NanoActive Sildenafil Citrate


Using the NanoActiveâ„¢ 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).

Solubility enhancement of Sildenafil Citrate
by the proprietary NanoActiveâ„¢ technology

Figure1
USP dissolution test of tablets containing
reference and NanoActive Sildenafil Citrate

Figure2

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).

tmax (h)
Fed Fasted
Reference Sildenafil Citrate 3.5 1.6
NanoActive Sildenafil Citrate 1.3 1.5
NanoActive Sildenafil Citrate eliminates delayed onset
of action of the reference drug observed in fed state

Figure3 & Table1