Yu Deng Guang, Yang Xiang Liang, Huang Wei Dong, Liu Jie, Wang Yun Gan, Xu Huibi
Institute of Materia Medica, College of Life Science and Technology, Huazhong University of Science and Technology, Wuhan 430074, China.
J Pharm Sci. 2007 Sep;96(9):2446-56. doi: 10.1002/jps.20864.
Complex tablets with zero-order drug release characteristics were fabricated using three-dimensional printing processes. The matrix tablets exhibited material gradients in radial direction and had drug-free release-barrier layers on both bases. The content of model drug acetaminophen incorporated in the tablets through premixing reached up to 68% of the tablets' weight. Tablets with ethylcellulose gradients showed acceptable mechanical and pharmacotechnical properties, as indicated by crushing strength, friability, and content uniformity tests. The structure and the gradients of ethylcellulose in the tablets were envisaged through environmental scanning electron microscopy and fluorescence tracing technique. Erosion and dissolution studies in vitro indicated that drug was released via a two-dimensional surface erosion mechanism, and 98% of the drug could be released linearly in 12 h. Tablets with other release-retardation material gradients such as sodium lauryl sulfate, stearic acid, and Eudragit RS-100 showed similar release-retardation effects by different release-retardation mechanisms. Through the printing of release-retardation materials, 3DP processes could easily prepare tablets with high dosage and special design features for furnishing the desired drug release characteristics.
采用三维打印工艺制备了具有零级药物释放特性的复方片剂。基质片剂在径向上呈现材料梯度，且在两个底部均有不含药物的释放阻挡层。通过预混法加入到片剂中的模型药物对乙酰氨基酚的含量高达片剂重量的68%。通过抗压强度、脆碎度和含量均匀度测试表明，具有乙基纤维素梯度的片剂具有可接受的机械性能和药剂学性能。通过环境扫描电子显微镜和荧光示踪技术观察了片剂中乙基纤维素的结构和梯度。体外侵蚀和溶出研究表明，药物通过二维表面侵蚀机制释放，98%的药物可在12小时内线性释放。具有其他缓释材料梯度（如十二烷基硫酸钠、硬脂酸和Eudragit RS - 100）的片剂通过不同的缓释机制表现出类似的缓释效果。通过打印缓释材料，三维打印工艺可以轻松制备具有高剂量和特殊设计特征的片剂，以提供所需的药物释放特性。
