Enhancing effect of pyrrolidone derivatives on the transdermal penetration of sulfaguanidine, aminopyrine and Sudan III.
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.
Sasaki
H
H
Faculty of Pharmaceutical Sciences, Nagasaki University, Japan.
Kojima
M
M
Nakamura
J
J
Shibasaki
J
J
D000279:Administration, Cutaneous; D000632:Aminopyrine / Q000008:administration & dosage / Q000493:pharmacokinetics*; D000818:Animals; D001391:Azo Compounds / Q000008:administration & dosage / Q000493:pharmacokinetics*; D002855:Chromatography, Thin Layer; D004347:Drug Interactions; D006146:Guanidines / Q000493:pharmacokinetics*; D008297:Male; D011760:Pyrrolidinones / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains; D012869:Skin Absorption / Q000187:drug effects*; D012995:Solubility; D013414:Sulfaguanidine / Q000008:administration & dosage / Q000493:pharmacokinetics*
D001391:Azo Compounds; D006146:Guanidines; D011760:Pyrrolidinones; D000632:Aminopyrine; D013414:Sulfaguanidine; C033006:sudan III