Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Athens, Athens, Greece.
Drug Dev Ind Pharm. 2011 Jan;37(1):113-20. doi: 10.3109/03639045.2010.495753. Epub 2010 Jul 8.
Pulsatile drug delivery system, based on a core-in-cup dry-coated tablet was examined and evaluated. The system consisted of three different parts: a core tablet (with increasing diameter), containing the active ingredient acting as reservoir; an impermeable outer shell; and a top cover layer barrier. The core tablet contained either caffeine or theophylline as model drugs.
To investigate and evaluate how the geometrical characteristics of the core tablets, drugs, and excipients influence the behavior of the system presented, namely, lag time and drug release.
Drug release exhibited a lag time period dependent on the core tablet size, drug solubility, and characteristics of polymer and polymer mixtures. The lag time was increased by increasing the core tablet diameter and the quantity of soluble lactose in the top cover layer.
The quantity and characteristics of materials, the core tablet size, and the erosion of the top cover layer were found to be important factors in controlling the lag time and release. Increase in core tablet diameter resulted in lower lag times and greater release and release rates. Similarly, by increasing sufficiently the quantity of the soluble excipient lactose, in the top layer we observed a decrease of the lag times and an increase of release.
基于核-杯干式包衣片的脉冲药物递送系统得到了研究和评估。该系统由三个不同部分组成:一个含有作为储库的活性成分的核心片剂(直径逐渐增大);一个不可渗透的外壳;以及一个顶层覆盖层阻挡层。核心片剂中含有咖啡因或茶碱作为模型药物。
研究和评估核心片剂、药物和赋形剂的几何特征如何影响所呈现系统的行为,即滞后时间和药物释放。
药物释放表现出与核心片剂尺寸、药物溶解度以及聚合物和聚合物混合物特性相关的滞后时间。通过增加核心片剂直径和顶层覆盖层中可溶乳糖的量,滞后时间增加。
发现材料的数量和特性、核心片剂尺寸以及顶层覆盖层的侵蚀是控制滞后时间和释放的重要因素。核心片剂直径的增加导致滞后时间更短、释放量和释放率更大。同样,通过在顶层中充分增加可溶赋形剂乳糖的量,我们观察到滞后时间的减少和释放的增加。