Semmelweis University, Department of Pharmaceutics, Hogyes E. Str. 7, H-1092 Budapest, Hungary.
J Pharm Biomed Anal. 2010 May 1;52(1):37-42. doi: 10.1016/j.jpba.2009.12.003. Epub 2009 Dec 6.
The purpose of the present work was developing an in vitro dissolution test to highlight the possible molecular background causing ciprofloxacin (CPFX)-milk interaction. The in vitro dissolution of CPFX from film-coated tablets (Ciprinol) 500mg) was examined at different pH values, simulating certain parts of the gastrointestinal tract, in the presence of water, low-fat milk, casein- or calcium enriched water. In order to determine the amount of dissolved CPFX, solid phase extraction sample preparation followed by high performance liquid chromatography coupled with mass spectrometry was applied. Comparing the dissolution efficiency values in various media, it can be concluded, that casein has a more pronounced effect on the absorbable amount of the antibiotic at each pH value studied, than calcium. In the case of concomitant intake of CPFX film-coated tablet and milk or other dairy products not only the complexation with calcium, but also the adsorption of CPFX on the surface of proteins decreases the absorbable amount of CPFX.
本工作旨在开发一种体外溶出试验，以揭示可能导致环丙沙星（CPFX）-牛奶相互作用的分子背景。研究了在不同 pH 值下，模拟胃肠道某些部位，在水、低脂牛奶、酪蛋白或富含钙的水中，薄膜包衣片（Ciprinol）500mg 的 CPFX 的体外溶出情况。为了确定溶解的 CPFX 的量，应用固相萃取样品制备，然后进行高效液相色谱-质谱联用。比较在不同介质中的溶出效率值，可以得出结论，在研究的每个 pH 值下，酪蛋白对吸收抗生素的量的影响比钙更为显著。在同时摄入 CPFX 薄膜包衣片和牛奶或其他乳制品的情况下，CPFX 与钙的络合以及 CPFX 在蛋白质表面的吸附不仅降低了 CPFX 的可吸收量。
