Fotemustine solid lipid nanoparticle and preparation method thereof

A technology of solid lipid nanometer and fomaustine, which is applied in the field of pharmacy, can solve the problems of difficulty in industrialized production of instruments and equipment, limited continuous application, poor product stability, etc., so as to improve the chemical stability and curative effect of medicines, and improve the bioavailability. high efficiency and low cost

Inactive Publication Date: 2009-12-23
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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AI Technical Summary

Benefits of technology

This patented technology involves making small particles called formsidone (also known as 2-chloro-4-((2'-trifluoromethyl)-5'H)-phenoxazin-6)) that contain medicine inside them. These tiny crystals help keep things stable during their journey from place to destination within our body. They then release these medicines at specific locations throughout your body where they work better treatments like chemotherapy.

Problems solved by technology

This patented technical problem addressed in this patents relates to improves the quality control and safety of formulating stable and safe medicines like formutonium oxynaphthylnitrogen acid esters called stannanes, including butterurtzimod hydrochlorothiaquartron compounds known as metastatic cancer treatments. However these substances often cause severe damage to cells due to their ability to cross cell membranes and enter lymphocytes. So finding ways to prevent them from entering the bloodstream could help extend the use of these agents beyond just pallixiding symptoms.

Method used

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  • Fotemustine solid lipid nanoparticle and preparation method thereof
  • Fotemustine solid lipid nanoparticle and preparation method thereof
  • Fotemustine solid lipid nanoparticle and preparation method thereof

Examples

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Embodiment 1

[0033] Take by weighing 208mg formustine, 1200mg stearic acid and 1000mg lecithin and dissolve in 20ml of methylene chloride, evaporate to dryness under reduced pressure at 40°C to form a lipid film, add 4ml of Tween-80 (2.5%) , ultrasonically dispersed for 30 minutes (ultrasonic power 600w), and the solid lipid nanoparticle suspension was obtained, which was stored at 2°C for later use. Its average particle size is 210nm, all particles are below 500nm, and the particle size distribution is narrow, showing that the size of solid lipid nanoparticles is relatively uniform; the solid lipid nanoparticle suspension can be stable for several days at room temperature and can Stable for 12 months, no precipitation was observed during storage.

Embodiment 2

[0035] Weigh 624mg of formustine, 6240mg of glyceryl monostearate and 3000mg of soybean lecithin into a 50ml conical flask with a stopper, add 10ml of ethanol: acetone (1:1) mixed solvent, ultrasonically dissolve it fully and heat to 60 °C, forming the organic phase. Another 500mg of Poloxamer-188 was dissolved in 30ml of double distilled water to form the water phase. Use a syringe to slowly inject the organic phase into the 60°C aqueous phase stirred at 1000r / min, and continue stirring until a translucent system is formed. The organic solvent was evaporated under reduced pressure at 40° C., the system was concentrated to 12 ml, and cooled to room temperature to obtain a solid lipid nanoparticle suspension.

Embodiment 3

[0037] Dissolve 0.624g of formustine, 12.48g of tripalmitin, 1.2g of stearyl alcohol, and 6.24g of dipalmitoylphosphatidylcholine in 20ml of ethanol, ultrasonically dissolve and heat to (50±2)°C to form an organic phase . Another 1g of myrj 53 was added into 40ml of double-distilled water, and ultrasonically dissolved to form an aqueous phase. Slowly inject the organic phase into the constant temperature water phase of (50±2)°C stirred at 1000r / min to form colostrum, and continue to stir for about 2-3 hours to completely evaporate the organic solvent and concentrate the system to about 2ml. Quickly mix the obtained translucent emulsion into another 10ml ice-water phase stirred at 1000r / min at 0-2°C, continue to stir for 2 hours, and then homogenize 5 times in a high-pressure homogenizer (homogeneous pressure is 15000psi) , to obtain solid lipid nanoparticle suspension.

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Abstract

The invention provides a fotemustine solid lipid nanoparticle for injection and oral administration. The nanoparticle is characterized in that a lipid material and an emulsifier are used to encapsulate the fotemustine to prepare the fotemustine solid lipid nanoparticle with small particle diameter, high encapsulation rate, good stability and low toxicity. The prepared fotemustine solid lipid nanoparticle improves the solubility and the stability of the fotemustine, reduces vascular stimulation of the fotemustine, and prolongs the circulating time of the medicament in blood, thereby improving the curative effect of medicaments, and ensuring that preparations made of the solid lipid nanoparticle have the characteristics of low toxicity, low fotemustine solid lipid nanoparticle with low stimulation and high efficiency. The invention also relates to a method for preparing the fotemustine solid lipid nanoparticle, which has simple preparation process and low cost, and is applicable to industrial production.

Description

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Claims

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Application Information

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Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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