Pharmacokinetics of the Active Compound Group From <i>Gerbera piloselloides</i> Herba: Absorption, Metabolism, and Excretion in Rats

ABSTRACT Gerbera piloselloides Herba (GP) is a traditional herb commonly used for asthma in China. Our previous studies have identified a key group of active components—arbutin, marmesin, and luteolin—that demonstrate significant efficacy in asthma treatment, showing promising therapeutic potential. Although we previously investigated the comparative pharmacokinetics (only absorption process) of 11 main components of GP in both control and asthmatic mice, the pharmacokinetics of these 3 active compounds, including absorption, metabolism, and excretion in rats, remain unclear. This study develops an efficient liquid chromatography (LC) method to explore these pharmacokinetic processes. Ultrahigh‐performance LC coupled with triple quadrupole mass spectrometry (UPLC–MS/MS) and Q‐Exactive hybrid quadrupole‐orbitrap high‐resolution accurate MS (UHPLC‐Q‐Exactive Plus HRMS) were employed to detect these compounds and their metabolites in biological samples. The results indicate that arbutin is rapidly absorbed, with a T max of 0.22 ± 0.15 h and a C max of 35 477 ± 6743 µg/L, and its cumulative urinary excretion rate is 60.136% ± 9.539%. Marmesin achieves a C max of 503 225 ± 89 848 µg/L and a T 1/2 of 3.58 ± 0.075 h, with significantly lower cumulative excretion over 36 h compared to the administered dose. Luteolin demonstrates a characteristic double‐peak pharmacokinetic profile, with a C max of 22.24 ± 4.84 ng/L. Notably, arbutin is primarily excreted via urine, whereas marmesin and luteolin are predominantly excreted through bile and urine, respectively. A total of 7 metabolites of arbutin, 13 metabolites of luteolin, and 22 metabolites of marmesin were identified in plasma, feces, urine, and bile, which involves such metabolic pathways as oxidation, reduction, methylation, sulfation, acetylation, hydration, glucuronidation, and glutathione conjugation. This establishes a stable, efficient analytical method for assessing the pharmacokinetic profiles of these key GP components, providing valuable insights for their further therapeutic development.