Characterization of the physicochemical properties of KRK-701P

Abstract

KRK-701P is a broad-spectrum antibiotic with methicillin-resistant antibacterial activity. The objective of this preformulation study was to determine the physicochemical properties of KRK-701P. The n-octanol-to-water partition coefficients of KRK-701P were 0.448 at pH 4 and 2.546 at pH 8. One crystal form and one amorphous form of KRK-701P were isolated by recrystallization and characterized by differential scanning calorimetry, powder X-ray diffractometry and thermogravimetric analysis. After storage for 1 month at 0% RH (silica gel, 20 °C), 52% RH (saturated solution of Na2Cr2O7.2H2O/20 °C) and 95% RH (saturated solution of Na2HPO4/20 °C), the two forms were not transformed.