Ghosh Bijaya, Baser Rashmi, Patil Uma A, Dinesh B M
Department of Pharmaceutical Technology, K.L.E. Society's College of Pharmacy, II Block, Rajajinagar, Bangalore-560010, Karnataka, India.
PDA J Pharm Sci Technol. 2010 Jan-Feb;64(1):20-7.
The present investigation is aimed at assessing the iontophoretic permeability of nicorandil to evaluate its feasibility for the development of an actively delivered transdermal system. Excised porcine skin was used for permeation study, and steady state flux was optimized with respect to donor concentration, current density, and voltage. Constant current iontophoresis was carried out at 0.3, 0.5, and 0.7 mA/cm(2), whereas constant voltage studies were carried out at 3, 5, and 6.5 V. The effect of donor drug concentration (11.8, 55.8, and 104.8 mg/mL) was studied at the optimized condition of 5 V. An apparent increase in steady state flux was observed in constant current studies, but the increment over the passive diffusion was statistically insignificant (P > 0.05). In contrast, steady state flux was found to be higher than that of passive fluxes when permeation was carried out at 5 and 6.5 V (P < 0.001). Incorporation of alcohol in the donor vehicle increased solubility, but there was a tradeoff in terms of lag time. Conformity with the Nernst-Planck convective transport model suggested that electroosmosis was the dominant mechanism of permeation.
本研究旨在评估尼可地尔的离子导入通透性，以评价其用于开发主动递送透皮系统的可行性。采用离体猪皮进行渗透研究，并针对供体浓度、电流密度和电压对稳态通量进行了优化。恒流离子导入分别在0.3、0.5和0.7 mA/cm²下进行，而恒压研究则在3、5和6.5 V下进行。在5 V的优化条件下研究了供体药物浓度（11.8、55.8和104.8 mg/mL）的影响。在恒流研究中观察到稳态通量明显增加，但相对于被动扩散的增加在统计学上不显著（P>0.05）。相比之下，当在5和6.5 V下进行渗透时，发现稳态通量高于被动通量（P<0.001）。在供体载体中加入乙醇可提高溶解度，但在滞后时间方面存在权衡。与能斯特-普朗克对流传输模型的一致性表明，电渗是主要的渗透机制。
