The intravenous formulation of levetiracetam (LEV)has been available in clinical practice worldwide for several years,but not in China.In the present study,we aimed to evaluate the bioequivalence of intravenous and or...The intravenous formulation of levetiracetam (LEV)has been available in clinical practice worldwide for several years,but not in China.In the present study,we aimed to evaluate the bioequivalence of intravenous and oral LEV (tablet), an antiepileptic drug,in healthy Chinese volunteers.Two randomized,single-dose (1500mg),open-label,2-period crossover trials were conducted as follows:study A,15-min infusion;study B,45-min infusion.A total of 22healthy men participated in study A,and 24healthy men and woman were enrolled in study B.In study A,blood samples were collected after termination of each treatment.In study B,samples were collected after oral or after the start of the intravenous administration.Safety and the ratio of intravenous/oral LEV for AUC 0-t and Cmax were evaluated.The 90% confidence intervals of Cmax and AUC0-t ratios for LEV 1500-mg tablets versus 15-min intravenous administration were outside the bioequivalence limits (80.00%-125.00%). For LEV 45-min intravenous administration,bioequivalence versus 1500-mg tablets was within the range for Cmax and AUC 0-t. The most frequently adverse event (AE)was somnolence.A total of eight subjects experienced nine mild AEs in study A, and 19subjects experienced 29mild AEs in study B.Intravenous infusions (15 and 45 min)of 1500-mg LEV were as well tolerated as the oral tablet.Bioequivalence was demonstrated by 45-min infusions.Therefore,direct conversion from oral to intravenous LEV 1500 mg (45-min infusion),or vice versa,was possible.展开更多
文摘The intravenous formulation of levetiracetam (LEV)has been available in clinical practice worldwide for several years,but not in China.In the present study,we aimed to evaluate the bioequivalence of intravenous and oral LEV (tablet), an antiepileptic drug,in healthy Chinese volunteers.Two randomized,single-dose (1500mg),open-label,2-period crossover trials were conducted as follows:study A,15-min infusion;study B,45-min infusion.A total of 22healthy men participated in study A,and 24healthy men and woman were enrolled in study B.In study A,blood samples were collected after termination of each treatment.In study B,samples were collected after oral or after the start of the intravenous administration.Safety and the ratio of intravenous/oral LEV for AUC 0-t and Cmax were evaluated.The 90% confidence intervals of Cmax and AUC0-t ratios for LEV 1500-mg tablets versus 15-min intravenous administration were outside the bioequivalence limits (80.00%-125.00%). For LEV 45-min intravenous administration,bioequivalence versus 1500-mg tablets was within the range for Cmax and AUC 0-t. The most frequently adverse event (AE)was somnolence.A total of eight subjects experienced nine mild AEs in study A, and 19subjects experienced 29mild AEs in study B.Intravenous infusions (15 and 45 min)of 1500-mg LEV were as well tolerated as the oral tablet.Bioequivalence was demonstrated by 45-min infusions.Therefore,direct conversion from oral to intravenous LEV 1500 mg (45-min infusion),or vice versa,was possible.
