| Autor: |
Shabatina TI; Department of Chemistry, M.V. Lomonosov Moscow State University, Leninskie Gori Build 1/3, 119991 Moscow, Russia.; Department of Chemistry, Faculty of Fundamental Sciences, Bauman Moscow State Technical University, 2nd Bauman Str. 5, 105905 Moscow, Russia., Morosov YN; Department of Chemistry, M.V. Lomonosov Moscow State University, Leninskie Gori Build 1/3, 119991 Moscow, Russia.; Department of Chemistry, Faculty of Fundamental Sciences, Bauman Moscow State Technical University, 2nd Bauman Str. 5, 105905 Moscow, Russia., Soloviev AV; Department of Chemistry, M.V. Lomonosov Moscow State University, Leninskie Gori Build 1/3, 119991 Moscow, Russia., Shabatin AV; A.N. Frumkin Institute of Physical Chemistry and Electrochemistry RAS, Lenin Prospect, 31 Build 4, 119071 Moscow, Russia., Vernaya OI; Department of Chemistry, M.V. Lomonosov Moscow State University, Leninskie Gori Build 1/3, 119991 Moscow, Russia., Melnikov MY; Department of Chemistry, M.V. Lomonosov Moscow State University, Leninskie Gori Build 1/3, 119991 Moscow, Russia. |
| Abstrakt: |
Increasing the effectiveness of known, well-tested drugs is a promising low-cost alternative to the search for new drug molecular forms. Powerful approaches to solve this problem are (a) an active drug particle size reduction down to the nanoscale and (b) thermodynamically metastable but kinetically stable crystal modifications of drug acquisition. The combined cryochemical method has been used for size and structural modifications of the antibacterial drug 2,3-quinoxalinedimethanol-1,4-dioxide (dioxidine). The main stage of the proposed technique includes the formation of a molecular vapor of the drug substance, combined with a carrier gas (CO 2 ) flow, followed by a fast condensation of the drug substance and CO 2 molecules on a cooled-by-liquid nitrogen surface of preparative cryostate. It was established that the molecular chemical structure of the drug substance remained unchanged during cryochemical modification; however, it led to a significant decrease of the drug particles' size down to nanosizes and changes in the crystal structures of the solid drug nanoforms obtained. Varying carrier gas (CO 2 ) flow led to changes in their solid phase composition. A higher dissolution rate and changes in antibacterial activity were demonstrated for cryomodified dioxidine samples in comparison to the properties of the initial pharmacopeia dioxidine. |
