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Nanoscale docetaxel and preparation method thereof

A docetaxel, nano-scale technology, applied in the direction of pharmaceutical formulations, medical preparations with no active ingredients, medical preparations containing active ingredients, etc., can solve the problem of low oral bioavailability, serious side effects, and the solubility of docetaxel Low-level problems, to achieve the effect of stable structure, low cost and simple production method

Active Publication Date: 2013-03-20
SHENZHEN GRADUATE SCHOOL TSINGHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Aiming at the defects of low solubility of docetaxel, low oral bioavailability, and serious side effects of existing docetaxel injections, the first purpose of the present invention is to provide a novel nanoscale docetaxel particle

Method used

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  • Nanoscale docetaxel and preparation method thereof
  • Nanoscale docetaxel and preparation method thereof
  • Nanoscale docetaxel and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0066] The nanoscale docetaxel of the present embodiment is prepared according to the following method:

[0067] 1. Docetaxel API (Shanghai Zhongxi Sanwei Pharmaceutical Co., Ltd.) 1g, add 20ml of absolute ethanol to dissolve;

[0068] 2. Add 2g of silica airgel after heat treatment at 500°C for adsorption;

[0069] 3. After the adsorption is complete, dry it in an oven at 60°C;

[0070] 4. After drying, add 100ml of pure water and emulsify with 25000rpm / min ordinary emulsifier for 5min;

[0071] 5. High-pressure homogenizer (Shanghai Donghua GYB 30-6S), 400bar, cycle 6 times, 10min;

[0072] 6. Spray-dry the homogeneous liquid in an experimental spray dryer (Shanghai Shunyi Technology SP-1500), parameters: temperature 130°C, flow rate 500ml / h, nozzle: 0.75mm, and obtain nano-sized docetaxel particles after drying.

Embodiment 2

[0074] The nanoscale docetaxel of the present embodiment is prepared according to the following method:

[0075] 1. Docetaxel API (Shanghai Zhongxi Sanwei Pharmaceutical Co., Ltd.) 1g, add 5ml of absolute ethanol to dissolve;

[0076] 2. Add 0.5g of silica airgel after heat treatment at 1000℃ for adsorption;

[0077] 3. After the adsorption is complete, dry naturally;

[0078] 4. After drying, add 20ml of pure water and emulsify with an ordinary emulsifier at 25000rpm / min for 5min;

[0079] 5. High pressure homogenizer (Shanghai Donghua GYB 30-6S), 400bar, cycle 8 times, 10min;

[0080] 6. Spray-dry the homogeneous liquid in an experimental spray dryer (Shanghai Shunyi Technology SP-1500), parameters: temperature 130°C, flow rate 500ml / h, nozzle: 0.75mm, and obtain nano-sized docetaxel particles after drying.

Embodiment 3

[0082] The nanoscale docetaxel of the present embodiment is prepared according to the following method:

[0083] 1. Paclitaxel API (Shanghai Zhongxi Sanwei Pharmaceutical Co., Ltd.) 1g, add 150ml of absolute ethanol to dissolve;

[0084] 2. Add 15g of hydrophilic silica airgel for adsorption;

[0085] 3. After the adsorption is complete, freeze-dry;

[0086] 4. After drying, add 150ml of pure water and emulsify with 25000rpm / min ordinary emulsifier for 5min;

[0087] 5. High-pressure homogenizer (Shanghai Donghua GYB 30-6S), 400bar, cycle 7 times, 10min;

[0088] 6. Spray-dry the homogeneous liquid in an experimental spray dryer (Shanghai Shunyi Technology SP-1500), parameters: temperature 130°C, flow rate 500ml / h, nozzle: 0.75mm, and obtain nano-sized docetaxel particles after drying.

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Abstract

The invention discloses nanoscale docetaxel and a preparation method thereof, and relates to the docetaxel which is an antitumor drug. Aiming at the defects of low solubility and low oral bioavailability of the docetaxel, and serious toxic and side effects of the conventional docetaxel injection, the invention aims at providing novel nanoscale docetaxel particles which are characterized by using silicon dioxide aerogel as a carrier of the docetaxel on the one hand; the invention aims at providing a preparation method of the novel nanoscale docetaxel particles on the other hand; and the preparation method is characterized by comprising the following steps: dissolving the docetaxel in anhydrous ethanol, adding the silicon dioxide aerogel according to proportion, drying after full absorption, adding purified water, feeding into an emulsifying machine for emulsification, homogenizing through a high pressure homogenizer, and drying the obtained homogenate to obtain the novel nanoscale docetaxel particles. The nanoscale docetaxel disclosed by the invention is especially suitable for oral administration.

Description

technical field [0001] The invention relates to an antitumor drug docetaxel, in particular to a nanoscale docetaxel and a preparation method thereof. Background technique [0002] Docetaxel is a taxane compound, which can be obtained by semi-synthesis from the non-cytotoxic precursor compound 10-deacylated baccatin II extracted from Taxus chinensis. It was approved by the US FDA in 1998 and is currently the It is the most effective taxane antineoplastic drug in clinical use. The mechanism of action of docetaxel is similar to paclitaxel, but its antitumor activity is 1.3-12 times that of paclitaxel, and it has good curative effect on breast cancer, pancreatic cancer, non-small cell lung cancer and other cancers. [0003] Due to the poor water solubility of docetaxel, the current clinical use mainly includes freeze-dried powder injection and water injection injection. In order to meet the concentration requirements for clinical injection, more surfactants Tween 80 and ethanol...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/337A61K47/04A61P35/00
CPCA61K9/14A61K31/337A61K9/0019A61K9/0031A61K9/0095A61K9/02A61K9/10A61K9/143A61K9/2009A61K9/485A61P35/00
Inventor 张旭旭张志安武超
Owner SHENZHEN GRADUATE SCHOOL TSINGHUA UNIV
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