Disposition of thiazinamium in humans after administration as an ion pair
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In order to investigate whether administration of an otherwise poorly absorbed drug as an ion pair would improve bioavailability, the disposition of the quaternary ammonium compound thiazinamium was studied in humans. For the ion pair, salicylate was selected as counter ion. The bioavailability was estimated by measuring the amount of unchanged drug excreted in urine during a period of 36 hours.
The results were compared with those obtained in the same subject after administration of the salt thiazinamium methylsulphate as reference substance. After oral administration absorption of the salicylate was found to be slightly better than that of the reference substance. These results suggest that administration of thiazinamium as ion pair would offer slight advantages over administration as a salt, but not to a degree that would be therapeutically significant.
KeywordsSalicylate Pharmaceutisch Weekblad Scientific Edition Methylsulphate Enteric Coated Capsule Hard Gelatine Capsule
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