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使用不同抗凝剂在体外血浆、全血和血清中进行异丁苯丙酸皮考诺酯水解实验。

Ibuprofen piconol hydrolysis in vitro in plasma, whole blood, and serum using different anticoagulants.

作者信息

Christensen J M, Stalker D

机构信息

College of Pharmacy, Oregon State University, Corvallis 97331.

出版信息

J Pharm Sci. 1991 Jan;80(1):29-31. doi: 10.1002/jps.2600800108.

Abstract

Hydrolysis kinetics of ibuprofen piconol to ibuprofen were determined in vitro in plasma, whole blood, and serum. Varying initial concentrations of ibuprofen piconol with different anticoagulants (EDTA, heparin, citrate, or no anticoagulant) were used in determining the effects each had on the rate of ibuprofen piconol hydrolysis. Varying the initial concentration of ibuprofen piconol did not alter the hydrolysis half-life (concentration range from 50 to 200 micrograms/mL). The anticoagulant used altered the hydrolysis half-life. For plasma, the half-life was shortest when no anticoagulant was present (t 1/2 = 2.5 h) and longer with the presence of anticoagulants; for citrate, t 1/2 = 8.0 h, for heparin; t 1/2 = 15.5 h; and for EDTA, t 1/2 = 161.8 h. Red blood cell uptake of ibuprofen piconol was minimal and ranged from 0.4 to 4.1% over the ibuprofen piconol concentrations used in the study.

摘要

在体外对血浆、全血和血清中匹考布洛芬水解为布洛芬的动力学进行了测定。在测定不同抗凝剂(乙二胺四乙酸、肝素、柠檬酸盐或无抗凝剂)对匹考布洛芬水解速率的影响时,使用了不同初始浓度的匹考布洛芬。改变匹考布洛芬的初始浓度不会改变水解半衰期(浓度范围为50至200微克/毫升)。所使用的抗凝剂会改变水解半衰期。对于血浆,不存在抗凝剂时半衰期最短(t1/2 = 2.5小时),存在抗凝剂时半衰期更长;对于柠檬酸盐,t1/2 = 8.0小时,对于肝素,t1/2 = 15.5小时,对于乙二胺四乙酸,t1/2 = 161.8小时。在所研究的匹考布洛芬浓度范围内,红细胞对匹考布洛芬的摄取极少,范围为0.4%至4.1%。

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