Ceulemans Jens, Ludwig Annick
Laboratory of Pharmaceutical Technology and Biopharmacy, Department of Pharmaceutical Sciences, University of Antwerp (UIA), Universiteitsplein 1, B-2610 Antwerp, Belgium.
Eur J Pharm Biopharm. 2002 Jul;54(1):41-50. doi: 10.1016/s0939-6411(02)00036-x.
The optimisation of the in vitro interaction between several poly(acrylic acid) derivatives (Carbopol 1342P NF, Carbopol 974P and Carbopol 980 NF) and mucin was performed by an analysis technique combining oscillatory shear rheology and experimental design in order to improve the formulation of carbomer viscous eye drops.First, standard oscillation procedures were used to characterise the polyacrylic acid and mucin dispersions, and to investigate the influence of several polymer-related factors (concentration, preparation, type of polymer used) on the rheological properties. Second, an experimental plan design was developed to investigate the effect of polymer-related factors on the mucoadhesive indexes (MAI(G') and MAI(G")) which were calculated using the viscoelastic data obtained from polymer/mucin, polymer/tearfluid and mucin/tearfluid mixtures. Optimal mucoadhesive interactions were determined based on the experimental design results. Finally, the optima were fully characterised rheologically to further verify the mucoadhesive capacity. The main conclusion is that the factor influencing most explicitly the mucoadhesive interaction of the viscous eye drop is the mucin concentration and neither the type of polyacrylic acid, nor its concentration.
为了改进卡波姆粘性滴眼液的配方，通过结合振荡剪切流变学和实验设计的分析技术，对几种聚丙烯酸衍生物（卡波姆1342P NF、卡波姆974P和卡波姆980 NF）与粘蛋白之间的体外相互作用进行了优化。首先，使用标准振荡程序对聚丙烯酸和粘蛋白分散体进行表征，并研究几种与聚合物相关的因素（浓度、制备方法、所用聚合物类型）对流变学性质的影响。其次，制定了一个实验方案设计，以研究与聚合物相关的因素对使用从聚合物/粘蛋白、聚合物/泪液和粘蛋白/泪液混合物获得的粘弹性数据计算得出的粘膜粘附指数（MAI(G')和MAI(G")）的影响。根据实验设计结果确定了最佳的粘膜粘附相互作用。最后，对流变学最佳值进行了全面表征，以进一步验证粘膜粘附能力。主要结论是，对粘性滴眼液粘膜粘附相互作用影响最明显的因素是粘蛋白浓度，而不是聚丙烯酸的类型及其浓度。
