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Prodrug of taxol or polyene-taxol with carbowax as carrier

A technology of docetaxel and polyethylene glycol, which is applied in the field of water-soluble paclitaxel or derivative compounds of docetaxel, which can solve the problems of large toxic side effects and inconvenient application, and achieve the effect of improving solubility

Active Publication Date: 2007-01-17
SHANGHAI ALLIST PHARM CO LTD
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Problems solved by technology

[0003] As we all know, paclitaxel has great application value and economic benefits, but its wide application has obvious disadvantages: the solubility of paclitaxel in water is 0.006mg / ml, and the key technology of its intravenous infusion preparation is to solve its solubility in water
This form of preparation has serious defects such as large toxic and side effects and inconvenient application.

Method used

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  • Prodrug of taxol or polyene-taxol with carbowax as carrier
  • Prodrug of taxol or polyene-taxol with carbowax as carrier
  • Prodrug of taxol or polyene-taxol with carbowax as carrier

Examples

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Embodiment 1

[0039] Example 1: Synthesis of polyethylene glycol 5000-succinic acid-glycolic acid-paclitaxel

[0040] 1. Functionalization of methoxy-terminated polyethylene glycol

[0041] In a 100ml there-necked flask, equipped with a reflux condensing device and a magnetic stirrer, the baking reaction device is ventilated three times (high-purity argon), under gas protection, add 10g of polymer and 1g of pre-weighed succinic anhydride, and An equimolar amount of dimethylaminopyridine (DMAP) was added to 60 ml of anhydrous and oxygen-free tetrahydrofuran, and the mixture was refluxed for 72 hours. After completion of the reaction, concentrate the solvent, then add 10ml of 0.1M aqueous sodium bicarbonate solution to the residue, acidify the filtrate with 10ml of 0.1N hydrochloric acid, adjust the pH value of the solution to 3-4 with hydrochloric acid, and then use 100ml of ethyl acetate to Wash the water layer three times with ester, combine the ethyl acetate solution and wash twice with ...

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Abstract

A precursor of taxol or polyenyl taxol with higher water solubility and tumor suppressing efficiency is prepared from polyethanediol as carrier, hydroxyacetic acid, or L-lactic acid, or their oligomer as linking arm, and taxol or polyenyl taxol through bonding reaction on the hydroxy groups at the site 2' or 7' of taxol or polyenyl taxol.

Description

technical field [0001] The invention relates to a prodrug of paclitaxel or docetaxel with polyethylene glycol as a carrier and a preparation method thereof, belonging to derivative compounds of water-soluble paclitaxel or docetaxel. technical background [0002] Paclitaxel (Taxol) is a natural product isolated from the bark of the Pacific Yew tree. Paclitaxel has good anticancer activity and has become the third-generation antineoplastic drug after doxorubicin and cisplatin. It is toxic to the mitotic spindle and is a strong cytostatic agent. Paclitaxel has good effects in the treatment of ovarian cancer and breast cancer, and has good effects in the treatment of prostate cancer, upper gastrointestinal cancer, small cell and non-small cell lung cancer. On February 29, 1992, the U.S. Food and Drug Administration officially approved paclitaxel as a new antineoplastic drug for the treatment of advanced ovarian cancer. [0003] As we all know, paclitaxel has great application ...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K31/337A61P35/00A61K47/59
Inventor 郭建辉张雪飞
Owner SHANGHAI ALLIST PHARM CO LTD
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