In order to eliminate the pronounced food effect a traditional, milled formula of Aprepitant was developed. It is marketed under the trade name Emend. We compared the in vitro/in vivo pharmacokinetic properties of the reference compound, Emend and our novel NanoActive Aprepitant.
Our method produces a stable amorphous solid form comprising self-assembled supramolecular particles having a particle size of less than 100 nm with instantaneous wetting and redispersibility characteristics and improved apparent solubility and permeability (figures 1-2).
In vivo beagle dog pharmacokinetic studies showed that the novel formula exhibited greatly improved pharmacokinetic properties when compared to the reference compound, while serum blood concentrations for the novel formula and for the traditional milled formula were similar (figures 3-4). The marked food effect observed for the reference compound was practically eliminated by our formulation method (table 1).
|Cmax fed / fasted ratio||AUClast fed / fasted ratio|