Bioavailability of phenytoin on single and multiple oral doses of two dosage forms in normal subjects. 1983

Y Kohda, and K Nishihara, and S Isozaki, and Y Saitoh, and F Nakagawa, and Z Tamura

The extent and rate of absorption of phenytoin (PHT) from tablet and powder were studied in four healthy adult volunteers. It was demonstrated by urinary and fecal excretion that the almost all quantity of PHT in tablet was absorbed through the gastrointestinal tract, and the observed values of the estimated free concentration (Cest.f) estimated from mixed saliva concentration of PHT in the multiple dose were in fair agreement with the calculated values of that by using computer simulation in case of tablet. On the contrary, the variations were observed in Cest.f using therapeutic dose of PHT powder. The values of Cest.f at steady-state in tablet administration were higher than those in powder administration. The absorption ratio of PHT powder was low and variable, and decreased upon increase of dose. The ratio calculated from the Cest.f values of both dosage forms at steady-state were in good correspondence to the observed values of PHT excreted in feces.

UI MeSH Term Description Entries
D007700 Kinetics The rate dynamics in chemical or physical systems.
D008297 Male Males
D008875 Middle Aged An adult aged 45 - 64 years. Middle Age
D010672 Phenytoin An anticonvulsant that is used to treat a wide variety of seizures. It is also an anti-arrhythmic and a muscle relaxant. The mechanism of therapeutic action is not clear, although several cellular actions have been described including effects on ion channels, active transport, and general membrane stabilization. The mechanism of its muscle relaxant effect appears to involve a reduction in the sensitivity of muscle spindles to stretch. Phenytoin has been proposed for several other therapeutic uses, but its use has been limited by its many adverse effects and interactions with other drugs. Diphenylhydantoin,Fenitoin,Phenhydan,5,5-Diphenylhydantoin,5,5-diphenylimidazolidine-2,4-dione,Antisacer,Difenin,Dihydan,Dilantin,Epamin,Epanutin,Hydantol,Phenytoin Sodium,Sodium Diphenylhydantoinate,Diphenylhydantoinate, Sodium
D005243 Feces Excrement from the INTESTINES, containing unabsorbed solids, waste products, secretions, and BACTERIA of the DIGESTIVE SYSTEM.
D005260 Female Females
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000328 Adult A person having attained full growth or maturity. Adults are of 19 through 44 years of age. For a person between 19 and 24 years of age, YOUNG ADULT is available. Adults
D001682 Biological Availability The extent to which the active ingredient of a drug dosage form becomes available at the site of drug action or in a biological medium believed to reflect accessibility to a site of action. Availability Equivalency,Bioavailability,Physiologic Availability,Availability, Biologic,Availability, Biological,Availability, Physiologic,Biologic Availability,Availabilities, Biologic,Availabilities, Biological,Availabilities, Physiologic,Availability Equivalencies,Bioavailabilities,Biologic Availabilities,Biological Availabilities,Equivalencies, Availability,Equivalency, Availability,Physiologic Availabilities
D012463 Saliva The clear, viscous fluid secreted by the SALIVARY GLANDS and mucous glands of the mouth. It contains MUCINS, water, organic salts, and ptylin. Salivas

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