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Taxadol slow release nano-particle, its preparation method and application

A paclitaxel and nanoparticle technology, which can be applied in pharmaceutical formulations, medical preparations with inactive ingredients, and medical preparations containing active ingredients, etc., can solve problems such as low quality of life and dyspnea, and achieve increased release and increased drug release. , to maintain the effect of effective therapeutic concentration

Inactive Publication Date: 2006-08-30
INST OF BIOMEDICAL ENG CHINESE ACAD OF MEDICAL SCI +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Malignant ascites is a common symptom of some advanced tumors, which can cause abdominal distension, abdominal pain, dyspnea, and poor quality of life in patients

Method used

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  • Taxadol slow release nano-particle, its preparation method and application
  • Taxadol slow release nano-particle, its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Polyε-caprolactone can be commercially available or self-prepared.

[0030] The preparation method of polyε-caprolactone:

[0031] 1. Under the protection of nitrogen, put caprolactone and stannous octoate in proportion (1-12:0.001-0.1) into a three-necked flask, seal it, stir and mix evenly, and vacuum degassing: room temperature, vacuum <80Pa, time 5 -15 minutes, and then filled with high-purity nitrogen;

[0032] 2. Transfer the mixed raw materials to the polymerization kettle under the protection of nitrogen, repeat the above vacuum degassing and nitrogen replacement process, close the ventilation valve after filling the nitrogen gas for the last time, and put the polymerization kettle in a constant temperature oven at 100-300°C for polymerization 24-96 hours.

[0033] After the polymerization is completed, the polymer is extruded from the discharge valve at the bottom of the polymerization kettle, cooled and solidified at room temperature.

Embodiment 2

[0035] The preparation method of paclitaxel slow-release nanoparticles:

[0036] The method of preparing nano-controlled release system includes polymerization reaction method and polymer material dispersion method. The former is emulsion polymerization and interfacial polymerization technology prepared by polymerization reaction using different monomers; the latter is such as emulsification-solvent evaporation method using high molecular polymer The method of preparation. In the present invention, the nanoparticles are prepared by a solvent substitution method. Compared with the commonly used emulsification-solvent evaporation method, the solvent substitution method is easy to operate, does not require high-speed emulsification or ultrasonic stirring, and requires low energy consumption.

[0037](1) 63 grams of molecular weight are 20,000 to 30,000 polyε-caprolactone, 6 grams of poloxamer 188 and 25 grams of paclitaxel dissolved in 4000 milliliters of acetone;

[0038] (2) ...

Embodiment 3

[0043] The preparation method of paclitaxel slow-release nanoparticles:

[0044] (1) 90.25 grams of polylactic acid with a molecular weight of 20,000 to 30,000, 2 grams of poloxamer 407 and 5 grams of paclitaxel were dissolved in 3000 milliliters of acetone;

[0045] (2) According to the ratio of 1:4 by volume, the solution made in step (1) is added to the poloxamer 188 aqueous solution with a molecular weight of 110,000 at a mass percentage concentration of 0.5%, and the addition speed is 5ml / min;

[0046] (3) Remove acetone under reduced pressure at 10°C;

[0047] (4) 0°C, 20000rpm, centrifuge for 20min, collect the solidified nanoparticles, wash with distilled water, and centrifuge once to remove Poloxamer 188 in the nanoparticle suspension;

[0048] (5) freeze-drying to obtain paclitaxel sustained-release nanoparticles.

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Abstract

A slow-releasing taxusol nanoparticle used for anticancer medicine is prepared through dissolving biodegradable high-molecular polyester, poloxamer 188 (or 407) or polyethylene glycol and taxusol in acetone, adding it to the aqueous solution of polyvinyl alcohol or poloxamer 188, removing acetone, centrifugal separation, washing with distilled water and freeze drying.

Description

technical field [0001] The invention relates to a sustained-release drug nanoparticle, a preparation method and an application thereof. Background technique [0002] Paclitaxel (paclitaxel) is a new anticancer drug isolated from the Taxus genus (Taxus), which has a unique mechanism of action, which can induce and promote tubulin polymerization, microtubule assembly and microtubule stabilization, thereby preventing The growth of tumor cells has a good anti-cancer effect on breast cancer, ovarian cancer, head and neck cancer, and prostate cancer. At the end of 1992, the US FDA first approved paclitaxel for metastatic ovarian cancer refractory to other chemotherapy drugs, and later approved it for metastatic breast cancer refractory to platinum drugs. [0003] Paclitaxel is a diterpenoid compound, almost insoluble in water (<0.003mg / ml). Most of the paclitaxel preparations that are currently used in clinic are injections made of Cremophor EL (polyoxyethyl castor oil) 50% (...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K47/34A61K31/337A61P35/00A61K47/10
Inventor 宋存先马桂蕾孙洪范
Owner INST OF BIOMEDICAL ENG CHINESE ACAD OF MEDICAL SCI
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