【摘要】 为了考察pH对利多卡因经皮渗透性的影响,用水平扩散池测定了盐酸利多卡因在不同pH 值下通过离体大鼠皮肤的稳态流量(JSS)等参数。结果表明利多卡因游离碱和盐酸盐的经皮渗透性有明显差别,前者的稳态流量为后者的14倍,且滞后时间较短,稳态流量对pH作图呈揝斝吻?pH 接近pKa时稳态流量突增。由此可见,介质的pH值影响利多卡因的经皮渗透性,制剂中应作为一个重要因素考察。更多还原

【Abstract】 The effect of pH on the permeation of Lidocaine hydrochloride (LH) across excised rat skin was studied, the steady state flux (JSS) at different pH being determined using improved Valia-Chien diffusion cells. JSS increased substantially when pH was close to the pKa of LH. The profile of JSS versus pH showed an 慡?shaped curve. JSS of Lidocaine free base (LFB) was fourteen times that of LH. The pH of vehicle influences the permeation of LH significantly and should be considered as an important factor when a formulation is developed.更多还原