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Doxofylline compound and medicine composition thereof

A technology of doxofylline and compounds, applied in the field of doxofylline compounds and pharmaceutical compositions thereof, can solve the problems of complexity, limited clinical use of doxofylline, poor water solubility and stability of doxofylline, etc. Effects of improved stability, improved safety and efficacy, and simple formulation process

Active Publication Date: 2013-06-19
湖北美林药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Commonly used dosage forms of doxofylline in clinical practice include: injection, powder injection, tablet, capsule, etc. Due to the poor water solubility and stability of doxofylline, the existing technology is difficult to solve or needs to add a lot of excipients And relatively strict process, these means are relatively complicated, which limits the clinical use of doxofylline

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

[0053] Embodiment 1 Preparation of doxofylline compound

[0054] Dissolve the crude product of doxofylline in a mixed solution of chloroform and methanol (volume ratio 6:1) at a weight ratio of 1:10 at 55°C at a stirring speed of 100 rpm; keep at 55°C and add doxofylline Activated carbon with an alkali weight of 1.5%, stirred at 150 rpm for 30 minutes, filtered to remove carbon, and filtered the filtrate through a 0.22 μm filter membrane; adjusted to 25°C, at a stirring speed of 150 rpm, slowly and uniformly while stirring ( 50mL / min) dropwise add a mixed solution of diethyl ether and petroleum ether with a volume ratio of 5:1 that is 8 times the weight of the mixed solution of chloroform and methanol; at the same time, cool down to 5°C at a constant speed (2.5°C / min), stop stirring, and (0.1°C / min) cool down to 1°C and let the crystal grow for 12 hours, filter; wash the filter cake obtained by filtering with 3 times the weight of a mixed solution of diethyl ether and petroleu...

Embodiment 2

[0056] Embodiment 2 Preparation of doxofylline compound

[0057] Dissolve the crude product of doxofylline in a mixed solution of chloroform and methanol (volume ratio 6:1) at a weight ratio of 1:12 at 60°C at a stirring speed of 100 rpm; keep at 60°C and add doxofylline Activated carbon with 1.5% alkali weight, stirred at 200 rpm for 30 minutes, filtered to remove charcoal, and filtered the filtrate through a 0.22 μm filter membrane; 60mL / min) dropwise add a mixed solution of diethyl ether and petroleum ether with a volume ratio of 5:1 that is 10 times the weight of the mixed solution of chloroform and methanol; at the same time, cool down to 10°C at a constant speed (2.5°C / min), stop stirring, and (0.1°C / min) cool down to 2°C and let the crystal grow for 12 hours, filter; wash the filter cake obtained by filtering with 3 times the weight of a mixed solution of diethyl ether and petroleum ether with a volume ratio of 5:1, and dry. That is, the doxofylline compound is obtaine...

Embodiment 3

[0059] Example 3 Preparation of Doxofylline Freeze-Dried Powder for Injection (Specification: 0.1g)

[0060] prescription:

[0061] Doxofylline Compound 100g

[0062] Mannitol 60g

[0063] Water for injection 2000mL

[0064] Make 1000 pieces

[0065] Process:

[0066] 1. Add the prescribed amount of doxofylline compound to 70% of the dosage of water for injection, adjust the pH to 5.00 with hydrochloric acid, stir and dissolve at 55°C, add water for injection to 80%, then add mannitol according to the prescribed amount and stir to dissolve, add Add water for injection to the full amount and stir evenly.

[0067] 2. Add 0.15% activated carbon to 1, stir for 20 minutes, decarbonize by filtration, and sterilize by filtration with a 0.22 μm filter membrane to detect intermediates.

[0068] 3. Freeze-drying:

[0069] ① Pre-freezing: put the filtrate in 2 into a half-packed and stoppered container and place it in a pre-cooled freezer at -30°C, keep it for 2 hours, then cool i...

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Abstract

The invention relates to a doxofylline crystal compound. Determined by adopting X-ray powder diffraction, the doxofylline crystal compound has he characteristic peak at 2theta+ / -0.2 degrees of 11.8 degrees, 13.3 degrees, 16.8 degrees, 19.2 degrees, 20.8 degrees, 23.3 degrees, 26.3 degrees, 26.7 degrees, 28.2 degrees, 29.9 degrees, 31.3 degrees, 32.7 degrees, 36.8 degrees and 41.1 degrees. The invention also relates to a preparation and a medicine composition preparation containing the doxofylline compound, wherein the medicine composition preparation is freeze-dried powder, injection, tablets and capsules. The doxofylline freeze-dried powder, injection, tablets and capsules which are provided by the invention are simple in formulation and technology, have obviously improved stability and improve the safety and effectiveness of medicine using.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a doxofylline compound and a pharmaceutical composition thereof. Background technique [0002] Doxofylline, its chemical name is: 1,3-Dimethyl-7-(1,3-dioxol-2-yl)methyl-3,7-dihydro-1H-purine-2 ,6-diketone. Doxofylline, a derivative of methylxanthine, is a bronchodilator that acts directly on the bronchi to relax bronchial smooth muscle. By inhibiting the action of phosphodiesterase in smooth muscle cells, it relaxes smooth muscle, thereby achieving the effect of inhibiting asthma. [0003] Clinically used for bronchial asthma, asthmatic chronic bronchitis and other dyspnea caused by bronchospasm. [0004] Commonly used dosage forms of doxofylline in clinical practice include: injection, powder injection, tablet, capsule, etc. Due to the poor water solubility and stability of doxofylline, the existing technology is difficult to solve or needs to add a lot of excipients And stri...

Claims

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Application Information

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IPC IPC(8): C07D473/08A61K31/522A61P11/06A61P11/00A61P29/00
Inventor 李美林胡成忠
Owner 湖北美林药业有限公司
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