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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Problems solved by technology

Malignant ascites is a common symptom of some advanced tumors, which can cause ab

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
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[0028] Example 1:

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

[0030] Preparation method of polyε-caprolactone:

[0031] 1. Under the protection of nitrogen, put caprolactone and stannous octoate in a ratio (1-12:0.001-0.1) into a three-necked flask. After airtight, stir and mix uniformly. Vacuum and degas: room temperature, vacuum degree <80Pa, time 5 -15 minutes, then fill with high-purity nitrogen;

[0032] 2. Under the protection of nitrogen, the mixed raw materials are transferred to the polymerization kettle, and the above vacuum degassing and nitrogen replacement process are repeated. After the last time is filled with nitrogen, the vent valve is closed, and the polymerization kettle is placed 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 vessel, and cooled to solidify at room temp...

Example Embodiment

[0034] Example 2

[0035] Preparation method of paclitaxel sustained-release nanoparticles:

[0036] The methods for preparing nano-controlled release systems include polymerization reaction method and polymer material dispersion method. The former is the emulsion polymerization and interfacial polymerization technology prepared by polymerization reaction using different monomers; the latter is the emulsification-solvent volatilization method using high molecular polymers. The method of preparation. In the present invention, a solvent substitution method is used to prepare nanoparticles. Compared with the commonly used emulsification-solvent volatilization method, the operation method of the solvent substitution method is simple, does not require high-speed stirring emulsification or ultrasound, and requires low energy consumption.

[0037](1) Dissolve 63 grams of polyε-caprolactone with a molecular weight of 20,000 to 30,000, 6 grams of Poloxamer 188 and 25 grams of paclitaxel in...

Example Embodiment

[0042] Example 3

[0043] Preparation method of paclitaxel sustained-release nanoparticles:

[0044] (1) Dissolve 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 in 3000 ml of acetone;

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

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

[0047] (4) Centrifuge at 0°C, 20000 rpm, for 20 minutes, 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 a paclitaxel sustained-release nanoparticle.

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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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