Фармакокинетика препарата Мексидол®

Фармакокинетика препарата Мексидол®

1. Фармакокинетика Мексидола в эксперименте и клинике (Обзор литературных данных в.н.с., д.м.н., профессора Сариева А.К.), Москва, Научный Центр неврологии РАМН, 2010г.

За основу обзора литературных данных были взяты собственные научные результаты, полученные автором (профессором Сариевым А.К.), а также результаты его учеников, выполненные в течение 25 лет исследований. В обзоре несколько разделов, посвященным вопросам исследования фармакокинетики и биотрансформации Мексидола (различных лекарственных форм), проведенные на животных, здоровых добровольцах и пациентах.
1. Фармакокинетика Мексидола у крыс после его внутрибрюшинного введения. Изучение фармакокинетики мексидола было проведено на 70 белых беспородных крысах-самцах с массой 160-180 гр. Водный раствор Мексидола вводили животным внутрибрюшинно в дозе 150 мг/кг. Установлено, что Мексидол у крыс всасывается из брюшной полости довольно быстро с периодом полуабсорбции 0,94 часа и определяется на протяжении 24 часов. Изучена биотрансформация Мексидола и выявлены 5 предварительных метаболитов, представленных деалкилированными и в основном конъюгированными продуктами превращения. Метаболит II (2,6-диметил-3-оксипиридин), наряду с неизмененным веществом, также обладает высокой фармакологической активностью. Выявленные корреляции между динамикой содержания Мексидола в плазме и мозге крыс, его анксиолитическим действием, а также изменениями электрофизиологических показателей, указывают на важную роль фармакокинетических закономерностей Мексидола в проявлении его различных видов фармакологической активности.

Результаты (английский) 1:

Pharmacokinetics of the drug mexidol ®1. Pharmacokinetics Mexidola experiment and clinic (a review of the literature data, MD, leading Professor A.k. Sarieva) Moscow, academic center of Neurology, 2010.The basis for the review of the literature data were taken their own scientific results obtained by the author (Professor Sariev a.c.), as well as the results of his students made over 25 years of research. In a review of several sections on research pharmacokinetics and biotransformation of Mexidole (different dosage forms), carried out on animals, healthy volunteers and patients. 1. Pharmacokinetics in rats-Mexidola after his intraperitoneal injection. Study of pharmacokinetics of mexidol was held at 70 noninbred albino male rats weighing 160-180 Gr. Aqueous solution of Mexidol injected intraperitoneally to animals in a dose of 150 mg/kg. Found that rats Mexidol absorbed from the abdominal cavity rather quickly with a period of poluabsorbcii 0.94 hours and determined for 12:00 am. Biotransformation is studied and identified preliminary 5 Mexidola metabolites, dealkilirovannymi and presented in the main application kongugirovannami products. Metabolite II (2.6-dimethyl-3-oksipiridin), along with unchanged substance also has high pharmacological activity. Identified a correlation between dynamics of Mexidol content in plasma and brain of rats, his anxiolytic action, as well as changes of electrophysiological indices indicate the important role of the pharmacokinetic of Mexidol regularities of its various types of pharmacological activity.

Результаты (английский) 2:

Pharmacokinetics MEXIDOL® 1. Pharmacokinetics Mexidol experimental and clinical (literature review leading researcher, Ph.D., professor Sariev AK), Moscow, Scientific Center of Neurology, 2010. The basis of literature review were taken own scientific the results obtained by the author (Professor Sariev AK), and the results of his students made ​​during 25 years of research. In a review of several sections devoted to research on the pharmacokinetics and biotransformation Mexidol (different dosage forms), carried out on animals, healthy volunteers and patients. 1. Mexidol pharmacokinetics in rats after intraperitoneal administration. A study of the pharmacokinetics mexidol was conducted on 70 white mongrel male rats weighing 160-180 g. The aqueous solution Mexidol administered intraperitoneally in a dose of 150 mg / kg. It was found that rats Mexidol absorbed from the abdominal cavity rather quickly with a period of 0.94 hours and poluabsorbtsii determined over 24 hours. Biotransformation Mexidol studied and identified the five preliminary metabolites submitted dealkylated and mainly conjugated products of transformation. Metabolite II (2,6-dimethyl-3-hydroxypyridin), along with the unmodified substance also has high pharmacological activity. The correlation between the dynamics of content Mexidol in the plasma and brain of rats, its anxiolytic effects, as well as changes in the electrophysiological indicators point to an important role of pharmacokinetic Mexidol regularities in the manifestation of its various types of pharmacological activity.

Результаты (английский) 3:

Pharmacokinetics drug lord Мексидол® 1. Pharmacokinetics Мексидола to experiment, and clinic (review literary data in.h.in., d.m.h., professor of NTRK is biased as well.to. ), Moscow, the Science Center neurology MD, 2010

The literary review data were taken its own scientific results, obtained by the author (professor Сариевым as well.to. ), as well as the results of his pupils, performed during the 25 years of research.