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目的:研究口服屈它维林产生药物不良反应者与正常者的血药浓度。方法:选取20名20岁左右的健康男性志愿者,每人单剂量口服80mg,HPLC法检测24h内的血药浓度。结果:在20名受试者中发现一例口服屈他维林后产生头昏,头痛,心慌等药物不良反应者,检测其最高血药浓度为1067μg·mL-1,AUC为 5520μg·L-1·h,都明显高于 468± 130μg·L-1·h(范围 234-668μg·L-1·h)和 2357±753μg·L-1·h(范围1456-4355μg·L-1·h)的其他19名正常者的平均值,分别是平均值的 2.28和 2.34倍。结论:口服屈它维林的最高血药浓度和生物利用度有较大的个体差异性,个别人血药浓度的一时性过高可能是药物不良反应的主要原因之一。
OBJECTIVE: To study the plasma concentration of oral warfarin in patients with adverse drug reactions and normal. Methods: Twenty healthy male volunteers, 20 years old, were enrolled in this study. One single oral dose of 80 mg and the HPLC method were used to detect the plasma concentrations within 24 hours. RESULTS: One patient who had dizziness, headache, palpitation and other adverse drug reactions was found in 20 subjects. The highest plasma concentration was 1067 μg · mL-1 and the AUC was 5520 μg · L-1 · H were significantly higher than 468 ± 130μg · L-1 · h (range 234-668μg · L-1 · h) and 2357 ± 753μg · L-1 · h (range 1456-4355μg · L-1 · h) Of the other 19 normal average, respectively, 2.28 and 2.34 times the average. Conclusions: The highest plasma concentration and bioavailability of oral warfarin have more individual differences. One-time hypernatremia of individual blood concentration may be one of the main causes of adverse drug reactions.