Bioavailability and Pharmacokinetic Parameters of Teraligen® Retard and Teraligen® Valenta Tablets After a Single Administration to Healthy Volunteers
Rejkhart D. V., Arnautov V. S., Globenko A. A., Kapashin A. V., Belostotskij A. V., Vasil’ev D. K.
Pharmaceutical Chemistry Journal
Vol.51, Issue8, P. 690-694
Опубликовано: 2017
Тип ресурса: Статья
DOI:10.1007/s11094-017-1675-3
Аннотация:
The bioavailability and pharmacokinetic parameters of film-coated Teraligen Retard (TR 20, 40, and 60 mg at doses of 20, 40, and 60 mg, respectively) and immediate-release film-coated Teraligen Valenta tablets (TV 5 mg at a dose of 20 mg) were compared using double blind randomized placebo-controlled investigations involving a single administration to healthy volunteers. The relative bioavailability (ratio of geometric mean 90[%] CI values) of TR 20, 40, and 60 mg tablets amounted to 80.95[%] (62.65 – 104.74[%]), 214.33[%] (165.64 – 277.34[%]), and 394.77[%] (305.08 – 510.83[%]) for 20, 40, and 60 mg tablets, respectively. An analysis of the dose–concentration relationship gave a linearity coefficient of 0.1902 ng/(mL·mg) for Cmax index and 4.6087 (h·ng)/(mL·mg) for AUC0-t. The results showed that the pharmacokinetic parameters could be considered linearly dose-dependent in the studied range (20 – 60 mg). The delay of drug release from film-coated TR 20, 40 and 60 mg tablets was evaluated by compari
Ключевые слова:
AUC; bioavailability; Cmax; clinical investigation; pharmacokinetics; stage I; T1/2; Teraligen Retard; Teraligen Valenta
alimemazine; teraligen; adult; area under the curve; Article; blood-to-plasma ratio; body height; body mass; controlled study; drug bioavailability; drug clearance; drug half life; drug labeling; drug packaging; drug release; drug specificity; elimination half-life; female; high performance liquid chromatography; human; limit of quantitation; male; maximum concentration; maximum plasma concentration; mean residence time; multiple reaction monitoring; normal human; pharmacokinetic parameters; retention time; signal noise ratio; single drug dose; tablet; time to maximum plasma concentration; ultra performance liquid chromatography
Язык текста: Английский
ISSN: 1573-9031
Rejkhart D. V. Dmitrij Vladimirovich 1971-
Arnautov V. S.
Globenko A. A.
Kapashin A. V.
Belostotskij A. V. Andrej Viktorovich 1967-
Vasil’ev D. K.
Рейхарт Д. В. Дмитрий Владимирович 1971-
Арнаутов В. С.
Глобенко А. А.
Капашин А. В.
Белостоцкий А. В. Андрей Викторович 1967-
Васил’ев Д. К.
Bioavailability and Pharmacokinetic Parameters of Teraligen® Retard and Teraligen® Valenta Tablets After a Single Administration to Healthy Volunteers
Текст визуальный непосредственный
Pharmaceutical Chemistry Journal
Springer New York Consultants Bureau
Vol.51, Issue8 P. 690-694
2017
Статья
AUC bioavailability Cmax clinical investigation pharmacokinetics stage I T1/2 Teraligen Retard Teraligen Valenta
alimemazine teraligen adult area under the curve Article blood-to-plasma ratio body height body mass controlled study drug bioavailability drug clearance drug half life drug labeling drug packaging drug release drug specificity elimination half-life female high performance liquid chromatography human limit of quantitation male maximum concentration maximum plasma concentration mean residence time multiple reaction monitoring normal human pharmacokinetic parameters retention time signal noise ratio single drug dose tablet time to maximum plasma concentration ultra performance liquid chromatography
The bioavailability and pharmacokinetic parameters of film-coated Teraligen Retard (TR 20, 40, and 60 mg at doses of 20, 40, and 60 mg, respectively) and immediate-release film-coated Teraligen Valenta tablets (TV 5 mg at a dose of 20 mg) were compared using double blind randomized placebo-controlled investigations involving a single administration to healthy volunteers. The relative bioavailability (ratio of geometric mean 90[%] CI values) of TR 20, 40, and 60 mg tablets amounted to 80.95[%] (62.65 – 104.74[%]), 214.33[%] (165.64 – 277.34[%]), and 394.77[%] (305.08 – 510.83[%]) for 20, 40, and 60 mg tablets, respectively. An analysis of the dose–concentration relationship gave a linearity coefficient of 0.1902 ng/(mL·mg) for Cmax index and 4.6087 (h·ng)/(mL·mg) for AUC0-t. The results showed that the pharmacokinetic parameters could be considered linearly dose-dependent in the studied range (20 – 60 mg). The delay of drug release from film-coated TR 20, 40 and 60 mg tablets was evaluated by compari