Naggar V F, Khalil S A
Pharmazie. 1978 Sep;33(9):593-5.
The adsorption of the antiepileptics sulthiame, phenytoin, mephenytoin, mesuximide, phensuximide, ethosuximide, and primidone on various antacids or adsorbents was studied at 37 degrees C. The antacids or adsorbents used were magnesium trisilicate, aluminium hydroxide, bismuth oxidcarbonate, magnesium oxide, talc, kaolin and calcium carbonate. Magnesium trisilicate was found to be the strongest adsorbent for most of the antiepileptics tested. The other antacids or adsorbents were without an appreciable effect. Sulthiame exhibited the highest degree of interaction with magnesium trisilicate. Mesuximide, phensuximide and primidone showed intermediate adsorption properties. Mephenytoin and phenytoin had lower adsorption characters, while ethosuximide was the least adsorbed antiepileptic tested. The extent of elution was found to be inversely proportional to adsorption. Alkaline solution gave relatively higher eluting power than acid solution. The mechanism of adsorption of the various antiepileptics on antacids was discussed. The effect of magnesium trisilicate on the bioavailability of coadministered antiepileptics has still to be confirmed by in vivo testing.
在37摄氏度下研究了抗癫痫药物舒噻美、苯妥英、甲妥英、乙琥胺、苯琥胺、乙琥胺和扑米酮在各种抗酸剂或吸附剂上的吸附情况。所用的抗酸剂或吸附剂有三硅酸镁、氢氧化铝、碱式碳酸铋、氧化镁、滑石粉、高岭土和碳酸钙。发现三硅酸镁对大多数测试的抗癫痫药物是最强的吸附剂。其他抗酸剂或吸附剂没有明显效果。舒噻美与三硅酸镁的相互作用程度最高。乙琥胺、苯琥胺和扑米酮表现出中等吸附特性。甲妥英和苯妥英的吸附特性较低,而乙琥胺是测试的抗癫痫药物中吸附最少的。发现洗脱程度与吸附成反比。碱性溶液比酸性溶液具有相对更高的洗脱能力。讨论了各种抗癫痫药物在抗酸剂上的吸附机制。三硅酸镁对同时服用的抗癫痫药物生物利用度的影响仍有待体内试验证实。