Bodor N S, Kiss-Buris S T, Buris L
Center for Drug Design and Delivery, College of Pharmacy, University of Florida, Gainesville 32610.
Steroids. 1991 Aug;56(8):434-9. doi: 10.1016/0039-128x(91)90032-q.
Evaluation of three "soft" steroids is described. The test compounds were compared with the standard anti-inflammatory steroids betamethasone and prednicarbate in two studies. Soft steroids are designed based on the "inactive metabolite approach" to be rapidly inactivated by predictable metabolism after performing their therapeutic function. Consequently, lower circulating (peripheral) levels of potentially harmful steroids result, and undesirable systemic and local side effects are minimized. The soft and standard steroids behaved similarly in an in vitro cell culture model, whereas in a whole animal study the advantages of the soft steroids were evident.
本文描述了对三种“软”类固醇的评估。在两项研究中,将受试化合物与标准抗炎类固醇倍他米松和丙酰倍他米松进行了比较。软类固醇是基于“无活性代谢物方法”设计的,在发挥其治疗功能后可通过可预测的代谢迅速失活。因此,潜在有害类固醇的循环(外周)水平降低,不良的全身和局部副作用降至最低。在体外细胞培养模型中,软类固醇和标准类固醇的表现相似,而在整体动物研究中,软类固醇的优势很明显。