Sasaki H, Kojima M, Nakamura J, Shibasaki J
Faculty of Pharmaceutical Sciences, Nagasaki University, Japan.
J Pharmacobiodyn. 1990 Mar;13(3):200-5. doi: 10.1248/bpb1978.13.200.
The enhancing effect of pyrrolidone derivatives on the percutaneous penetration of sulfaguanidine, aminopyrine and sudan III was investigated using in vitro technique and excised rat skin. 1-Methyl (MP), 1-hexyl (HP) and 1-lauryl-2-pyrrolidone (LP) were used as penetration enhancers. Aminopyrine showed high penetration through skin although sulfaguanidine and sudan III showed little penetration. Pyrrolidone derivatives enhanced their penetrations. Especially HP and LP enhanced the penetration of sulfaguanidine to a high extent. Sudan III was not detected in the receptor phase regardless of the presence of enhancer. Pyrrolidone derivatives significantly increased the skin accumulation of sulfaguanidine, aminopyrine and sudan III. Penetration of pyrrolidone derivatives was also determined. MP and HP showed high penetrations. LP was not detectable in the receptor phase. MP, HP and LP showed high skin accumulations. These results suggested the usefulness of pyrrolidone derivatives as percutaneous penetration enhancers.
采用体外技术和大鼠离体皮肤，研究了吡咯烷酮衍生物对磺胺胍、氨基比林和苏丹Ⅲ经皮渗透的增强作用。使用1-甲基（MP）、1-己基（HP）和1-月桂基-2-吡咯烷酮（LP）作为渗透促进剂。氨基比林经皮肤的渗透率较高，而磺胺胍和苏丹Ⅲ的渗透率较低。吡咯烷酮衍生物可提高它们的渗透率。特别是HP和LP能极大地提高磺胺胍的渗透率。无论是否存在促进剂，在接受液相中均未检测到苏丹Ⅲ。吡咯烷酮衍生物显著增加了磺胺胍、氨基比林和苏丹Ⅲ在皮肤中的蓄积量。还测定了吡咯烷酮衍生物的渗透率。MP和HP的渗透率较高。在接受液相中未检测到LP。MP、HP和LP在皮肤中的蓄积量较高。这些结果表明吡咯烷酮衍生物作为经皮渗透促进剂具有实用性。
