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Nanometer solid taxol lipoid particle and its prepn process

A technology of solid lipid nanometer and paclitaxel, which is applied in the directions of liposome delivery, drug combination, pharmaceutical formulation, etc., can solve problems such as poor water solubility, and achieve the effects of preventing hydrolysis and oxidation, increasing compliance, and ensuring stability.

Inactive Publication Date: 2007-03-21
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, paclitaxel substances have poor water solubility. For example, the currently commercially available docetaxel injection (40g L-1) uses Tween-80 (tween-80) as a solvent, and is equipped with a diluent containing 13% (φ) ethanol

Method used

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  • Nanometer solid taxol lipoid particle and its prepn process

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036]Take by weighing 20mg paclitaxel, 100mg stearic acid and 100mg lecithin and dissolve in 20ml of methylene chloride, evaporate to dryness under reduced pressure on a rotary evaporator, form a lipid film, add 30ml of Tween-80 (2.5%), and ultrasonically Disperse to obtain the SLN suspension system, and store it at 2°C for later use. Its average particle diameter is 80nm, accounts for 80%, and all particles are all below 150nm, and particle size distribution is narrow, shows that solid lipid nanoparticle size is comparatively uniform; Stable for 12 months, no precipitation and degradation of paclitaxel substances were observed during storage.

Embodiment 2

[0038] Weigh 15mg of docetaxel, 60mg of stearic acid, and 120mg of soybean lecithin into a 50ml Erlenmeyer flask with a stopper, add 10ml of acetone, and ultrasonically dissolve it fully to form an 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 removed by evaporation under reduced pressure, and the temperature was lowered to room temperature to obtain a solid lipid nanoparticle suspension.

Embodiment 3

[0040] Take 20 mg of paclitaxel, 100 mg of stearic acid, 400 mg of lecithin and 10 ml of methylene chloride, add them into a 25 ml pear-shaped bottle with a stopper, and ultrasonically dissolve to form an organic phase. Another 300 mg of polyoxyethylene fatty acid ester Myrj53 was added into 30 ml of double-distilled water, and ultrasonically dissolved to form a water phase. Slowly inject the organic phase into the water phase at a constant temperature of (75±2)°C stirred at 1000r / min to form a microemulsion, and continue stirring for about 2-3 hours to completely evaporate the organic solvent and concentrate the system to about 5ml. Quickly mix the obtained translucent microemulsion into 10 ml of ice-water phase stirred at 1000 r / min at -0 to 2°C, and continue to stir for 2 hours to obtain solid lipid nanoparticles.

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Abstract

The present invention provides one kind of nanometer solid taxol lipoid particle capable of being used for injection and oral taking and its solid preparation, and features that taxol matter is coated with carrier material and surfactant so as to prepare nanometer solid taxol lipoid particle with small size, high coating rate, high stability, low toxicity and easy surface modification. The nanometer solid taxol lipoid particle has raised targeting effect on cancer cell, enhanced tumor cell killing effect, high curative effect, less toxic side effect, and reduced medicine resistance. The present invention also provides several preparation processes of nanometer solid taxol lipoid particle, and the preparation processes are simple, low in cost and suitable for industrial production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and specifically relates to solid lipid nanoparticles containing paclitaxel substances as antitumor active ingredients and a preparation method thereof. Background technique [0002] Paclitaxel can inhibit the mitosis and proliferation of cancer cells by promoting the assembly of microtubule dimers into microtubules, and stabilizing microtubules by preventing the process of depolymerization, arresting cells in G2 and M phases. It is effective for advanced breast cancer, non-small cell lung cancer, ovarian cancer, prostate cancer, pancreatic cancer, liver cancer, head and neck cancer, gastric cancer, etc. However, paclitaxel substances have poor water solubility. For example, the currently commercially available docetaxel injection (40g L-1) uses Tween-80 (tween-80) as a solvent, and is equipped with a diluent containing 13% (φ) ethanol . Because Tween-80 is hemolytic, it will cause al...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/337A61K9/127A61K9/14A61P35/00
Inventor 李亚平陈伶俐顾王文
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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