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Docetaxel liposome formulation and preparation method thereof

A docetaxel and liposome technology, applied in the field of medicine, can solve the problems of not having long circulation, affecting the curative effect, small drug loading of a fat emulsion, etc., and achieving the effects of improving circulation time, good drug efficacy and reducing toxicity

Inactive Publication Date: 2007-08-15
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The fat emulsion prepared by this method has a small drug loading, the maximum is 1.0mg / ml, and it does not have the characteristics of long circulation in the body, which affects the efficacy of the drug.
[0009] The above two patents still have certain deficiencies in fully exerting the drug effect of docetaxel and reducing toxicity

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] 100mg of docetaxel, 1500mg of soybean lecithin, 150mg of cholesterol, 100mg of polyethylene glycol-distearoylphosphatidylethanolamine (PEG-DSPE), and 6.8mg of vitamin E were ultrasonically dissolved in 10ml of absolute ethanol to obtain solution A.

[0019] A film was formed by rotary evaporation in a water bath at 50°C to obtain film B.

[0020] Fully mix 5ml of phosphate buffer (pH7.4) with membrane B to hydrate for 30 minutes, ultrasonically oscillate for 5 minutes, pass through a 0.22μm microporous membrane, fill with nitrogen, and seal.

Embodiment 2

[0022] 100mg of docetaxel, 1200mg of soybean lecithin, 300mg of hydrogenated saturated phospholipid, 100mg of cholesterol, 50mg of ganglioside (GM), and 6.5mg of vitamin E were ultrasonically dissolved in 50ml of absolute ethanol to obtain solution A.

[0023] A film was formed by rotary evaporation in a water bath at 50°C to obtain film B.

[0024] Fully mix 50ml of phosphate buffer (pH7.4) with membrane B and hydrate for 30 minutes, circulate and homogenize for 5 to 6 times with a high-pressure homogenizer, then pass through a 0.22μm microporous membrane, subpackage, fill with nitrogen, and potting Instantly.

Embodiment 3

[0026] 100mg of docetaxel, 1000mg of soybean lecithin, 250mg of cholesterol, 100mg of polyethylene glycol-distearoylphosphatidylethanolamine (PEG-DSPE), 6.5mg of vitamin E, and 100mg of oleic acid were ultrasonically dissolved in 50ml of absolute ethanol to obtain Solution A.

[0027] A film was formed by rotary evaporation in a 60°C water bath to obtain film B.

[0028] Fully mix 50ml of water for injection with membrane B and hydrate for 30 minutes, circulate and homogenize for 5 to 6 times with a high-pressure homogenizer, then pass through a 0.22μm microporous membrane, sub-package, fill with nitrogen, and pot.

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Abstract

The invention belongs to the field of medical technology, and discloses new medicament form of polyene paclitaxel liposome and its preparation method. The invention adopts film dispersion method and organic solvent injection method for preparing common polyene paclitaxel liposome, or modifying liposome with phospholipid modified by PEG or other lipid material for preparing long-cycling liposome, performing ultrasound, extrusion, or homogenization under high pressure, and making into Chinese medicinal injection and freeze drying preparation. Compared with common injection, the common polyene paclitaxel liposome of the invention can reduce adverse side effect, long-cycling liposome improves cycle time of liposome in vivo to make the medicine target at tumour effectively for a long time, exerts drug effect and reduces toxicity.

Description

Technical field: [0001] The invention belongs to the technical field of medicine, and relates to a new dosage form of targeted drug delivery preparation docetaxel liposome and a preparation method thereof, more specifically refers to a semi-synthetic taxane anticancer drug-docetaxel prepared with appropriate auxiliary materials Docetaxel achieves tumor-targeting effect by preparing ordinary and long-circulating liposomes. Background technique: [0002] Liposome is a new dosage form of targeted drug delivery system, which is the latest and most promising drug delivery system in pharmacy. As a member of this system, liposome has always been a hot spot in pharmaceutical research. It can selectively deliver drugs to the target site and play a therapeutic role without affecting the function of normal cells, tissues or organs, thereby improving the quality of life. Curative effect, reduce the purpose of side effects. [0003] Ordinary liposomes are quickly swallowed by the retic...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/337A61K9/127A61K9/19A61K47/24A61K47/26A61K47/34A61P35/00A61K47/10
Inventor 王东凯李为理张翠霞张文涛林立峰周雪梅
Owner SHENYANG PHARMA UNIVERSITY
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