medsovetМедицинский СоветMeditsinskiy sovet = Medical Council2079-701X2658-5790REMEDIUM GROUP Ltd.10.21518/ms2024-039medsovet-8231Research ArticleГАСТРОЭНТЕРОЛОГИЯGASTROENTEROLOGYКомпендиум рН-чувствительных полимеров в лекарственных препаратах, применяемых в гастроэнтерологии: фокус на кишечнорастворимые оболочкиCompendium of pH-sensitive polymers in gastroenterology drugs: focus on enteric coatingshttps://orcid.org/0000-0002-7163-7119СереброваС. Ю.SerebrovaS. Yu.

Сереброва Светлана Юрьевна, д.м.н., ведущий научный сотрудник научного отдела клинической фармакологии, Научный центр экспертизы средств медицинского применения; профессор кафедры клинической фармакологии и пропедевтики внутренних болезней, Первый Московский государственный медицинский университет имени И.М. Сеченова (Сеченовский Университет)

127051, Москва, Петровский бульвар, д. 8, стр. 2,

119991, Москва, ул. Трубецкая, д. 8, стр. 2

Svetlana Yu. Serebrova, Dr. Sci. (Med.), Leading Researcher of the Scientific Department of Clinical Pharmacology, Scientific Centre for Expert Evaluation of Medicinal Products; Professor of the Department of Clinical Pharmacol ogy and Propaedeutics of Internal Diseases, Sechenov First Moscow State Medical University (Sechenov University)

8, Bldg. 2, Petrovsky Boulevard, Moscow, 127051,

8, Bldg. 2, Trubetskaya St., Moscow, 119991

svetaserebrova@mail.ruhttps://orcid.org/0000-0002-6150-5796ЕвтеевВ. А.EvteevV. A.

Евтеев Владимир Александрович, старший аналитик научного отдела клинической фармакологии

127051, Москва, Петровский бульвар, д. 8, стр. 2

Vladimir A. Evteev, Senior Analyst of the Scientific Department of Clinical Pharmacology

8, Bldg. 2, Petrovsky Boulevard, Moscow, 127051

evteev@expmed.ruhttps://orcid.org/0000-0003-1972-4386ДемченковаЕ. Ю.DemchenkovaE. Yu.

Демченкова Елена Юрьевна, к.фарм.н., ведущий аналитик научного отдела клинической фармакологии, Научный центр экспертизы средств медицинского применения; ассистент кафедры клинической фармакологии и пропедевтики внутренних болезней, Первый Московский государственный медицинский университет имени И.М. Сеченова (Сеченовский Университет)

127051, Москва, Петровский бульвар, д. 8, стр. 2,

119991, Москва, ул. Трубецкая, д. 8, стр. 2

Elena Yu. Demchenkova, Cand. Sci. (Рharm.), Leading Analyst of the Scientific Department of Clinical Pharmacology, Scientific Centre for Expert Evaluation of Medicinal Products; Assistant of the Department of Clinical Pharmacology and Propaedeutics of Internal Diseases, Sechenov First Moscow State Medical University (Sechenov University)

8, Bldg. 2, Petrovsky Boulevard, Moscow, 127051,

8, Bldg. 2, Trubetskaya St., Moscow, 119991

demchenkova@expmed.ruhttps://orcid.org/0000-0001-7024-5546ПрокофьевА. Б.ProkofievA. B.

Прокофьев Алексей Борисович, д.м.н., начальник научного отдела клинической фармакологии, Научный центр экспертизы средств медицинского применения; профессор кафедры клинической фармакологии и пропедевтики внутренних болезней, Первый Московский государственный медицинский университет имени И.М. Сеченова (Сеченовский Университет)

127051, Москва, Петровский бульвар, д. 8, стр. 2,

119991, Москва, ул. Трубецкая, д. 8, стр. 2

Alexey B. Prokofiev, Dr. Sci. (Med.), Head of the Scientific Department of Clinical Pharmacology, Scientific Centre for Expert Evaluation of Medicinal Products; Professor of the Department of Clinical Pharmacology and Propaedeutics of Internal Diseases, Sechenov First Moscow State Medical University (Sechenov University)

8, Bldg. 2, Petrovsky Boulevard, Moscow, 127051,

8, Bldg. 2, Trubetskaya St., Moscow, 119991

prokofiev@expmed.ruНаучный центр экспертизы средств медицинского применения; Первый Московский государственный медицинский университет имени И.М. Сеченова (Сеченовский Университет)РоссияScientific Centre for Expert Evaluation of Medicinal Products; Sechenov First Moscow State Medical University (Sechenov University)Russian FederationНаучный центр экспертизы средств медицинского примененияРоссияScientific Centre for Expert Evaluation of Medicinal ProductsRussian FederationНаучный центр экспертизы средств медицинского применения; Первый Московский государственный медицинский университет имени И.М. Сеченова (Сеченовский Университет)РоссияScientific Centre for Expert Evaluation of Medicinal Products; Sechenov First Moscow State Medical University (Sechenov University)Russian Federation20241005202405134142Copyright © Сереброва С.Ю., Евтеев В.А., Демченкова Е.Ю., Прокофьев А.Б., 20242024Сереброва С.Ю., Евтеев В.А., Демченкова Е.Ю., Прокофьев А.Б.Serebrova S.Y., Evteev V.A., Demchenkova E.Y., Prokofiev A.B.Данная работа распространяется под лицензией Creative Commons Attribution 4.0.This work is licensed under a Creative Commons Attribution 4.0 License.https://www.med-sovet.pro/jour/article/view/8231

В компендиуме для врачей-гастроэнтерологов и гепатологов представлена информация о рН-чувствительных полимерах, используемых в лекарственных формах для перорального введения и доставки лекарственных средств к тем или иным участкам ЖКТ. Дополнительно приведены сведения о рН-нечувствительных полимерах в составе слабительных, гепатологических противовирусных препаратов и препаратов для введения в прямую кишку. Приведены справочные сведения о химической, пространственной структуре и свойствах рН-чувствительных и отдельных рН-нечувствительных полимеров, физиологическое обоснование их преобразований при определенных характеристиках среды в просвете ЖКТ, т. е. об аспектах их использования в системах таргетной доставки лекарственных препаратов, применения в качестве действующих веществ или «увеличителей» молекулярной массы иных действующих веществ. Основное внимание уделено высокомолекулярным соединениям, используемым в производстве кишечнорастворимых оболочек для таблеток и гранул (пеллет). Материал проиллюстрирован примерами зарегистрированных в Российской Федерации и перспективных препаратов с лекарственными формами для диффузного нанесения антибиотиков на слизистую оболочку желудка, для таргетной доставки лекарственных препаратов в 12-перстную кишку, другие отделы тонкой и толстой кишок. Описаны гидрогели на основе хитозана, липосомальная форма доксициклина, кишечнорастворимые лекарственные формы с рН-чувствительными полимерами, более сложные системы доставки с двумя триггерами высвобождения препарата, лекарственные формы с термочувствительными полимерами. Таким образом, полимеры, являющиеся непреложной составляющей окружающей среды, условий быта современного человека, все больше входят в фармакотерапевтическую область в качестве действующих веществ или компонентов, увеличивающих интенсивность локального фармакодинамического эффекта, биодоступность или замедляющих выведение лекарственных средств. Знание химических, структурных особенностей высокомолекулярных соединений, их изменений в определенных средовых условиях необходимо для принятия правильных решений в областях медицины, где используются лекарственные препараты с разными по свойствам полимерами, в частности, в гастроэнтерологии и гепатологии.

This compendium for gastroenterologists and hepatologists contains information about pH-sensitive polymers used in dosage forms for oral administration and delivery of drugs to certain parts of the gastrointestinal tract. There is more information here on pH-insensitive polymers in laxatives, hepatology antivirals and rectal agents. There is also background information on the chemical, spatial structure and properties of pH-sensitive and individual pH-insensitive polymers, the physiological basis for their transformations under certain characteristics of the environment in the lumen of the gastrointestinal tract. These are aspects of their use in targeted drug delivery systems, use as active ingredients or “increasers” of the molecular weight of other active ingredients. The main attention is paid to polymers used in the production of enteric coatings for tablets and granules (pellets). The material is illustrated with examples of drugs registered in the Russian Federation and promising drugs with dosage forms for diffuse application of antibiotics to the gastric mucosa, for targeted delivery of drugs to the duodenum and other parts of the small and large intestines. Chitosan-based hydrogels, a liposomal form of doxycycline, enteric dosage forms with pH-sensitive polymers, more complex delivery systems with two drug release triggers, and dosage forms with thermosensitive polymers have been described. Thus, polymers, which are an essential component of the environment and living conditions of modern humans, entered the pharmacotherapeutic field as active substances or components that increase the the local pharmacodynamic effect, bioavailability or slow down the excretion of drugs. Knowledge of the chemical and structural features of high-molecular compounds, their changes in certain environmental conditions is necessary for making the right decisions in those areas of medicine where drugs with polymers of different properties are used, in particular, in gastroenterology, proctology and hepatology.

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The authors declare that there are no conflicts of interest present.