Characterization of the physicochemical properties of KRK-701P

摘要

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 degrees C), 52 % RH (saturated solution of Na2Cr2O7.2H(2)O/20 degrees C) and 95 % RH (saturated solution of Na2HPO4/20 degrees C), the two forms were not transformed.