Freezing-dried composite contg. dexrazoxane and its prepn. method

A technology of dexrazoxane and composition, which is applied in the field of freeze-dried composition containing dexrazoxane and its preparation, and can solve the problems of instability to light, affecting solubility, non-degradation, etc.

Inactive Publication Date: 2004-10-20
SHANGHAI INST OF PHARMA IND CO LTD +1
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0011] The color of the product disclosed by the patent US Patent4963551 (1990) is light red, and when the moisture was greater than 2%, the freeze-dried product would form crystals and affect its solubility; though the product provided by the patent WO93 / 07873 was white, the freeze-drying time was shorter Long, the moisture must be below 2% to ensure that the drug does not degrade
Both patents believe that dexrazoxane is unstable to light, but it is found in the test that its aqueous solution, even in a dark room, also increases with time, related substances (i.e. oxidizing substances), and the aqueous solution of the drug changes from no to light in half an hour. The color changes from pink to yellowish at about the same rate as under normal indoor light

Method used

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  • Freezing-dried composite contg. dexrazoxane and its prepn. method

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Effect test

Embodiment 1

[0026] Formula: dexrazoxane 20mg / ml, sodium metabisulfite 1mg / ml, hydrochloric acid 0.1mol / ml.

[0027] Preparation method: first prepare 1000ml of 0.1mol / l hydrochloric acid, inject nitrogen gas into the above-mentioned hydrochloric acid solution, add the prescribed amount of antioxidant, add the main drug dexrazoxane, and divide into 30ml / 15ml freeze-dried bottles, each bottle 25ml / 12.5ml, the liquid level of the lyophilized liquid is about 25mm, and it is cooled to -45°C in a lyophilizer to lyophilize.

[0028] Raise the temperature to -25°C at a heating rate of 15°C / hr, the water will sublimate, and the sublimation time is 18 hours; then, under the condition of 10°C, continue to sublimate the water to dry the remaining water, and the sublimation drying time is 20 hours, freeze-drying curve such as figure 1 , to obtain dexrazoxane for injection described in this patent. The moisture content of the freeze-dried product is 1.89%, and the color is white.

Embodiment 2

[0030] Formula: dexrazoxane 30mg / ml, sodium bisulfite 10mg / ml, hydrochloric acid 0.15mol / ml.

[0031] Preparation method: first prepare 1000ml of 0.5mol / l hydrochloric acid, inject nitrogen gas into the above hydrochloric acid solution, add the prescribed amount of antioxidant, add the main drug dexrazoxane, divide into 30ml freeze-dried bottles, 25ml per bottle, and freeze-dry The height of the liquid level is about 25mm, and it is cooled to -54°C in a lyophilizer for lyophilization.

[0032] Raise the temperature to -15°C at a heating rate of 2°C / hr, the water will sublimate, and the sublimation time is 25 hours; then, under the condition of 15°C, the water will continue to sublimate to dry the remaining water, and the sublimation drying stage time For 20 hours, the dexrazoxane for injection described in this patent can be obtained. The moisture content of the freeze-dried product is 2.8%, and the color is white.

Embodiment 3

[0034]Using the same method and formula as in Example 1, substituting L-ascorbic acid for sodium metabisulfite, the dexrazoxane for injection described in this patent was obtained. The moisture content of the freeze-dried product is 2.1%, and the color is white.

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Abstract

A freeze dried composition containing dexrazoxane is disclosed. Its preparing process is also disclosed, which features use of antioxidizing agent to make its product have high antioxidizing stability.

Description

technical field [0001] The invention relates to a freeze-dried composition containing dexrazoxane and a preparation method thereof. Background technique [0002] Malignant tumor is one of the common chronic diseases in clinical practice. In China, its incidence rate ranks first among all diseases; in developed countries such as Europe and America, its incidence rate is second only to cardiovascular diseases, accounting for the second place in the total incidence rate. Anthracyclines such as doxorubicin are broad-spectrum anti-tumor antibiotics widely used clinically. Since their listing in the 1970s, sales have been at the forefront of anti-tumor drugs and have continued to increase. They have become a class of tumor chemicals. mainstay of treatment. However, the dose-limiting toxicity of doxorubicin-congestive heart failure limits the use of doxorubicin in patients, leading to interruption of chemotherapy or death due to toxicity. How to reduce the cardiotoxicity of doxor...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K31/496A61K47/02A61K47/06A61P35/00
Inventor 金方肖旭华杨珲珲
Owner SHANGHAI INST OF PHARMA IND CO LTD
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