Research Institute of Pharmaceutical Sciences, Musashino University, Japan; Faculty of Pharmacy, Musashino University, Japan.
Faculty of Pharmacy, Musashino University, Japan.
Int J Pharm. 2018 Mar 25;539(1-2):31-38. doi: 10.1016/j.ijpharm.2018.01.020. Epub 2018 Jan 31.
The relationships between the physicochemical properties of milled starch and drug release from tablets were investigated quantitatively using a drug release kinetic method and X-ray computed tomography (XCT). The samples were prepared from raw β-starch by milling in a planetary ball mill. The tablets, containing 5% theophylline (TH), 94% milled starch, and 1% magnesium stearate, were compressed at 6 kN. The drug-release and gel-forming processes were measured simultaneously using an original dissolution tester with an XCT instrument. Drug release from the tablet was delayed with increasing milling time, because the TH tablet formed a typical gel-layer on the outside of the tablet. The relationship between the crystallinity of milled starch and mean drug release time (MDT) for the TH tablets showed almost a straight inverse proportional relationship. The plots of MDT against area under the curve of the swelling ratio profiles of the TH tablets had a good straight line.
采用药物释放动力学方法和 X 射线计算机断层扫描（XCT）定量研究了粉碎淀粉的物理化学性质与片剂药物释放之间的关系。使用行星式球磨机将生 β-淀粉进行粉碎来制备样品。将含有 5%茶碱（TH）、94%粉碎淀粉和 1%硬脂酸镁的片剂在 6 kN 下压缩。使用带有 XCT 仪器的原始溶解测试仪同时测量药物释放和凝胶形成过程。随着研磨时间的增加，药物释放延迟，因为 TH 片剂在片剂的外部形成了典型的凝胶层。粉碎淀粉的结晶度与 TH 片剂的平均药物释放时间（MDT）之间的关系几乎呈直线反比关系。MDT 与 TH 片剂的溶胀率曲线下面积的关系图呈良好的直线关系。
