NanoActive Aprepitant


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).

Superior solubility of the NanoActive Aprepitant in FaSSIF
and FeSSIF (Fasted and Fed-state simulated intestinal fluid) media

Figure1
Superior PAMPA permeability of the
NanoActive Aprepitant in FaSSIF and FeSSIF media

Figure2

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).

Serum blood concentrations of Aprepitant after oral
administration of the NanoActive, reference and
milled formula in dogs under fasted condition

Figure3
Serum blood concentrations of Aprepitant after oral
administration of the NanoActive, reference and
milled formula in dogs under fed condition

Figure4
Cmax fed / fasted ratio AUClast fed / fasted ratio
Reference 2.6 2.9
Emend 1.4 1.3
NanoActive 1.1 1.2
Eliminated food effect by the NanoActive formulation
Table1