Tiwari Sandip B, Udupa N
Department of Pharmaceutics, College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal, Karnataka, India.
Drug Deliv. 2003 Jul-Sep;10(3):161-8. doi: 10.1080/713840394.
The effect of different factors on the iontophoretic transport of ketorolac was analyzed. In vitro experiments were performed in a diffusion cell with a cellulose membrane as a barrier. The results indicated that an increase in current density or drug concentration enhanced the transmembrane permeation of the drug. The presence of extraneous ions (such as NaCl) or an increase in viscosity of the donor medium slowed down the iontophoretic transport of the drug. The pH does not seem to be an important factor determining iontophoretic transport of ketorolac as statistically insignificant difference was observed in flux at pH 5.6, 7.2, and 8. Also, the relative importance of the transport contributions involved in iontophoresis, namely diffusive iontophoretic and electro-osmotic fluxes, was investigated using glucose as a nonionizable drug. The results indicated that the total flux of ketorolac is a result of two contributions: passive diffusion and iontophoretic flux. The contribution of electro-osmosis appears to be negligible.
分析了不同因素对酮咯酸离子导入转运的影响。在以纤维素膜为屏障的扩散池中进行了体外实验。结果表明,电流密度或药物浓度的增加会增强药物的跨膜渗透。外来离子(如氯化钠)的存在或供体介质粘度的增加会减缓药物的离子导入转运。pH似乎不是决定酮咯酸离子导入转运的重要因素,因为在pH 5.6、7.2和8时通量的差异无统计学意义。此外,以葡萄糖作为非离子化药物研究了离子导入中涉及的转运贡献的相对重要性,即扩散离子导入通量和电渗通量。结果表明,酮咯酸的总通量是被动扩散和离子导入通量两种贡献的结果。电渗的贡献似乎可以忽略不计。