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Bioavailability of ACC‐9653 (Phenytoin Prodrug)
Author(s) -
Browne Thomas R.,
Davoudi Hamid,
Donn Karl H.,
Dougherty Carol L.,
Dukes George E.,
Evans Barbara,
Evans James E.,
Jamerson Brenda,
Kres Jan,
McEntegart Carol M.,
Messenheimer John A.,
Powell J Robert,
Quon Check Y.,
Szabo George K.
Publication year - 1989
Publication title -
epilepsia
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.687
H-Index - 191
eISSN - 1528-1167
pISSN - 0013-9580
DOI - 10.1111/j.1528-1157.1989.tb05822.x
Subject(s) - bioavailability , phenytoin , pharmacokinetics , pharmacology , crossover study , volunteer , chemistry , anticonvulsant , prodrug , medicine , epilepsy , alternative medicine , pathology , psychiatry , agronomy , biology , placebo
Summary: The bioavailability of phenytoin from ACC‐9653 versus intravenously administered sodium phenytoin was determined using a crossover design for intravenous and intramuscular administration of ACC‐9653 to healthy volunteers. Absolute bioavailability of phenytoin derived from ACC‐9653 in each subject was calculated as the ratio of the phenytoin area under the plasma concentration time curve for time 0 to infinity [AUC(0‐inf)] after ACC‐9653 divided by the phenytoin AUC(O‐inf) after intravenous sodium phenytoin. The mean absolute bioavailability of ACC‐9653 was 0.992 after intravenous administration and 1.012 after intramuscular administration. These data establish that the bioavailability of ACC‐9653 is complete following intravenous or intramuscular administration in single‐dose volunteer studies. The absolute bioavailability of phenytoin derived from ACC‐9653 in subjects with therapeutic plasma phenytoin concentrations is being studied in patients given simultaneous infusions of stable isotope‐labeled tracer doses of ACC‐0653 and sodium phenytoin.