Rodríguez Cruz M S, González Alonso I, Sánchez-Navarro A, Sayalero Marinero M L
Department of Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy, University of Salamanca, Spain.
Pharm Acta Helv. 1999 Feb;73(5):237-45. doi: 10.1016/s0031-6865(98)00029-6.
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.
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解动力学的影响，以及这类体外数据预测因不同因素（如喹诺酮类药物与阳离子在体内广泛记录的相互作用）导致的体内吸收过程变化的有用性。通过非线性回归方法将实验数据拟合到不同的理论体外溶解曲线，并从原始实验数据计算统计矩。对溶解曲线应用残差分析以及对估计参数进行统计比较，以评估体外相互作用。结果显示，由于阳离子的存在，这些喹诺酮类药物的溶解曲线有显著变化，特别是对于Fe2+，它使环丙沙星的最大溶解量降低了34.7%，使氧氟沙星的最大溶解量降低了29.1%。Al3+也会使溶解的喹诺酮类药物总量减少，尽管其影响程度小于Fe2+。残差分析被证明是评估整个溶解曲线差异的最佳统计方法，至少在所使用的实验条件下是如此。
