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Preparation and application of taxane prodrug

A technology of taxanes and prodrugs, which is applied in the field of taxanes prodrugs and their preparation, can solve the problems of strong irritation, poor targeting, increased stability and targeting, and achieve good stability, Good tumor cell targeting effect and improved long cycle time effect

Inactive Publication Date: 2016-08-24
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Based on the above background technology, aiming at the deficiencies of existing antitumor drugs, such as strong irritation, strong side effects, poor stability, and poor targeting, the purpose of the present invention is to provide a prodrug of antitumor drugs, which can be made into Acceptable dosage forms for injection or oral administration, improve the activity of anti-tumor drugs, reduce toxicity, increase stability and targeting, thus facilitating the development of preparations

Method used

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  • Preparation and application of taxane prodrug
  • Preparation and application of taxane prodrug
  • Preparation and application of taxane prodrug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Paclitaxel Prodrug Nanoparticles

[0043] Accurately weigh 10.0 mg of PTX-SS-CIT and 2.5 mg of poloxamer 188 and dissolve them in an organic solvent, slowly add them dropwise into 5 mL of buffer solution at room temperature, stir at 500 r / min for 1 h to allow the organic solvent to dry naturally, and obtain the final precursor drug nanoparticle solution.

[0044] The paclitaxel prodrug nanoparticles of the present invention have better stability. The stability of nanoparticles was examined by room temperature placement experiment, and the particle size and PDI of nanoparticles were measured at 0 day, 1 day, 2 days, 4 days, 7 days, 15 days, 1 month, and 2 months. The results showed that paclitaxel prodrug nanoparticles had good stability, and no change in particle size occurred during placement. (See figure 1 )

Embodiment 2

[0046] Paclitaxel Prodrug Nanoparticles

[0047] Precisely weigh 10.0mg of PTX-SS-CIT and 1.0mg of Tween 80 and dissolve them in an organic solvent, slowly drop them into 5mL of buffer solution at room temperature, stir at 400r / min for 2h, and let the organic solvent dry up naturally to obtain the final prodrug Nanoparticle solution.

Embodiment 3

[0049] Cabazitaxel Prodrug Nanoparticles

[0050] Accurately weigh 10.0 mg of CTX-SS-CIT, 2.0 mg of distearoylphosphatidylethanolamine-polyethylene glycol 2000 and dissolve them in an organic solvent, slowly add them dropwise into 5 mL of buffer solution at room temperature, stir at 800 r / min for 1 h to make the organic The solvent was evaporated to dryness naturally to obtain the final prodrug nanoparticle solution.

[0051] The cabazitaxel prodrug nanoparticles of the present invention have better redox-sensitive release behavior. Using pH 7.4 phosphate buffer (containing 0.5% Tween 80) with two glutathione concentrations (1mM or 1μM) as the release medium, take an appropriate amount of nanoparticles and place them in a dialysis bag at 37.0°C with a rotation speed of 100r / Under the condition of 1 min, take 1ml of the solution at 1h, 2h, 3h, 6h, 12h, and 24h respectively, filter through a 0.45 μm filter membrane, discard the initial filtrate, and use the subsequent filtrate...

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Abstract

The invention belongs to the technical field of drugs and relates to preparation and an application of a taxane prodrug. The prodrug is prepared from citronellol and an anticancer drug which are joined through a disulfide bond. The anticancer drug is one of paclitaxel and cabazitaxel. A dosage form which is clinically acceptable and capable of being injected or orally taken can be prepared from the prodrug of the anticancer drug and a pharmaceutically acceptable carrier. The dosage form comprises nanoparticles and lipidosome or emulsion. The prodrug and a preparation can obviously improve the activity of the anticancer drug, reduce the toxicity and increase the stability and the targeting property, so that development of the preparation is facilitated.

Description

technical field [0001] The invention relates to a prodrug of an antineoplastic drug, in particular to a taxane prodrug and its preparation method and application. Background technique [0002] The application and research of taxane drugs have been widely valued by researchers at home and abroad. These drugs can promote the assembly of microtubules by binding to tubulin, and at the same time prevent the disintegration of assembled microtubules, thereby inhibiting tumor cells. The function of mitotic and interphase cells. However, as of 2016, there are not many such anti-tumor drugs approved by the US FDA. More importantly, even the drug approved by the US FDA in 2010 It is the latest generation of taxane antineoplastic drugs (cabazitaxel), and it also has higher surfactant concentration and non-aqueous solvent than the previous preparations, which makes it more irritating and toxic to patients in clinical use. The side effects are large, and there are certain problems in s...

Claims

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Application Information

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IPC IPC(8): C07D305/14A61K31/337A61K47/48A61P35/00
CPCC07D305/14
Inventor 王永军刘丹薛鹏张娜赵临襄何仲贵
Owner SHENYANG PHARMA UNIVERSITY
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