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Minuteness anti-cancer medicine paclitaxel of novel technique supercritical fluid

An anticancer drug, paclitaxel technology, which is applied in the direction of anticancer drugs, drug combinations, and devices that make drugs into special physical or ingestible forms, and can solve the problem of drug particle size, shape characteristics, and physical properties in the field of drug preparation. and other problems, to achieve the effect of easy popularization and application, simple method and high purity

Inactive Publication Date: 2008-02-27
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The purpose of the present invention is to provide a new method for miniaturizing medicines, so as to solve the problems of drug particle size, morphology and physical properties that cannot be prepared in the field of medicines by traditional methods.

Method used

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  • Minuteness anti-cancer medicine paclitaxel of novel technique supercritical fluid

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] (1). Anticancer drug paclitaxel organic solution

[0018] Add 200-300 mg of paclitaxel to the reaction bottle, add a certain amount of organic solvent, and dissolve at room temperature.

[0019] (2). Modulation of system process parameters

[0020] After reaching the temperature and pressure required by the experiment, supercritical CO 2 The high-pressure plunger pump passes through the outer channel of the coaxial two-flow nozzle on the top of the autoclave, and the organic solution is pumped into the autoclave through the high-performance liquid chromatography (HPLC) pump through the inner channel of the nozzle, and the supercritical CO 2 As a dispersion medium, the organic solution is forced to disperse, and it also acts as an anti-solvent to absorb the organic solvent in the dissolved solution.

Embodiment 2

[0022] (1).Polymer organic solution

[0023] Add 200-300 mg of polymer to the reaction bottle, change the amount of organic solvent, adjust the drug concentration of paclitaxel, and dissolve at room temperature.

[0024] (2). Modulation of system process parameters

[0025] After changing the temperature and pressure required by the experiment, supercritical CO 2 The high-pressure plunger pump passes through the outer channel of the coaxial two-flow nozzle on the top of the autoclave, and the organic solution is pumped into the autoclave through the high-performance liquid chromatography (HPLC) pump through the inner channel of the nozzle, and the supercritical CO 2 As a dispersion medium, the organic solution is forced to disperse, and it also acts as an anti-solvent to absorb the organic solvent in the dissolved solution.

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Abstract

The paclitaxel has broad spectrum antineoplastic activity, which is used to treat oophoron cancer and breast cancer, has the significant effect, and is known as a anti-cancer drug with the wide developing prospect, but the particle diameter of paclitaxel medicine powder is bigger so that the paclitaxel medicine powder isn't absorbed by administer orally, has the lower bioavailability, and limits the clinic application of paclitaxel. The invention makes Paclitaxel fine with supercritical flow new technique. The experiment makes Paclitaxel fine with above-critical CO2 as the dissolvent and with supercritical flow forced disperse solution technique, which researches the influence of the pressure, the temperature, the concentration of the solution and the flow speed of the solution for the shape, grain diameter and the distribution of fine paclitaxel. The result indicates that the nanometer grain diameter can be changed in the finite range by changing the technology parameter, wherein the prepared surface of the nanometer grain is smooth, and has the good sphericity, and the average grain diameter is 670nm-940nm, the concentration of the solution and the flow speed is the main factor.

Description

technical field [0001] The invention belongs to the field of new preparation method and application technology for changing the physical characteristics of medicine and medicine dosage form, and in particular relates to micronization of medicine by adopting new method and new technology. Background technique [0002] Paclitaxel has broad-spectrum anti-tumor activity and can be used in the treatment of ovarian cancer, breast cancer, non-small cell lung cancer, malignant black solid tumors and some other solid tumors, especially for the treatment of metastatic ovarian cancer and breast cancer. Development of promising new anticancer drugs. At present, more than 50 countries have approved the sale of synthetic paclitaxel. According to the forecast of the National Cancer Institute (NCI), paclitaxel will become one of the first-choice anti-cancer drugs in the next 10-15 years. [0003] Due to the large particle size of paclitaxel drug powder, it is almost not absorbed orally, a...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K31/337A61P35/00A61J3/02
Inventor 康云清尹光福姚亚东黄忠兵廖晓明
Owner SICHUAN UNIV
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