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Reverse-dialysis can be misleading for drug release studies in emulsions as demonstrated by NMR dilution experiments
International Journal of Pharmaceutics ( IF 5.3 ) Pub Date : 2021-09-15 , DOI: 10.1016/j.ijpharm.2021.121093
Zhaoyuan Gong 1 , Mohammad Hossein Tootoonchi 2 , Christopher A Fraker 2 , Jamie D Walls 1
Affiliation  

Emulsions are an important class of carriers for the delivery of hydrophobic drugs. While knowledge of drug release kinetics is critical to optimizing drug carrying emulsions, there remain many open questions about the validity of standard characterization methods such as the commonly used reverse-dialysis. In this paper, the kinetic parameters of isoflurane release in perfluorotributylamine emulsions determined from both reverse-dialysis and nuclear magnetic resonance (NMR) dilution experiments are compared. The NMR-determined kinetic parameters of isoflurane release were found to be approximately seven orders of magnitude larger than those determined from conventional reverse-dialysis and were also shown to be consistent with prior in vivo observations of the anesthetization of rats.



中文翻译:


NMR 稀释实验证明,反向透析可能会误导乳液中的药物释放研究



乳剂是用于递送疏水性药物的一类重要载体。虽然药物释放动力学的知识对于优化载药乳液至关重要,但关于标准表征方法(例如常用的反透析)的有效性仍然存在许多悬而未决的问题。本文比较了反渗析和核磁共振(NMR)稀释实验测定的全氟三丁胺乳液中异氟烷释放的动力学参数。核磁共振测定的异氟烷释放动力学参数比传统反透析测定的动力学参数大大约七个数量级,并且也与先前对大鼠麻醉的体内观察结果一致。

更新日期:2021-09-23
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