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Paclitaxel nano lipid carrier and preparation method thereof

A nano-lipid carrier, paclitaxel technology, applied in the directions of liposome delivery, pharmaceutical formulations, medical preparations of inactive ingredients, etc. Narrow distribution of effects

Inactive Publication Date: 2009-05-27
SHENYANG WOSEN PHARMA INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The problem with solid lipid nanoparticles (SLN) is that the SLN is made of a single lipid material, and after high-pressure homogeneous cooling during the preparation process, the lipid tends to form more regular crystals, which causes the outer surface of the encapsulated drug. Row or crystallize out in the SLN dispersed aqueous phase
In addition, highly ordered lipid crystals limit their drug-loading capacity

Method used

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  • Paclitaxel nano lipid carrier and preparation method thereof
  • Paclitaxel nano lipid carrier and preparation method thereof
  • Paclitaxel nano lipid carrier and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Take 800mg of paclitaxel, 12.0g of glyceryl monostearate, 10.0g of MCT, 803.0g of Tween, add appropriate amount of ethanol to dissolve, evaporate the organic solvent under reduced pressure, and heat to dissolve at 70°C as the oil phase. Poloxamer 188 3.0g, dissolved in 100ml of water for injection, heated to 70°C as the water phase. The water phase was dropped into the oil phase under stirring at 70°C, and the obtained colostrum was homogenized under high pressure at 70°C to obtain paclitaxel nano-lipid carrier, which was sealed and stored at 4°C. After diluting with normal saline, measure the average diameter particle size with a COULTER LS230 particle size analyzer, see figure 1 .

[0038] Average particle diameter = 124nm, SD = 16nm, encapsulation efficiency = 87.9wt%.

Embodiment 2

[0040] Take 80 mg of paclitaxel, 1.2 g of glyceryl monostearate, 1.1 g of MCT, and 1.2 g of phospholipids, add an appropriate amount of chloroform to dissolve, spin evaporate the organic solvent to dryness, heat and dissolve at 70°C as the oil phase. Poloxamer 1880.6g was dissolved in 10ml water for injection and heated to 70°C as the aqueous phase. The water phase was dropped into the oil phase under stirring at 70°C, and the obtained colostrum was sonicated with a 400W probe at 70°C for 3 minutes to obtain paclitaxel nano-lipid carrier, which was sealed and stored at 4°C. After diluting with normal saline, measure the average diameter particle size with a COULTER LS230 particle size analyzer, see figure 2 .

[0041] Average particle diameter = 126nm, SD = 17nm, encapsulation efficiency = 88.4wt%.

Embodiment 3

[0043] Take 800 mg of paclitaxel, 12.0 g of glyceryl behenate, 7.0 g of soybean oil, and 803.5 g of Tween, add appropriate amount of tetrahydrofuran to dissolve, rotary evaporate the organic solvent to dryness, heat and dissolve at 80°C as the oil phase. Dissolve 3.0 g of Poloxamer 1888 in 100 ml of water for injection, and heat to 80° C. as the water phase. The water phase was dropped into the oil phase under stirring at 70°C, and the obtained colostrum was homogenized under high pressure at 70°C to obtain paclitaxel nano-lipid carrier, which was sealed and stored at 4°C. Adopt dialysis to measure the release degree of medicine: take the phosphate buffer saline (PBS) 1000ml that contains 1% Tween as pH value 7.4 as release medium, stirring speed is 100 revolutions per minute, and temperature is 37 ± 0.5 ℃. After sampling, inject 20 μl of sample for HPLC determination, and calculate the cumulative drug release percentage, see image 3 .

[0044] Average particle diameter = 13...

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Abstract

The invention belongs to the field of a drug preparation, and relates to a paclitaxel nanometer lipid carrier and a preparation method. The paclitaxel nanometer lipid carrier basically comprises paclitaxel, solid state lipid materials, liquid oil, emulsifier, PEG-modified ester and injection water which are of therapy effective dose. The paclitaxel nanometer lipid carrier has stable paclitaxel structure, is beneficial to avoiding phagocytosis of reticuloendothelial system in a body, and can be stably stored.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a paclitaxel nano lipid carrier and a preparation method thereof. More specifically, the present invention relates to a paclitaxel nano-lipid carrier which has a stable paclitaxel structure, helps to avoid the phagocytosis of the reticuloendothelial system in vivo, and can be stored stably and its preparation method. Background technique [0002] Paclitaxel is a diterpene component extracted from Taxus brevifolia or Taxus brevifolia. Paclitaxel is a new type of anti-microtubule drug approved by the US FDA in July 1994, and it is a broad-spectrum anti-cancer drug. It is now used as a first-line drug for ovarian cancer and breast cancer, and it is also effective for refractory ovarian cancers such as platinum-based drugs. Paclitaxel is a new generation of tumor chemotherapy drugs with major breakthroughs. But paclitaxel also has significant toxic and side effects, mainly ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K47/14A61K47/10A61K47/24A61K47/32A61K47/34A61K47/44A61K31/337A61P35/00A61K47/22A61K47/26
Inventor 德瑞克·王李翔徐飒
Owner SHENYANG WOSEN PHARMA INST
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