Intestinal absorption of saquinavir in the rat: Insights in possible mechanisms

An Examination of the Effect of Intestinal First Pass Extraction on Intestinal Lymphatic Transport of Saquinavir in the Rat

“…The effect of specific modulators of P-gp and/or CYP, such as verapamil, ketoconazole and cyclosporine, on increasing intestinal permeability of saquinavir has been demonstrated in vitro in Caco 2 cell lines (5). Furthermore, a number of in situ/in vivo studies have demonstrated the effect of inhibition of Pgp/CYP like processes on increasing portal and systemic blood levels of saquinavir (9,17). To this end, saquinavir therapy is now generally recommended in combination with another protease inhibitor, ritonavir, primarily on the basis of a favorable pharmacokinetic interaction (i.e.…”