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Azithromycin nanostructured lipid carrier and preparation method thereof

A technology of nanostructured lipids and azithromycin, applied in the field of carrier systems, can solve problems such as the limitation of ophthalmic diseases, and achieve the effect of simple and convenient preparation process, good stability and high repeatability

Inactive Publication Date: 2012-08-15
苏州纳康生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The purpose of the present invention is to provide a nanostructured lipid carrier of azithromycin with high stability and good compatibility, which solves the problems in the prior art that the effect of systemic or local administration of azithromycin in the treatment of ophthalmic diseases is limited due to the special physiological barrier.

Method used

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  • Azithromycin nanostructured lipid carrier and preparation method thereof
  • Azithromycin nanostructured lipid carrier and preparation method thereof
  • Azithromycin nanostructured lipid carrier and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Example 1 Preparation of Azithromycin Nanostructured Lipid Carrier

[0041] Composition formula:

[0042]

[0043] Preparation:

[0044] 1. Weigh 21 grams of polyoxyl stearate S-40, 9 grams of poloxamer F-68, 2.5 grams of glyceryl monostearate and 2.5 grams of castor oil, and put them into the sample tube;

[0045] Heated in a water bath at 2.75°C to make it completely melted, then added 0.5 g of azithromycin and stirred magnetically to obtain a clarified system;

[0046] 3. Add 65 ml of distilled water at 75°C to the above clarification system;

[0047] 4. Stir for 15 minutes;

[0048] 5. Perform 3 cycles of high-pressure homogenization of the above-mentioned colostrum at 800 bar;

[0049] 6. Naturally cool to room temperature to obtain azithromycin lipid nanoparticle dispersion.

[0050] The average particle diameter after preparation is 74.5 nanometers, and the average particle diameter after storage for 0.5 months is 75.2 nanometers

Embodiment 2

[0051] Example 2 Preparation of Azithromycin Nanostructured Lipid Carrier

[0052] Composition formula:

[0053]

[0054] Preparation:

[0055] 1. Weigh 16.8 grams of polyoxyl stearate S-40, 7.2 grams of poloxamer F-68, 2 grams of glyceryl monostearate, and 2 grams of glyceryl triacetate, and put them into the sample tube;

[0056] 2. Heating in a water bath at 70°C to make it completely melted and then adding 0.4 g of azithromycin to obtain a clarified system;

[0057]3. Add 62 ml of distilled water at 60°C to the above clarification system;

[0058] 4. Stir for 10 minutes;

[0059] 5. Carry out 4 cycles of high-pressure homogenization of the above-mentioned colostrum at 700 bar.

[0060] 6. Cool naturally to room temperature to obtain the azithromycin lipid nanoparticle dispersion.

Embodiment 3

[0061] Example 3 Preparation of Azithromycin Nanostructured Lipid Carrier

[0062] Composition formula:

[0063]

[0064]

[0065] Preparation:

[0066] 1. Weigh 12.6 grams of polyoxyl stearate S-40, 5.4 grams of poloxamer F-68, 1.5 grams of glyceryl monostearate, and 1.5 grams of castor oil, and put them into the sample tube;

[0067] 2. Heating in a water bath at 70°C to make it completely melted and then adding 0.3 g of azithromycin to obtain a clarified system;

[0068] 3. Add 79 ml of distilled water at 60°C to the above clarification system;

[0069] 4. Stir for 10 minutes;

[0070] 5. Carry out 4 cycles of high-pressure homogenization of the above-mentioned colostrum at 600 bar.

[0071] 6. Cool naturally to room temperature to obtain the azithromycin lipid nanoparticle dispersion.

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Abstract

The invention discloses an azithromycin nanostructured lipid carrier and a preparation method thereof. The components of the carrier are as follows according to mass percentage: 0.1-1 percent of azithromycin, 20-40 percent of emulsifier, 3-8 percent of lipid materials and the balance of water. The composition has good stability and higher bioavailability, simple and controllable preparation method, and good repeatability, and can be applied to the preparation of azithromycin antibacterials of eye dose.

Description

technical field [0001] The invention belongs to the technical field of carrier systems in cosmetics and food preparation technologies, and relates to a nanoscale carrier and a preparation method thereof, in particular to a nanostructured lipid carrier composition containing an active ingredient of azithromycin and a preparation method thereof. Background technique [0002] Azithromycin (Azithromycin) is a macrolide antibiotic that can inhibit a variety of Gram-negative cocci, mycoplasma, chlamydia, etc., and has a high concentration in tissues and cells, and can effectively kill intracellular pathogens. It has a good curative effect on skin and soft tissue infections. However, systemic administration can stimulate the gastrointestinal tract, and due to the blood-aqueous humor barrier, the concentration of the drug absorbed into the eye tissue is low, so it is necessary to study its ocular drug delivery system. [0003] At present, there are many methods of eye administratio...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K31/7052A61K47/34A61K47/44A61K47/14A61P31/04A61P31/00A61P27/02
Inventor 夏强吴家莹
Owner 苏州纳康生物科技有限公司