College of Pharmacy, The University of Texas at Austin, 2409 University Avenue, Austin, TX 78712, USA; MRL, Merck & Co, Inc., 126 E. Lincoln Ave, Rahway, NJ 07065, USA.
MRL, Merck & Co, Inc., 126 E. Lincoln Ave, Rahway, NJ 07065, USA.
Int J Pharm. 2019 Feb 25;557:390-401. doi: 10.1016/j.ijpharm.2018.11.067. Epub 2018 Dec 6.
Hydrophobic and hydrophilic thermoplastic poly(urethane) (TPU) mixtures offer the opportunity to tune water swelling capacity and diffusion rate for drugs exhibiting broadly different properties. We sought to (1) assess the range of drug diffusion rates achieved by varying hydrophilic-to-hydrophobic TPU ratio relative to varying ethylene vinyl acetate (EVA) crystallinity; (2) investigate the effect of mixture ratio on permeability of emtricitabine; and (3) investigate the impact of the extrusion process on mixing of the two TPUs and the resulting impact on drug diffusion. The permeability of water-soluble emtricitabine exhibited a 736-fold range across the blends of TPU, but only a 3.4-fold range across the EVA grades investigated. Varying hydrophilic content of the TPU mixture from 0% to 25% (w/w) led to a negligible permeability change, while changing hydrophilic content from 55% to 100% resulted in a linear 3-fold increase in drug permeability. Interestingly, an 123-fold permeability change occurred between 50% and 55% hydrophilic polymer. Extrusion process parameters exhibited minimal impact on homogeneity and drug diffusion. These findings suggest that hydrophilic polymer domains form a continuous network at levels above 55% hydrophilic TPU, thus facilitating a water-filled porous network when exposed to water that provides a mechanism for accelerated drug diffusion.
疏水性和亲水性热塑性聚氨酯(TPU)混合物为调节具有广泛不同性质的药物的水膨胀能力和扩散速率提供了机会。我们旨在:(1)评估通过改变亲水-疏水 TPU 比相对于改变乙烯-醋酸乙烯酯(EVA)结晶度来实现药物扩散速率的范围;(2)研究混合物比例对恩曲他滨渗透性的影响;(3)研究挤出工艺对两种 TPU 混合的影响以及对药物扩散的影响。水溶性恩曲他滨的渗透性在 TPU 混合物的整个范围内变化了 736 倍,但在研究的 EVA 等级范围内仅变化了 3.4 倍。从 0%到 25%(w/w)改变 TPU 混合物的亲水性含量导致渗透性几乎没有变化,而从 55%到 100%改变亲水性含量则导致药物渗透性线性增加 3 倍。有趣的是,亲水性聚合物为 50%到 55%时,渗透性发生了 123 倍的变化。挤出工艺参数对均匀性和药物扩散的影响最小。这些发现表明,亲水性聚合物域在高于 55%亲水 TPU 的水平上形成连续网络,从而在暴露于水中时形成充满水的多孔网络,这为药物扩散提供了一种机制。