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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。
In order to investigate the effect of pH on the transdermal permeability of lidocaine, steady-state flow rate (JSS) and other parameters of lidocaine hydrochloride in isolated rat skin at different pH values were measured by a horizontal diffusion cell. The results showed that the transdermal permeability of lidocaine free base and hydrochloride were significantly different, the former steady-state flow of the latter 14 times, and the lag time is short, the steady-state flow rate of pH plot was 揝 斝 Steady state flow suddenly increases when pH approaches pKa. Thus, the pH value of the medium affects the transdermal permeability of lidocaine, the formulation should be considered as an important factor.