Despite the rapid development of medical technologies, chemotherapy treatment still\noccupies an important place in clinical oncology. In this regard, the current research in this area\nfocuses on the synthesis of new highly effective antitumor substances that have minimal side effects\nand the development of stable pharmaceutical formulations (PF) on their basis. In order to solve this\nproblem, the I. Ya. Postovsky Institute of Organic Synthesis of the Ural Branch of the Russian Academy\nof Sciences actively sought for original substances, namely, nitrosourea (NU) derivatives, one of the\nmost promising classes of anticancer drugs. As a result of this research, a novel NU derivative was\nsynthesized, namely ormustine, which showed high antitumor activity in preliminary preclinical\ntrials. It is now crucial to develop an ormustine pharmaceutical formulation. Conducted technological\nstudies showed that the most suitable solvent for the drug substance is 0.1Mhydrochloric acid, which\nensures its rapid dissolution by ultrasonic treatment. A significant reduction in the concentration\nof the active ingredient during the storage of the solution required the development of a technique\nof its lyophilization and the selection of a shaper such as a Kollidon 17 PF. Upon completion of the\ndevelopment of a pharmaceutical formulation of ormustine, its stability after lyophilization was\ndemonstrated, and a sufficient amount of the drug has been acquired for preclinical research.
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