There is a strong need to search for more effective compounds with bone anti-resorptive properties, which will cause fewer complications than commonly used bisphosphonates. To achieve this goal, it is necessary to search for new techniques to characterize the interactions between bone and drug. By studying their interaction with hydroxyapatite (HA), this study used three forms of ceramic materials, two of which are bone-stimulating materials, to assess the suitability of new active substances with anti-resorptive properties. In this study, three methods based on HA in loose form, polycaprolactone/HA (a polymer-ceramic materials containing HA), and polymer-ceramic monolithic in-needle extraction (MINE) device (a polymer inert skeleton), respectively, were used. The affinity of risedronate (a standard compound) and sixteen aminomethylenebisphosphonates (new compounds with potential antiresorptive properties) to HA was defined according to the above-mentioned methods. Ten monolithic materials based on 2-hydroxyethyl methacrylate/ethylene dimethacrylate are prepared and studied, of which one was selected for more-detailed further research. Simulated body fluids containing bisphosphonates were passed through the MINE device. In this way, sorption–desorption of bisphosphonates was evaluated using this MINE device. The paper presents the advantages and disadvantages of each technique and its suitability for assessing new active substances. All three methods allow for the selection of several compounds with potentially higher anti-resorptive properties than risedronate, in hope that it reflects their higher bone affinity and release ability.

中文翻译：

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基于三种形式陶瓷材料的双膦酸盐抗再吸收性能测定：吸附和释放过程评估

迫切需要寻找具有骨抗吸收特性的更有效的化合物，这将比常用的双膦酸盐引起更少的并发症。为了实现这一目标，有必要寻找新技术来表征骨骼与药物之间的相互作用。通过研究它们与羟基磷灰石（HA）的相互作用，本研究使用了三种形式的陶瓷材料（其中两种是骨刺激材料）来评估具有抗再吸收特性的新型活性物质的适用性。在这项研究中，分别使用了三种基于松散形式HA的方法：聚己内酯/HA（一种含有HA的聚合物陶瓷材料）和聚合物陶瓷整体针内提取（MINE）装置（一种聚合物惰性骨架） 。根据上述方法定义了利塞膦酸盐（标准化合物）和十六种氨基亚甲基二膦酸盐（具有潜在抗再吸收特性的新化合物）对HA的亲和力。制备并研究了十种基于甲基丙烯酸2-羟乙酯/二甲基丙烯酸乙二酯的整体材料，并选择其中一种进行更详细的进一步研究。含有双膦酸盐的模拟体液通过 MINE 装置。通过这种方式，使用该 MINE 装置评估了双膦酸盐的吸附-解吸。本文介绍了每种技术的优点和缺点及其评估新活性物质的适用性。所有三种方法都允许选择比利塞膦酸盐具有潜在更高抗吸收特性的几种化合物，希望它能反映它们更高的骨亲和力和释放能力。