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Nanoscale doxorubicin hydrochloride and preparation method thereof

A doxorubicin hydrochloride, nano-scale technology, applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problems of serious side effects and low bioavailability, and achieve cost Low cost, simple production method, and stable structure

Active Publication Date: 2014-10-08
SHENZHEN GRADUATE SCHOOL TSINGHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] Aiming at the low oral bioavailability of doxorubicin and the serious side effects of the existing doxorubicin hydrochloride injection, the first object of the present invention is to provide a novel nanoscale doxorubicin hydrochloride particle

Method used

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  • Nanoscale doxorubicin hydrochloride and preparation method thereof
  • Nanoscale doxorubicin hydrochloride and preparation method thereof
  • Nanoscale doxorubicin hydrochloride and preparation method thereof

Examples

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Effect test

Embodiment 1

[0057] The nanoscale doxorubicin hydrochloride of the present embodiment is prepared by the following method:

[0058] 1. Doxorubicin hydrochloride API (Wuhan Dahua Weiye Pharmaceutical Co., Ltd.) 1g, add 30ml of purified water to dissolve;

[0059] 2. Add 3g of silica airgel after heat treatment at 500°C for adsorption;

[0060] 3. After the adsorption is complete, dry it in an oven at 60°C;

[0061] 4. After drying, add 100ml of pure water and emulsify with 25000rpm / min ordinary emulsifier for 5min;

[0062] 5. High-pressure homogenizer (Shanghai Donghua GYB 30-6S), 400bar, cycle 6 times, 10min;

[0063] 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 doxorubicin hydrochloride particles after drying .

Embodiment 2

[0065] The nanoscale doxorubicin hydrochloride of the present embodiment is prepared by the following method:

[0066] 1. Doxorubicin hydrochloride raw material (Wuhan Dahua Weiye Pharmaceutical Co., Ltd.) 1g, add 5ml of purified water to dissolve completely;

[0067] 2. Add 0.5g of silica airgel after heat treatment at 1000℃ for adsorption;

[0068] 3. After the adsorption is complete, dry naturally;

[0069] 4. After drying, add 20ml of pure water and emulsify with an ordinary emulsifier at 25000rpm / min for 5min;

[0070] 5. High pressure homogenizer (Shanghai Donghua GYB 30-6S), 400bar, cycle 8 times, 10min;

[0071] 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 doxorubicin hydrochloride particles after drying .

Embodiment 3

[0073] The nanoscale doxorubicin hydrochloride of the present embodiment is prepared by the following method:

[0074] 1. Doxorubicin hydrochloride API (Wuhan Dahua Weiye Pharmaceutical Co., Ltd.) 1g, add 150ml of purified water to dissolve completely;

[0075] 2. Add 15g of hydrophilic silica airgel for adsorption;

[0076] 3. After the adsorption is complete, freeze-dry;

[0077] 4. After drying, add 150ml of pure water and emulsify with 25000rpm / min ordinary emulsifier for 5min;

[0078] 5. High-pressure homogenizer (Shanghai Donghua GYB 30-6S), 400bar, cycle 7 times, 10min;

[0079] 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 doxorubicin hydrochloride particles after drying .

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Abstract

Nanoscale doxorubicin hydrochloride and a preparation method thereof relate to antitumor drug doxorubicin hydrochloride. Aiming at the low oral bioavailability of doxorubicin and the severe defects of existing doxorubicin hydrochloride injections, the first object of the present invention is to provide a novel nanoscale doxorubicin hydrochloride particle, which is characterized in that: With silica airgel as the carrier of doxorubicin hydrochloride; Another object of the present invention is to provide the preparation method of above-mentioned nanoscale doxorubicin hydrochloride particles, it is characterized in that: first doxorubicin hydrochloride is dissolved in pure water, Then add silica airgel according to the proportion, after the adsorption is complete, dry, then add pure water, and send it to an emulsifier for emulsification, and then homogenize it through a high-pressure homogenizer, and the obtained homogeneous liquid is dried to obtain nano Grade doxorubicin hydrochloride granules. The nanoscale doxorubicin hydrochloride of the present invention has extremely high oral bioavailability and is suitable for oral administration.

Description

technical field [0001] The invention relates to an antitumor drug doxorubicin hydrochloride, in particular to a nanoscale doxorubicin hydrochloride and a preparation method thereof. Background technique [0002] Doxorubicin, also known as daunorubicin, oxybutamycin, and doxorubicin, is an anthracycline anti-malignant tumor antibiotic commonly used in clinic. It has broad anti-tumor spectrum, strong activity and good curative effect. Its mechanism of action is mainly Doxorubicin molecules intercalate into DNA, inhibiting nucleic acid synthesis. Doxorubicin can produce a wide range of biochemical effects on the body, so it is widely used in the treatment of acute leukemia, non-Hodgkin's lymphoma, breast cancer, lung cancer, gastric cancer, liver cancer, ovarian cancer and sarcoma and other malignant tumors. However, after intravenous injection of the drug, the side effects are severe. In addition to myelosuppression, gastrointestinal toxicity and hair loss, it can also cause ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K31/704A61K47/04A61P35/00
CPCA61K31/704A61K47/02A61K9/16A61K9/5115A61P35/00A61P35/04
Inventor 张旭旭张志安武超
Owner SHENZHEN GRADUATE SCHOOL TSINGHUA UNIV
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