Pharmacokinetic profile of a novel slow release preparation of molsidomine.
A novel slow release preparation containing 24 mg molsidomine has been investigated in 6 healthy subjects. Individual concentration/time-profiles after the tablet showed two separate concentration peaks at 2.2 h and 15.0 h. The relative bioavailability of the slow release preparation in comparison to an aqueous solution of molsidomine was 0.67. The in vivo dissolution profile revealed either a progressive decrease in dissolution velocity caused by altered physico-chemical conditions in the ileum and the colon or a progressive reduction in the absorption constant. In all subjects deconvolution revealed a punctual increase in absorption about 15 h post-dose, coinciding with the second peak of the concentration/time-profile. Therapeutic plasma levels of molsidomine (greater than 5 ng.ml-1) were not maintained over 24 h by this slow release formulation.
Rietbrock
S
S
Department of Clinical Pharmacology, Johann Wolfgang Goethe-University, Frankfurt, FRG.
Keller-Stanislawski
B
B
Thürmann
P
P
Brockmeier
D
D
D000328:Adult; D001682:Biological Availability; D003692:Delayed-Action Preparations; D006801:Humans; D007408:Intestinal Absorption; D008297:Male; D008981:Molsidomine / Q000008:administration & dosage / Q000493:pharmacokinetics*; D012995:Solubility
D003692:Delayed-Action Preparations; D008981:Molsidomine