Ubels J L, Edelhauser H F
Arch Ophthalmol. 1982 Nov;100(11):1828-31. doi: 10.1001/archopht.1982.01030040808021.
In vitro perfusion of corneas of normal and vitamin A-deficient rabbits provided a model in which to study the pharmacokinetics of corneal permeability and uptake of retinoic acid and retinol. The permeability coefficients of retinoic acid and retinol were 1.49 x 10(-5) and 0.61 x 10(-5) cm/s, respectively. Removal of the corneal epithelium did not affect the permeability of these lipid-soluble retinoids; however, diffusion through xerophthalmic, vitamin A-deficient corneas was significantly reduced. The corneal uptake of retinoic acid and retinol was reduced by 50% on removal of the epithelium, was nonspecific, and was not affected by xerophthalmia. High-performance liquid chromatography indicated that these retinoids were not metabolized during diffusion through the cornea. These results show that topical application of retinoids is a rational approach to the treatment of such corneal diseases as xerophthalmia and epithelial defects.
对正常和维生素A缺乏的兔子角膜进行体外灌注，提供了一个研究视黄酸和视黄醇角膜通透性及摄取的药代动力学模型。视黄酸和视黄醇的通透系数分别为1.49×10⁻⁵和0.61×10⁻⁵ cm/s。去除角膜上皮不影响这些脂溶性类视黄醇的通透性；然而，通过干眼症、维生素A缺乏的角膜的扩散显著减少。去除上皮后，视黄酸和视黄醇的角膜摄取减少50%，是非特异性的，且不受干眼症影响。高效液相色谱表明，这些类视黄醇在通过角膜扩散过程中未被代谢。这些结果表明，局部应用类视黄醇是治疗干眼症和上皮缺损等角膜疾病的合理方法。
