In a previous study, the specific NOX1/2/4 inhibitor
Ewha-18278 was confirmed as a possible treatment for
osteoporosis both in vitro and in vivo. Here, we investigated the pharmacokinetics (PK) of the compound by intravenous (IV) and
oral administrations to rats.
Dimethyl sulfoxide (
DMSO)-based and
diazepam injection-based formulations were used to dissolve the compound. In the latter formulation applicable to humans, the changes in PK parameters were monitored at two different concentrations (1 mg/mL and 2 mg/mL). The area under the plasma concentration-time curve from zero time to infinity (AUCinf) of
Ewha-18278 was highest in the
DMSO-based formulation (2 mg/mL). Also, the concentration was increased 1.6-fold at the low concentration of the
diazepam injection-based formulation compared to the high concentration. There was no statistical significance in the AUCinf of the compound between
DMSO-based formulation (2 mg/mL) and
diazepam injection-based formulation (1 mg/mL). These results suggest that
Ewha-18278 can be delivered to humans by both IV and oral routes. In addition, the
diazepam injection-based formulation of
Ewha-18278 appears to be a suitable candidate for dosage development for future toxicity test and clinical trial.