Burch J E, Hullin R P
Psychopharmacology (Berl). 1981;74(1):43-50. doi: 10.1007/BF00431755.
Two separate single doses of Lentizol (W. R. Warner, Pontypool, U.K.), a sustained-release preparation of amitriptyline (AT) were taken by each of six healthy subjects. Plasma concentrations of AT and of nortriptyline (NT) were determined at intervals over a period of 48 or 72 h. Faeces were collected and their drug content measured. Results were compared with those obtained when the same subjects took ordinary AT tablets. AT was found in the faeces after the ingestion of Lentizol or of ordinary AT tablets. However, after NT tablets negligible amounts of NT appeared in the faeces. AT was sometimes absorbed slowly from Lentizol, but on other occasions it was absorbed as rapidly as from ordinary tablets. Plasma levels of AT 24 h after the dose were usually not higher after Lentizol than after an equal dose of ordinary tablets. The systemic bioavailability of Lentizol as judged by areas under the plasma concentration-time curves, both for AT and for the NT formed metabolically, was on average lower than that of the ordinary tablets. However, the amounts of AT found in the faeces were not large enough to account for the AT area reduction by simple failure of absorption. Possible explanations of the discrepancy are discussed.
六名健康受试者每人服用了两剂单独的缓释阿米替林（AT）制剂Lentizol（英国庞蒂浦的W. R. 华纳公司生产）。在48或72小时的时间段内定期测定血浆中AT和去甲替林（NT）的浓度。收集粪便并测量其中的药物含量。将结果与同一受试者服用普通AT片剂时获得的结果进行比较。服用Lentizol或普通AT片剂后，粪便中均发现了AT。然而，服用NT片剂后，粪便中出现的NT量可忽略不计。AT有时从Lentizol中吸收缓慢，但在其他情况下，其吸收速度与从普通片剂中吸收的速度一样快。服用剂量24小时后，Lentizol后的AT血浆水平通常不比等剂量普通片剂后的高。根据血浆浓度-时间曲线下的面积判断，Lentizol中AT及其代谢形成的NT的全身生物利用度平均低于普通片剂。然而，粪便中发现的AT量不足以通过单纯的吸收失败来解释AT曲线下面积的减少。讨论了这种差异的可能解释。
