Jorgensen A
Eur J Clin Pharmacol. 1977 Nov 14;12(3):187-90. doi: 10.1007/BF00609858.
A sustained release preparation of amitriptyline has been compared with conventional tablets in eight healthy human volunteers. The tablet produced a distinct peak in serum concentration shortly after administration, whereas the sustained release preparation caused a slow rise to a plateau. The maximum serum concentration and the time of its occurrence differed significantly between the two preparations. The differences between the serum concentration curves of the two preparations can be explained on the basis of a two compartment model of amitriptyline pharmacokinetics and from a difference in the absorption rate. The similar clinical effect obtained with a lower daily dose of the sustained release preparation than of the tablet cannot be accounted for in terms of pharmacokinetics. It is possible that a single evening dose of sustained release amitriptyline gives a more appropriate serum concentration profile of amitriptyline and its active metabolite nortriptyline than a conventional tablet taken three times a day.
在8名健康志愿者中，对阿米替林缓释制剂与传统片剂进行了比较。服用传统片剂后血清浓度很快出现明显峰值，而缓释制剂则使血清浓度缓慢上升至平稳状态。两种制剂的最大血清浓度及其出现时间差异显著。两种制剂血清浓度曲线的差异可根据阿米替林药代动力学的二室模型及吸收速率差异来解释。与传统片剂相比，较低日剂量的缓释制剂能产生相似的临床效果，这无法从药代动力学角度进行解释。与每日服用3次的传统片剂相比，单次晚间服用缓释型阿米替林可能会使阿米替林及其活性代谢物去甲替林的血清浓度分布更为合适。
