Doxofylline compound and medicine composition thereof

A technology of doxofylline and compound, applied in the field of medicine, can solve the problems of reduced active ingredient content, insufficient quality stability, unfavorable clinical drug safety and the like

Inactive Publication Date: 2015-11-11
杭州科源医药技术有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] After research and analysis, it is found that the above-mentioned disclosed doxofylline raw materials and preparations have deficiencies in quality stability. During long-term storage, the content of active ingredients decreases significantly, and the dissolution rate significantly decreases, which is not conducive to ensuring the safety of clinical medication.

Method used

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  • Doxofylline compound and medicine composition thereof
  • Doxofylline compound and medicine composition thereof
  • Doxofylline compound and medicine composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] The preparation of embodiment 1 doxofylline compound

[0038] At 50-60° C. and a stirring speed of 100-150 rpm, theophylline and 2-bromo-1,3-dioxolane are added to the reactor in a weight ratio of 1:1.2. After adding sodium carbonate as a catalyst and dimethylformamide as a solvent, the temperature starts to rise, and the reaction temperature is kept at 110-115°C. After the reaction was finished, dimethylformamide was recovered by distillation under reduced pressure. Cool the reaction to 20-25°C, filter and rinse with pure water. To the filtered crude product of doxofylline, add about 1.5% of the weight of doxofylline with activated carbon and a small amount of toluene, stir at 150-200 rpm for 30 minutes, filter to remove carbon, and filter the filtrate through a 0.22 μm filter membrane. The toluene was then removed by drying at 95-100°C for 6 hours. The doxofylline is dried to a constant weight in a vacuum tray dryer at 95-100° C., namely the doxofylline dry powder....

Embodiment 2

[0039] The preparation of embodiment 2 doxofylline compound

[0040] At 50-60° C. and a stirring speed of 100-150 rpm, theophylline and 2-bromo-1,3-dioxolane are added to the reactor in a weight ratio of 1:1. After adding sodium carbonate as a catalyst and dimethylformamide as a solvent, the temperature starts to rise, and the reaction temperature is kept at 110-115°C. After the reaction was finished, dimethylformamide was recovered by distillation under reduced pressure. Cool the reaction to 20-25°C, filter and rinse with pure water. To the filtered crude product of doxofylline, add about 1.5% of the weight of doxofylline with activated carbon and a small amount of toluene, stir at 150-200 rpm for 30 minutes, filter to remove carbon, and filter the filtrate through a 0.22 μm filter membrane. The toluene was then removed by drying at 95-100°C for 6 hours. The doxofylline is dried to a constant weight in a vacuum tray dryer at 95-100° C., namely the doxofylline dry powder. ...

Embodiment 3

[0041] The preparation of embodiment 3 doxofylline injection

[0042] prescription:

[0043] Doxofylline Compound 10g

[0044] Water for injection 1L

[0045] Made of 100

[0046]Dissolve the prescribed amount of doxofylline compound with 80% of the total amount of water for injection at 50°C, adjust the pH to 5.8-6.4 with hydrochloric acid, add water for injection to the full amount, stir evenly, filter with a 0.22 μm filter membrane, and fill in an ampoule , filled with nitrogen, melt-sealed, and sterilized with damp heat at 121° C. for 30 minutes to obtain 10 g: 10 ml doxofylline injection.

[0047] The doxofylline injection prepared in Example 3 of this experiment and the commercially available doxofylline injection were investigated for long-term stability (25°C±2°C; 60%±5%RH), and the results are shown in Table 1.

[0048] Table 1 Long-term stability investigation table of doxofylline injection

[0049]

[0050] Conclusion: The quality indicators of doxofylline i...

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Abstract

The invention belongs to the technical field of medicines and in particular provides a doxofylline compound and a medicine composition thereof. Characteristic peaks of X-ray powder diffraction, measured by using a Gu-Kalpha ray, of the doxofylline compound are shown at 31.1 degrees, 32 degrees, 34.3 degrees, 37.5 degrees, 41.3 degrees, 43 degrees, 53.8 degrees, 56.5 degrees, 58 degrees and 62.5 degrees. The melting point of the doxofylline compound is 136-137 DEG C. The doxofylline compound has crystal purity higher than 99.9%. Doxofylline has good stability. Tablets and injections prepared by using the doxofylline medicine composition containing doxofylline have good stability and have total impurity rates lower than 0.5% after being placed for 36 months.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a doxofylline compound and a pharmaceutical composition containing doxofylline. Background technique [0002] Asthma is a common disease in my country, frequently-occurring, extremely harmful, and seriously threatens the health of the people. Some of them can become chronic diseases for life. In addition, wheezing is the main symptom of respiratory diseases. Patients suffer from physical and mental difficulties. Endure, there is an urgent need for safe and effective antiasthma drugs to relieve and eliminate symptoms. Doxofylline has a good market prospect as an inexpensive anti-asthma drug. [0003] Doxofylline, a derivative of methylxanthine, is a bronchodilator that acts directly on the bronchi to relax tracheal smooth muscle. Doxofylline relaxes smooth muscle by inhibiting phosphodiesterase in smooth muscle cells, thereby achieving the effect of inhibiting asthma...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D473/08A61K31/522
CPCC07D473/08A61K9/0019A61K9/08A61K9/2059C07B2200/13
Inventor 陈广平
Owner 杭州科源医药技术有限公司
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