Schoenwald R D, Ward R L
J Pharm Sci. 1978 Jun;67(6):786-8. doi: 10.1002/jps.2600670614.
Permeability rates were determined across excised rabbit corneas for 11 steroids. Permeability coefficients for each steroid were calculated, and their logarithms were plotted against their respective log octanol-water partition coefficients. A parabolic relationship resulted, with an optimum log permeability and coefficient observed at a log Po of 2.9. From these experimental results, an improvement in ophthalmic bioavailability of dexamethasone acetate as compared to dexamethasone is predicted and correlates with literature results.
测定了11种类固醇通过切除的兔角膜的渗透率。计算了每种类固醇的渗透系数,并将其对数与各自的正辛醇-水分配系数的对数作图。结果得到一种抛物线关系,在log Po为2.9时观察到最佳的对数渗透率和系数。根据这些实验结果,预计醋酸地塞米松与地塞米松相比,其眼用生物利用度会有所提高,且与文献结果相关。