Dubois J P, Küng W, Theobald W, Wirz B
Clin Chem. 1976 Jun;22(6):892-7.
To quantitatively determine tricyclic antidepressant agents, we used a combined gas chromatograph/mass spectrometer system, and deuterium-labeled internal standards. Recovery exceeds 95% and the coefficient of variation is less than 4% for human whole-blood samples supplemented with 5 to 15 ng of clomipramine hydrochloride or 20 to 60 ng of dehydroimipramine hydrogen fumarate per milliliter. For both amines, the detection limit is 0.3 mug/liter; Six healthy volunteers who received a single oral dose of 50 mg of clomipramine hydrochloride showed peak drug concentrations in the blood 3 to 5 h after administration, ranging between 14.4 and 30.1 mug/liter. Plasma/whole blood concentration ratios varied from 0.70 to 1.20, and the cumulative renal elimination from 0 to 72 h is less than 0.2% of the dose. This method is suitable for in vivo bioavailability studies of unchanged clomipramine, dehydroimipramine, and imipramine after a single oral dose of as little as 25 mg.
为了定量测定三环类抗抑郁药，我们使用了气相色谱/质谱联用系统以及氘标记内标。对于每毫升添加5至15纳克盐酸氯米帕明或20至60纳克富马酸氢去甲丙咪嗪的人全血样本，回收率超过95%，变异系数小于4%。对于这两种胺类，检测限均为0.3微克/升；六名健康志愿者单次口服50毫克盐酸氯米帕明后，给药后3至5小时血液中药物浓度达到峰值，范围在14.4至30.1微克/升之间。血浆/全血浓度比在0.70至1.20之间，0至72小时的累积肾脏清除率小于给药剂量的0.2%。该方法适用于单次口服低至25毫克后未变化的氯米帕明、去甲丙咪嗪和丙咪嗪的体内生物利用度研究。
