pH对萘普生透皮速率的影响

Effect of pH on percutaneous absorption of naproxen

目的:通过对萘普生在不同pH条件下透皮速率的研究,考察介质pH对药物透皮吸收的影响。方法:测定萘普生在不同pH介质中的溶解度,使用Valia-Chien扩散池测定萘普生通过大鼠皮肤的体外透皮速率。结果:萘普生的稳态透皮速率随pH升高而增大,而表现渗透系数则随pH升高而减少。根据分子型药物与离子型药物通过皮肤的途径不同,用平行扩散模型建立了稳态透皮速率和表现渗透系数与氢离子浓度的关系式。结论:当药物在介质中饱和时,可以通过调节pH增加萘普生或一些弱酸性和弱碱性药物的经皮渗透速率。

OBJECTIVE: To study the effect of pH on penetration of naproxen through skin. METHODS: Thesolubilities of naproxen in different pH vehicles was determined. The penetration rate of naproxen through rat skin in vitro was measured using Valia-Chien diffusion cell. RESULTS: When the pH in the donor compartment of the diffusion cell was increased the steady state flux of naproxen was increased, on the contrary, the apparent permeability coefficient was decreased. A mathematical formula was derived from the parallel diffusion mold to explaine relationship between the concentration of hydrogen ion and the steady state flux as well as apparent permeability coefficient. CONCLUSION: On the saturation condition of drug in vehicle, changing the pH may increse the penetration rate of naproxen or other weak acid and base drugs through the skin.