Chen D, Xu X Y, Wang M R, Li R, Zang G A, Zhang Y, Qian H N, Yan G R, Fan T Y
Department of Pharmaceutics, Beijing Key Laboratory of Molecular Pharmaceutics and New Drug Delivery Systems, Peking University School of Pharmaceutical Sciences, Beijing 100191, China.
School of Mechanical Engineering and Automation, Beihang University, Beijing 100191, China.
Beijing Da Xue Xue Bao Yi Xue Ban. 2021 Mar 19;53(2):348-354. doi: 10.19723/j.issn.1671-167X.2021.02.020.
To explore the feasibility of preparing gastric floating formulations by fused de-position modeling (FDM) 3D printing technology, to evaluate the properties of the prepared FDM 3D printed gastric floating formulations, and to compare the influence of different external shapes of the formulation with their properties.
Verapamil hydrochloride and polyvinyl alcohol (PVA) were used as the model drug and the excipient, respectively. The capsule-shaped and hemisphere-shaped gastric floating formulations were then prepared by FDM 3D printing. The infill percentages were 15%, the layer heights were 0.2 mm, and the roof or floor thicknesses were 0.8 mm for both the 3D printed formulations, while the number of shells was 3 and 4 for capsule-shaped and hemisphere-shaped formulation, respectively. Scanning electron microscopy (SEM) was used to observe the morpho-logy of the surface and cross section of the formulations. Gravimetric method was adopted to measure the weights of the formulations. Texture analyzer was employed to evaluate the hardness of the formulations. High performance liquid chromatography method was used to determine the drug contents of the formulations. The floating and drug release behavior of the formulations were also characterized.
SEM showed that the appearance of the FDM 3D printed gastric floating formulations were both intact and free from defects with the filling structure which was consistent with the design. The weight variations of the two formulations were relatively low, indicating a high reproducibility of the 3D printing fabrication. Above 800.0 N of hardness was obtained in two mutually perpendicular directions for the two formulations. The drug contents of the two formulations approached to 100%, showing no drug loss during the 3D printing process. The two formulations floated without any lag time, and the floating time of the capsule-shaped and hemisphere-shaped formulation were (3.97±0.41) h and (4.48±0.21) h, respectively. The release of the two formulations was significantly slower than that of the commercially available immediate-release tablets.
The capsule-shaped and hemisphere-shaped verapamil hydrochloride gastric floating formulations were prepared by FDM 3D printing technology successfully. Only the floating time was found to be influenced by the external shape of the 3D printed formulations in this study.
探讨采用熔融沉积建模（FDM）3D打印技术制备胃漂浮制剂的可行性，评价所制备的FDM 3D打印胃漂浮制剂的性质，并比较制剂不同外部形状对其性质的影响。
分别以盐酸维拉帕米和聚乙烯醇（PVA）作为模型药物和辅料。然后通过FDM 3D打印制备胶囊形和半球形胃漂浮制剂。两种3D打印制剂的填充率均为15%，层高均为0.2 mm，胶囊形和半球形制剂的顶部或底部厚度分别为0.8 mm，而胶囊形和半球形制剂的壳层数分别为3层和4层。采用扫描电子显微镜（SEM）观察制剂表面和横截面的形态。采用重量法测量制剂的重量。采用质构分析仪评价制剂的硬度。采用高效液相色谱法测定制剂的药物含量。还对制剂的漂浮和药物释放行为进行了表征。
SEM显示，FDM 3D打印胃漂浮制剂外观完整、无缺陷，填充结构与设计一致。两种制剂的重量差异相对较小，表明3D打印制备具有较高的重现性。两种制剂在两个相互垂直的方向上硬度均达到800.0 N以上。两种制剂的药物含量接近100%，表明在3D打印过程中无药物损失。两种制剂均无延迟地漂浮，胶囊形和半球形制剂的漂浮时间分别为（3.97±0.41）h和（4.48±0.21）h。两种制剂的释放明显慢于市售速释片。
成功采用FDM 3D打印技术制备了胶囊形和半球形盐酸维拉帕米胃漂浮制剂。本研究中发现只有漂浮时间受3D打印制剂外部形状的影响。
