sodium-dodecyl-sulfate and efonidipine

The aim of this study was to improve the oral bioavailability of a practically insoluble drug, efonidipine hydrochloride (EFH), by agglomeration in acid solution/gastric fluid. The EFH nanosuspension was prepared by the wet-milling method with F68 as a dispersing agent, SDS as an auxiliary stabilizer and l-arginine as a pH adjusting agent. The EFH nanosuspension have been prepared in industrial scale-up. The dissolution rate of the EFH nanosuspension was greater than that of bulk EFH. An in vitro intestinal permeability study showed a clear increase in the apparent permeability of different intestinal segments compared with bulk EFH. Also, a pharmacokinetic study showed that the C

Topics: Animals; Area Under Curve; Arginine; Biological Availability; Calcium Channel Blockers; Chemistry, Pharmaceutical; Dihydropyridines; Excipients; Hydrogen-Ion Concentration; Male; Nanoparticles; Nitrophenols; Organophosphorus Compounds; Poloxamer; Rats; Rats, Sprague-Dawley; Sodium Dodecyl Sulfate; Solubility; Suspensions; Tablets