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Polyenic taxusol nano lipid carrier and preparation method thereof

A nano-lipid carrier and docetaxel technology, which is applied in the directions of liposome delivery, pharmaceutical formulations, and inactive medical preparations, can solve problems such as limiting drug-carrying capacity, improve injection safety, and avoid phagocytosis. , the effect of prolonging the cycle time

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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  • Polyenic taxusol nano lipid carrier and preparation method thereof
  • Polyenic taxusol nano lipid carrier and preparation method thereof
  • Polyenic taxusol nano lipid carrier and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Take 600 mg of docetaxel, 10.0 g of glyceryl monostearate, 8.0 g of MCT, and 2.0 g of Tween80, add an appropriate amount of absolute ethanol to dissolve, and rotate the organic solvent under reduced pressure to dry the organic solvent, and heat and dissolve at 70°C to form the oil phase. Poloxamer 188 4.0g, dissolved in 100ml 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 processed by a high-pressure homogenization method at 70°C, and the docetaxel nanolipid carrier was sealed and stored at 4°C. After diluting with physiological saline, measure the flat diameter particle size with COULTER LS230 particle size analyzer, see figure 1 .

[0041] Average particle size=126nm, SD=17nm, encapsulation rate=90.3wt%.

Embodiment 2

[0043] Take 60 mg of docetaxel, 1.0 g of glyceryl monostearate, 0.8 g of MCT, and 0.4 g of phospholipid to dissolve in an appropriate amount of chloroform, rotate and evaporate the organic solvent, and heat and dissolve at 70° C. as the oil phase. Poloxamer 188 0.3g is dissolved in 10ml water for injection and heated to 70°C as the water phase. The water phase was dropped into the oil phase under stirring at 70°C, the obtained colostrum was sonicated with a 500W probe at 70°C for 2 minutes, and the docetaxel nanolipid carrier was sealed and stored at 4°C. After diluting with physiological saline, measure the flat diameter particle size with COULTER LS230 particle size analyzer, see figure 2 .

[0044] Average particle size=129nm, SD=18nm, encapsulation rate=87.5wt%.

Embodiment 3

[0046] Take 500 mg of docetaxel, 8.0 g of glyceryl behenate, 5.0 g of soybean oil, and 1.5 g of Tween80, add an appropriate amount of chloroform to dissolve, dry the organic solvent under reduced pressure, and heat and dissolve at 80° C. as an oil phase. Dissolve 5.0 g of PEG 400 and 2.0 g of Poloxamer 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 80°C, and the obtained colostrum was homogenized under high pressure at 70°C, and the docetaxel nanolipid carrier was sealed and stored at 4°C. The dialysis method was used to determine the drug release rate: 1000ml of phosphate buffered saline (PBS) containing 1% Tween and pH 7.4 was used as the release medium, the stirring speed was 100 revolutions per minute, and the temperature was 37±0.5°C. After sampling, inject 20μl for HPLC determination to calculate the cumulative release percentage, see image 3 .

[0047] Average particle size=133nm, SD=2...

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Abstract

The invention belongs to the field of a drug preparation, and relates to a docetaxel nanometer lipid carrier and a preparation method. The docetaxel nanometer lipid carrier basically comprises docetaxel, solid state lipid materials, liquid oil, an emulsifier, PEG-modified ester and injection water which are of therapy effective dose. The docetaxel nanometer lipid carrier has stable docetaxel 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 docetaxel nano lipid carrier and a preparation method thereof. More specifically, the present invention relates to a docetaxel nano-lipid carrier which has a stable docetaxel structure, helps avoid the phagocytosis of the reticuloendothelial system in the body, and can be stably stored, and a preparation method thereof. Background technique [0002] Docetaxel is a new generation of taxane anti-tumor drugs developed in recent years. It is a mitotic inhibitor. Docetaxel is a new semi-synthetic anti-tumor drug. It has strong anti-tumor activity against a variety of solid tumors. In vitro experiments It is suggested that docetaxel can inhibit the growth of SPC A1 lung adenocarcinoma cells, and the inhibitory effect increases with the increase of the dose. This effect is related to the drug-induced GZM phase arrest of cells. Studies on Lewis lung cancer in vivo show that docetaxel...

Claims

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Application Information

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