The degradation behavior of eight tricyclic antidepressants (TCAs; amitriptyline, amoxapine (AMX), imipramine, clomipramine, desipramine, doxepin, dothiepin, and nortriptyline) in artificial gastric juice was investigated to estimate their pharmacokinetics in the stomach. As a result, among the eight TCAs, only AMX was degraded in artificial gastric juice. The degradation was a pseudo first-order reaction; activation energy (Ea) was 88.70 kJ/mol and activation entropy (ΔS) was −80.73 J/K·mol. On the other hand, the recovery experiment revealed that the degradation product did not revert to AMX and accordingly, this reaction was considered to be irreversible. In the AMX degradation experiment, peaks considered to be degradation products A (I) and B (II) were detected at retention times of around 3 min and 30 min in LC/UV measurements, respectively. Structural analysis revealed that compound (I) was [2-(2-aminophenoxy)-5-chlorophenyl]-piperazin-1-yl-methanone, a new compound, and compound (II) was 2-chlorodibenzo[b,f][1,4]oxazepin-11(10H)-one. As for the degradation behavior, it was estimated that AMX was degraded into (II) via (I), i.e., (II) was the final product. The results are expected to be useful in clinical chemistry and forensic science, including the estimation of drugs to be used at the time of judicial dissection and suspected drug addiction.

研究了八种三环抗抑郁药（TCA;阿米替林，阿莫沙平（AMX），丙咪嗪，氯米帕明，地昔帕明，多塞平，多西平和去甲替林）的降解行为，以评估其在胃中的药代动力学。结果，在八个TCA中，只有AMX在人造胃液中降解了。降解是假的一级反应。活化能（Ea）为88.70kJ / mol，活化熵（ΔS）为-80.73J / K·mol。另一方面，回收率实验表明降解产物没有还原为AMX，因此该反应被认为是不可逆的。在AMX降解实验中，峰被视为降解产物A（I）和B（II）在LC / UV测量中分别在约3分钟和30分钟的保留时间被检测到。结构分析表明，化合物（I）为新化合物[2-（2-氨基苯氧基）-5-氯苯基]哌嗪-1-基-甲酮，化合物（II）为2-氯二苯并[b，f] [ 1,4]氧杂ze-11（10 H）-1 。至于退化行为，据估计，AMX被降解成（II）通过（我），即，（II）是最终产品。预期该结果可用于临床化学和法医科学，包括在司法解剖和怀疑毒品成瘾时估计要使用的药物。