Effect of penetration enhancers on isosorbide dinitrate penetration through rat skin from a transdermal therapeutic system.
Percutaneous absorption of isosorbide dinitrate (ISDN) from a transdermal therapeutic system (TTS) with or without penetration enhancers was studied. The concentration of ISDN and its metabolites, isosorbide-5-mononitrate (IS-5-MN) and isosorbide-2-mononitrate (IS-2-MN), was determined in rat plasma during a 48 h application of TTS. The increased skin-penetration enhancing effect of oleic acid and propylene glycol in comparison to polyethylene glycol 400 and isopropyl myristate on percutaneous permeation of ISDN was shown. It was expressed by higher values of C(max) and AUC. After the application of TTS, a lower ISDN and molar ratio of its metabolites was observed than after oral administration.
Gabiga
H
H
Department of Pharmaceutical Technology, Medical University of Gdańsk, Al. Gen. Hallera 107, 80-416, Gdańsk-Wrzeszcz, Poland.
Cal
K
K
Janicki
S
S
D000279:Administration, Cutaneous; D000818:Animals; D019540:Area Under Curve; D001711:Biotransformation; D005079:Excipients; D007275:Injections, Intravenous; D007548:Isosorbide Dinitrate / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D008297:Male; D009226:Myristates; D019301:Oleic Acid; D011092:Polyethylene Glycols; D019946:Propylene Glycol; D051381:Rats; D017208:Rats, Wistar; D012869:Skin Absorption / Q000187:drug effects*; D014665:Vasodilator Agents / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*
D005079:Excipients; D009226:Myristates; D014665:Vasodilator Agents; C008205:isopropyl myristate; D019301:Oleic Acid; D011092:Polyethylene Glycols; D019946:Propylene Glycol; D007548:Isosorbide Dinitrate