Pharmacokinetics and bioavailability of reduced and oxidized N-acetylcysteine.
The pharmacokinetics and bioavailability of N-acetylcysteine (NAC) have been determined after its intravenous and oral administration to 6 healthy volunteers. According to a randomized cross-over design each subject received NAC 200 mg i.v. and 400 mg p.o., and blood samples were collected for 30 h. Reduced NAC had a volume of distribution (VSS) of 0.59 l.kg-1 and a plasma clearance of 0.84 l.h-1.kg-1. The terminal half-life after intravenous administration was 1.95 h. The oral bioavailability was 4.0%. Based on total NAC concentration, its volume of distribution (VSS) was 0.47 l.kg-1 and its plasma clearance was 0.11 l.h-1.kg-1. The terminal half-life was 5.58 h after intravenous administration and 6.25 h after oral administration. Oral bioavailability of total NAC was 9.1%.
Olsson
B
B
Research and Development Department, ACO Läkemedel AB, Solna, Sweden.
Johansson
M
M
Gabrielsson
J
J
Bolme
P
P
D000111:Acetylcysteine / Q000008:administration & dosage / Q000097:blood / Q000378:metabolism / Q000493:pharmacokinetics*; D000284:Administration, Oral; D000328:Adult; D001682:Biological Availability; D004334:Drug Administration Schedule; D005260:Female; D006207:Half-Life; D006801:Humans; D007275:Injections, Intravenous; D008297:Male; D010084:Oxidation-Reduction; D011897:Random Allocation; D013223:Statistics as Topic; D013607:Tablets; D013997:Time Factors
D013607:Tablets; D000111:Acetylcysteine