Yarce Cristhian J, Pineda Diego, Correa Clara E, Salamanca Constain H
Pharmaceutical Physical Chemistry Laboratory, Natura Research Group, Pharmaceutical Chemistry Program, Faculty of Natural Sciences, ICESI University, Cali 760031, Colombia.
Pharmaceuticals (Basel). 2016 Jun 24;9(3):34. doi: 10.3390/ph9030034.
The performance of compressed tablet drug delivery systems made using polymeric materials depend on multiple factors, such as surface properties like contact angle, surface free energy and water absorption rate, besides the release mechanisms driven by the kind of polymer used. Hence, it should be possible to establish a relationship between the surface properties and the drug release kinetics. Compressed tablets with different proportions of poly(maleic acid-alt-octadecene) potassium salt (0%, 10%, 20%, 30% and 40%) were prepared. Blends of a model drug (ampicillin trihydrate) and the polymer material were analyzed by DSC. The surface properties of the tablets were determined by the sessile drop method, while the surface energy was determined using the semi-empirical Young-Dupre, Neumann and OWRK models. The release profiles were determined simulating in vitro conditions (buffer solutions pH 1.2 and pH 7.4 with ionic strength of 1.5 M at 37 °C (310.15 K)). A kinetic analysis of the dissolution profiles using different models (zero order, first order, Higuchi and Korsmeyer-Peppas) was realized. The results showed a significant effect of the proportion of polymer in both the surface properties of the tablets and the dissolution release, indicating a relationship between the kinetic and thermodynamic properties.
使用聚合材料制成的压制片药物递送系统的性能取决于多个因素，除了所用聚合物种类驱动的释放机制外，还包括表面性质，如接触角、表面自由能和吸水率。因此，应该能够建立表面性质与药物释放动力学之间的关系。制备了具有不同比例聚（马来酸-alt-十八碳烯）钾盐（0%、10%、20%、30%和40%）的压制片。通过差示扫描量热法（DSC）分析了模型药物（三水合氨苄西林）与聚合物材料的混合物。片剂的表面性质通过静滴法测定，而表面能则使用半经验的杨氏-杜普雷、诺伊曼和OWRK模型测定。在模拟体外条件（37°C（310.15K）下，pH值为1.2和pH值为7.4、离子强度为1.5M的缓冲溶液）下测定释放曲线。使用不同模型（零级、一级、 Higuchi和Korsmeyer-Peppas）对溶解曲线进行了动力学分析。结果表明，聚合物比例对片剂的表面性质和溶解释放均有显著影响，表明动力学性质与热力学性质之间存在关系。
