title: Lack of bioequivalence between disulfiram formulations. Exemplified by a tablet/effervescent tablet study.
abstract: A comparison of the bioavailability of disulfiram (DSF) after administration of non-effervescent Antabuse tablets (CP Pharmaceuticals, UK) and Antabuse effervescent tablets Antabuse (A/S Dumex, DK) has been made in two cross-over studies. The first study included 6 volunteers who were given 400 mg DSF after an overnight fast. The bioavailability of DSF after administration of non-effervescent was found to be only 27% of that achieved with effervescent tablets. The second study included 24 volunteers who were given 800 mg DSF after a light standardized meal. The relative bioavailability of DSF after administration of non-effervescent compared with effervescent tablets was found to be only 34%. In addition to the difference in bioavailability of DSF after administration of the two preparations, a considerable difference was seen between the two studies. A light meal seems both to increase the bioavailability of DSF and to reduce the interindividual variation. A two to threefold increase in the bioavailability of DSF was found. Thus, the bioavailability of DSF appears to depend on both the formulation (preparation) and the mode of administration. A lack of bioequivalence between the two investigated DSF preparations was found.
authors: Pharmacokinetic Laboratory, A/S Dumex (Dumex Ltd.), Copenhagen.
authors: M P
authors: MP
authors: Andersen
mesh_terms: D000284:Administration, Oral; D000328:Adult; D001682:Biological Availability; D004221:Disulfiram / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics*; D004304:Dosage Forms; D004435:Eating; D005260:Female; D006801:Humans; D008297:Male
chemical_list: D004304:Dosage Forms; D004221:Disulfiram