Effects of Altered Formulation on the Bioequivalence of Tacrolimus in Healthy Female and Male Volunteeers
Status:
Completed
Trial end date:
2018-01-20
Target enrollment:
Participant gender:
Summary
Amorphous solid dispersion (ASD) formulations are increasingly used by the pharmaceutical
industry to develop poorly water-soluble drugs into effective oral dosage forms. Examples
include the antifungal drug itraconazole, the HIV protease inhibitor combination,
lopinavir/ritonavir and the immunosuppressive, tacrolimus. There is potential for significant
variation in bioavailability of ASD and thus heightened concern regarding the therapeutic
efficacy as generic versions of these poorly water-soluble compounds become approved. The
variation in bioavailability is to be expected because of our limited understanding of the
precise physical chemistry of drug polymer amorphous solid dispersion formulations.