Department of Industrial Pharmacy, Beijing University of TCM, China.
Arch Pharm Res. 2010 May;33(5):691-6. doi: 10.1007/s12272-010-0507-8. Epub 2010 May 29.
The objective of this research was to study the in situ and in vivo nasal absorption of Geniposide (Ge) co-administered with borneol. A rat in situ nasal perfusion technique with a novel volumeadjusted calculation was used to examine the absorption rate and extent of Ge. The influence of different experimental conditions such as purity of extract, drug concentration, co-administration with synthetic borneol or natural borneol were also investigated. Results indicated nasal absorption of Ge was primarily by passive diffusion that resembled first order kinetics. Following co-administration with borenol, the drug absorption was increased by 1.4 and 1.7 folds for natural borneol and synthetic borneol, respectively. However, the effect of other factors on drug absorption was not significant. In addition, it was also observed that there is a positive correlation between the absorption of water and Ge by the nasal route. In vivo studies carried out in rats where Ge was co-administered with NB and the pharmacokinetic profile obtained following intranasal administration were compared with those after intravenous administration. The bioavailability of Ge by intranasal was 101.5% and T(max) was 2.04 +/- 0.64 min. MRT was 218.7 +/- 74.1 min and 44.4 +/- 8.9 min for intranasal and intravenous, respectively. Combined with the borneol, Ge can be promptly and thoroughly absorbed intranasally in rats.
本研究旨在研究京尼平苷（Ge）与冰片共给药时的原位和体内鼻内吸收。采用新型体积调节计算的大鼠原位鼻灌注技术来检查 Ge 的吸收速率和程度。还研究了不同实验条件（如提取物的纯度、药物浓度、与合成冰片或天然冰片共给药）对吸收的影响。结果表明，Ge 的鼻内吸收主要是通过被动扩散，类似于一级动力学。与冰片共给药后，天然冰片和合成冰片分别使药物吸收增加了 1.4 倍和 1.7 倍。然而，其他因素对药物吸收的影响并不显著。此外，还观察到水和 Ge 通过鼻途径吸收之间存在正相关。在大鼠中进行的体内研究中，将 Ge 与 NB 共给药，并比较了鼻内给药后获得的药代动力学曲线与静脉内给药后的曲线。Ge 的鼻内生物利用度为 101.5%，T(max)为 2.04 +/- 0.64 min。MRT 分别为 218.7 +/- 74.1 min 和 44.4 +/- 8.9 min，用于鼻内和静脉内给药。与冰片结合，Ge 可在大鼠中迅速而彻底地经鼻内吸收。
