Saxifraga stolonifera (S. stolonifera) has been used to cure various diseases effectively while little is known about the pharmacokinetic properties of the bioactive components of S. stolonifera. The aim of this study is to develop an UHPLC-ESI-MS/MS method for simultaneous determination of gallic acid (GA), bergenin (BG) and quercetin-3-O-β-L-rhamnopyranoside (QR), three bioactive compounds of S. stolonifera, and to apply the method for pharmacokinetic study to learn how dosage variations of S.