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Teniposide solid lipid nanoparticle and preparation method thereof

A technology of solid lipid nanometer and teniposide, which is applied in the field of pharmacy, can solve the problems that do not meet the requirements of drug safety and industrial production, and achieve the effects of improving bioavailability, ensuring stability and increasing stability

Inactive Publication Date: 2009-12-09
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, most of these new dosage forms are currently in the research stage of the laboratory, and most of them do not meet the requirements of drug safety and industrial production. So far, there have been no clinical or market reports

Method used

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Take by weighing 100mg teniposide, 800mg lecithin and be dissolved in the dichloromethane of 20ml, evaporate to dryness under reduced pressure at 50 ℃, form lipid film, add the Tween-80 (2.5%) of 10ml, ultrasonic dispersion 30min ( Ultrasonic power 600W), the solid lipid nanoparticle suspension was obtained, and stored at 2°C for later use. Its average particle size is 245nm, 90% of the particles are all below 500nm, and the particle size distribution is narrow, indicating that the size of solid lipid nanoparticles is relatively uniform; Stable for 12 months, no precipitation was observed during storage.

Embodiment 2

[0040] Weigh 100mg of teniposide, 500mg of glyceryl monostearate and 600mg of soybean lecithin into a 50ml conical flask with stopper, add 10ml of ethanol: acetone (1:1) mixed solvent, ultrasonically dissolve it fully and heat to 75 °C, forming the organic phase. Another 200mg 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 75°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., and cooled to room temperature to obtain a solid lipid nanoparticle suspension.

Embodiment 3

[0042] Dissolve 200mg of teniposide, 2400mg of tripalmitin, 600mg of stearyl alcohol, and 800mg of dipalmitoylphosphatidylcholine in 10ml of ethanol, ultrasonically dissolve and heat to (80±2)°C to form an organic phase. Another 1200mg of myrj 53 was added into 30ml of double-distilled water, and ultrasonically dissolved to form an aqueous phase. Slowly inject the organic phase into the constant temperature water phase of (80±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 5ml. Quickly mix the obtained translucent emulsion into another 20ml 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 discloses a teniposide solid lipid nanoparticle and a preparation method thereof in industrial application. The teniposide solid lipid nanoparticle comprises an effective treatment dose of teniposide, a lipid material and an emulsifier, has smaller grain diameter, high entrapment rate and good stability, improves the solubility and the stability of the teniposide, reduces the toxicity of the teniposide, prolongs the cycle time of medicaments in blood and improves the therapeutic index of the medicaments, thereby having the characteristics of low toxicity and irritability and high efficiency in clinical application.

Description

technical field [0001] The invention belongs to the field of pharmacy, and in particular relates to solid lipid nanoparticles containing teniposide, an antitumor active ingredient, and a preparation method thereof. Background technique [0002] Teniposide (VM-26) is a semi-synthetic derivative of podophyllotoxin, which belongs to plant-derived antineoplastic drugs. It is a cycle-specific cytotoxic drug that inhibits DNA topoisomerase II, resulting in double-strand or single-strand damage, causing cell mitosis to stop in late S or early G2, thereby hindering tumor cell division and inhibiting tumor growth. Teniposide has a remarkable curative effect, and its biological activity is 5-10 times that of the same type of drug etoposide, and clinical data show that teniposide has few side effects, less toxicity, and has no effect on liver and kidney functions. Due to its extensive clinical antitumor activity, teniposide is now widely used in nervous system tumors, malignant lympho...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K9/127A61K31/7048A61P35/00
Inventor 李亚平陈伶俐顾王文
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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