Kondo Keita, Niwa Toshiyuki, Ozeki Yuichi, Ando Masaki, Danjo Kazumi
Faculty of Pharmacy, Meijo University, Nagoya, Japan.
Chem Pharm Bull (Tokyo). 2011;59(10):1214-20. doi: 10.1248/cpb.59.1214.
In this study, in order to address the problems with manufacturing orally rapidly disintegrating tablets (ODT) containing functional (taste masking or controlled release) coated particles, such as the low compactability of coated particles and the rupture of coated membrane during compression, a novel ODT containing taste-masked coated particles (TMP) in the center of the tablets were prepared using one-step dry-coated tablets (OSDrC) technology. As a reference, physical-mixture tablets (PM) were prepared by a conventional tableting method, and the properties of the tablets and the effect of compression on the characteristics of TMP were evaluated. OSDrC was found to have higher tensile strength and far lower friability than PM, but the oral disintegration time of OSDrC is slightly longer than that of PM following high compression pressure. Consequently, OSDrC approaches the target tablet properties of ODT, whereas PM does not. The deformation of TMP in OSDrC due to compression is slight, and the release rate of acetaminophen (AAP) from OSDrC is the same as from TMP. However, TMP on the surface of PM are considerably deformed, and the release rate of AAP from PM is faster than from TMP. These findings suggest that OSDrC technology is a useful approach for preparing ODT containing functional coated particles. Furthermore, we demonstrate that the elastic recovery of tablets can affect differences in the properties of OSDrC, PM and placebo tablets (PC).
在本研究中，为了解决制备含有功能性（掩味或控释）包衣颗粒的口腔速崩片（ODT）时存在的问题，如包衣颗粒的低可压性以及压片过程中包衣膜的破裂，采用一步干包衣片（OSDrC）技术制备了一种在片剂中心含有掩味包衣颗粒（TMP）的新型ODT。作为对照，通过传统压片方法制备了物理混合物片（PM），并对片剂的性质以及压片对TMP特性的影响进行了评估。结果发现，OSDrC的抗张强度高于PM，脆碎度远低于PM，但在高压力压片后，OSDrC的口腔崩解时间略长于PM。因此，OSDrC接近ODT的目标片剂性质，而PM则不然。OSDrC中TMP因压片产生的变形较小，且OSDrC中对乙酰氨基酚（AAP）的释放速率与TMP相同。然而，PM表面的TMP变形较大，且PM中AAP的释放速率比TMP快。这些发现表明，OSDrC技术是制备含有功能性包衣颗粒的ODT的一种有用方法。此外，我们证明片剂的弹性恢复会影响OSDrC、PM和安慰剂片（PC）性质的差异。
