Bun H, Philip F, Berger Y, Necciari J, Al-Mallah N R, Serradimign A, Cano J P
Arzneimittelforschung. 1987 Feb;37(2):199-202.
The pharmacokinetics of tetrazepam (Myolastan, Musaril), were studied in 12 healthy volunteers. Tetrazepam was given orally as a single dose of 50 mg and repeated administration for 5 consecutive days of 50 mg at 12-h intervals, in tablet form. Tetrazepam was measured in plasma using a selective and sensitive GLC method. Tetrazepam is rapidly absorbed after oral administration with a peak plasma level of 0.49 +/- 0.10 mg/l at 0.94 +/- 0.47 h. The drug is widely distributed in the organism with an apparent volume of distribution of 6.7 +/- 2.1 l/kg. Tetrazepam is eliminated with a half-life of 22 +/- 4 h and can be classified as a benzodiazepine with medium half-life value. This medium half-life is the result of the high hepatic clearance of the drug in spite of its large distribution volume. Since in this study 6 male and 6 female volunteers were studied it was possible to compare the pharmacokinetic profile in the two groups. No significant differences were observed. No differences were observed between the pharmacokinetic values after a single dose or after repeated administration.
在12名健康志愿者身上研究了四氮唑安定（Myolastan、Musaril）的药代动力学。四氮唑安定以片剂形式口服，单次剂量为50毫克，并以50毫克的剂量每12小时给药一次，连续给药5天。采用选择性灵敏的气相色谱法测定血浆中的四氮唑安定。口服给药后，四氮唑安定吸收迅速，在0.94±0.47小时达到血浆峰值水平0.49±0.10毫克/升。该药物在体内广泛分布，表观分布容积为6.7±2.1升/千克。四氮唑安定的消除半衰期为22±4小时，可归类为具有中等半衰期值的苯二氮䓬类药物。尽管其分布容积较大，但该药物肝脏清除率高，导致其半衰期中等。由于本研究中对6名男性和6名女性志愿者进行了研究，因此可以比较两组的药代动力学特征。未观察到显著差异。单次给药或重复给药后的药代动力学值之间也未观察到差异。
