White C, Doyle E, Chasseaud L F, Taylor T
Eur J Clin Pharmacol. 1976 Sep 30;10(5):343-7. doi: 10.1007/BF00565624.
Concentrations of methaqualone have been measured in the serum of five male human subjects receiving five consecutive evening doses of a combination formulation containing methaqualone (250 mg), carbromal (300 mg) and benactyzine (0.33 mg) in each tablet. After administration of the first dose, mean peak serum concentrations of methaqualone (1.2 mug/ml) occurred at 3 h. After obtaining peak levels, mean concentrations of methaqualone declined rapidly during the next 6 h and thereafter more slowly during the next 18 h. After administration of the last (fifth) dose, mean peak serum concentrations of methaqualone (1.9 mug/ml; 1.5 mug/ml above the predose level) occurred at 2 h. After attaining peak levels, mean concentrations of methaqualone declined rapidly during the next 6 h, and thereafter more slowly, with a half-life of approximately 10 h. Mean concentrations of methaqualone in serum samples 24 h after the second, third, fourth or fifth doses were not significantly different (0.3 mug/ml - 0.6 mug/ml) during this period of dosing. This suggests that significant accumulation of methaqualone in the serum did not occur during a period of five consecutive evening doses of the combination formulation.
对五名男性受试者进行了研究，他们连续五个晚上服用了一种复方制剂，每片制剂含甲喹酮（250毫克）、溴米那（300毫克）和苯乃嗪（0.33毫克），并测定了血清中甲喹酮的浓度。服用首剂后，甲喹酮的血清平均峰值浓度（1.2微克/毫升）在3小时出现。达到峰值水平后，甲喹酮的平均浓度在接下来的6小时内迅速下降，之后在接下来的18小时内下降更为缓慢。服用最后一剂（第五剂）后，甲喹酮的血清平均峰值浓度（1.9微克/毫升；比给药前水平高1.5微克/毫升）在2小时出现。达到峰值水平后，甲喹酮的平均浓度在接下来的6小时内迅速下降，之后下降更为缓慢，半衰期约为10小时。在给药期间，第二、第三、第四或第五剂后24小时血清样本中甲喹酮的平均浓度无显著差异（0.3微克/毫升 - 0.6微克/毫升）。这表明在连续五个晚上服用该复方制剂期间，血清中甲喹酮未出现显著蓄积。
