微渗析技术研究克拉霉素亚微乳剂相分布

Investigation of phase distribution of clarithromycin submicron emulsion by microdialysis technique

目的:利用微渗析技术研究克拉霉素(clarithromycin,CLA)亚微乳剂相分布,考察离子对增溶剂及NaOH用量对乳剂相分布的影响。方法:以维生素E琥珀酸酯(tocopherol succinate,TS)、油酸为离子对增溶剂,制备CLA亚微乳剂;浓差法测定探针回收率与传递率,以亚微乳剂为渗析介质,用反相渗析法测定回收率。结果:反相渗析法测得回收率为86.2%;90%以上的药物分布于乳剂油相中。结论:微渗析技术可以用于测定乳剂的相分布,TS促进CLA于乳剂油相分布的能力更强,且对体系pH值变化较不敏感。

Objective：To investigate the phase distribution of clarithromycin submicron emulsion by microdialysis technique,and observe the effects of ion pairing reagents and NaOH amount on the phase distribution of the emulsion.Methods：Clarithromycin parenteral emulsion was prepared using tocopherol succinate and oleic acid as ion pairing reagents.Zero net flux methods were used to assess the recovery and delivery of the probe.Retrodialysis method was employed to determine the recovery using submicron emulsion as the surrounding medium.Results：The recovery of the microdialysis probe was 86.2%,and more than 90% of clarithromycin distributed into the oil phase of the emulsion.Conclusion：Microdialysis technique could be utilized to investigate the phase distribution of clarithromycin submicron emulsion.Tocopherol succinate facilitated the distribution of clarithromycin into the oil phase of the emulsion,and the capacity of which was stronger and less sensitive to the pH value than that of oleic acid.