Pirarubicin or pirarubicin hydrochloride lipid nano granule and preparation method thereof

A technology of pirarubicin hydrochloride and lipid nanoparticles, which is applied in liposome delivery, pharmaceutical formulations, medical preparations containing active ingredients, etc., can solve the problems of large toxic side effects and poor stability, and achieve reduced toxicity, Effect of reducing toxicity and increasing concentration

Inactive Publication Date: 2009-01-28
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The object of the present invention is to provide a kind of pirarubicin lipid nanoparticle that is stable in nature and can be industrially produced by the prior art, so as to overcome the above-mentioned problems of large toxic and side effects and poor stability

Method used

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  • Pirarubicin or pirarubicin hydrochloride lipid nano granule and preparation method thereof

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Experimental program
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Effect test

Embodiment 1

[0033] Get the pirarubicin of 20mg, 100mg stearic acid and dissolve in 20ml dichloromethane, as organic phase, 100mg poloxamer 108 is added in 50ml water as water phase, organic phase is added in the water phase and carries out high-speed shearing ( 6000rpm, 100s) emulsification, and then use a rotary evaporator to remove the organic solvent in a water bath at 60°C, and emulsify 5 times under high pressure at 300 atmospheres to obtain a lipid nanoparticle dispersion system. Its average particle size is 120nm, accounting for 80%, all particles are below 250nm, and the particle size distribution is narrow, indicating that the size of lipid nanoparticles is relatively uniform. The nanoparticle suspension can be stable for several days at room temperature and stable at 4°C At 12 months, no precipitation or degradation of pirarubicin was observed during storage.

Embodiment 2

[0035] Dissolve 10mg of pirarubicin and 800mg of lecithin in 60ml of chloroform as the organic phase, add 250mg of Benze 78 into 80ml of water as the water phase, add the organic phase to the water phase for high-speed shear (10000rpm, 160s) emulsification , and then use a rotary evaporator to remove the organic solvent in a water bath at 65° C., and perform high-pressure emulsification at 500 atmospheres for 10 times to obtain a lipid nanoparticle dispersion system. Its average particle size is 80nm, accounting for 80%, all particles are below 140nm, and the particle size distribution is narrow, indicating that the size of lipid nanoparticles is relatively uniform. The nanoparticle suspension can be stable for several days at room temperature and stable at 4°C 12 months.

Embodiment 3

[0037]Take 15 mg of pirarubicin and 600 mg of glyceryl monostearate dissolved in 50 ml of cyclohexane as the organic phase, add 200 mg of sodium cholate into 100 ml of water as the water phase, add the organic phase to the water phase for high-speed shearing (6000rpm, 50s) emulsification, and then remove the organic solvent with a rotary evaporator in a water bath at 45°C, and emulsify 4 times at 200 atmospheres of pressure to obtain a lipid nanoparticle dispersion system. Its average particle size is 300nm, accounting for 70%, and all particles are below 500nm. The nanoparticle suspension is stable for several days at room temperature and 12 months at 4°C.

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Abstract

The invention provides a pirarubicin hydrochloride or pirarubicin lipid nanoparticle which can be used for injection and oral administration and a preparation method thereof; the invention is characterized that in the existence of a surface active agent, a carrier material packs the pirarubicin hydrochloride or pirarubicin and the prepared lipid nanoparticle has small particle size, high entrapment rate, good stability and low toxicity. The prepared lipid nanoparticle of the invention can enhance the targeting function to cancer cells, improve the inhibiting and killing function of the pirarubicin to tumor cells and improve the curative effect; the various preparation method of the pirarubicin or the pirarubicin hydrochloride lipid nanoparticle related by the invention has simple preparation technique and low cost and is applicable to industrial production on a large scale.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to lipid nanoparticles containing antitumor active ingredient pirarubicin hydrochloride or pirarubicin and a preparation method thereof. Background technique [0002] Pirarubicin or its hydrochloride (also known as: pirarubicin; English abbreviation: THP) is a new generation of anthracycline antibiotics successfully developed in 1979 by Professor Umezawa Binfu of the Institute of Microbial Chemistry in Japan and others. Tumor antibiotics, patented by Japanese compounds. [0003] Pirarubicin has a broader spectrum and stronger anti-tumor effect than doxorubicin, and its main mechanism is to quickly enter cells, embed in the double helix strand of DNA, inhibit DNA polymerase α and β, prevent nucleic acid synthesis, and make tumors Cell stops at G 2 In this stage, cells cannot divide, leading to tumor cell death. Experimental studies have shown that pirarubicin has a signi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/704A61P35/00
Inventor 李亚平顾王文陈伶俐
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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