Vahlquist A, Rollman O
Department of Dermatology, Uppsala University, Akademiska Hospital, Sweden.
Dermatologica. 1987;175 Suppl 1:20-7. doi: 10.1159/000248850.
The bioavailability, plasma transport and tissue distribution of various retinoids are largely determined by their physicochemical properties; some are extremely lipidsoluble whereas others are relatively hydrophilic. Isotretinoin, a 1st generation retinoid, lacks the problematic affinity for fat. Etretinate, a 2nd generation aromatic retinoid, has been shown to accumulate in both fat tissues and in the adrenals. Etretin, the main free-acid metabolite of etretinate, is less lipophilic and is presently being tested as an alternative drug. Arotinoid ethyl ester, a 3rd generation aromatic retinoid which has as yet only undergone limited trials, is extremely potent making pharmacological evaluation difficult. The search for more potent retinoids has not so far resulted in a complete resolution of the efficacy and toxicity of the drugs.
各种类视黄醇的生物利用度、血浆转运和组织分布在很大程度上取决于它们的物理化学性质；有些类视黄醇具有极高的脂溶性，而其他的则相对亲水。第一代类视黄醇异维A酸对脂肪没有问题性的亲和力。第二代芳香族类视黄醇阿维A酯已被证明会在脂肪组织和肾上腺中蓄积。阿维A是阿维A酯的主要游离酸代谢产物，亲脂性较低，目前正在作为替代药物进行测试。第三代芳香族类视黄醇芳维A酸乙酯目前仅进行了有限的试验，效力极强，使得药理学评估变得困难。到目前为止，寻找更有效的类视黄醇尚未完全解决这些药物的疗效和毒性问题。
