贝诺酯在人血浆和人肝脏中的水解作用。
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
- 已对贝诺酯（4-乙酰氨基苯基-O-乙酰水杨酸酯）在人血浆、人肝微粒体和胞质溶胶中的体外水解情况进行了研究。2. 贝诺酯通过一条途径水解，该途径涉及乙酰基首先水解生成非那西汀，随后水解为对乙酰氨基酚和水杨酸。通过乙酰水杨酸的水解作用较小。3. 贝诺酯在肝细胞溶胶中的水解比在微粒体中更活跃，且比在血浆中快约10倍。4. 给志愿者单次口服4克贝诺酯后，血浆中仅检测到水杨酸和对乙酰氨基酚。5. 贝诺酯的治疗作用似乎是由水杨酸和对乙酰氨基酚介导的。
相似文献
1
Benorylate hydrolysis by human plasma and human liver.贝诺酯在人血浆和人肝脏中的水解作用。
Br J Clin Pharmacol. 1989 Dec;28(6):703-8. doi: 10.1111/j.1365-2125.1989.tb03563.x.
2
Comparative metabolism of benorylate and an equivalent mixture of aspirin and paracetamol in neonate and adult rabbits.
Xenobiotica. 1977 Sep;7(9):561-71. doi: 10.3109/00498257709038691.
3
Absence of mutagenic activity of benorylate, paracetamol and aspirin in the Salmonella/mammalian microsome test.
Mutat Res. 1987 Feb;190(2):95-100. doi: 10.1016/0165-7992(87)90038-8.
4
Esterase activity in rat hepatocytes.
Biochem Pharmacol. 1991 Feb 15;41(4):527-31. doi: 10.1016/0006-2952(91)90624-e.
5
Distribution of benorylate in plasma, synovial fluid and tissue in rheumatoid arthritis.
Scand J Rheumatol Suppl. 1975;13:13-7. doi: 10.3109/03009747609095637.
6
[The distribution of benorylate in plasma, synovial fluid and synovial tissue in rheumatoid arthritis].[贝诺酯在类风湿关节炎患者血浆、滑液及滑膜组织中的分布]
Z Rheumatol. 1975 Nov-Dec;34(11-12):400-7.
7
A review of benorylate - a new antirheumatic drug.
Scand J Rheumatol Suppl. 1975;13:5-8.
8
The absorption and metabolism in man of 4-acetamidophenyl-2-acetoxybenzoate (benorylate).
Xenobiotica. 1972 Jul;2(4):339-47. doi: 10.3109/00498257209111061.
9
Simultaneous pharmacokinetics of benorylate in plasma and synovial fluid of patients with rheumatoid arthritis.
Scand J Rheumatol Suppl. 1975;13:9-12.
10
引用本文的文献
1
Exploring acetaminophen prodrugs and hybrids: a review.对乙酰氨基酚前药与杂合物的研究综述
RSC Adv. 2024 Mar 22;14(14):9691-9715. doi: 10.1039/d4ra00365a. eCollection 2024 Mar 20.
2
Conversion and pharmacokinetics profiles of a novel pro-drug of 3-n-butylphthalide, potassium 2-(1-hydroxypentyl)-benzoate, in rats and dogs.新型 3-正丁基苯酞前药，2-(1-羟戊基)苯甲酸钾在大鼠和犬体内的转化和药代动力学特征。
Acta Pharmacol Sin. 2018 Feb;39(2):275-285. doi: 10.1038/aps.2017.90. Epub 2017 Sep 14.
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.阿司匹林在术后牙痛中的代谢及疗效
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.口服水溶液后阿司匹林在人体中的吸收动力学。
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.药物代谢的血清酶
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.
Zotero 插件