Nanoscale capecitabine and preparation method thereof

A capecitabine nano-scale technology, applied in the direction of pharmaceutical formulations, medical preparations containing active ingredients, organic active ingredients, etc., can solve problems such as hair loss, liver function damage, inhibition, etc., achieve structural stability, production The effect of simple method and low cost

Active Publication Date: 2013-03-13
SHENZHEN GRADUATE SCHOOL TSINGHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Although capecitabine itself already has the function of targeted therapy, and the curative effect of its oral formulations can exceed that of intravenous administration, adverse reactions will inevitably occur in clinical applications, s

Method used

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  • Nanoscale capecitabine and preparation method thereof
  • Nanoscale capecitabine and preparation method thereof
  • Nanoscale capecitabine and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

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

[0075] 1. Capecitabine API (Jinan Fuchuang Pharmaceutical Technology Co., Ltd.) 1g, add 20ml of absolute ethanol to dissolve;

[0076] 2. Add 2g of silica airgel after heat treatment at 500°C for adsorption;

[0077] 3. After the adsorption is complete, dry it in an oven at 60°C;

[0078] 4. After drying, add 100ml of pure water and emulsify with 25000rpm / min ordinary emulsifier for 5min;

[0079] 5. High-pressure homogenizer (Shanghai Donghua GYB 30-6S), 400bar, cycle 6 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 nanoscale capecitabine particles after drying .

Embodiment 2

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

[0083] 1. Capecitabine API (Jinan Fuchuang Pharmaceutical Technology Co., Ltd.) 1g, add 5ml of absolute ethanol to dissolve;

[0084] 2. Add 0.5g of silica airgel after heat treatment at 1000℃ for adsorption;

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

[0086] 4. After drying, add 20ml of pure water and emulsify with an ordinary emulsifier at 25000rpm / min for 5min;

[0087] 5. High pressure homogenizer (Shanghai Donghua GYB 30-6S), 400bar, cycle 8 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 nanoscale capecitabine particles after drying .

Embodiment 3

[0090] The nanoscale capecitabine of the present embodiment is prepared according to the following method:

[0091] 1. Capecitabine API (Jinan Fuchuang Pharmaceutical Technology Co., Ltd.) 1g, add 150ml of absolute ethanol to dissolve;

[0092] 2. Add 15g of hydrophilic silica airgel for adsorption;

[0093] 3. After the adsorption is complete, freeze-dry;

[0094] 4. After drying, add 150ml of pure water and emulsify with 25000rpm / min ordinary emulsifier for 5min;

[0095] 5. High-pressure homogenizer (Shanghai Donghua GYB 30-6S), 400bar, cycle 7 times, 10min;

[0096] 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 nanoscale capecitabine particles after drying .

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Abstract

The invention discloses nanoscale capecitabine and a preparation method thereof, relating to an antitumor drug capecitabine. In order to further improve the targeted treatment function, further improve the bioavailability, reduce the toxic and side effects and improve the treat effect, the invention firstly aims at providing a novel nanoscale capecitabine particle which is characterized by taking silicon dioxide aerogel as a carrier of the capecitabine; the invention secondly aims at providing a preparation method of the nanoscale capecitabine particle; and the preparation method is characterized by comprising the steps of: dissolving the capecitabine in absolute ethyl alcohol, adding the silicon dioxide aerogel according to a proportion, drying after complete adsorption, adding purified water and sending into an emulsifying machine for emulsification, homogenizing through a high-pressure homogenizer, and drying the obtained homogenate to obtain the nanoscale capecitabine particle. The nanoscale capecitabine has extremely high bioavailability for oral administration.

Description

technical field [0001] The invention relates to an antitumor drug capecitabine, in particular to a nanoscale capecitabine and a preparation method thereof. Background technique [0002] Capecitabine (trade name: Xeloda) is a new prodrug of 5-fluorouracil (5-FU) developed by Roche, Switzerland, which can inhibit cell division and interfere with RNA and protein synthesis. An oral cytotoxic agent that has a selective effect on tumor cells. It has no cytotoxicity itself, but it can be converted into cytotoxic 5-fluorouracil, which is transformed at the site of the tumor through the tumor-associated vascular factor thymophosphorylase, Therefore, the damage of 5-fluorouracil to normal human cells is greatly reduced, and it has good curative effect and strong safety for adjuvant therapy and metastatic tumor therapy. It is mainly used for the treatment of advanced primary or metastatic breast cancer, rectal cancer, colon cancer and gastric cancer. It is also suitable for the furthe...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/7068A61K47/02A61P35/00A61P35/04
CPCA61K31/7068A61K9/501A61K47/02A61K9/16A61P35/00A61P35/04
Inventor 张旭旭张志安武超
Owner SHENZHEN GRADUATE SCHOOL TSINGHUA UNIV
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