Comparative pharmacokinetic analysis of sporoderm‐broken and sporoderm‐removed Ganoderma lucidum spore in rat by using a sensitive plasma UPLC–QqQ–MS method

Abstract Previous studies have found that removing the sporoderm significantly enhanced antitumor and immunoregulatory activities of Ganoderma lucidum spore (GLS) compared with breaking the sporoderm. However, the pharmacokinetics of sporoderm‐removed GLS (RGLS) and sporoderm‐broken GLS (BGLS) remain elusive. To compare the pharmacokinetic differences between the two products, we developed a UPLC–QqQ MS method for determining nine representative triterpenoid concentrations. Chloramphenicol was used as an internal standard. The samples were separated on a reversed‐phase column using acetonitrile–0.1% formic acid and water–0.1% formic acid as mobile phases. Nine triterpenoids were analyzed using multiple reaction monitoring mode. The results showed that the area under the concentration–time curve from dosing to time t of all nine components was increased in RGLS compared with BGLS. And the time to the maximum concentration in BGLS was delayed compared with that of RGLS. These indicated that the absorption of RGLS was better than that of BGLS, and the sporoderm might hinder the absorption of the active components. These results increase our understanding of the bioavailability of BGLS and RGLS and indicate that increased bioavailability is one of the main reasons for the enhanced efficacy of RGLS.