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Long circulation liposome prepn of polyene taxol and its prepn process

A technology of long-circulating liposome and docetaxel, which is applied in the field of medicine, can solve the problems of no long circulation, small drug loading of fat emulsion, influence on curative effect, etc., and achieves the advantages of improving circulation time, reducing toxicity and good efficacy. Effect

Inactive Publication Date: 2006-10-18
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

[0016] 10 mg of docetaxel, 150 mg of soybean lecithin, 15 mg of cholesterol, 20 mg of polyethylene glycol-distearoylphosphatidylethanolamine (PEG-DSPE), and 0.68 mg of vitamin E were ultrasonically dissolved in 10 ml of absolute ethanol to obtain solution A.

[0017] A film was formed by rotary evaporation in a water bath at 50°C to obtain film B.

[0018] Mix 5ml of phosphate buffer (pH7.4) with membrane B to hydrate for 30 minutes, oscillate ultrasonically for 5 minutes, pass through a 0.22μm microporous membrane, fill with nitrogen, and potting.

Embodiment 2

[0020] 100mg of docetaxel, 1200mg of soybean lecithin, 300mg of hydrogenated saturated phospholipid, 100mg of cholesterol, 200mg of polyethylene glycol-distearoylphosphatidylethanolamine (PEG-DSPE), and 6.5mg of vitamin E were ultrasonically dissolved in 100ml of absolute ethanol, Solution A is obtained.

[0021] A film was formed by rotary evaporation in a water bath at 50°C to obtain film B.

[0022] 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 Vested.

Embodiment 3

[0024] 100mg of docetaxel, 1000mg of soybean lecithin, 250mg of cholesterol, 100mg of polyethylene glycol-distearoylphosphatidylethanolamine (PEG-DSPE), 6.2mg of vitamin E, and 100mg of oleic acid were ultrasonically dissolved in 100ml of absolute ethanol to obtain Solution A.

[0025] A film was formed by rotary evaporation in a water bath at 50°C to obtain film B.

[0026] Fully mix 50ml of water for injection with membrane B and hydrate for 30 minutes, circulate and homogenize with a high-pressure homogenizer for 5 to 6 times, then pass through a 0.22μm microporous membrane, subpackage, fill with nitrogen, and potting.

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Abstract

The long circulation liposome of polyene taxol is prepared with phosphatide, cholestol and other supplementary material as membrane material, and through surface modification with long circulation supplementary material. During the preparation, charge regulator or surface regulator may be also added. The preparation has average grain size smaller than 600 nm, liposome / medicine molar ratio of 1-20, molar ratio between the long circulation supplementary material and the common phosphatide of 1 / 50-1 / 5 and ultimate polyene taxol concentration of 1-10 mg / ml. The present invention adopts thin dispersing process or organic solvent injecting process to prepare liposome, and high pressure homogenizing process or extruding process to reduce grain size of the prepared liposome and homogenize liposome. The present invention has prolonged intracorporeal circulation period of liposome, effective targeting of medicine to the tumor, high medicine effect and lower toxicity.

Description

Technical field: [0001] The present invention relates to the field of medical technology, relates to targeted drug delivery preparations in the drug delivery field, and more specifically refers to a long-circulation liposome made from a semi-synthetic taxane anticancer drug-docetaxel and appropriate auxiliary materials. Docetaxel achieves tumor targeting through the preparation of growing circulating liposomes. The invention also relates to a preparation method of the long-circulation liposome. 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, liposomes have always been a hot spot in pharmaceutical research. It can selectively deliver drugs to tumor sites and play a therapeutic role without affecting the functions of normal cells, tissues or organs, thereby improving the efficacy , The purpose of reducing toxic and side effects. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/337A61P35/00
Inventor 王东凯张翠霞张文涛
Owner SHENYANG PHARMA UNIVERSITY
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