Arayne M Saeed, Sultana Najma, Afzal M
Department of Chemistry, University of Karachi, Karachi-75270, Pakistan.
Pak J Pharm Sci. 2007 Jul;20(3):179-84.
The present work comprises of interaction studies of cephradine with antacids. Cephradine is included among the first generation cephalosporin, which is active against a wide range of Gram positive and Gram-negative bacteria including penicillinase-producing staphylococci. Since the presence of complexing ligand may affect the bioavailability of a drug in blood or tissues, therefore, in order to study the probable interaction of cephradine with antacids all the reaction conditions were simulated to natural environments. Antacids are commonly used in patients complaining of GI irritations. The behavior of cephradine in presence of seven antacids i.e., simethicone, magaldrate, magnesium carbonate, magnesium hydroxide, magnesium trisilicate, sodium bicarbonate and aluminium hydroxide was studied by using standard dissolution apparatus. Cephradine was monitored both by UV and by high performance liquid chromatography. The results revealed that antacids containing polyvalent cations retarded the in vitro availability of cephradine. Moreover, these studies indicated that cephradine was strongly adsorbed on antacids; magnesium trisilicate and simeco tablets (powdered) exhibited relatively higher adsorption capacities.
本研究工作包括头孢拉定与抗酸剂的相互作用研究。头孢拉定属于第一代头孢菌素,对多种革兰氏阳性菌和革兰氏阴性菌均有活性,包括产青霉素酶的葡萄球菌。由于络合配体的存在可能会影响药物在血液或组织中的生物利用度,因此,为了研究头孢拉定与抗酸剂可能的相互作用,所有反应条件均模拟自然环境。抗酸剂常用于抱怨胃肠道不适的患者。使用标准溶出装置研究了头孢拉定在七种抗酸剂(即西甲硅油、氢氧化铝镁、碳酸镁、氢氧化镁、三硅酸镁、碳酸氢钠和氢氧化铝)存在下的行为。通过紫外光和高效液相色谱法对头孢拉定进行监测。结果表明,含有多价阳离子的抗酸剂会延迟头孢拉定的体外可用性。此外,这些研究表明头孢拉定在抗酸剂上有强烈吸附;三硅酸镁和西甲硅油片(粉末状)表现出相对较高的吸附能力。