Study of the Technological Methods Effect on Dissolution of the X-ray Amorphous Efavirenz-mesoporous Carrier System

Introduction . The low solubility of active pharmaceutical ingredients (APIs) in the physiological pH range intestinal tract can adversely affect their absorption and bioavailability. Various methods increasing APIs have been proposed recent decades. Among them there are preparation solid dispersions, micronization, solubilization other methods, including ones based on amorphization crystalline substances, such as, spray drying, hot melt extrusion, mesoporous carriers as magnesium aluminosilicate, silica, etc. Aim Study technological effect dissolution at temperature practically insoluble API efavirenz amorphized by carriers. Materials Efavirenz form ? (EFA) (LLC "AMEDART", Russia, batch 010520). reference standard (USP ? R09740). Mesoporous (MC): Silica – Syloid ® 244FP (244), XDP 3150 (3150) (W.R. Grace&Co.-Conn, USA); FujiSil ™ (FSL) (Fuji Chemical Industries Co., Ltd., Japan); Aeroperl 300 (APL) (Evonik, Germany); Parteck SLC (SLC) (Merck Millipore, Synthetic aluminometasilicate Neusilin US2 (US2), UFL (UFL) Industry Japan). MC was performed via solvent wetting extrusion methods. Results discussion increases series following: > FSL = 244 3150. data consistent with an increase surface area a decrease pore size MC. state system efavirenz-Aeroperl is caused largest size. It obvious according to that method gives better results comparison obtaining X-ray amorphous systems efavirenz-MC. Conclusion. Solvent technology recommended for APIs. preferable silica or synthetic US2.