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Amphotericin B cubic liquid crystal gel, cubic liquid crystal nanoparticles and preparation method thereof

A technology of amphotericin and nanoparticles, applied in capsule delivery, liquid delivery, microcapsules, etc., can solve the problems of low oral bioavailability, light and heat sensitivity, etc., and achieve poor physical and chemical stability, strong affinity, The effect of overcoming the dissolution barrier

Inactive Publication Date: 2017-06-13
GUANGZHOU ZHONGDA NANSHA TECH INNOVATION IND PARK +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, amphotericin B is sensitive to light and heat, easy to degrade, and has very low oral bioavailability

Method used

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  • Amphotericin B cubic liquid crystal gel, cubic liquid crystal nanoparticles and preparation method thereof
  • Amphotericin B cubic liquid crystal gel, cubic liquid crystal nanoparticles and preparation method thereof
  • Amphotericin B cubic liquid crystal gel, cubic liquid crystal nanoparticles and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0059] Embodiment 1: the preparation of amphotericin B cubic liquid crystal nanoparticles

[0060] see figure 1 , the preparation method of the amphotericin B cubic liquid crystal nanoparticles of the present embodiment comprises the steps:

[0061] Preparation of amphotericin B sodium deoxycholate micelles: Weigh 0.5g amphotericin B raw material drug and 0.41g sodium deoxycholate (mass ratio 1:0.82), add to 30mL distilled water, then add dropwise 0.1mol ·L -1 Sodium hydroxide solution until the amphotericin B bulk drug is completely dissolved, and then use 0.01mol L of pH 6.2 -1 Phosphate buffer solution was diluted to a total volume of 100 mL. The obtained solution was placed in a freeze dryer to avoid light, and was frozen for 48 hours at a cold trap temperature of -50° C. and a vacuum of 0.1 Mbar to obtain yellow amphotericin B sodium deoxycholate micelle powder. Protect from light, airtight, and store in a refrigerator at 4°C.

[0062] Preparation of amphotericin B c...

Embodiment 2

[0067] Embodiment 2: the preparation of amphotericin B cubic liquid crystal nanoparticles

[0068] The preparation method of the amphotericin B cubic liquid crystal nanoparticles of the present embodiment comprises the following steps:

[0069] Preparation of amphotericin B micelles: According to the composition shown in Table 2, the amphotericin B bulk drug and micellar materials were weighed, and the amphotericin B micelles were prepared according to the method in Example 1.

[0070] Preparation of amphotericin B cubic liquid crystal gel: Weigh each raw material according to recipe 1-9 in Example 1, and prepare according to the method of Example 1.

[0071] Preparation of amphotericin B cubic liquid crystal nanoparticles: same as Example 1

[0072] The preparation raw material of table 2 amphotericin B micelles

[0073]

Embodiment 3

[0083] The particle size and encapsulation efficiency of the amphotericin B cubic liquid crystal nanoparticles prepared in Examples 1-2 and Comparative Examples 1-4 were determined.

[0084] The particle size measurement method is as follows: After the cubic liquid crystal nanoparticles are diluted 100 times with ultrapure water, take 1mL sample and add it to the sample cell, equilibrate at 25°C for 1min, and the dispersion viscosity is 0.8872cPa. Zetasizer Nano ZS90 measures the particle size parameters of the cubic liquid crystal nanoparticles , the particle size analyzer software calculates the particle size and polydispersity index (PDI) of cubic liquid crystal nanoparticles. PDI is an index that reflects the change of the particle size distribution range. The smaller the PDI, the more uniform and concentrated the particle size, and the larger the PDI, the uneven particle size and significant difference.

[0085] Encapsulation efficiency measurement method: take 1mL amphot...

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Abstract

The invention relates to an amphotericin B cubic liquid crystal gel, cubic liquid crystal nanoparticles and a preparation method thereof. The amphotericin B cubic liquid crystal gel is prepared from the following main raw materials in parts by mass: 0.1-1 part of amphotericin B, 0.04-1.7 parts of a micelle material, 16-20 parts of a liquid crystal material, 0.8-3 parts of a stabilizer and 15-25 parts of water, wherein the mass ratio of the amphotericin B to the micelle material is 1 to (0.3-2); the mass ratio of the liquid crystal material to the stabilizer is 9 to (0.4-1.5). The amphotericin B cubic liquid crystal gel is further prepared into amphotericin B cubic liquid crystal nanoparticles; the dissolution barrier and the permeation barrier of the amphotericin B in the oral administration process can be overcome; the stability of the amphotericin B is improved; the oral bioavailability of the amphotericin B can be obviously improved.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to an amphotericin B cubic liquid crystal gel, nanoparticles and a preparation method thereof. Background technique [0002] Amphotericin B (Amphotericin B, AmB) is a polyene broad-spectrum antifungal antibiotic, an isolated product in the culture medium of Streptomyces nodosus, a macrolide derivative of this kind, and its molecular structure contains a nonpolar Heptene and a polar polyol, insoluble in water, ethanol, easily destroyed by light, heat and acid. The antibacterial mechanism of amphotericin B is: selectively combined with ergosterol on the fungal cell membrane, forming membrane pores on the cell membrane, increasing the permeability of the cell membrane, resulting in a variety of intracellular potassium ions, nucleotides, amino acids, etc. Leakage of small molecular substances disrupts normal metabolism and causes cell death. [0003] Clinically, amphotericin...

Claims

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Application Information

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IPC IPC(8): A61K9/06A61K9/50A61K47/34A61K47/10A61K31/7048A61P31/10
CPCA61K9/0002A61K9/0053A61K9/06A61K9/5015A61K9/5031A61K31/7048
Inventor 吴传斌梅丽玲陈锦填黄莹潘昕杨志文陈航平
Owner GUANGZHOU ZHONGDA NANSHA TECH INNOVATION IND PARK
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