Zhang, Hongwei published the artcileThe preparation of felodipine/zein amorphous solid dispersions and in vitro evaluation using a dynamic gastrointestinal system, Application In Synthesis of 72509-76-3, the main research area is felodipine zein amorphous solid dispersion spray drying gastrointestinal system; TIM-1 model; Zein; amorphous solid dispersions; bioavailability; solid-state characterization; spray drying.
Felodipine has been widely used as a poorly water-soluble model drug for various studies to improve its oral bioavailability and in vivo efficacy. In this study, we developed amorphous solid dispersions (ASDs) via spray drying to enhance the bioavailability of felodipine through using natural zein protein as a novel polymeric excipient. The solid state characterization results demonstrated a single glass transition temperature (Tg) around 128.6°C and good phys. stability post 3 mo accelerated study under the condition of 40°C and 75% relative humidity (RH), which is possibly accounted for the mol. immobilization and hydrogen bonding interactions between felodipine and zein. By combining the in vitro dissolution study with TIM-1 gastrointestinal simulation investigation, it is indicated that felodipine was rapidly released from the ASD in 30 mins, and the supersaturation of felodipine was well maintained over 6 h, which resulted in a significant enhancement of felodipine bioavailability during simulated digestive processes in the upper GI tract. This study suggests that spray drying combined with natural excipient zein is an efficient formulation strategy for the development of ASDs with enhanced aqueous solubility and bioavailability.
Pharmaceutical Development and Technology published new progress about Crystal structure. 72509-76-3 belongs to class pyridine-derivatives, name is 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C18H19Cl2NO4, Application In Synthesis of 72509-76-3.