Radioimmunoassay of flurazepam in human plasma.

Radioimmunoassay of flurazepam in human plasma.
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人血浆中氟西泮的放射免疫测定。

DOI:
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发表时间:
1980
期刊:
Journal of Pharmacy and Science
影响因子:
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通讯作者:
R. Dixon
R. Dixon
中科院分区:
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文献类型:
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作者:
W. Glover;J. Earley;M. Delaney;R. Dixon

文献摘要

被引文献

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建立了测定催眠药氟西潘血药浓度的放射免疫分析方法。在口服治疗剂量后,测量了完整氟西潘的血药浓度。该方法使用3-琥珀酰氧氟西潘与牛血清白蛋白共价偶联的兔抗血清和氚标记的氟西潘作为放射性配基。在分析前,通过Sephadex LH-20从血浆提取物中分离氟西潘来实现分析的特异性。该方法的灵敏度为0.1 ng/ml血浆样品,批内和批间变异系数在0.1-5 ng/ml范围内不超过9%,8名受试者单次注射30 mg氟西泮后0.5-1小时血药浓度达峰值,1名受试者血药浓度峰值出现在4小时。氟西潘的血药浓度下降,平均表观半衰期为2.3小时。
A radioimmunoassay for the determination of the hypnotic flurazepam in plasma was developed. Plasma levels of intact flurazepam were measured following oral administration of therapeutic doses to humans. The procedure employs an antiserum obtained from a rabbit immunized with 3-hemisuccinyloxyfluorazepam covalently coupled to bovine serum albumin and tritium-labeled flurazepam as the radioligand. Assay specificity was achieved by chromatographic isolation of flurazepam from plasma extracts on Sephadex LH-20 prior to analysis. The method has a sensitivity limit of 0.1 ng of flurazepam/ml using a 1-ml plasma sample, and the intra- and interassay coefficients of variation did not exceed 9% over a range of 0.1-5 ng/ml. In eight subjects who received a single 30-mg dose of flurazepam, peak plasma concentrations of 0.5-3.0 ng of intact drug/ml were reached after 0.5-1 hr, except in one subject where the peak occurred at 4 hr. The plasma concentrations of flurazepam declined with a harmonic mean apparent half-life of 2.3 hr.