Docetaxel long-circulation formulation

A docetaxel and long-circulation technology, applied in the field of long-circulation preparations, can solve the problems of inconvenient clinical medication, high viscosity of Tween-80, etc., achieve strong inhibitory effect, strong hydrophilicity, and avoid phagocytosis

Inactive Publication Date: 2008-12-10
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

In order to remind doctors and patients to realize the seriousness of the side effects of the drug, a serious warning term has been added to the drug product instructions in the United States for the side effects of anaphylaxis and shock of the product; Inconvenience

Method used

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  • Docetaxel long-circulation formulation
  • Docetaxel long-circulation formulation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035]Accurately weigh 15.8mg of lecithin, 7.8mg of cholesterol, 0.6mg of PEG2000-DSPE, 0.1mg of vitamin E, and 2mg of docetaxel and dissolve them in 5ml of chloroform. After removing the chloroform and forming a uniform transparent film on the wall of the eggplant-shaped flask, add 6ml of 0.02mol / L pH6.8 phosphate buffer solution, and continue to rotate in a water bath at 37°C for 30min under normal pressure to make the film swell and hydrate. The suspension was vortexed for 10 min. After ultrasonic dispersion at room temperature for 1 min, the docetaxel stealth liposome solution was obtained, and the salt was removed by dialysis. Add 20ml of water for dilution, add 1.0g of mannitol as a proppant and freeze-dry to make freeze-dried powder injection. The average particle diameter of the sample was measured using deionized water as the dispersion medium, and the measured particle diameter was 20-500 nm, with an average particle diameter of 120 nm. see results figure 1 .

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Embodiment 2

[0039] Accurately weigh 20 mg of lecithin, 5.6 mg of cholesterol, 1.0 mg of PEG4000-DSPE, and 5 mg of docetaxel and dissolve them in 10 ml of dichloromethane. The resulting solution is placed in a 50 ml eggplant-shaped flask, and the dichloromethane is removed under reduced pressure in a water bath at 37°C. After forming a uniform transparent film on the wall of the eggplant-shaped flask, add 10ml of 0.01mol / L pH6.8 phosphate buffer solution, and continue to rotate in a water bath at 37°C under normal pressure for 30min to make the film swell and hydrate, and the resulting suspension Vortex for 10 min. After ultrasonic dispersion at room temperature for 1 min, the docetaxel stealth liposome solution was obtained, and the salt was removed by dialysis. Add 20ml of water for dilution, add 0.5g of mannitol and 0.4g of glucose as proppants, freeze-dry to make freeze-dried powder injection. The average particle diameter of the sample was measured using deionized water as the disper...

Embodiment 3

[0043] Get docetaxel 10mg, be dissolved in 25ml dehydrated alcohol, inject 30mg containing polyethylene glycolated polyhexadecyl cyanoacrylate (PEG6000-PHDCA, its preparation method is the conventional method in the prior art, specifically as follows : Dissolve PHDCA20mg, N,N-dicyclohexylcarboimide 10mg, N-hydroxysuccinimide 10mg in dimethyl sulfoxide 25ml, stir for 3 hours, filter to get the filtrate, PEG600020mg is dissolved in dichloromethane 15ml Add it, continue to stir for 4 hours, filter to take the filtrate, place it at 0°C for 24 hours to recrystallize, filter, freeze-dry, and obtain. After that, W / O colostrum is obtained. Then add this colostrum into 50ml, 4% PVA solution, under ice bath, then pulse ultrasonic with ultrasonic cell pulverizer for 5 minutes, obtain W / O / W double emulsion. The obtained double emulsion was added to 120 mL of a solution containing 1 wt% PVA, evaporated under reduced pressure at room temperature, and dichloromethane was removed to obtain a...

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Abstract

The invention provides a long-circulating preparation which is an invisible nano particle, a stealth lipidosome, or an invisible micelle containing docetaxle, carrier materials and additive. The long-circulating preparation is prepared by wrapping the docetaxle with the carrier materials that are modified by polyethylene glycol, a hydrotropic substance. The long-circulating preparation of the docetaxel can avoid being captured or swallowed by the hepatolienal reticular endothelial system in the body, thus prolonging circulation time in blood. Compared with the common injection of the docetaxel or the non-stealth lipidosome of the docetaxel, the long-circulating preparation of the docetaxel provided by the invention has stronger inhibit function on a tumor.

Description

technical field [0001] The present invention relates to a long-circulation preparation of the antineoplastic drug docetaxel, which can be stealth nanoparticles, stealth liposomes and stealth micelles, and especially relates to the main carrier material used in the preparation, the preparation method and application of the preparation . Background technique [0002] Docetaxel (Taxotere) is a new type of antineoplastic drug. Molecular formula is C 43 h 53 NO 14 , the structural formula is: [0003] [0004] It is a semi-synthetic anti-tumor drug developed by the former Rhone-Poulenc Rorer of France and the current Sanofi-Aventis company. It was first launched in Mexico in April 1995, and it is currently available in China, Europe, the United States, Japan, etc. Nearly 100 countries or regions in the world have been approved for sale. On September 27, 2003, Aventis (China) Investment Co., Ltd. was the first to register for imported products. Docetaxel injection was inc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K9/19A61K31/337A61P35/00
Inventor 李亚平顾王文陈伶俐
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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