Laboratory of Pharmaceutical Technology and Biopharmaceutics, University of Bonn, Germany.
Talanta. 2011 Apr 15;84(2):437-42. doi: 10.1016/j.talanta.2011.01.049. Epub 2011 Feb 3.
The bisphosphonates clodronate and alendronate are drugs in the therapy of osteoporosis or Paget's disease. They are highly hydrophilic and therefore of low oral bioavailability. Determination methods for bisphosphonates are often laborious and expensive equipment is needed. The presented quantification method based on kinetic measurement of the fluorescence decrease of an Al(3+)-morin complex can be used to determine the bisphosphonate content in aqueous and plasma samples. The intra- and inter-assay accuracies were found to be within 98.8% and 102.3% of the target samples for clodronate and within 97.2% and 105.0% of the target samples for alendronate. The LOQ was defined as 15.6 ng/ml for clodronate and 62.5 ng/ml for alendronate. In serum samples, intra- and inter-assay accuracy was found to be within 99.0% and 101.6% of the target samples for clodronate and within 97.8% and 102.6% of the target samples for alendronate. In serum samples, the LOQ was defined as 1.55 mg/ml for clodronate and 0.39 mg/ml for alendronate. Though less sensitive in serum, the presented method could support research on the development of drug delivery systems in vitro and in vivo for the investigated and other structurally related bisphosphonates.
双膦酸盐氯屈膦酸盐和阿仑膦酸盐是治疗骨质疏松症或 Pagets 病的药物。它们具有很强的亲水性,因此口服生物利用度较低。双膦酸盐的测定方法通常繁琐,需要昂贵的设备。本文提出的基于 Al(3+) - 美罗昔康络合物荧光强度降低的动力学测定方法,可用于测定水溶液和血浆样品中的双膦酸盐含量。氯屈膦酸盐和阿仑膦酸盐的内、日间精密度分别为 98.8%和 102.3%及 97.2%和 105.0%。LOQ 定义为氯屈膦酸盐 15.6ng/ml 和阿仑膦酸盐 62.5ng/ml。在血清样品中,氯屈膦酸盐和阿仑膦酸盐的内、日间精密度分别为 99.0%和 101.6%及 97.8%和 102.6%。血清样品中,氯屈膦酸盐的 LOQ 定义为 1.55mg/ml,阿仑膦酸盐的 LOQ 定义为 0.39mg/ml。虽然在血清中的灵敏度较低,但本文提出的方法可以支持研究用于研究和其他结构相关双膦酸盐的体外和体内药物传递系统的开发。