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目的考察盐酸美金刚胺前药MeN-1和MeN-2在人工胃肠液中的稳定性。方法采用HPLC法测定盐酸美金刚胺前药MeN-1和MeN-2在人工胃液和人工肠液中的浓度,并比较两者的稳定性。结果 MeN-1在人工胃液中孵育3 h后,其相对含量为90%,但在人工肠液中降至约70%;而MeN-2在人工胃肠液中孵育1 h后,其相对含量均降至90%以下。结论在人工胃液中,MeN-1较MeN-2稳定,表明MeN-1更适于开发为口服制剂。
Objective To investigate the stability of memantine hydrochloride prodrug MeN-1 and MeN-2 in artificial gastrointestinal fluid. Methods The concentrations of MeN-1 and MeN-2 in artificial gastric juice and artificial intestinal juice of memantine hydrochloride were determined by HPLC, and their stability was compared. Results The relative content of MeN-1 in artificial gastric juice was 90% after incubation for 3 h, but decreased to about 70% in artificial intestinal juice. The relative content of MeN-2 in artificial gastric juice for 1 h Below 90%. Conclusions MeN-1 is more stable than MeN-2 in artificial gastric juice, suggesting that MeN-1 is more suitable for development as an oral formulation.