Colorcon Inc., Global Headquarters, 275 Ruth Road, Harleysville, Pennsylvania, 19438, USA,
AAPS PharmSciTech. 2014 Feb;15(1):149-60. doi: 10.1208/s12249-013-0040-4. Epub 2013 Nov 13.
Push-pull osmotic pump (PPOP) tablets of a practically insoluble model drug were developed and the effect of various formulation and process parameters on tablet performance was evaluated in order to identify critical factors. The formulation factors such as the viscosity grade of polyethylene oxide as the primary polymer as well as the level and location of osmogen within the bilayer tablets led to a difference in performance of osmotic tablets and hence should be critically evaluated in the design of such dosage forms. Modification of granulation process, i.e., the granulating liquid composition or drying method of granules, did not impact the drug release from the osmotic tablets at the evaluated scale of this study. The influence of varying dose and aqueous solubility of other model drugs (i.e., theophylline, acetaminophen, and verapamil HCl) on the developed PPOP template was also investigated. Results showed that irrespective of the perceived complexity of development and manufacturing of osmotic pumps, the osmotic tablets in this study demonstrated a robust and yet flexible platform in accommodating different types of drug candidates, regardless of solubility, for the dose levels below 25% w/w of the pull layer formulation.
研制了一种实际难溶性模型药物的推-拉渗透泵（PPOP）片剂，并评估了各种制剂和工艺参数对片剂性能的影响，以确定关键因素。制剂因素，如作为主要聚合物的聚环氧乙烷的粘度等级以及双层片剂中渗透压剂的水平和位置，导致渗透片剂的性能存在差异，因此在设计此类剂型时应进行严格评估。制粒工艺的改进，即制粒液的组成或颗粒的干燥方法，在本研究评估的规模上不会影响渗透片剂中药物的释放。还研究了不同剂量和其他模型药物（即茶碱、对乙酰氨基酚和盐酸维拉帕米）的水溶性对开发的 PPOP 模板的影响。结果表明，尽管渗透泵的开发和制造看起来很复杂，但在本研究中，渗透片剂表现出了强大而灵活的平台，可以适应不同类型的候选药物，无论溶解度如何，对于低于 25%w/w 推拉层制剂的剂量水平。
