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用于生物制药研究的血浆样本中布比卡因的高效液相色谱测定及其在其他七种局部麻醉药中的应用。

High-performance liquid chromatographic determination of bupivacaine in plasma samples for biopharmaceutical studies and application to seven other local anaesthetics.

作者信息

Le Guévello P, Le Corre P, Chevanne F, Le Verge R

机构信息

Laboratoire de Pharmacie Galénique, Université de Rennes I, France.

出版信息

J Chromatogr. 1993 Dec 22;622(2):284-90. doi: 10.1016/0378-4347(93)80279-d.

DOI:10.1016/0378-4347(93)80279-d
PMID:8150879
Abstract

A sensitive analytical procedure for bupivacaine dosing in plasma samples by reversed-phase high-performance liquid chromatography is described. After a two-step extraction, the analysis was performed using a C18 column and a mobile phase of 0.01 M sodium dihydrogen-phosphate (pH 2.1)-acetonitrile (80:20, v/v). The extraction yield of bupivacaine from plasma was 73.5 +/- 5.1% (mean +/- S.D., n = 10). The within-day and between-day reproducibilities at a concentration of 100 ng/ml were 2.1% and 5.6%, respectively (n = 10). Calibration curves were linear (r2 = 0.9996) between 5 and 1000 ng/ml. The limit of detection, defined by a signal-to-noise ratio of 3:1, was 2 ng/ml. The accuracy at a concentration of 100 ng/ml was 2.3%. This method could be applied to the plasma analysis of seven other local anaesthetics (articaine, etidocaine, lidocaine, mepivacaine, pramocaine, procaine and tetracaine). The procedure was used in bioavailability studies of bupivacaine-loaded poly(D,L-lactide) (i.e. PLA) and poly(D,L-lactide-co-glycolide) (i.e. PLGA) microspheres after subcutaneous and intrathecal administrations in rabbits.

摘要

描述了一种采用反相高效液相色谱法测定血浆样品中布比卡因剂量的灵敏分析方法。经过两步萃取后,使用C18柱和0.01 M磷酸二氢钠(pH 2.1)-乙腈(80:20,v/v)的流动相进行分析。布比卡因从血浆中的萃取率为73.5±5.1%(平均值±标准差,n = 10)。在浓度为100 ng/ml时,日内和日间重现性分别为2.1%和5.6%(n = 10)。校准曲线在5至1000 ng/ml之间呈线性(r2 = 0.9996)。由3:1的信噪比定义的检测限为2 ng/ml。在浓度为100 ng/ml时的准确度为2.3%。该方法可应用于其他七种局部麻醉剂(阿替卡因、依替卡因、利多卡因、甲哌卡因、丙胺卡因、普鲁卡因和丁卡因)的血浆分析。该程序用于研究布比卡因负载的聚(D,L-丙交酯)(即PLA)和聚(D,L-丙交酯-共-乙交酯)(即PLGA)微球在兔皮下和鞘内给药后的生物利用度。

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