The State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing, 100191, China.
Beijing Key Laboratory of Molecular Pharmaceutics and New Drug Delivery Systems, School of Pharmaceutical Sciences, Peking University, Beijing, 100191, China.
AAPS PharmSciTech. 2019 Nov 21;21(1):6. doi: 10.1208/s12249-019-1521-x.
The aim of the study is to investigate the feasibility of fabricating FDM 3D-printed gastric floating tablets with low infill percentages and the effect of infill percentage on the properties of gastric floating tablets in vitro. Propranolol hydrochloride was selected as a model drug, and drug-loaded polyvinyl alcohol (PVA) filaments were produced by hot melt extrusion (HME). Ellipsoid-shaped gastric floating tablets with low infill percentage of 15% and 25% (namely E-15 and E-25) were then prepared respectively by feeding the extruded filaments to FDM 3D printer. Thermogravimetric analysis (TGA), differential scanning calorimetry (DSC), X-ray powder diffraction (XRD), and scanning electron microscopy (SEM) were employed to characterize the filaments and 3D-printed tablets, and a series of evaluations were performed to the 3D-printed tablets, including the weight variation, drug content, hardness, in vitro floating behavior, and drug release of the tablets. The SEM results showed that the drug-loaded filaments and 3D-printed tablets appeared intact without defects, and the printed tablets were composed of filaments deposited uniformly layer by layer. The model drug and the excipients were thermally stable under the process temperature of extruding and printing, with a small amount of drug crystals dispersing in the drug-loaded filaments and 3D-printed tablets. Both E-15 and E-25 could float on artificial gastric fluids without any lag time and released in a sustained manner. Compared with E-15, the E-25 presented less weight variation, higher tablet hardness, shorter floating time, and longer drug release time.
本研究旨在探讨采用低填充率熔融沉积 3D 打印（FDM）技术制备胃漂浮片剂的可行性，以及填充率对体外胃漂浮片剂性能的影响。选用盐酸普萘洛尔作为模型药物，采用热熔挤出（HME）法制备载药聚乙烯醇（PVA）长丝。然后，分别采用低填充率为 15%和 25%（即 E-15 和 E-25）的挤出长丝通过 FDM 3D 打印机制备椭球型胃漂浮片剂。采用热重分析（TGA）、差示扫描量热法（DSC）、X 射线粉末衍射（XRD）和扫描电子显微镜（SEM）对长丝和 3D 打印片剂进行表征，并对 3D 打印片剂进行了一系列评价，包括片剂的重量变化、药物含量、硬度、体外漂浮行为和药物释放。SEM 结果表明，载药长丝和 3D 打印片剂完整无缺陷，打印片剂由均匀沉积的长丝层组成。模型药物和辅料在挤出和打印的工艺温度下热稳定性良好，少量药物晶体分散在载药长丝和 3D 打印片剂中。E-15 和 E-25 均能在人工胃液中无滞后时间地漂浮，并持续释放。与 E-15 相比，E-25 表现出更小的重量变化、更高的片剂硬度、更短的漂浮时间和更长的药物释放时间。
