arthyperАртериальная гипертензия"Arterial’naya Gipertenziya" ("Arterial Hypertension")1607-419X2411-8524Antihypertensive League10.18705/1607-419X-2016-22-3-309-315arthyper-437Research ArticleКЛИНИЧЕСКИЕ ИССЛЕДОВАНИЯCLINICAL TRIALSФармакокинетика фимасартана — нового представителя класса блокаторов АТ1‑рецепторов к ангиотензину II в российской популяцииPharmacokinetics of Fimasartan, a novel angiotensin II receptor type 1 antagonist in Russian populationКобалаваЖ. Д.KobalavaZh. D.

доктор медицинских наук, профессор, заведующая кафедрой пропедевтики внутренних болезней РУДН

MD, PhD, DSc, Professor, Head, Department of Propedeutics of Internal Diseases, PFUR

КотовскаяЮ. В.KotovskayaYu. V.

доктор медицинских наук, профессор кафедры пропедевтики внутренних болезней РУДН

MD, PhD, DSc, Professor, Professor, Department of Propedeutics of Internal Diseases, PFUR

ТолкачеваВ. В.TolkachevaV. V.

кандидат медицинских наук, консультант, кафедры пропедевтики внутренних болезней РУДН

MD, PhD, Consultant, Department of Propedeutics of Internal Diseases, PFUR

КорневаЕ. В.KornevaE. V.

кандидат медицинских наук, научный советник Научного отдела Медицинского департамента АО «Р‑Фарм»

MD, PhD, Scientific adviser, Medical Department, JSC “R‑Pharm”

ХозяиноваН. Ю.KhozyainovaN. Yu.

доктор медицинских наук, профессор, медицинский советник Научного отдела Медицинского департамента АО «Р‑Фарм»

MD, PhD, DSc, Professor, Medical Adviser, Clinical Development & Medical Affairs, Medical Department, JSC “R‑Pharm”

khozyainova@rpharm.ruСамсоновМ. Ю.SamsonovM. Yu.

кандидат медицинских наук, медицинский директор Научного отдела Медицинского департамента АО «Р‑Фарм»

MD, PhD, Chief Medical Officer, Medical Department, JSC “R‑Pharm”

КолодаД. Е.KolodaD. E.

руководитель Научного отдела Медицинского департамента АО «Р‑Фарм»

MD, Head of Clinical Development & Medical Affairs Medical Department, JSC “R‑Pharm”

КонрадиА. О.KonradiA. O.

доктор медицинских наук, профессор, заместитель генерального директора по научной работе ФГБУ «СЗФМИЦ им. В. А. Алмазова» Минздрава России

MD, PhD, DSc, Professor, The Deputy Director General of Science, V.A. Almazov Federal North-West Medical Research Centre

Федеральное государственное автономное образовательное учреждение высшего образования «Российский университет дружбы народов», Москва, РоссияРоссияPeoples’ Friendship University of Russia, Moscow, RussiaRussian FederationНаучный отдел Медицинского департамента АО «Р‑Фарм», Москва, РоссияРоссияJSC “R‑Pharm”, Moscow, RussiaRussian FederationНаучный отдел Медицинского департамента АО «Р‑Фарм», Москва, Россия Ленинский пр., д. 111 Б, Москва, Россия, 119421. Тел.: +7(495)956–79–37. Факс: +7(495)956–79–38РоссияJSC “R‑Pharm”, Moscow, Russia 111B, Leninsky avenue, Moscow, 119421 Russia. Phone: +7(495)956–79–37. Fax: +7(495)956–79–38Russian FederationФедеральное государственное бюджетное учреждение «Северо-Западный федеральный медицинский исследовательский центр имени В. А. Алмазова» Министерства здравоохранения Российской Федерации, Санкт-Петербург, РоссияРоссияV. A. Almazov Federal North-West Medical Research Centre, St Petersburg, RussiaRussian Federation201622082016223309315Copyright © Кобалава Ж.Д., Котовская Ю.В., Толкачева В.В., Корнева Е.В., Хозяинова Н.Ю., Самсонов М.Ю., Колода Д.Е., Конради А.О., 20162016Кобалава Ж.Д., Котовская Ю.В., Толкачева В.В., Корнева Е.В., Хозяинова Н.Ю., Самсонов М.Ю., Колода Д.Е., Конради А.О.Kobalava Z.D., Kotovskaya Y.V., Tolkacheva V.V., Korneva E.V., Khozyainova N.Y., Samsonov M.Y., Koloda D.E., Konradi A.O.Данная работа распространяется под лицензией Creative Commons Attribution 4.0.This work is licensed under a Creative Commons Attribution 4.0 License.https://htn.almazovcentre.ru/jour/article/view/437

Фимасартан — новый мощный блокатор АТ1‑рецепторов к ангиотензину II, изученный в широком спектре доклинических и клинических исследований в Республике Корея.

Цель исследования — оценить фармакокинетические (ФК) параметры фимасартана в российской популяции.

Материалы и методы

Материалы и методы. В открытое исследование фармакокинетики фимасартана после однократного приема в дозе 60 мг включены 15 пациентов с артериальной гипертензией (АГ) 1–2‑й степени. Концентрацию препарата определяли валидированным методом с использованием преципитации белка для экстракции образцов с последующей жидкостной хроматографией с тандемной масс-спектрометрией.

Результаты

Результаты. Фимасартан 60 мг быстро всасывался, максимальные концентрации в плазме наблюдались через 1,0 час, индивидуальный диапазон значений — от 0,50 до 4,00 часов. После достижения максимальной концентрации наблюдалось двухфазное снижение, при этом начало фазы элиминации — через 2,5–8,0 часов после приема препарата. Количественно определяемые концентрации фимасартана в плазме наблюдались до последней временной точки сбора образцов через 24 часа после приема препарата в диапазоне от 1,33 до 11,2 нг/мл. Значение конечного периода полувыведения — 5,8 часа, данные варьировали от 4,40 до 7,93 часа.

Заключение

Заключение. ФК параметры фимасартана у больных АГ в российской популяции соответствовали данным корейских пациентов с АГ и здоровых добровольцев.

Objective

Objective. Fimasartan, a novel potent angiotensin II receptor blocker, was evaluated in various preclinical and clinical studies in Korea. Considering that Korean population were studied in pivotal clinical trials, determination of Fimasartan pharmacokinetics in Russian patients was performed.

Design and methods

Design and methods. Open-label study on fimasartan pharmacokinetics after single use of fimasartan 60 mg included 15 patients with established arterial hypertension (HTN) 1–2 grade. Drug concentration was evaluated by protein precipitation for sample extraction followed by liquid chromatograph mass spectrometry.

Results

Results. Fimasartan 60 mg was quickly absorbed after oral uptake, and maximal product concentrations in plasma were observed after 1,0 hour (tmax median), individual range of tmax values was from 0,50 to 4,00 hours after product uptake. After Сmax was achieved fimasartan concentration biphasic reduction started, and elimination phase began 2,5–8 hours after medication uptake in all patients. Fimasartan plasma concentration was identifiable until last timepoint of sampling 24 hours after drug uptake in the range of 1,33 to 11,2 ng/ml. Apparent terminal half-life period (t1/2) was 5.8 hours, individual data was in the range of 4,40 to 7,93 hours.

Conclusions

Conclusions. Pharmacokinetics of fimasartan in HTN patients in Russian population correlates well to the data obtained in Korean patients with HTN as well as in healthy volunteers.

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