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Nanoscale docetaxel and preparation method thereof

A paclitaxel and nano-level technology, applied in the field of nano-level paclitaxel and its preparation, can solve the problems of low oral bioavailability, serious toxic and side effects, low solubility of paclitaxel, etc., and achieve the effects of stable structure, low cost and simple preparation method.

Active Publication Date: 2014-09-17
SHENZHEN GRADUATE SCHOOL TSINGHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Aiming at the defects of low solubility of paclitaxel, low oral bioavailability, and severe toxic and side effects of existing paclitaxel injections, the first object of the present invention is to provide a novel nano-scale paclitaxel 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

[0108] The nanoscale paclitaxel of the present embodiment is prepared according to the following method:

[0109] 1. Paclitaxel API (Yunnan Hande Pharmaceutical Co., Ltd.) 1g, add 20ml of absolute ethanol to dissolve;

[0110] 2. Add 2g of silica airgel after heat treatment at 500°C for adsorption;

[0111] 3. After the adsorption is complete, dry it in an oven at 60°C;

[0112] 4. After drying, add 100ml of pure water and emulsify with 25000rpm / min ordinary emulsifier for 5min;

[0113] 5. High-pressure homogenizer (Shanghai Donghua GYB 30-6S), 400bar, cycle 6 times, 10min;

[0114] 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 paclitaxel particles after drying.

Embodiment 2

[0116] The nanoscale paclitaxel of the present embodiment is prepared according to the following method:

[0117] 1. Paclitaxel API (Yunnan Hande Pharmaceutical Co., Ltd.) 1g, add 5ml of absolute ethanol to dissolve;

[0118] 2. Add 0.5g of silica airgel after heat treatment at 1000℃ for adsorption;

[0119] 3. After the adsorption is complete, dry naturally;

[0120] 4. After drying, add 20ml of pure water and emulsify with an ordinary emulsifier at 25000rpm / min for 5min;

[0121] 5. High pressure homogenizer (Shanghai Donghua GYB 30-6S), 400bar, cycle 8 times, 10min;

[0122] 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 paclitaxel particles after drying.

Embodiment 3

[0124] The nanoscale paclitaxel of the present embodiment is prepared according to the following method:

[0125] 1. Paclitaxel API (Yunnan Hande Pharmaceutical Co., Ltd.) 1g, add 150ml of absolute ethanol to dissolve;

[0126] 2. Add 15g of hydrophilic silica airgel for adsorption;

[0127] 3. After the adsorption is complete, freeze-dry;

[0128] 4. After drying, add 150ml of pure water and emulsify with 25000rpm / min ordinary emulsifier for 5min;

[0129] 5. High-pressure homogenizer (Shanghai Donghua GYB 30-6S), 400bar, cycle 7 times, 10min;

[0130] 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 paclitaxel particles after drying.

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Abstract

Nanoscale paclitaxel particles and a preparation method thereof. The nanoscale paclitaxel particles use silicon dioxide aerogel as a carrier of the paclitaxel. The preparation method is as follows: first dissolving the paclitaxel in anhydrous ethanol, then adding the silicon dioxide aerogel, drying after full adsorption, subsequently adding purified water, feeding into an emulsifying machine for emulsification, homogenizing through a high pressure homogenizer, and drying the obtained homogenate to obtain the nanoscale paclitaxel particles.

Description

technical field [0001] The invention relates to an antineoplastic drug paclitaxel, in particular to a nanoscale paclitaxel and a preparation method thereof. Background technique [0002] Paclitaxel is a diterpenoid extracted from the bark of Taxus genus Taxus. It is a new type of microtubule stabilizer, and it is also the antitumor drug with the best curative effect and the largest amount of clinical use in the world. It is considered by the National Cancer Institute of the United States to be the most important progress in tumor chemotherapy in the past 15 to 20 years. The drug has been listed as a first-line drug for a variety of tumors. [0003] Although paclitaxel has good antitumor activity, its solubility in water is very small. According to literature reports, paclitaxel is soluble in organic solvents such as methanol, ethanol, and dimethyl sulfoxide, while its solubility in water is less than 30 μg / mL. Such a small solubility limits the dosage form of paclitaxel a...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/00A61K31/337A61K47/04A61P35/00
CPCA61K31/337A61K9/14A61K9/5115A61P35/00
Inventor 张旭旭蒋宇扬
Owner SHENZHEN GRADUATE SCHOOL TSINGHUA UNIV
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