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High-solubility doxofylline compound

A technology of doxofylline and high solubility is applied in the field of medicines in the field of medicine, and can solve the problems that the amount of impurities cannot be effectively controlled, the method for purifying doxofylline compounds has not been studied and disclosed in detail, and there are many types of impurities, To achieve the effect of reducing market risk, the method is simple and easy, and the solubility is high

Active Publication Date: 2012-11-14
天津梅花生物医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0021] During the research process, repeating the method of the patent literature prepared above, the crude product of doxofylline obtained has many types of impurities, and the amount of impurities cannot be effectively controlled. The refining method of doxofylline compound has not been studied and disclosed in detail.

Method used

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  • High-solubility doxofylline compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] In a 5000ml reaction bottle equipped with stirring, thermometer and condenser, add 100g of doxofylline and 2000ml of water-acetone=1:5 mixture, start stirring, heat up to 55°C-60°C, and stir for 30 minutes , filter, the filtrate is cooled to 10°C-15°C under stirring, the speed is 260 rpm, add diethyl ether, then cool to 0°C-5°C, keep stirring for 10-12 hours, filter, and wash three times with 30ml of anhydrous ether , placed indoors for 1 hour, then moved to a vacuum drying oven, and vacuum-dried at room temperature for 3 hours to obtain 90.8 grams of doxofylline compound powder, and the moisture measured by the Karl Fischer method was 0.11%.

[0050] The X-ray diffraction pattern of the compound is shown in figure 1 . Instrument model and measurement conditions: Rigaku D / max2500 diffractometer; CuKa 40Kv 100mA; 2θ scanning range: 0-50°.

[0051] The infrared spectrum of the compound is shown in figure 2 , Determination with KBr tablet.

[0052] The HPLC chromatogr...

Embodiment 2

[0054] In a 5000ml reaction bottle equipped with stirring, thermometer and condenser, add 100g of doxofylline and 2000ml of water-acetone=1:3 mixture, start stirring, heat up to 55°C-60°C, and stir for 30 minutes , filter, cool the filtrate to 10°C-15°C, stir at 260 rpm, add diethyl ether, then cool to 0°C-5°C, keep stirring for 10-15 hours, filter, and wash with 30ml of anhydrous ether in three equal parts , placed indoors for 1 hour, then moved to a vacuum drying oven, and vacuum-dried at room temperature for 3 hours to obtain 91.5 grams of doxofylline compound powder, and the moisture measured by the Karl Fischer method was 0.15%.

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Abstract

The invention belongs to the technical field of medicines, and particularly relates to a doxofylline compound and a preparation method thereof. The space group of the doxofylline compound is Cc; and cell parameters are as follows: alpha is 90.00 degrees, gamma is 90.00 degrees, and z is 4. The doxofylline compound provided by the invention has high purity and good stability; even if in a high-humidity condition, the weight gain caused by moisture absorption is not obvious, and related substances do not grow; and compared with doxofylline in other crystalline states, the doxofylline compound is higher in solubility.

Description

technical field [0001] The invention relates to medicines in the field of medicine, in particular to a high-soluble doxofylline compound. Background technique [0002] With the global air pollution and environmental deterioration, the morbidity and mortality of asthma are increasing year by year. Experts predict that the anti-asthma drug market will be one of the ten most promising drug markets in the next 20 years. The incidence rate is relatively high in different regions, with Fujian being the highest at 3.03%, followed by Guangdong at 2.53%, and less in the north and inland areas. The incidence of asthma is higher in winter, followed by late autumn and early spring, and the lowest in summer. Bronchial asthma and chronic bronchitis, pulmonary Emphysema and other chronic obstructive pulmonary diseases (COPD) are the most common. Asthma factors are difficult to cure and expensive. Among respiratory diseases, chronic obstructive pulmonary diseases (COPD) such as bronchial as...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D473/08
Inventor 梅开忠黄欣
Owner 天津梅花生物医药科技有限公司
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