Fincher T K, Yoo S D, Player M R, Sowell J W, Michniak B B
College of Pharmacy, University of South Carolina, Columbia 29208, USA.
J Pharm Sci. 1996 Sep;85(9):920-3. doi: 10.1021/js9600787.
A series of N-dodecanoyl-L-amino acid methyl esters (1-10) and n-pentyl N-acetylprolinate (11) were evaluated for dermal enhancement properties using an in vitro diffusion cell technique. Methods of synthesis of these compounds were described. Enhancers were applied 1 h prior to drug treatment. Hydrocortisone was used as the model drug and was applied to excised hairless mouse skin as a saturated suspension in propylene glycol. Enhancement ratios (ER) were determined for permeability coefficient, 24 h diffusion cell receptor concentration (Q24), and 24 h full-thickness skin steroid content. Controls received no enhancer pretreatment of the skin. N-Dodecanoyl-L-proline (10) showed the highest Q24 value for total steroid (ER 13.7) while N-dodecanoyl-L-phenylalanine (5) showed the highest total steroid skin retention (ER 16.5).
使用体外扩散池技术评估了一系列N-十二烷酰-L-氨基酸甲酯（1-10）和正戊基N-乙酰脯氨酸酯（11）的皮肤增强特性。描述了这些化合物的合成方法。在药物处理前1小时应用增强剂。氢化可的松用作模型药物，并以丙二醇中的饱和悬浮液形式应用于切除的无毛小鼠皮肤。测定了渗透系数、24小时扩散池受体浓度（Q24）和24小时全层皮肤类固醇含量的增强率（ER）。对照组未对皮肤进行增强剂预处理。N-十二烷酰-L-脯氨酸（10）显示总类固醇的Q24值最高（ER 13.7），而N-十二烷酰-L-苯丙氨酸（5）显示总类固醇皮肤保留率最高（ER 16.5）。
