Naggar V F, Khalil S A, Daabis N A
Pharmazie. 1976 Jul;31(7):461-5.
The adsorption of sodium salicylate, salicylamide, acetylsalicylic acid, paracetamol, mefenamic acid, flufenamic acid, phenylbutazone, oxyphenbutazone, phenazone, aminophenazone, indometacin and methiazinic acid on some antacids was studied. The antacids used were magnesium trisilicate, magnesium oxide, aluminium hydroxide, bismuth oxycarbonate, calcium carbonate and kaolin. Magnesium oxide, followed by aluminium hydroxide and bismuth oxycarbonate showed a fairly high adsorptive capacity for salicylates, mefenamic acid, flufenamic acid, methiazinic acid, indometacin and to a lesser extent for phenylbutazone and oxyphenbutazone. On the other hand, magnesium trisilicate exhibited a tendency to adsorb phenazone, aminophenazone, indometacin and methiazinic acid. Kaolin was found to be a good adsorbent for anthranilic acid derivatives, indometacin and methiazinic acid. Calcium carbonate showed a weak adsorptive capacity for all drugs tested. The adsorption of phenylbutazone and salicylates on magnesium oxide, aluminium hydroxide and/or bismuth oxycarbonate obeyed the Freundlich adsorption isotherm. Elution study showed that salicylates and anthranilic acid derivatives were tenaciously held by magnesium oxide while magnesium trisilicate showed an intermediate retention power for phenazone and aminophenazone. Sodium hydrogen carbonate solution gave, in general, a higher eluting power than hydrochloric acid solution. A marked reduction in the apparent partition coefficients of all drugs tested was observed in the presence of magnesium trisilicate or aluminium hydroxide. Careful in vitro and in vivo testing of drug availability is advisable prior to the concomitant administration of antirheumatics with antacids or other adsorbents.
研究了水杨酸钠、水杨酰胺、乙酰水杨酸、对乙酰氨基酚、甲芬那酸、氟芬那酸、保泰松、羟布宗、非那宗、氨基非那宗、吲哚美辛和甲硫噻嗪酸在某些抗酸剂上的吸附情况。所用抗酸剂为三硅酸镁、氧化镁、氢氧化铝、碱式碳酸铋、碳酸钙和高岭土。氧化镁,其次是氢氧化铝和碱式碳酸铋,对水杨酸盐、甲芬那酸、氟芬那酸、甲硫噻嗪酸、吲哚美辛表现出相当高的吸附能力,对保泰松和羟布宗的吸附能力稍弱。另一方面,三硅酸镁表现出吸附非那宗、氨基非那宗、吲哚美辛和甲硫噻嗪酸的倾向。发现高岭土是邻氨基苯甲酸衍生物、吲哚美辛和甲硫噻嗪酸的良好吸附剂。碳酸钙对所有测试药物的吸附能力较弱。保泰松和水杨酸盐在氧化镁、氢氧化铝和/或碱式碳酸铋上的吸附符合弗罗因德利希吸附等温线。洗脱研究表明,水杨酸盐和邻氨基苯甲酸衍生物被氧化镁牢固吸附,而三硅酸镁对非那宗和氨基非那宗的保留能力中等。碳酸氢钠溶液通常比盐酸溶液具有更高的洗脱能力。在存在三硅酸镁或氢氧化铝的情况下,观察到所有测试药物的表观分配系数显著降低。在将抗风湿药与抗酸剂或其他吸附剂联合给药之前,建议仔细进行药物可用性的体外和体内测试。