In vitro study of the interaction between quinolones and polyvalent cations

Ma Sonia Rodrı́guez Cruz, Isabel González Alonso, Amparo Sánchez–Navarro, Ma Luisa Sayalero Marinero
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引用次数: 24

Abstract

The aim of the present study was to evaluate the influence of aluminium and iron on the in vitro dissolution kinetics of ciprofloxacin and ofloxacin as well as the usefulness of this type of in vitro data to predict modifications in in vivo absorption processes as a consequence of different factors, such as the widely documented in vivo interaction between quinolones and cations. Fitting of experimental data to different theoretical in vitro dissolution profiles was performed by non-linear regression methods and the statistical moments were calculated from raw experimental data. Analysis of residuals applied to dissolution curves as well as statistical comparison of the estimated parameters were carried out to evaluate the in vitro interaction. The results reveal significative modifications of the dissolution profiles of these quinolones as a consequence of the presence of cations, especially for Fe2+ which decreases 34.7% the maximum amount dissolved for ciprofloxacin and 29.1% for ofloxacin. Al3+ also produces a decrease of the total amount of quinolone dissolved although less relevant than Fe2+. Analysis of residuals proved to be the best statistical method to evaluate differences between whole dissolution profiles, at least under the experimental conditions used.

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喹诺酮类药物与多价阳离子相互作用的体外研究
本研究的目的是评估铝和铁对环丙沙星和氧氟沙星体外溶出动力学的影响,以及这种类型的体外数据在预测体内吸收过程因不同因素而发生的变化方面的有用性,例如广泛记录的喹诺酮类药物与阳离子之间的体内相互作用。采用非线性回归方法对实验数据与不同理论体外溶出度曲线进行拟合,并根据原始实验数据计算统计矩。对溶出曲线进行残差分析,并对估计参数进行统计比较,评价其体外相互作用。结果表明,由于阳离子的存在,这些喹诺酮类药物的溶出谱发生了显著的变化,特别是对Fe2+,环丙沙星的最大溶出量降低了34.7%,氧氟沙星的最大溶出量降低了29.1%。Al3+也会导致喹诺酮溶解总量的减少,尽管其相关性不如Fe2+。残差分析被证明是评估整个溶出曲线差异的最佳统计方法,至少在实验条件下是这样。
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