口服屈它维林产生药物不良反应者与正常者血药浓度的对比研究

The Study on Plasma Concentration of Drotaverine in Normal Volunteers and Volunteer with Adverse Reaction

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 concentrations of drotaverine in normal volunteers and volunteer with adverse reaction. METHOD: 20 healthy males were selected as volunteers. after administration of single 80 mg oral doses, the plasma concentrations of the drug were determined by HPLC with UV detector. RESULTS: a volunteer accompanied transiant dizziness, headache and palpitation was discovered. His Cmax and AUC of the drug were 1067ug.L-1.h and 5520ug.L-1.h respectively, and were 2.28and 2.34 times higher of the mean values of the Cmax (468 f 130g.L-1.h)and AUC (2357 1 753pg.L-1.h), respectively. CONCLUSION: The bioavailability of drotaverine was of significant interindividual difference.The high concentration in blood may be the reason of adverse reaotion.