Novel preparation techniques for cardiac glycosides

For example, to prepare the highly active cardiovascular medication digoxin effective methods have to be developed to extract medicinal substances – glycosides. Such a problem is solved successfully by scientists from the State Research Institute of Organic Chemistry and Technology under the direction of the Project Manager Galina Mikhailovna Komissarova. The International Science and Technology Centre supports the scientific research.

During a 200-year history of the application of cardiac glycosides in medical practice views on the mechanism of their action and the methods of obtaining the medications of the series of cardiotonic glycosides have changed considerably. But one thing remains unchanged – the application of cardiac glycosides at the initial or latent stage of heart failure can correct available functional cardiac abnormalities and prevent the development of obvious heart failure.

A number of patented methods of preparing digoxin from Digitalis lanata with the use of natural enzymes are presently available. However, these patented methods have a number of major shortcomings. “The most essential among them, – says Galina Mikhailovna Komissarova, – is low stability of the fermentation process owing to the quality of herbal raw materials”. Secondly, toxic and explosive solvents, which are costly materials, are used in these methods. Besides, a great number of technological purification stages have to be performed to obtain the final medication; this is a very laborious process.

During project realization the developers from the State Scientific Centre “State Research Institute of Organic Chemistry and Technology” succeeded in avoiding all of the above shortcomings, owing to totally new techniques of growing, picking, drying and storing Digitalis lanata. The obtained plant raw materials are characterized by a stably high content of highly active enzymes. The technique of preparing digoxin by means of enzymatic degradation in aqueous media at 45oC was elaborated, with the process proceeding completely without hindrance to the subsequent extraction and cleaning stages.

The advantages of the proposed method are controlled standard conditions in aqueous media during the formation of digoxin and the modification of conventional stages of digoxin extraction.

The novelty and uniqueness of the proposed Project is that it proposes a method for controlling the activity of enzymes in the raw material; it is designed to facilitate the production of a protein concentrate with certain enzymatic activity, and examination of activity standards required for effectively performing the raw material fermentation stage in the production of digoxin. Using novel techniques, the developers have managed to obtain a test sample – 50 grams of digoxin. In future it is planned to modernize the extraction and purification methods of cardiotonic glycosides and methods of analytical production control that will help to provide medical organizations with the necessary quantity of this medication and it will give people the chance to recover from this serious illness.

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