The effect of food on the bioavailability and kinetics of the anticancer drug amsacrine and a new analogue, N‐5‐dimethyl‐9‐[(2‐methoxy‐4‐methylsulphonylamino)phenylamino]‐4 acridinecarboxamide in rabbits
Identifieur interne : 003414 ( Main/Exploration ); précédent : 003413; suivant : 003415The effect of food on the bioavailability and kinetics of the anticancer drug amsacrine and a new analogue, N‐5‐dimethyl‐9‐[(2‐methoxy‐4‐methylsulphonylamino)phenylamino]‐4 acridinecarboxamide in rabbits
Auteurs : James W. Paxton [Nouvelle-Zélande]Source :
- Journal of Pharmacy and Pharmacology [ 0022-3573 ] ; 1986-11.
Abstract
Both amsacrine and its analogue, N‐5‐dimethyl‐9‐[(2‐methoxy‐4‐methylsulphonylamino)phenylamino]‐4‐acridinecarboxamide (CI‐921) are absorbed from the gastrointestinal tract in rabbits. The mean bioavailability for amsacrine was 50% ± 17 (s.d.) in non‐fasting animals, and was significantly increased in fasting animals (mean, 90% ± 10). The bioavailability for CI‐921 (mean, 26% ± 11) in the non‐fasting animal was significantly less than that found for amsacrine, but this difference disappeared in the fasting animal when the bioavailability of CI‐921 was significantly increased to 69% ± 23. Oral administration of both agents resulted in significantly prolonged elimination half‐lives and mean residence times compared to the i.v. infusion, but no significant difference was observed in these parameters between the fasting and non‐fasting state. This study suggests that oral dosing may be a possible alternative route for the administration of these anticancer agents.
Url:
DOI: 10.1111/j.2042-7158.1986.tb04505.x
Affiliations:
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