Benorylate hydrolysis by human plasma and human liver.
作者信息
Williams F M, Moore U, Seymour R A, Mutch E M, Nicholson E, Wright P, Wynne H, Blain P G, Rawlins M D
机构信息
Wolfson Unit of Clinical Pharmacology, Department of Operative Dentistry, Medical School, University of Newcastle upon Tyne.
出版信息
Br J Clin Pharmacol. 1989 Dec;28(6):703-8. doi: 10.1111/j.1365-2125.1989.tb03563.x.
Abstract
- 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.
摘要
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本文引用的文献
1
Plasma aspirin esterases in normal individuals, patients with alcoholic liver disease and rheumatoid arthritis: characterization and the importance of the enzymic components.
Eur J Clin Invest. 1980 Oct;10(5):413-20. doi: 10.1111/j.1365-2362.1980.tb00054.x.
2
Aspirin metabolism and efficacy in postoperative dental pain.
Br J Clin Pharmacol. 1984 Jun;17(6):697-701. doi: 10.1111/j.1365-2125.1984.tb02406.x.
3
Absorption kinetics of aspirin in man following oral administration of an aqueous solution.
J Pharm Sci. 1972 Mar;61(3):379-85. doi: 10.1002/jps.2600610312.
4
The absorption and metabolism in man of 4-acetamidophenyl-2-acetoxybenzoate (benorylate).
Xenobiotica. 1972 Jul;2(4):339-47. doi: 10.3109/00498257209111061.
5
Comparison of aspirin and benorylate in the treatment of rheumatoid arthritis.
Br Med J. 1972 May 27;2(5812):483-5. doi: 10.1136/bmj.2.5812.483.
6
Serum enzymes of drug metabolism.
Pharmacol Ther. 1987;34(1):99-109. doi: 10.1016/0163-7258(87)90094-5.
7
Human liver and plasma aspirin esterase.
J Pharm Pharmacol. 1989 Jun;41(6):407-9. doi: 10.1111/j.2042-7158.1989.tb06487.x.
8
The efficacy of benorylate in postoperative dental pain.
Eur J Clin Pharmacol. 1989;36(1):35-8. doi: 10.1007/BF00561020.
9
A comparison of benorylate and naproxen in degenerative arthritis.
Rheumatol Rehabil. 1978 Feb;17(1):29-33. doi: 10.1093/rheumatology/17.1.29.
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