Su Jiping, Bachmann G, Tang Anzhou, Zumegen C, Michel O, Wittekindt C
Department of Otolaryngology, First Affiliated Hospital, Guangxi Medical University, Nanning 530021.
Lin Chuang Er Bi Yan Hou Ke Za Zhi. 2003 Oct;17(10):615-7.
The present study was to analysis the pharmacokinetics of prednisolone-21-hydrogensuccinate in the perilymph after local and systemic application.
On the local application, 5% prednisolone-21-hydrogensuccinate was directly applied into the round window niche under the microscopy. On the systemic application, the drug (60 mg/kg) was used intraperitoneal. Perilymphatic samples were obtained after variable periods of application. Levels of prednisolone-21-hydrogensuccinate in perilymph were measured by using HPLC.
The highest level of the drug was on (952.3 +/- 382.7) mg/L after 180 min. And remained on (18.72 +/- 16.97) mg/L after 960 min in the local application groups. In the systemic application group, the highest level of the drug was on(14.71 +/- 7.05) mg/L after 150 min.
The results demonstrate that high levels and long time remain of prednisolone-21-hydrogensuccinate in perilymph are achievable by a single dose local application into the round window niche.
本研究旨在分析局部和全身应用后泼尼松龙 - 21 - 氢琥珀酸酯在外淋巴中的药代动力学。
局部应用时，在显微镜下将5%泼尼松龙 - 21 - 氢琥珀酸酯直接应用于圆窗龛。全身应用时，药物（60mg/kg）腹腔注射。在不同应用时间段后获取外淋巴样本。使用高效液相色谱法测量外淋巴中泼尼松龙 - 21 - 氢琥珀酸酯的水平。
局部应用组在180分钟后药物最高水平为（952.3±382.7）mg/L，960分钟后仍为（18.72±16.97）mg/L。全身应用组在150分钟后药物最高水平为（14.71±7.05）mg/L。
结果表明，通过向圆窗龛单次局部应用，可在外淋巴中实现泼尼松龙 - 21 - 氢琥珀酸酯的高浓度和长时间留存。
