Okazaki Fuminori, Hattori Yusuke, Sasaki Tetsuo, Otsuka Makoto
Faculty of Pharmacy, Musashino University, 1-1-20 Shinmachi, Nishi-Tokyo 202-8585, Tokyo, Japan.
Graduate School of Medical Photonics, Shizuoka University, 3-5-1 Johoku, Naka-ku, Hamamatsu 432-8011, Shizuoka, Japan.
Gels. 2022 Mar 15;8(3):181. doi: 10.3390/gels8030181.
To design a controlled drug release preparation based on a safe natural material, a Konjac glucomannan (KGM) mixture containing 16.0 % calcium hydroxide (Ca(OH)) was ground in a planetary ball mill for 0-120 min. The mechanochemical effect on the physicochemical properties of the KGM ground product was investigated by Fourier-transform infrared spectroscopy (FT-IR), powder X-ray spectroscopy, scanning electron microscopy with energy-dispersive X-ray spectroscopy, and drug release testing. The FT-IR spectra of the ground KGM indicated that the deacetylation reaction of KGM was accelerated in the Ca(OH)-containing sols by mechanochemical energy, and the degree of deacetylation of KGM was dependent on the grinding time. The time required for tablet disintegration of the KGM matrix tablets containing theophylline increased as the grinding time increased; therefore, drug release was sustained. The Higuchi plots of the matrix tablets obtained from KGM ground for 60-120 min exhibited good linearity because they maintained their gel matrix tablet shape during the release test. However, KGM tablets ground for 0-30 min exhibited nonlinear curves, which were caused by tablet disintegration. This suggests that drug release from the KGM matrix tablet can be freely controlled by the degree of mechanochemical treatment.
为了基于一种安全的天然材料设计一种控释药物制剂，将含有16.0%氢氧化钙（Ca(OH)₂）的魔芋葡甘聚糖（KGM）混合物在行星式球磨机中研磨0至120分钟。通过傅里叶变换红外光谱（FT-IR）、粉末X射线光谱、带能谱仪的扫描电子显微镜以及药物释放测试，研究了机械化学作用对KGM研磨产物物理化学性质的影响。研磨后的KGM的FT-IR光谱表明，通过机械化学能，KGM在含Ca(OH)₂的溶胶中的脱乙酰化反应加速，且KGM的脱乙酰化程度取决于研磨时间。含有茶碱的KGM基质片剂的崩解时间随着研磨时间的增加而延长；因此，药物释放得以持续。从研磨60至120分钟的KGM获得的基质片剂的Higuchi图呈现出良好的线性，因为它们在释放测试期间保持了凝胶基质片剂的形状。然而，研磨0至30分钟的KGM片剂呈现出非线性曲线，这是由片剂崩解引起的。这表明从KGM基质片剂中的药物释放可以通过机械化学处理程度自由控制。
