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抗酸剂对口服降糖药活性的影响。

Effect of antacids on activity of oral hypoglycemics.

作者信息

Said S A, Abdullah M E

出版信息

J Pharm Sci. 1981 Jun;70(6):621-4. doi: 10.1002/jps.2600700612.

Abstract

The effect of some antacids on the dissolution and hypoglycemic activity of acetohexamide, tolazamide, and tolbutamide tablets was investigated, as was the adsorption of the three drugs onto the antacids. The dissolution rates of the three drugs in the presence of magnesium oxide, aluminum hydroxide, magnesium carbonate, and calcium carbonate increased (0.5-1 hr) and then plateaued or decreased (1-3 hr). Magnesium trisilicate directly suppressed the dissolution of the three drugs. The antacids reduced the hypoglycemic activity of tolbutamide in the following order:magnesium trisilicate greater than magnesium oxide greater than aluminum hydroxide greater than magnesium carbonate greater than calcium carbonate. The same order occurred for the first three antacids with acetohexamide and tolazamide. Decreased hypoglycemic activity of the drugs may have been due to their adsorption to the coadministered antacids.

摘要

研究了一些抗酸剂对醋磺己脲、甲苯磺丁脲和妥拉磺脲片剂的溶出度及降血糖活性的影响,以及这三种药物在抗酸剂上的吸附情况。在氧化镁、氢氧化铝、碳酸镁和碳酸钙存在的情况下,这三种药物的溶出速率先升高(0.5 - 1小时),然后趋于平稳或下降(1 - 3小时)。三硅酸镁直接抑制这三种药物的溶出。抗酸剂降低甲苯磺丁脲降血糖活性的顺序为:三硅酸镁>氧化镁>氢氧化铝>碳酸镁>碳酸钙。对于醋磺己脲和妥拉磺脲,前三种抗酸剂也呈现相同的顺序。药物降血糖活性降低可能是由于它们吸附到同时服用的抗酸剂上。

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