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Nanometer cyclophosphamide and preparation method thereof

A cyclophosphamide, nano-level technology, applied in pharmaceutical formulations, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc., can solve the problem of low bioavailability, poor absorption, and insoluble cyclophosphamide. Water and other problems, to achieve the effect of low cost and simple production method

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

[0004] The first object of the present invention is to provide a novel nano-scale cyclophosphamide particle to improve the problems of cyclophosphamide insoluble in water, poor oral absorption and low bioavailability, reduce its toxic and side effects, and improve the therapeutic effect

Method used

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  • Nanometer cyclophosphamide and preparation method thereof
  • Nanometer cyclophosphamide and preparation method thereof
  • Nanometer cyclophosphamide and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0061] The nanoscale cyclophosphamide of the present embodiment is prepared according to the following method:

[0062] 1. Cyclophosphamide API (Hubei Haiboyuan Chemical Co., Ltd.) 1g, add 20ml of absolute ethanol to dissolve;

[0063] 2. Add 2g of silica airgel after heat treatment at 500°C for adsorption;

[0064] 3. After the adsorption is complete, dry it in an oven at 60°C;

[0065] 4. After drying, add 100ml of pure water and emulsify with 25000rpm / min ordinary emulsifier for 5min;

[0066] 5. High-pressure homogenizer (Shanghai Donghua GYB 30-6S), 400bar, cycle 6 times, 10min;

[0067] 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-scale cyclophosphamide particles after drying.

Embodiment 2

[0069] The nanoscale cyclophosphamide of the present embodiment is prepared according to the following method:

[0070] 1. Cyclophosphamide API (Hubei Haiboyuan Chemical Co., Ltd.) 1g, add 5ml of absolute ethanol to dissolve;

[0071] 2. Add 0.5g of silica airgel after heat treatment at 1000℃ for adsorption;

[0072] 3. After the adsorption is complete, dry naturally;

[0073] 4. After drying, add 20ml of pure water and emulsify with an ordinary emulsifier at 25000rpm / min for 5min;

[0074] 5. High pressure homogenizer (Shanghai Donghua GYB 30-6S), 400bar, cycle 8 times, 10min;

[0075] 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-scale cyclophosphamide particles after drying.

Embodiment 3

[0077] The nanoscale cyclophosphamide of the present embodiment is prepared according to the following method:

[0078] 1. Cyclophosphamide API (Hubei Haiboyuan Chemical Co., Ltd.) 1g, add 150ml of absolute ethanol to dissolve;

[0079] 2. Add 15g of hydrophilic silica airgel for adsorption;

[0080] 3. After the adsorption is complete, freeze-dry;

[0081] 4. After drying, add 150ml of pure water and emulsify with 25000rpm / min ordinary emulsifier for 5min;

[0082] 5. High-pressure homogenizer (Shanghai Donghua GYB 30-6S), 400bar, cycle 7 times, 10min;

[0083] 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-scale cyclophosphamide particles after drying.

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Abstract

The invention discloses nanometer cyclophosphamide and a preparation method thereof, which relate to cyclophosphamide, an antitumor drug. For solving the problem that cyclophosphamide is difficult to dissolve in water, poor in oral absorption and low in bioavailability, and reducing the side effects of cyclophosphamide and improving the therapeutic effect of cyclophosphamide, the invention firstly aims to provide a novel nanometer cyclophosphamide particle, which is characterized by taking silica aerogel as a carrier of cyclophosphamide; and the other purpose of the invention is to provide a method for preparing the nanometer cyclophosphamide particle, which is characterized by comprising the steps of dissolving cyclophosphamide into anhydrous ethanol firstly; then adding the silica aerogel in proportion; after the obtained product is completely adsorbed, drying the obtained object, and adding pure water into the obtained object; and feeding the obtained mixture into an emulsifying machine to emulsify, homogenizing the emulsified product by using a high-pressure homogenizer, and drying the obtained homogenized liquid so as to obtain the nanometer cyclophosphamide particle. The novel nanometer cyclophosphamide disclosed by the invention is especially suitable for oral administration.

Description

technical field [0001] The invention relates to an antitumor drug cyclophosphamide, in particular to a nanoscale cyclophosphamide and a preparation method thereof. Background technique [0002] Cyclophosphamide is the most commonly used alkylating agent anti-tumor drug. It has no anti-tumor activity in vitro. After entering the body, it is first converted into aldophosphamide by microsomal functional oxidase in the liver, and aldoamide is unstable. It is decomposed into amide nitrogen mustard and acrolein in the cell, and amide nitrogen mustard has cytotoxic effect on tumor cells. Cyclophosphamide is a bifunctional alkylating agent and a non-specific cell cycle drug, which can interfere with DNA and RNA functions, especially the former. It cross-links with DNA and inhibits DNA synthesis. It has the most obvious effect on S phase. Clinically used for malignant lymphoma, multiple myeloma, leukemia, breast cancer, ovarian cancer, cervical cancer, prostate cancer, colon cancer,...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/675A61K47/04A61P35/00
CPCA61K31/675A61K9/16A61K9/5115A61P35/00
Inventor 张旭旭张志安武超
Owner SHENZHEN GRADUATE SCHOOL TSINGHUA UNIV
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