Amphotericin B nano composite, and preparation method thereof

A nanocomposite and amphotericin technology, applied in the fields of pharmaceutical formulation, drug delivery, organic active ingredients, etc.

Active Publication Date: 2015-08-26
CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] Nanoparticles are easily recognized and phagocytized by the immune recognition system in the body. To solve this problem, methoxypolyethylene glycol 2000-distearate phosphatidylethanolamine (mPEG2000-DSPE) is usually added to make long-circulation nano-formulations

Method used

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  • Amphotericin B nano composite, and preparation method thereof
  • Amphotericin B nano composite, and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Preparation of amphotericin B nanocomplexes (organic solvent injection method).

[0024] Accurately weigh amphotericin B, sodium cholesteryl sulfate and cholesterol-PEG with a molar ratio of 10:10:0 or 10:9:1 and dissolve them in an appropriate amount of dimethyl sulfoxide as the oil phase. Prepare 95 g / L lactose, 0.564 g / L tromethamine, and 37.2 mg / L edetate disodium aqueous solution as the water phase. Put the water phase (25°C) in a suitable container, stir it with a mixing emulsifier (1200rpm / min), slowly inject the oil phase into the water phase, control the oil-water ratio to 1:17.5, and continue stirring for 2-3 minutes; The obtained colostrum is ultra-filtered to remove dimethyl sulfoxide; micro-jet is used to sizing to obtain nanocomposites with uniform particle size; and then it is divided into vials and freeze-dried.

Embodiment 2

[0026] Cholesterol-PEG addition range screening.

[0027] Adopt the method for Example 1 to prepare amphotericin B, sodium cholesteryl sulfate and cholesterol-PEG molar ratio is 10:10:0, 10:9:1, 10:8:2, 10:7:3, 10:6: 4 amphotericin B nanocomposites, under the same granulation conditions, the particle size was measured after microfluidic sizing, and the results showed that 10:7:3 and 10:6:4 amphotericin B nanocomposites had larger PDI , indicating that the particle size is not uniform, and the particle size of the nano-preparation will affect its safety and effectiveness, so the amount of cholesterol-PEG added in the prescription is limited to less than or equal to 20% (that is, the total molar amount of cholesterol-PEG in cholesterol-PEG and cholesterol sodium sulfate accounted for less than or equal to 20%).

[0028]

[0029]

[0030] Note: PDI is polydispersity index, which reflects the uniformity of particle size.

Embodiment 3

[0032]Accurately weigh amphotericin B, sodium cholesteryl sulfate and mPEG2000-DSPE with a molar ratio of 10:9:1 and dissolve them in an appropriate amount of dimethyl sulfoxide as the oil phase. Prepare 95 g / L lactose, 0.564 g / L tromethamine, and 37.2 mg / L edetate disodium aqueous solution as the water phase. Put the water phase (25°C) in a suitable container, stir it with a mixing emulsifier (1200rpm / min), slowly inject the oil phase into the water phase, control the oil-water ratio to 1:17.5, and continue stirring for 2-3 minutes; The obtained colostrum is ultra-filtered to remove dimethyl sulfoxide; micro-jet is used to sizing to obtain nanocomposites with uniform particle size; and then it is divided into vials and freeze-dried.

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Abstract

The invention relates to an amphotericin B nano composite containing amphotericin B, cholesteryl sodium sulfate, and cholesterol-PEG. According to the amphotericin B nano composite, cholesterol-PEG is used for modifying a nano composite containing amphotericin B and cholesteryl sodium sulfate, so that particle size and encapsulation efficiency are desirable, and excellent long circulation properties are achieved.

Description

technical field [0001] The invention relates to an amphotericin B nanocomposite and a preparation method thereof, belonging to the technical field of pharmaceutical preparations. Background technique [0002] Amphotericin B (AMB) is a polyene antifungal drug isolated from the culture fluid of Streptomyces. Its antifungal mechanism is to combine with sterols (mainly ergosterol) on the fungal cell membrane, change the membrane permeability, and the cell contents flow out, thereby causing fungal cell death. It is clinically used to treat serious visceral or systemic infections caused by deep fungi. [0003] Amphotericin B is insoluble in water. In order to improve its solubility, sodium deoxycholate was first used to solubilize it. The trade name of the marketed product is Fungizone®. However, Fungizone® has strong nephrotoxicity, and almost all patients may experience varying degrees of renal dysfunction, proteinuria, casturia, elevated blood urea nitrogen and creatinine, de...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K9/19A61K31/7048A61K47/34A61K47/28A61P31/10
Inventor 李春雷修宪李永丰王红叶陈东健赵曦王彩霞杜艳玲梁敏
Owner CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD
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