Shanghai Key Laboratory for Pharmaceutical Metabolite Research, School of Pharmacy, Second Military Medical University, No. 325 Guohe Road, Shanghai 200433, PR China.
Int J Pharm. 2013 Jun 25;450(1-2):304-10. doi: 10.1016/j.ijpharm.2013.04.013. Epub 2013 Apr 15.
β-Caryophyllene (BCP), a natural sesquiterpene existing in the essential oil of many plants, has exhibited a wide range of biological activities. However, its volatility and poor water-solubility limit its application in pharmaceutical field. β-Cyclodextrin (β-CD) has intrinsic ability to form specific inclusion complexes with different drugs to enhance their stability, solubility and bioavailability. The aim of this study is to investigate and compare the oral bioavailability and the pharmacokinetics of free BCP and BCP/β-CD inclusion complex after a single oral dose of 50mg/kg on rats. A simple, rapid, and sensitive gas chromatography-mass spectrometry method in selected ion monitoring (GC-MS/SIM) mode was developed on determination of BCP in rat plasma. The in vivo data showed that BCP/β-CD inclusion complex displayed earlier Tmax, higher Cmax and the AUC0-12h was approximately 2.6 times increase than those of free BCP. These results demonstrated that BCP/β-CD inclusion complex has significantly increased the oral bioavailability of the drug in rats than free BCP.
β-石竹烯（BCP）是一种天然倍半萜烯，存在于许多植物的精油中，具有广泛的生物活性。然而，其挥发性和较差的水溶性限制了其在制药领域的应用。β-环糊精（β-CD）具有与不同药物形成特定包合络合物的固有能力，以提高其稳定性、溶解度和生物利用度。本研究旨在考察和比较大鼠单次口服 50mg/kg 剂量后游离 BCP 和 BCP/β-CD 包合物的口服生物利用度和药代动力学。建立了一种简单、快速、灵敏的气相色谱-质谱法（GC-MS/SIM）在选择离子监测模式下测定大鼠血浆中 BCP 的方法。体内数据表明，BCP/β-CD 包合物显示出更早的 Tmax、更高的 Cmax，AUC0-12h 约增加 2.6 倍。这些结果表明，与游离 BCP 相比，BCP/β-CD 包合物显著提高了药物在大鼠体内的口服生物利用度。
