Lack of Bioequivalence Between Disulfiram Formulations

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  • Topic: Pharmacokinetics, Bioavailability, Pharmacology
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Lack of bioequivalence between disulfiram formulations
Exemplified by a tablet/effervescent tablet study
Andersen, M. P. Lack of bioequivalence between disulfiram formulations. Acta Psychiatr Scand 1992: 86: 31-35.

M. P. Andersen
Pharmacokinetic Laboratory AIS Dumex (Dumex Ltd.), DK-2300 Copenhagen

Abstract - A comparison of the bioavailability of disulfiram (DSF) after administration of non-effervescent Antabusea tablets (CP Pharmaceuticals, UK) and Antabuse@effervescent tablets Antabus@(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 noneffervescent was found to be only 27 Vo 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 Yo. 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 o n both the formulation (preparation) and the mode of administration. A lack of bioequivalence between the two investigated DSF preparations was found.

Keywords: Disulfiram, methyldiethyldithiocarbamate, bioavailability, pharmacokinetics

Although Disulfiram (DSF) has been used in the treatment of alcoholism for many years [l], its pharmacokinetics, including bioavailability and metabolism, are not very well known. Recent years have seen the introduction of better analytical equipment and some light has been shed on the metabolism of I X F , but new...
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