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克拉霉素(CAM)是临床上广泛应用的一种大环内酯类抗菌素。前期试验中观察到在羧酸盐缓冲液(如枸橼酸缓冲液)中,CAM从片剂中的释放会受到抑制,释放速率明显下降。这种抑制作用可归因于片剂表面形成了凝胶,所形成的凝胶会抑制溶剂渗透进入片剂,进而抑制片剂崩解。对市售片剂的试验中也观察到了崩解迟缓的现象。这提示应避免同时摄入CAM和羧酸盐类物质。对CAM枸橼酸盐的晶体结构研究表明,在晶体内CAM的分子链通过氢键与枸橼酸盐基团交联,这提示在存
Clarithromycin (CAM) is a macrolide antibiotic widely used clinically. It has been observed in previous experiments that the release of CAM from the tablets is inhibited in carboxylate buffers (such as citrate buffer) and the release rate is significantly reduced. This inhibitory effect can be attributed to the gel formed on the surface of the tablet, and the gel formed inhibits solvent penetration into the tablet, thereby inhibiting tablet disintegration. The phenomenon of slow disintegration was also observed in the commercial tablet test. This suggests avoiding the simultaneous ingestion of CAM and carboxylates. Crystal structure studies of CAM citrate have shown that the intramolecular CAM chains cross-link with citrate groups via hydrogen bonds, suggesting that in the presence of