Optimization of tocol emulsions for the intravenous delivery of clarithromycin
作者： Jie Li , Shufang Nie , Xingang Yang , Changguang Wang , Shuxia Cui
DOI: 10.1016/J.IJPHARM.2007.12.046
关键词: Chromatography 、 Poloxamer 、 Zeta potential 、 Antibacterial agent 、 Box–Behnken design 、 Clarithromycin 、 Irritation 、 Oleic acid 、 Emulsion 、 Stereochemistry 、 Chemistry
摘要: In the present study, novel less-painful tocol emulsions for intravenous delivery of clarithromycin were prepared and optimized. The therapeutically effective concentration clarithromycin, 5mg/ml, was achieved using tocopherol succinate (TS) combined with oleic acid as lipophilic counterions. possibility employing microdialysis technique to investigate distribution drug in explored. A three-level three-factorial Box-Behnken experimental design utilized conduct experiments. effects selected variables, succinate/oleic relation, poloxamer 188 content 0.1M NaOH amount, on three considered responses investigated. particle size, zeta potential oil phase optimized formulation observed be 138.5 nm, -32.16 mV 97.28%, respectively. formula demonstrated good physical stability during storage at 4 degrees C room temperature. histopathological examination rabbit ear vein irritation test indicated that could eliminated by formulating a emulsion.
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