Benorylate hydrolysis by human plasma and human liver.
1. Benorylate (4-acetamido phenyl-O-acetylsalicylate) hydrolysis in vitro by human plasma and by human liver microsomes and cytosol has been investigated. 2. Benorylate was hydrolysed by a route involving initial hydrolysis of the acetyl group to yield phenetsal followed by hydrolysis to paracetamol and salicylate. Hydrolysis via acetylsalicylate was minor. 3. Benorylate was more actively hydrolysed by liver cytosol than microsomes and about 10 times faster than plasma. 4. Following a single oral dose benorylate (4 g) to volunteers only salicylate and paracetamol were detected in the plasma. 5. The therapeutic effects of benorylate appear to be mediated by salicylate and paracetamol.
Williams
F M
FM
Wolfson Unit of Clinical Pharmacology, Department of Operative Dentistry, Medical School, University of Newcastle upon Tyne.
Moore
U
U
Seymour
R A
RA
Mutch
E M
EM
Nicholson
E
E
Wright
P
P
Wynne
H
H
Blain
P G
PG
Rawlins
M D
MD
D000082:Acetaminophen / Q000097:blood; D001241:Aspirin / Q000097:blood / Q000378:metabolism; D002851:Chromatography, High Pressure Liquid; D003600:Cytosol / Q000378:metabolism; D004950:Esterases / Q000378:metabolism; D005260:Female; D006801:Humans; D006868:Hydrolysis; D066298:In Vitro Techniques; D008099:Liver / Q000378:metabolism*; D008297:Male; D008862:Microsomes, Liver / Q000378:metabolism; D012459:Salicylates / Q000097:blood / Q000378:metabolism*
D012459:Salicylates; D000082:Acetaminophen; D004950:Esterases; D001241:Aspirin