Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, The Hashemite University, Zarqa, 13115, Jordan.
Faculty of Pharmacy, Applied Science Private University, Amman, Jordan.
Eur J Pharm Sci. 2020 Apr 30;147:105292. doi: 10.1016/j.ejps.2020.105292. Epub 2020 Mar 7.
Hydrophobic starch esters have potential as tablet matrix formers in controlled drug delivery. The mechanical properties of native starch (SN), starch acetate (SA) and starch propionate (SP) were studied at particle and compact level. Particle microhardness and modulus of elasticity were evaluated by nanoindentation. Force-displacement data of compressed powder were analyzed using Heckel in conjunction with piecewise regression, Kuentz-Leuenberger, Kawakita and Adams models, and yield pressure parameters were derived. Starches were characterized for chemical structure by Raman spectroscopy, crystallinity from powder x-ray diffraction (PXRD) patterns and surface energy from apparent contact angle measurements. A-type starch reflections were absent in the PXRDs of esters indicating greater amorphicity. Consequently, the particle microhardness of starch esters decreased leading to greater deformation during compaction and lower values of yield pressure parameters. These parameters increased with microhardness and ranked the starches in the order: SP < SA < SN. Fitting the experimental data into Hiestand's bonding index equation, a linear correlation (R = 0.902) was established between experimental and calculated tablet strength describing results of all starches, when Adams (τ') yield pressure was used as the 'effective compression pressure' in the above equation.
疏水淀粉酯具有作为控制药物释放的片剂基质形成剂的潜力。研究了天然淀粉 (SN)、淀粉醋酸酯 (SA) 和淀粉丙酸酯 (SP) 在颗粒和压片水平下的力学性能。通过纳米压痕法评估了颗粒显微硬度和弹性模量。使用 Heckel 结合分段回归、Kuentz-Leuenberger、Kawakita 和 Adams 模型分析压缩粉末的力-位移数据,并得出屈服压力参数。通过拉曼光谱对淀粉进行化学结构表征,通过粉末 X 射线衍射 (PXRD) 图谱对结晶度进行表征,通过表观接触角测量对表面能进行表征。酯类的 PXRD 中没有 A 型淀粉反射,表明其非晶度更高。因此,淀粉酯的颗粒显微硬度降低,导致压片过程中的变形更大,屈服压力参数值更低。这些参数随显微硬度增加,将淀粉按以下顺序排列:SP<SA<SN。将实验数据拟合到 Hiestand 的结合指数方程中,当 Adams(τ')屈服压力作为上述方程中的“有效压缩压力”时,建立了实验和计算片剂强度之间的线性相关性(R=0.902),可以描述所有淀粉的结果。