Eureka AIR delivers breakthrough ideas for toughest innovation challenges, trusted by R&D personnel around the world.

Preparation method for azithromycin micro-emulsion eye drops

A technology for azithromycin and eye drops, which is applied in the fields of emulsion delivery, medical preparations containing active ingredients, and pharmaceutical formulas, and can solve problems such as inaccurate dosage, inaccurate dosage, and poor reproducibility

Inactive Publication Date: 2017-12-01
沈小玲
View PDF1 Cites 1 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Eye ointments can provide long drug residence time but suffer from poor patient compliance due to inaccurate dosing, prone to blurred vision and eyelid crusting, and are usually only used at bedtime
Gel is latex thick liquid or semi-solid, which has the advantages of simple preparation, strong affinity with medicinal parts, especially mucosal tissues, long residence time, and small toxic and side effects, making it especially suitable as a carrier for ophthalmic drug delivery. However, there are also disadvantages of inaccurate dosage and poor reproducibility

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Preparation method for azithromycin micro-emulsion eye drops
  • Preparation method for azithromycin micro-emulsion eye drops
  • Preparation method for azithromycin micro-emulsion eye drops

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0107] A kind of azithromycin microemulsion eye drop, it comprises the following components according to the total mass percentage of raw materials:

[0108]

[0109] Preparation:

[0110] 1) After mixing and dissolving Miglyol 812, Tween 80, and polyoxyethylene castor oil, stir continuously at 40-50°C to form solution Ⅰ;

[0111] 2) Dissolve citric acid and sodium citrate with water for injection, the amount of water for injection is 50% of the total amount, then add the prescribed amount of azithromycin, L-cysteine, mannitol and benzalkonium chloride, at 40-50°C Stir continuously, and adjust the pH to 6.5 with a pH regulator to form solution II;

[0112] 3) Slowly inject and drop solution I into solution II, while stirring continuously at 40-50°C, stirring evenly to form solution III;

[0113] 4) Weigh the carboxylated chitosan, place it in water for injection (the amount is 20% of the total amount), and after the carboxylated chitosan is dissolved, add solution III, an...

Embodiment 2

[0116] A kind of azithromycin microemulsion eye drop, it comprises the following components according to the total mass percentage of raw materials:

[0117]

[0118] The preparation method is the same as that of Example 1 to obtain the finished product of Example 2 microemulsion eye drops.

Embodiment 3

[0120] A kind of azithromycin microemulsion eye drop, it comprises the following components according to the total mass percentage of raw materials:

[0121]

[0122] The preparation method is the same as that of Example 1 to obtain the finished product of Example 3 microemulsion eye drops.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
Particle sizeaaaaaaaaaa
The average particle sizeaaaaaaaaaa
Zeta potentialaaaaaaaaaa
Login to View More

Abstract

The invention discloses a preparation method for azithromycin micro-emulsion eye drops. The preparation method comprises the following steps: under the condition of 40-50 DEG C of the temperature, slowly dropwise adding an oil phase using midchain oil as a matrix into a water phase in which azithromycin, an organic acid and buffer salt thereof are dissolved, adding an emulgator, and uniformly stirring to obtain the azithromycin micro-emulsion eye drops. The preparation method is capable of, under the heating condition, using the midchain oil as the oil phase matrix which is dropwise added into water solution in which the azithromycin and the organic acid and the buffer salt thereof are dissolved, embedding the acidized azithromycin dissolved in the water, and remarkably improving the bioavailability of the eye drops. In addition, O / W microemulsion is formed by a self-emulsifying method under the situation without adding an organic solvent, the permeability of cell membranes is greatly increased, the storage stability of the eye drops is improved, the slow release of the azithromycin in the eyes is realized, the untoward effect of the larger eye irritation by drugs is relieved, the eye drops has the good biocompatibility, the drug loss is reduced, the vision is not affected, the administration frequency is reduced, and the patient adaptability is improved.

Description

technical field [0001] The invention relates to the field of eye drops, in particular to a preparation method of azithromycin microemulsion eye drops. Background technique [0002] Bacterial conjunctivitis is the most common infection. It is widely spread among different countries, races, ages and genders. It is easy to infect in densely populated areas such as kindergartens and schools. Although it has self-healing properties, it is resistant to infection Treatment can shorten the course of the disease, prevent infection, and reduce complications. Gram-positive Staphylococci, Streptococcus pneumoniae, and Haemophilus influenzae were the most common pathogens. [0003] Acute bacterial conjunctivitis is a highly contagious acute conjunctival inflammation with bacteria as the pathogen that occurs mainly in summer and autumn. It is the most frequently encountered eye disease in daily ophthalmology first visits. Bacterial keratitis and conjunctivitis often cause varying degree...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): A61K31/7052A61K9/107A61K47/44A61P27/02A61P31/04
CPCA61K31/7052A61K9/1075A61K47/44
Inventor 沈小玲
Owner 沈小玲
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Eureka Blog
Learn More
PatSnap group products