Department of Industrial Pharmacy, School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing 100102, China.
J Zhejiang Univ Sci B. 2011 Feb;12(2):143-8. doi: 10.1631/jzus.B1000121.
Both geniposide (Ge) and natural borneol (NB) are bioactive substances derived from traditional Chinese herbs. The effect of NB on the pharmacokinetics of Ge in rat via intranasal administration was investigated. The concentrations of Ge in plasma were determined by reversed-phase high-performance liquid chromatography (HPLC) after intranasal administration of Ge (4 mg/kg) alone and combined with different doses (0.08, 0.8, and 8 mg/kg) of NB. The intravenous administration was given as a reference (4 mg/kg of Ge and 8 mg/kg of NB). Compared with the intravenous administration, the absolute bioavailability of Ge was 76.14% through intranasal administration combined with NB. Compared with the intranasal administration of Ge alone, Ge could be absorbed rapidly in the nasal cavity combined with NB; the peak time of Ge in the plasma became shorter (3-5 min vs. 40 min); the peak concentration became higher (1.32-4.25 μg/ml vs. 0.67 μg/ml); and, the relative bioavailability of Ge combined with NB was 90.3%-237.8%. The enhancing effect was attenuated as the dose of NB decreased. The results indicated that NB can accelerate the absorption of Ge dose-dependently in the nasal cavity.
栀子苷（Ge）和天然冰片（NB）均为来源于传统中药的生物活性物质。本研究考察了 NB 通过鼻腔给药对 Ge 药代动力学的影响。Ge 单独（4 mg/kg）及与不同剂量（0.08、0.8 和 8 mg/kg）NB 联合鼻腔给药后，采用反相高效液相色谱法（HPLC）测定血浆中 Ge 的浓度。静脉给药作为参考（4 mg/kg Ge 和 8 mg/kg NB）。与静脉给药相比，NB 联合鼻腔给药使 Ge 的绝对生物利用度提高至 76.14%。与 Ge 单独鼻腔给药相比，Ge 与 NB 联合可在鼻腔中快速吸收；Ge 在血浆中的达峰时间变短（3-5 min 比 40 min）；峰浓度升高（1.32-4.25 μg/ml 比 0.67 μg/ml）；与 NB 联合时 Ge 的相对生物利用度为 90.3%-237.8%。随着 NB 剂量的降低，增强作用减弱。结果表明，NB 可剂量依赖性地促进 Ge 在鼻腔中的吸收。
