Preparation of Probucol Loaded Mixed Micelles and Its Pharmacokinetic Behavior In Rats

OBJECTIVE Development of probucol loaded mixed micelles (PMM) for enhancing its oral bioavailability. METHODS PMM was prepared with soybean phosphatidylcholine (EPC) and sodium deoxycholate (SD) by a co-precipitation method. The in vitro properties and in vivo pharmacokinetic behavior of PMM was evaluated. RESULTS The formulation of PMM was optimized as EPC︰SD︰probucol (3︰4︰1). PMM was self-assembled with average diameter of 82.28 nm and polydispersity index of 0.179. Probucol may exhibit as amorphous state in PMM. The in vivo pharmacokinetical results indicated that the peak concentration (Cmax) and area under concentration-time curve (AUC) was significantly improved by 2.28-fold and 4.43-fold, respectively. CONCLUSION The oral bioavailability of probucol was significantly improved by PMM, which could be potential for enhancing the oral absorption of insoluble drugs.