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Cucurbitacin solid lipid nanoparticle preparation and preparation method thereof

A technology of solid lipid nanometer and cucurbitacin, which is applied in the field of medicine, can solve the problems of poor stability and poor quality, and achieve the effect of good stability, good quality and simple prescription

Inactive Publication Date: 2009-12-30
ZHENGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] In view of the above situation, in order to overcome the defects of the prior art, the purpose of the present invention is to provide a cucurbitacin solid lipid nanoparticle preparation and a preparation method thereof, which can effectively solve the problems of poor stability and poor quality, and the technical solution is, The preparation consists of cucurbitacin, lipid material and surfactant in weight ratio: 0.001-30: 0.01-99: 0.01-50 (that is: cucurbitacin: lipid material: surfactant=0.001-30: 0.01- 99:0.01-50), the sum of cucurbitacin, lipid material and surfactant is 0.1-40% of the total weight of nanoparticle preparation raw materials; its basic preparation method is to avoid lipid material, surfactant and cucurbitacin Light heating to melt and fully mix, add water phase to disperse to the nanometer level, filter and cool while maintaining the molten state, the basic steps are:

Method used

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  • Cucurbitacin solid lipid nanoparticle preparation and preparation method thereof

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Embodiment 1

[0024] In practice, the present invention is made of: cucurbitacin BE 0.003g, glyceryl palmitate stearate 0.35g, glyceryl monostearate 0.15g, poloxamer 1880.25g, ultrapure water 10ml, wherein, precision Weigh each component, heat and melt glyceryl palmitate stearate, glyceryl monostearate and poloxamer 188 at 90°C, add cucurbitacin BE, stir quickly with a glass rod, and place in the refrigerator Freeze the layer to make it solidify, and then transfer the solidified mixture to an ultrasonic tube with a thermal insulation sleeve. The ultrasonic temperature is 75°C, add 10ml of ultrapure water, and use an ultrasonic cell pulverizer to sonicate 18 times at an ultrasonic power of 400W. Ultrasound for 10 seconds (10 seconds), interval of 10 seconds (that is, stop for 10 seconds between each time, and then proceed to the next ultrasound), then keep warm (75°C) to absorb the dispersion after ultrasound, and pass it through a 0.22 μm microporous membrane while it is hot. The filtrate w...

Embodiment 2

[0026] The present invention can also be prepared by: cucurbitacin B 0.008g, glyceryl stearate 0.5g, glyceryl monostearate 0.2g, poloxamer 4070.3g, lecithin 0.1g, ethanol 2mL, ultrapure water 8ml Among them, each component was accurately weighed, after heating and melting glyceryl palmitate, glyceryl monostearate and poloxamer 407 at a temperature of 90°C, add cucurbitacin B, and stir rapidly with a glass rod Mix well, put it in the freezer layer of the refrigerator to solidify, then transfer the solidified mixture to an ultrasonic tube with an insulating sleeve, the ultrasonic temperature is 70°C, add 2mL ethanol and 8ml ultrapure water, and use an ultrasonic cell pulverizer at ultrasonic power Sonicate 36 times under the condition of 400W, each time for 5S, with an interval of 5S, and then keep warm (70°C) to absorb the dispersion after ultrasonication, pass it through a 0.22μm microporous filter membrane while it is hot, cool the filtrate at room temperature and fill it with...

Embodiment 3

[0028] The present invention can also be made up of: cucurbitacin E 0.05g, glyceryl behenate 0.3g, glyceryl monostearate 0.2g, poloxamer 1880.2g, polyoxyethylene ether (35) castor oil 0.3g, ultrapure water 20ml, among which, accurately weigh each component, heat and melt glyceryl behenate, glyceryl monostearate and poloxamer 188 at 95°C, add cucurbitacin E, and stir quickly with a glass rod Mix well, put it in the freezer layer of the refrigerator to solidify, then transfer the solidified mixture to an ultrasonic tube with an insulating sleeve, the ultrasonic temperature is 80°C, add 20ml of ultrapure water, and use an ultrasonic cell pulverizer under the condition of ultrasonic power 600W Ultrasound 18 times, 10S each time, 10S interval, and then keep warm (80°C) to absorb the dispersion after ultrasound, pass through a 0.22μm microporous filter membrane, cool the filtrate at room temperature and fill it with nitrogen to melt seal, and then get cucurbitacin solid lipid Qualit...

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Abstract

The invention aims at providing a cucurbitacin solid lipid nanoparticle preparation and a preparation method thereof, which can effectively solve the problems of poor stability and low quality in the prior art. The technical scheme provided by the invention is that: in the preparation, the weight ratio of cucurbitacin, lipid material and surface active agent is 0.001-30:0.01-99:0.01-50, and the sum of the cucurbitacin, the lipid material and the surface active agent accounts for 0.1-40% of the total weight of the raw materials of the nanoparticle preparation. The preparation method is as follows: heating and melting the lipid material, the surface active agent and the cucurbitacin in dark place, fully and evenly stirring; adding water for dispersing to nanoscale; filtering and cooling in the melting state. The invention has scientific and simple composition, scientific compatibility, reasonable dosage, convenient use and fine stability. The invention integrates the advantages of high physical stability and low drug leakage of polymer nanoparticles with low toxicity and capability of large-scale production of liposome and emulsion, which is an innovation in cucurbitacin solid lipid nanoparticle preparation and has enormous economical and social benefits.

Description

1. Technical field [0001] The invention relates to medicine, in particular to a cucurbitacin solid lipid nanoparticle preparation and a preparation method thereof. 2. Background technology [0002] Cucurbitacins are a class of tetracyclic triterpenoids extracted from plants. The basic carbon-hydrogen skeleton is 19-carbo-9β-methyl-10α-lanostene-5. So far, more than 40 Among them, cucurbitacin B (Cucurbitacin B) and E are the most widely used, in addition to cucurbitacin A, D, I and so on. These ingredients have various biological activities such as anti-tumor, anti-chemical carcinogenesis, liver protection, and improvement of body immunity. It is also found in large fungi (Yang Kai, Zheng Gang. Research progress on the pharmacological effects of cucurbitacin BE. International Journal of Traditional Chinese Medicine, 2006, 28(1): 27-29). [0003] At present, the cucurbitacin raw material medicine (cucurbitacin BE) extracted from the melon pedicle of the Cucurbitaceae plant ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K9/48A61K9/06A61K9/00A61K9/02A61K9/12A61K9/20A61K31/575A61K47/12A61K47/10A61K47/14A61K47/28A61K47/34A61K47/24A61P35/00A61P1/16A61P37/04
Inventor 王艳芝郑甲信徐炳欣
Owner ZHENGZHOU UNIV
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