pH对奥沙普秦渗透性的影响

Effects of pH on penetration of oxaprozin

研究 pH对奥沙普秦渗透性的影响。采用Valia Chien扩散池对奥沙普秦进行大鼠离体皮肤的体外渗透性实验 ,并测定奥沙普秦在不同 pH介质中的溶解度。随着供药池中饱和溶液 pH的增加 ,奥沙普秦的表观渗透系数从 1 7 85 4 4× 1 0 -6cm·s-1减小到 1 1 932× 1 0 -6cm·s-1,而稳态渗透速率却从 0 36 78× 1 0 -3 μg·cm-2 ·s-1增加到 1 2 5 96× 1 0 -3 μg·cm-2 ·s-1。因此在经皮给药制剂中 ,通过调节基质的 pH可以提高药物的稳态渗透速率。

This paper is to study the effect of pH on penetration of oxaprozin through the skin. The penetration rate of oxaprozin through the rat skin in vitro was measured using Valia Chien diffusion cell.The solubilities of oxaprozin in different pH vehicles were determined. When the pH in the donor compartment of the diffusion cell was increased the steady state flux of oxaprozin was increased from 0 367 8 ×10 -3 μg·cm -2 ·s -1 to 1 259 6×10 -3 μg·cm -2 ·s -1 , on the contrary, the apparent permeability coefficient was decreased from 17 854 4 ×10 -6 cm·s -1 to 1 193 2 ×10 -6 cm·s -1 . Under the saturation condition of the drug in a vehicle, changing the pH may increase the penetration rates of drugs through the skin.