Bioavailability of ACC-9653 (phenytoin prodrug)

Epilepsia. 1989:30 Suppl 2:S27-32. doi: 10.1111/j.1528-1157.1989.tb05822.x.

Abstract

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(0-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.

Publication types

  • Clinical Trial
  • Controlled Clinical Trial
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Biological Availability
  • Clinical Trials as Topic
  • Humans
  • Phenytoin / administration & dosage
  • Phenytoin / analogs & derivatives*
  • Phenytoin / metabolism
  • Prodrugs / administration & dosage
  • Prodrugs / metabolism*
  • Random Allocation

Substances

  • Prodrugs
  • Phenytoin
  • fosphenytoin