Unlock instant, AI-driven research and patent intelligence for your innovation.

Acebrophylline, surfolase and composition thereof

A technology of composition and vinegar tea, which is applied in the direction of drug combinations, active ingredients of heterocyclic compounds, respiratory diseases, etc., and can solve problems such as poor stability, crystal water or crystal solvent, long crystallization time, etc.

Inactive Publication Date: 2009-12-23
TIANJIN HANKANG PHARMA BIOTECH
View PDF1 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] The above six crystal forms exist: long crystallization time (1-7 days, average 2 days); crystal water or crystallization solvent; poor stability and other defects

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Acebrophylline, surfolase and composition thereof
  • Acebrophylline, surfolase and composition thereof
  • Acebrophylline, surfolase and composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046]In a 2000ml reaction flask equipped with stirring, thermometer, and condenser, add 100g of bromoxol and 350ml of N.N-dimethylformamide (DMF), start stirring, heat up to 45±2°C, and completely dissolve. Adjust the stirring speed to 40-50 revolutions per minute, then add 35ml of acetone and 840ml of ethyl acetate, stir and lower the temperature to 15±2°C, and keep stirring for 1.2 hours. Crystals were precipitated, filtered, washed with 30 ml of ethyl acetate, placed in a solid chamber for 2 hours, then moved to a vacuum oven, and vacuum-dried (0.05-0.06 Mpa) for 6 hours to obtain 96 grams of crystalline powder.

[0047] The X-ray diffraction pattern of this crystalline powder is shown in figure 1 . Instrument model and measurement conditions: Rigaku D / max2500 diffractometer; CuKa 40Kv 100mA; 2θ scanning range: 0-50°;

[0048] The infrared spectrogram of this crystalline powder is shown in figure 2 , Determination with KBr tablet.

[0049] The high performance liquid ...

Embodiment 2

[0052] Granules containing broxolin crystal form of vinegar tea

[0053] Prescription: 100 grams of new crystal bromoxol, 600 grams of microcrystalline cellulose, 300 grams of lactose, 75 grams of crospovidone, 100 grams of PEG-6000, 105 grams of hydroxypropyl methylcellulose, appropriate amount of distilled water , made into 1000 bags.

[0054] Process: PEG-6000 and new crystal bromoxol are pulverized together, passed through 80 mesh sieve, mixed with other materials, made soft material with distilled water, granulated, dried at low temperature and then packed into granules.

Embodiment 3

[0056] Capsules containing broxolin crystalline form of vinegar tea

[0057] Prescription: 100 grams of new crystal form of bromoxol vinegar, 1.5 ml of propylene glycol, 70 grams of starch, made into 1000 capsules.

[0058] Process: wet the new crystal form of bromoxol and starch with 15% propylene glycol aqueous solution, mix well, sieve and granulate, dry at 60°C, granulate, and fill capsules.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention relates to a crystal form of acebrophylline, surfolase and a preparation method thereof. The invention also relates to a pharmaceutical composition containing the crystal form and the application of the new crystal form in the preparation of medicine which is used for relieving cough and eliminating phlegm as well as has double functions of bronchiectasis and mucolysis.

Description

technical field [0001] The invention relates to a pharmaceutical composition containing a new crystal form of acebrophylline (also known as surfolase, ambroxolacephyllinate), a preparation method of the new crystal form and the use of the new crystal form in the production of antitussive and anti-inflammatory agents with dual effects of bronchodilation and mucolysis. Use in expectorant drugs. Background technique [0002] Acebrophylline (acebrophylline, has another name called surfolase, ambroxol acephyllinate), CASNo.96989-76-3, is a kind of double salt formed by equimolar ambroxol (ambroxol) and acephylline (acephylline), therefore, has The pharmacological action and clinical curative effect of ambroxol and acetophylline are used to manufacture antitussive and expectorant drugs with dual effects of bronchodilator and mucolysis. The drug was first launched in Italy by Pharmacia (now Pfizer, Pfizer) under the trade name surfolase in 1992, and then successively launched in B...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): C07D473/08C07C215/44A61K31/522A61K31/137A61P11/08A61P11/12A61P11/10A61P11/14A61P11/06A61P11/00
Inventor 严洁刘建邦黄欣
Owner TIANJIN HANKANG PHARMA BIOTECH