Влияние дейтерия на свойства фармацевтических субстанций (обзор)

Введение. Обзор посвящен влиянию изотопа водорода – дейтерия на биологическую активность фармацевтических субстанций.

Текст. Рассмотрены два аспекта влияния дейтерия на свойства активных фармацевтических ингредиентов и вспомогательных веществ. Первый связан с использованием дейтерированных субстанций – новых соединений или полученных замещением протия в известных протиевых аналогах. Кинетический изотопный эффект (КИЭ), выражающийся в снижении скорости биотрансформации в результате дейтерирования, позволяет прогнозировать быстрое развитие нового направления в разработке лекарственных средств. При идентичном терапевтическом эффекте дейтерированные аналоги обеспечивают улучшение фармакокинетических характеристик, снижение токсичности, блокировку эпимеризации оптически активных субстанций, изменение механизмов биотрансформации. Второй аспект влияния дейтерия отражает возрастание КИЭ в процессах с участием известных фармацевтических субстанций в водных растворах с соотношением дейтерий/протий (D/H) ниже природного. Впервые на диаграмме «доза – ответ» показана идентичность дейтерия эссенциальным микроэлементам, когда недостаток и избыток элемента снижает жизнеспособность организма. Улучшенные кинетические характеристики продемонстрированы для молекулярного и организменного уровня разной иерархической градации. В частности, они заключаются в возможности увеличения скорости растворения субстанций, влияния на процессы мутаротации углеводов и оптическую активность хиральных субстанций, возрастание накопления эссенциальных элементов в лекарственных растениях и других процессах.

Заключение. Полученные результаты позволяют прогнозировать механизмы влияния дейтерия на биохимические превращения фармацевтических субстанций в организме.

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