Paclitaxel antitumor preparation and preparation method thereof

A technology of paclitaxel and anti-tumor drugs, which is applied in the directions of anti-tumor drugs, pharmaceutical formulations, and medical preparations with inactive ingredients, etc., can solve the problems of no reported particle anti-tumor effect, low synthesis efficiency, loss of drug adaptability, etc.

Inactive Publication Date: 2014-06-18
SUZHOU YOULIN BIO TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Chinese patent 20121002970.5 discloses covalently bonded folic acid-dextran-iron oxide nanoparticles, which have an in vitro targeting effect, but it has not reported the anti-tumor effect of the particle itself (actually basically none), and the inventors found that its It is to synthesize dextran-iron oxide nanoparticles first, and then carry out folic acid conjugation, the synthesis efficiency is low, and the adaptability of excipients to drugs is lost

Method used

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  • Paclitaxel antitumor preparation and preparation method thereof
  • Paclitaxel antitumor preparation and preparation method thereof
  • Paclitaxel antitumor preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0067] Example 1: Preparation of folic acid-dextran conjugates

[0068] 1. Synthesis of Succinylated Dextran

[0069] The synthetic route is as follows:

[0070]

[0071] Take 10.0g dextran (average molecular weight 20KDa, Mw / Mn=1.3, available from Shanghai Sunshine Reagent Co., Ltd.) and dissolve it in anhydrous dimethylformamide (DMF), stir for 20 minutes to form a clear solution, and then add 1670 mg succinic anhydride and 200.0 mg 4-dimethylaminopyridine (DMAP), stir rapidly until all solids dissolve. Place at room temperature (25°C) to allow the entire reaction solution to react for 24 hours, then put the reaction solution into a Spectra / Por3 dialysis bag (molecular weight cut-off 3,500) and dialyze in water for 2 days. The solution in the dialysis bag was then freeze-dried to obtain white succinylated dextran. Nuclear magnetic resonance (NMR) results are as follows: 1H-NMR (d-DMSO): 2.8 (-CH 2 CH 2 -, succinylated dextran), 3.2-3.6 (dextran), 4.4-5.8 (dextran). ...

Embodiment 2

[0081] Example 2: Preparation and Stability Test of Freeze-dried Powder Injection of Paclitaxel Encapsulated by Folic Acid-Dextran Conjugate

[0082] Take 1000 mg of the folic acid-dextran conjugate prepared in Example 1 and dissolve it in 100 ml of 15 mM phosphate buffer (pH=7.4). After dissolving, place it on a magnetic stirrer and stir at 400 rpm. During the stirring process, 250 mg of paclitaxel was dissolved in 5 mL of ethanol, added dropwise to the stirred solution, and placed in the FS-1 type high-speed homogenizer (available from Jintan Zhongzheng Instrument Manufacturing Co., Ltd.) , Homogenize 6 times at maximum power, 1 minute each time, stop for 2 minutes, then put the homogenate into Spectra / Por3 dialysis bag (molecular weight cut-off 3,500), dialyze in 15mM phosphate buffer (pH=7.4) 12 hours to remove ethanol, then add 2500mg mannitol to adjust the osmotic pressure, and pass through a 0.2μm membrane filter to sterilize. After being detected by a particle size te...

Embodiment 3

[0086] Example 3: Pharmacodynamic study of paclitaxel freeze-dried powder injection coated with folic acid-dextran conjugate

[0087] The tumor cytotoxicity test was carried out on the freeze-dried powder injection prepared in Example 2, and the tested cells were human non-lobular lung cancer cells. Freeze-dried powder injections of different concentrations were added to the IC50 was calculated after 72 hours of treatment in cell culture medium. The results showed that the cytotoxicity of paclitaxel encapsulated by various concentrations of folic acid-dextran conjugates was similar to that of paclitaxel of the same concentration without any treatment, and the calculated IC50 was 10nM, while the cytotoxicity of folic acid-dextran conjugate itself is very small, IC50>0.05mg / ml, it can be seen that the cytotoxicity in vitro mainly comes from paclitaxel, and the folic acid-dextran conjugate basically does not affect paclitaxel exert cytotoxicity.

[0088] The lyophilized powd...

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Abstract

The invention discloses a paclitaxel antitumor preparation which is obtained fromwrapping paclitaxel for a folic acid-glucan conjugate. The invention further discloses a preparation method of the pharmaceutical composition and an antitumor application (such as non small lung cancers).

Description

technical field [0001] The present invention is an invention of Chinese patent application No. 201210543504.9, and enjoys a filing date of December 14, 2012. [0002] The present invention belongs to the field of pharmaceutical preparations, in particular, the present invention relates to an anti-tumor pharmaceutical composition obtained by coating paclitaxel with folic acid-dextran conjugates, wherein folic acid-dextran conjugates are used as auxiliary materials in addition to improving the physical and chemical properties of the drug In addition, they can even act synergistically and can improve the tolerance of paclitaxel. In addition, the present invention also relates to the preparation method of the pharmaceutical composition and its anti-tumor application and the like. Background technique [0003] Most anticancer drugs currently used clinically, such as paclitaxel, Docetaxel (docetaxel), doxorubicin, etc., have poor solubility in normal saline and cannot be directly...

Claims

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Application Information

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IPC IPC(8): A61K47/36A61K31/337A61K9/19A61P35/00C08B37/02
Inventor 李军游绍进陈琼
Owner SUZHOU YOULIN BIO TECH
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