Abstract：
β-Caryophyllene (BCP), a common constituent of many spice and food plants, is gaining increased attention due to recent research identifying numerous potential health benefits. Due to limited oral bioavailability observed in preclinical models, the described benefits of BCP may be maximized by using a suitable delivery system. Additionally, human pharmacokinetics (PK) remain unknown. This study evaluates the relative oral bioavailability of BCP formulated in a self-emulsifying drug delivery system (SEDDS) based on VESIsorb® formulation technology (BCP-SEDDS) compared to BCP neat oil. Hence, a randomized, double-blind, cross-over design, single oral dose study (100 mg BCP) in 24 healthy subjects (12 men/12 women) was performed under fasting conditions. Pharmacokinetic parameters were analyzed from individual concentration-time curves. The data show that BCP-SEDDS resulted in a 2.2/2.0-fold increase in AUC0-12h/AUC0-24h and a 3.6-fold increase in Cmax compared to BCP neat oil. Moreover, BCP was absorbed faster from BCP-SEDDS (Tmax: 1.43 h) compared to BCP neat oil (Tmax: 3.07 h). Gender analysis revealed that there is no significant difference between men and women for both the investigated formulations and all investigated PK endpoints. In conclusion, BCP-SEDDS offers a well-tolerated and effective oral delivery system to significantly enhance the oral bioavailability of BCP in humans.
摘要：
β-石竹烯(BCP),许多香料和食用植物的常见成分，由于最近的研究确定了许多潜在的健康益处，正在获得越来越多的关注。由于在临床前模型中观察到的口服生物利用度有限，所描述的BCP的益处可以通过使用合适的递送系统来最大化。此外,人体药代动力学（PK）仍然未知。本研究评估了基于VESISorb®制剂技术(BCP-SEDDS)在自乳化药物递送系统(SEDDS)中配制的BCP与BCP纯油的相对口服生物利用度。因此，一个随机的，双盲,交叉设计，在禁食条件下对24名健康受试者(12名男性/12名女性)进行单次口服剂量研究(100mgBCP)。从个体浓度-时间曲线分析药代动力学参数。数据显示,与BCP纯油相比,BCP-SEDDS导致AUC0-12h/AUC0-24h增加2.2/2.0倍,Cmax增加3.6倍。此外，与BCP纯油(Tmax:3.07h)相比,BCP从BCP-SEDDS(Tmax:1.43h)更快吸收。性别分析显示,对于所研究的制剂和所有所研究的PK终点,男性和女性之间没有显著差异。总之,BCP-SEDDS提供了一种耐受性良好且有效的口服给药系统，可显着提高BCP在人体中的口服生物利用度。
