Role of Self-Association and Supersaturation in Oral Absorption of a Poorly Soluble Weakly Basic Drug

Authors: Narang AS, Badawy S, Ye Q, Patel D, Raghavan K, Huang Y, Vig BS, Crison J, Xu Y, Ramirez A, Galella M, Rinaldi FA
Publication: Pharm Res
Keywords: alanine transaminase, calorimetry, colloids, computer simulation, humans, hydrogen-ion concentration, intestinal absorption, magnetic, molecular models, oral administration, particle size, pharmaceutical chemistry, resonance spectroscopy, solubility, surface tension, triazines
Software: GastroPlus®

Purpose

Precipitation of weakly basic drugs in intestinal fluids can affect oral drug absorption. In this study, the implications of self-association of brivanib alaninate in acidic aqueous solution, leading to supersaturation at basic pH condition, on its solubility and oral absorption were investigated.