Import substitution: Scientists from AltSU are developing a pharmaceutical substance for the treatment of lung diseases

Levosalbutamol has a relaxing effect on the smooth muscles of the bronchi, improves airway patency, prevents or relieves spasm. Preparations based on it are also relevant for the rehabilitation of patients who have recovered from COVID-19, as they increase the vital capacity of the lungs, mucociliary clearance, stimulate mucus secretion, and activate the functions of the ciliated epithelium.

To date, there is no production of such a substance in Russia. The drug levosalbutamol was created in the 90s of the twentieth century by the Sunovion company (USA). It contains only the R-isomer of salbutamol. Clinical studies have shown that its bronchodilator efficacy is 4 times higher than that of the salbutamol produced in the form of a racemic mixture, and also fewer undesirable side effects are observed with its use.

Today, pharmaceutical manufacturers both in Russia and abroad buy a less effective substance in India in the form of a racemic mixture of two enantiomers, which is used to prepare an aerosol preparation, the effectiveness of which is significantly lower and has a number of side effects. In this regard, it is relevant to organize the production of levosalbutamol in the Russian Federation in order to meet the needs of our country and neighboring countries in a highly effective substance for the preparation of vital drugs in various dosage forms (aerosols, solutions for inhalation, etc.).

At present, a research group of scientists from the Department of Organic Chemistry of the Institute of Chemistry and Chemical-Pharmaceutical Technologies of Altai State University under the leadership of Doctor of Chemical Sciences, Professor, Head of the Department Natalia Bazarnova, together with AO "Altaivitaminy" and
NS Kurnakova Institute of General and Inorganic Chemistry RAS conducted research on the development of an aerosol preparation "salbutamol" using an optically pure substance in the form of the R-isomer of salbutamol.

The study was carried out within the framework of the grant “Creation of high-tech production of the vital anti-asthma drug salbutamol in aerosol form based on an enantiomerically pure, micronized substance obtained using supercritical fluid technologies.”

A method has been developed for the preparative separation of racemic salbutamol to obtain an optically pure R-isomer of salbutamol base using supercritical fluid chromatography. It is protected by a patent owned by AO “Altaivitamy”. On the basis of the enterprise, research was carried out to develop a technology for obtaining an optically pure substance.

Altai State University has a semi-preparative supercritical fluid chromatograph necessary for operation, and the equipment necessary for production - an industrial chromatograph - is available at AO “Altaivitaminy”.

In order to organize the production of the levosalbutamol substance in the form of an optically pure R-isomer, it is necessary to conduct some research and development work and organize a technological site that meets GMP (good manufacturing practice) standards. With this project, the university plans to get into the import substitution program.