Naggar V F, Khalil S A
Pharmazie. 1980;35(7):412-6.
The adsorption of the oral antidiabetics metformin hydrochloride, glibenclamide, acetohexamide, tolbutamide, carbutamide, tolazamide and glymidine on various antacids or adsorbents was studied at 37 degrees C. The antacids or adsorbents used were magnesium trisilicate, aluminium hydroxide, calcium carbonate, magnesium oxide, bismuth oxycarbonate, talc, kaolin as well as charcoal. None of the substances tested, with the exception of charcoal, exhibited superior adsorptive properties for all the drugs. Magnesium trisilicate and calcium carbonate were the best adsorbents for metformin hydrochloride. Acetohexamide and glibenclamide were adsorbed to an appreciable extent on most antacids. Tolbutamide showed an adsorption tendency towards talc. Most antacids slightly adsorbed carbutamide, while magnesium trisilicate showed a higher adsorption capacity for tolazamide and glymidine. The dissolution rate of acetohexamide in magnesium oxide suspension (5:400) increased about 40-fold after 10 min, whle in magnesium trisilicate suspension (5:400) it increased about 7-fold. On the other hand, magnesium trisilicate did not influence the dissolution rate of metformin hydrochloride. The probable variation in the bioavailability of orally administered antidiabetics when coadministered with antacids was discussed. However, further in vivo studies are needed before a final assessment for such drug-antacid interaction can be confirmed.
在37摄氏度下研究了口服抗糖尿病药物盐酸二甲双胍、格列本脲、醋磺己脲、甲苯磺丁脲、卡比马脲、妥拉磺脲和格列嘧啶在各种抗酸剂或吸附剂上的吸附情况。所使用的抗酸剂或吸附剂有三硅酸镁、氢氧化铝、碳酸钙、氧化镁、碱式碳酸铋、滑石粉、高岭土以及木炭。除木炭外,所测试的物质对所有药物均未表现出优异的吸附性能。三硅酸镁和碳酸钙是盐酸二甲双胍的最佳吸附剂。醋磺己脲和格列本脲在大多数抗酸剂上有相当程度的吸附。甲苯磺丁脲对滑石粉有吸附倾向。大多数抗酸剂对卡比马脲有轻微吸附,而三硅酸镁对妥拉磺脲和格列嘧啶表现出更高的吸附能力。醋磺己脲在氧化镁混悬液(5:400)中的溶解速率在10分钟后增加了约40倍,而在三硅酸镁混悬液(5:400)中增加了约7倍。另一方面,三硅酸镁不影响盐酸二甲双胍的溶解速率。讨论了口服抗糖尿病药物与抗酸剂合用时生物利用度可能的变化。然而,在最终确定这种药物 - 抗酸剂相互作用之前,还需要进一步的体内研究。