F. Moolenaar, J. Visser, T. Huizinga
1980
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Quality indicators
Journal
International Journal of Pharmaceutics
Abstract
Abstract In this report it will be shown that rectal administration of glafenine and its salt can not be considered as a rotional therapy. Plasma concentrations of glafenine and glafenic acid were measured, by means of HPLC analysis, after single oral and rectal doses of glafenine (400 mg), suspended in aqueous vehicles. After oral administration negligible plasma concentrations of free glafenine could be detected, probably due to a substantial first-pass effect. Peak concentrations of glafenic acid were reached after one hour. The decline in plasma concentrations was observed to be multiphasic. Rectal adsorption of glafenine (from micro-enemas) or glafenine HCl (from fatty suppositories) was extremely slow and incomplete, due to the slight water-solubility of glafenine at the prevailing pH in the rectum lumen.