A novel mechanical antrum model for the prediction of the gastroretentive potential of dosage forms

作者:Neumann Marco; Schneider Felix; Koziolek Mirko; Garbacz Grzegorz; Weitschies Werner*
来源:International Journal of Pharmaceutics, 2017, 530(1-2): 63-70.
DOI:10.1016/j.ijpharm.2017.07.067

摘要

The development of gastroretentive dosage forms can be significantly enhanced by the reliable estimation of gastroretentive properties in vitro. In this context, it is mandatory to consider the propulsive contraction waves that occur in the antral region of the stomach, since they are regarded as the major physiological hurdle to overcome. Therefore, the aim of this study was to develop an in vitro model that allowed the evaluation of the gastroretentive potential of objects with different properties (e.g. size, shape and elasticity). The model enabled a realistic simulation of the human antrum and occurring contraction waves. We could demonstrate that larger objects made of elastic polyurethane foam were more rapidly emptied by the model than smaller objects having the same shape. Compared to this, rigid as well as slippery objects showed decreased gastroretentive properties. In contrast, a self-formed trichobezoar - an indigestible object known to remain in the stomach - showed the highest gastroretentive potential. We suggest that the gastroretentive potential of objects of a certain size increases if they exhibit compressible and elastic properties along with certain dimensions. The data showed that the development of novel gastroretentive dosage forms may be facilitated with the aid of the mechanical antrum model.

  • 出版日期2017-9-15