Caron J C, Shroot B
J Pharm Sci. 1984 Dec;73(12):1703-6. doi: 10.1002/jps.2600731210.
Two high-performance liquid chromatographic (HPLC) techniques have been used for the determination of the lipophilicity of 50 glucocorticosteroids. For a log P range of 1 to 3, we used a persilylated octadecylsilane phase saturated with 1-octanol, which was eluted with 1-octanol saturated phosphate buffer (pH = 7). For log P values greater than or equal to 3.00, the same phase was used without 1-octanol saturation and was eluted with different methanol-buffer mixtures. These two procedures allowed the determination of log P values ranging from 1.00 to greater than 5.00. Good agreement was found between these procedures and others described in the literature. The effect of different structural changes in the glucocorticosteroid molecule on the lipophilicity is discussed.
两种高效液相色谱(HPLC)技术已被用于测定50种糖皮质激素的亲脂性。对于log P范围为1至3的情况,我们使用了用1-辛醇饱和的全硅烷化十八烷基硅烷相,并用1-辛醇饱和的磷酸盐缓冲液(pH = 7)洗脱。对于log P值大于或等于3.00的情况,使用相同的相但不进行1-辛醇饱和,并使用不同的甲醇-缓冲液混合物洗脱。这两种方法能够测定log P值范围从1.00至大于5.00。这些方法与文献中描述的其他方法之间具有良好的一致性。讨论了糖皮质激素分子中不同结构变化对亲脂性的影响。