Bioavailability and Anticonvulsant Activity of a Monoglyceride-derived Prodrug of Phenytoin After Oral-administration To Rats
(1995) Journal of Pharmaceutical Sciences — Vol. 84, n° 3, p. 300-302 (1995)
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- Abstract
- The plasma levels of phenytoin after oral administration of phenytoin and phenytoin 2-monoglyceride, a phenytoin prodrug, to rats were determined by gas chromatography. Compared to the application of the parent drug, administration of the prodrug resulted in a 3-fold increase of C-max and a 4-fold increase of the AUC. This correlated with an earlier onset and peaking of the anticonvulsant activity determined in the maximal electroshock (MES) test. The peak effect was reached 1 h after dosing the monoglyceride compared to 2 h after application of phenytoin itself. On the basis of the median effective dose, the prodrug was 3 times more effective antagonizing MES-induced seizures than the parent drug. It is concluded that phenytoin 2-monoglyceride might be a useful prodrug for the oral delivery of phenytoin.
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Scriba, GKE., Lambert, DM., & Poupaert, J. (1995). Bioavailability and Anticonvulsant Activity of a Monoglyceride-derived Prodrug of Phenytoin After Oral-administration To Rats. Journal of Pharmaceutical Sciences, 84(3), 300-302. https://doi.org/10.1002/jps.2600840307 (Original work published 1995)