Esumi Satoru, Kitamura Yoshihisa, Yokota-Kumasaki Hitomi, Ushio Soichiro, Yamada-Takemoto Akane, Nagai Ryo, Ogawa Atsushi, Kawasaki Yoichi, Sendo Toshiaki
Department of Hospital Pharmacy, Okayama University Medical School.
Department of Pharmacy, Osaka General Medical Center.
Biol Pharm Bull. 2018;41(11):1727-1731. doi: 10.1248/bpb.b18-00392.
Duloxetine is a serotonin/noradrenaline reuptake inhibitor that is used as an antidepressant. However, it is known to cause constipation as a side effect. Magnesium compounds, such as magnesium oxide and magnesium hydroxide aqueous solution, are often combined with duloxetine to ameliorate the constipation caused by duloxetine. However, there is concern that these magnesium compounds might alter the effects of duloxetine via physicochemical interactions. In this study, we attempted to clarify the interactions that take place between duloxetine and magnesium oxide using in vivo and in vitro experiments. We evaluated the influence of magnesium oxide on in vitro duloxetine concentrations using HPLC. In addition, we examined the in vivo antidepressant-like effects and serum concentrations of duloxetine in rats. In the in vitro experiment, the duloxetine concentration was significantly decreased by co-treatment with magnesium oxide. In the in vivo experiment, the antidepressant-like effects of duloxetine were not affected by the combined oral administration of magnesium oxide and a duloxetine formulation although the serum duloxetine level was significantly decreased. However, the antidepressant-like effects of a duloxetine reagent were significantly attenuated by the co-administration of magnesium oxide. These results suggest that duloxetine and magnesium oxide directly interact and that such interactions affect the absorption and antidepressant-like effects of duloxetine.
度洛西汀是一种用作抗抑郁药的5-羟色胺/去甲肾上腺素再摄取抑制剂。然而,已知它会引起便秘这一副作用。镁化合物,如氧化镁和氢氧化镁水溶液,常与度洛西汀联合使用以改善度洛西汀引起的便秘。然而,人们担心这些镁化合物可能通过物理化学相互作用改变度洛西汀的效果。在本研究中,我们试图通过体内和体外实验阐明度洛西汀与氧化镁之间发生的相互作用。我们使用高效液相色谱法评估了氧化镁对体外度洛西汀浓度的影响。此外,我们研究了氧化镁对大鼠体内度洛西汀的抗抑郁样作用和血清浓度的影响。在体外实验中,与氧化镁共同处理后度洛西汀浓度显著降低。在体内实验中,尽管血清度洛西汀水平显著降低,但氧化镁与度洛西汀制剂联合口服给药并不影响度洛西汀的抗抑郁样作用。然而,氧化镁与度洛西汀试剂共同给药显著减弱了度洛西汀的抗抑郁样作用。这些结果表明度洛西汀与氧化镁直接相互作用,且这种相互作用会影响度洛西汀的吸收和抗抑郁样作用。