycin cationic liposome eye drop, comprises natamycin and phosphate buffer saline, and described eye drop also comprises lecithin, cholesterol and octadecylamine, and concrete component quantity is as follows:

[0043]

[0044]

[0045] The preparation technology of above-mentioned natamycin cationic liposome eye drops, comprises the steps:

[0046] Step 1: Dissolve natamycin in an appropriate amount of methanol, lecithin, cholesterol and octadecylamine in an appropriate amount of chloroform, mix them in a water bath at 48°C, rotate at 110 rpm, and evaporate at a reduced pressure of 0.08-0.09 MPa until a thin film is formed;

[0047] Step 2: Add PBS pH=7.0, 40°C water bath, rotate 140rpm for elution;

[0048]Step 3: Stir the obtained suspension magnetically for 30 minutes, and sonicate in an ultrasonic cleaner for 10 minutes to obtain the natamycin cationic liposome suspension.

[0049] In order to further evaluate the quality and therapeutic benefi...

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Abstract

The invention relates to a natamycin eye drop and particularly relates to a natamycin cationic liposome eye drop and a preparation method thereof. The natamycin cationic liposome eye drop contains natamycin and a phosphate buffer solution and also comprises lecithin, cholesterol and octadecylamine, wherein the concentration (mass percentage) of natamycin in the eye drop is 0.1-0.2%; the mass ratio of lecithin to cholesterol is 4:1; the mass ratio of lecithin to natamycin is 15:1; and the mass ratio of lecithin to octadecylamine is 20:1. The natamycin cationic liposome eye drop disclosed by the invention has the characteristics of high transmembrane transportation rate, slow-release effect and low toxicity; and meanwhile, due to the adoption of cationic microparticles with positive charges, the cornea detention time of a drug can be remarkably prolonged, and the curative effect of a drug can be remarkably improved.

Description

technical field [0001] The invention relates to natamycin eye drops, in particular to a natamycin cationic liposome eye drop and a preparation process thereof. Background technique [0002] Fungal keratitis is an infectious corneal disease with a high rate of blindness, and it has a high incidence in developing countries. In my country, plant trauma is the main cause of fungal keratitis. With the increase in the number of immunodeficiency patients, the widespread application of immunochemotherapy, the abuse of glucocorticoids and broad-spectrum antibiotics, and the long-term use of contact lenses, the incidence of fungal keratitis has increased year by year. Fusarium and Aspergillus were the main pathogens. The pathogenesis of fungal keratitis is complicated, the types of pathogenic bacteria are many, and the clinical manifestations are complicated, which increases the difficulty of treatment of fungal keratitis. At present, there is still a lack of broad-spectrum and hig...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/7048A61P31/10A61P27/02
Inventor 赵桂秋王雪林静徐强胡丽婷王谦姜楠朱铖铖
Owner THE AFFILIATED HOSPITAL OF QINGDAO UNIV
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