Plasma Concentrations and Bioavailability of Clofibrate After Administration to Human Subjects

Plasma Concentrations and Bioavailability of Clofibric Acid from Its Calcium Salt in Humans

“…Peak plasma levels in individual subjects were similar after administration of Formulations A (mean of 71 pg/ml f 17 S D ) and C (mean of 73 pg/ml f 15 SD) and higher after Formulation B (mean of 85 pg/mI 13 SD). Plasma clofibric acid levels were slightly higher than those reported previously(10).The mean half-life of clofibric acid in plasma after administration of Formulation B (15.4 hr f 3.0 SD) was slightly shorter but not significantly different(Tables I1 and 111)from those after administration of Formulations A and C (17.2 f 2.0 and 16.9 f 3.0 hr f SD, respectively). Similar half-lives of 19 and 15-17 hr were reported…”

Drug Concentration Asymmetry in Tissues and Plasma for Small Molecule–Related Therapeutic Modalities

“…4, in the activation and hydrolysis mechanism, enzyme kinetics of activation/hydrolysis, target tissue, and pharmacologic mechanism of target inhibition. Whereas the relatively simple ester hydrolysis of clofibrate and oseltamivir might suggest that an obvious relationship exists between the plasma exposure of the liberated acid and pharmacologic response, this would ignore the confounding effects of the site of hydrolysis and the endpoints used to assess pharmacologic activity (Chasseaud et al, 1974;Miller and Spence, 1998;Shi et al, 2006;Wattanagoon et al, 2009). These relationships between target loading, hydrolysis, and pharmacologic mechanism become even more complicated considering tenofovir and sofosbuvir (Oberg, 2006;Ray et al, 2016;Rivero-Juarez et al, 2018).…”