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Docetaxel nano preparation and preparation method thereof

A technology of docetaxel and nano-formulations, which is applied in the directions of pill delivery, pharmaceutical formulations, and inactive medical preparations, can solve the problems of low bioavailability, unsatisfactory stability and storage stability, etc. Good stability, long-term release, good stability

Inactive Publication Date: 2012-02-22
SUZHOU NASIDA BIO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, according to this patent document, the docetaxel nanoparticles are mainly composed of phospholipid materials, which are easily oxidized, and their in vivo stability and storage stability are not ideal, and are only suitable for making injections. If they are made into oral preparations, biological Utilization is very low

Method used

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  • Docetaxel nano preparation and preparation method thereof
  • Docetaxel nano preparation and preparation method thereof
  • Docetaxel nano preparation and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0031] This example provides a nano freeze-dried powder injection of docetaxel, which is prepared by the following steps:

[0032] Weigh 15 mg of docetaxel and 100 mg of polybenzyl glutamate with a weight average molecular weight of 64,000, add them to 10 ml of organic solvent ethyl acetate, stir and dissolve, and take 3 mg of vitamin E polyethylene glycol amber Ester (self-made, using PEG1000), dissolved in 150ml ultra-pure water, and prepared as an aqueous solution; the organic phase was added to the aqueous solution, and the O / W The colostrum is then subjected to high-speed shear (shear rate range 10000-12000rpm) for 0.1-5min to prepare a stable emulsion. Then evaporate under reduced pressure at room temperature to remove ethyl acetate to obtain a colloidal solution of nanoparticles. After the colloidal solution is centrifuged at 11500 rpm for 30 minutes at 4°C, the supernatant is discarded, and the precipitate is washed 3 times with ultrapure water to obtain Doxyl Taxel n...

Embodiment 2

[0035] This example provides a nano freeze-dried powder injection of docetaxel, which is prepared by the following steps:

[0036] Weigh 15 mg of docetaxel and 100 mg of polybenzyl glutamate with a weight average molecular weight of 64,000, add it to 10 ml of organic solvent methylene chloride, stir and dissolve, and use it as the organic phase; another 15 mg of cholesterol polyethylene glycol succinic acid Esters (self-made, using PEG 2000), dissolved in 150ml ultrapure water, and prepared as an aqueous solution; the organic phase was added to the aqueous solution, and the O / W The colostrum is then subjected to high-speed shear (shear rate range 10000-12000rpm) for 0.1-5min to prepare a stable emulsion. Then dichloromethane was volatilized under reduced pressure at room temperature to obtain a colloidal solution of nanoparticles. After the colloidal solution was centrifuged at 11,500 rpm for 30 minutes at 4°C, the supernatant was discarded, and the precipitate was washed 3 ti...

Embodiment 3

[0039] This example provides a nano freeze-dried powder injection of docetaxel, which is prepared by the following steps:

[0040] Weigh 25 mg of docetaxel and 375 mg of poly(lactic-co-glycolic acid) copolymer with a weight average molecular weight of 15,000, add it to 25 ml of organic solvent ethyl acetate, stir and dissolve, and take 1.9 mg of vitamin E polyethylene glycol Succinate (self-made, using PEG 1000), dissolved in 375ml ultrapure water, was prepared as an aqueous solution; the organic phase was added to the aqueous solution, and O / W colostrum, and then quickly pour the formed O / W colostrum into the SPG membrane emulsifier, and pass through the membrane 3 to 5 times under the pressure of 0.6-1.8Mpa. Then, the organic solvent was evaporated under reduced pressure at room temperature to obtain a colloidal solution of nanoparticles. After the solution was centrifuged at 11500 rpm for 30 minutes at 4°C, the supernatant was discarded, and the precipitate was washed 3 ti...

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Abstract

The invention relates to a docetaxel nano preparation and a preparation method thereof. The average grain diameter of the docetaxel nano preparation ranges from 20 nm to 500 nm. The docetaxel nano preparation comprises, by weight, 0.1% to 20% of docetaxel, 65% to 99% of biodegradable carrier material and 0.01% to 15% of stabilizing agent, wherein the stabilizing agent is one or combination of more selected from polyvinylpyrrolidone and ethylene glycol succinic acid ester derivatives. Compared with preparations in the market, the docetaxel nano preparation is higher in stability and longer in cycle time in vivo, can achieve long-time release of medicines, and improves medicine effect. Compared with ordinary nano preparations, the docetaxel nano preparation is more stable, has a larger area under concentration-time curve (AUC), and has stronger inhibitory action on a tumor. In addition, when the docetaxel nano preparation is taken orally, retention time and curative effect which are several times better than ordinary clinical injecta can be achieved, the toxic and side effects are remarkably reduced, and the bioavailability is remarkably improved.

Description

technical field [0001] The invention relates to a docetaxel nano preparation and a preparation method thereof. Background technique [0002] Docetaxel, also known as docetaxel, Taxotere, belongs to taxane compounds, is a new generation of taxane anticancer drugs, molecular formula is C 43 h 53 NO 14 , the molecular weight is 807.88, and the structural formula is as follows: [0003] [0004] Docetaxel is a semi-synthetic anti-tumor drug developed by Sanofi-Aventis, France, and is used as a chemotherapy drug for breast cancer and non-small cell lung cancer. Docetaxel was first launched in Mexico, South Africa and Canada in 1995. In 1996, docetaxel was approved by the FDA for the treatment of metastatic breast cancer failed in chemotherapy and metastatic non-small cell lung cancer failed in platinum therapy, and was subsequently marketed in 33 countries including the UK, the US, France and Germany. The drug has a broad anti-tumor spectrum and is the most effective sing...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K9/19A61K9/10A61K9/20A61K9/48A61K31/337A61K47/32A61K47/34A61P35/00
Inventor 张志平谭松巍
Owner SUZHOU NASIDA BIO PHARMA
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