Metzner J, Bekemeier H, Schneidewind E M, Wenzel U
Pharmazie. 1979;34(3):185-7.
The present investigation into the pharmacokinetic behaviour of the propolis constituent pinocembrin which produces a relatively good antimicrobial effect in vitro, points to possible causes of its therapeutical failure when mice infected with Candida albicans were used as a model. The biological half-life periods for the phases of invasion and elimination were 26 and 268 min, respectively. The biological availability was 25%. Almost 15% of pinocembrin are excreted unchanged in faeces and urine. Even in case of oral application of doses of up to 500 mg/kg, the serum pinocembrin concentrations did not equal the MIC (minimal inhibitor concentration) values required in vitro. A considerable first-pass effect and accelerated processes of elimination are discussed as possible causes. It appears from the present findings that pinocembrin may be utilizable only for the external treatment of stomatomycoses.
目前对蜂胶成分松属素药代动力学行为的研究表明,以感染白色念珠菌的小鼠为模型时,其在体外具有较好的抗菌效果,但却可能是导致其治疗失败的原因。侵袭期和消除期的生物半衰期分别为26分钟和268分钟。生物利用度为25%。近15%的松属素以原形经粪便和尿液排出。即使口服高达500mg/kg的剂量,血清松属素浓度也未达到体外所需的最低抑菌浓度(MIC)值。讨论了可能的原因,包括相当大的首过效应和加速的消除过程。从目前的研究结果来看,松属素可能仅适用于口腔真菌病的外部治疗。