Plasma concentrations of isosorbide dinitrate after oral administration of a sustained-release formulation to human subjects.
1. A peak of mean plasma concentrations of isosorbide dinitrate of 5.8 ng/ml was reached at 0.5 h after a single oral dose of 5 mg in a standard tablet formulation. Thereafter mean concentrations declined with a half-life of about 48 min. 2. A peak of mean concentrations of isosorbide dinitrate of 3.2 ng/ml was reached at 2--4 h after a single oral dose of 20mg in a sustained-realease capsule formulation (Iso Mack Retard). Thereafter mean concentrations declined by about twofold during 6 h and were still detectable at 12 h after dosing. 3. When corrected by dose/bodyweight variations, the mean area under the isosorbide dinitrate plasma concentration curve from the sustained-release capule was 76% of that from the standard tablet and this formulation-related difference in bioavailability was statistically significant (p less than 0.05). 4. The results showed that sustained-release formulation is a useful way to maintain plasma concentrations of isosorbide dinitrate for several hours.
D000328:Adult; D001682:Biological Availability; D003692:Delayed-Action Preparations; D006801:Humans; D007548:Isosorbide Dinitrate / Q000008:administration & dosage / Q000097:blood*; D007700:Kinetics; D008297:Male
D003692:Delayed-Action Preparations; D007548:Isosorbide Dinitrate