Using the NanoActive™ technology we achieved considerable improvement in apparent solubility (figure 1) and dissolution rate. We also developed a tablet formulation from the NanoActive Sildenafil Citrate and performed USP dissolution tests. The NanoActive compound shows improved dissolution characteristics when compared to drug release from a tablet with the same composition containing reference Sildenafil Citrate (figures 2).
The major PK related problem associated with the administration of Sildenafil Citrate is a delay in the absorption of the compound when taken after a high fat meal. Our method produces a novel form that eliminates this problem. Following administration of the developed NanoActive Sildenafil Citrate to dogs fed by a high fat meal significantly shortened tmax values were detected when compared to the reference compound (figure 3). The marked food effect was practically eliminated by our formulation method (table 1).
|Reference Sildenafil Citrate||3.5||1.6|
|NanoActive Sildenafil Citrate||1.3||1.5|