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。
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