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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 transdermal absorption of naproxen in different pH conditions. Methods: The solubility of naproxen in different pH media was determined. The in vitro dermal penetration rate of naproxen through rat skin was measured by using Valia-Chien diffusion cell. Results: The steady-state transdermal rate of naproxen increased with the increase of pH, but the permeability coefficient of naproxen decreased with the increase of pH. According to the different route of molecular drugs and ionic drugs through the skin, the steady-state transdermal rate and the relationship between the permeability coefficient and hydrogen ion concentration are established by the parallel diffusion model. CONCLUSIONS: Transdermal permeation rates of naproxen or some weakly acidic and weakly basic drugs can be increased by adjusting pH when the drug is saturated in the medium.