Charoenying Thapakorn, Patrojanasophon Prasopchai, Ngawhirunpat Tanasait, Rojanarata Theerasak, Akkaramongkolporn Prasert, Opanasopit Praneet
Pharmaceutical Development of Green Innovations Group (PDGIG), Faculty of Pharmacy, Silpakorn University, Nakhon Pathom 73000, Thailand.
Pharmaceutical Development of Green Innovations Group (PDGIG), Faculty of Pharmacy, Silpakorn University, Nakhon Pathom 73000, Thailand.
Eur J Pharm Sci. 2020 Dec 1;155:105555. doi: 10.1016/j.ejps.2020.105555. Epub 2020 Sep 16.
The aim of this study was to produce capsule-shaped floating devices (CFD) using a fused deposition modeling (FDM) three-dimensional (3D) printer, for controlling the release and gastric retention of domperidone (DOM) tablets (Motilium-M). In order to enhance the buoyancy of the devices, a hollow cap with different wall thicknesses (1.2-1.5 mm) was printed with a hydrophilic (polyvinyl alcohol, PVA) filament. The body of the device was made from a hydrophobic (polylactic acid, PLA) filament. Bodies with aperture sizes (1-2 mm) were produced to investigate how this would affect drug release. Morphology, weight variation, ex vivo and in vivo floating time and drug release characteristics were examined. The results revealed that increasing the cap thickness of the devices (1.2 to 1.3 mm) increased the total floating time (TFT). The maximum TFT (10 h) with floating lag time (FLT) < 5 s was observed from Motilium-M incorporated CFD3-5 (cap with 1.3-mm wall thickness). Decreasing the size of the holes on the devices led to the sustained release of DOM. The CFD5 (cap with 1.3-mm cap thickness and 1.5-mm hole width) delivered approximately 98% release in 10 h, and the release kinetics fit well with the zero-order kinetics (R > 0.95). In vivo floating studies in rabbits showed that the floating time of CFD5 was more than 10 h. These results demonstrated that the CFD was successfully designed to provide gastro-retentive drug delivery with the capacity to float and provide sustained drug release.
本研究的目的是使用熔融沉积建模(FDM)三维(3D)打印机制造胶囊形状的漂浮装置(CFD),以控制多潘立酮(DOM)片剂(吗丁啉-M)的释放和胃滞留。为了增强装置的浮力,用亲水性(聚乙烯醇,PVA)细丝打印了具有不同壁厚(1.2-1.5毫米)的空心帽。装置的主体由疏水性(聚乳酸,PLA)细丝制成。制造了具有不同孔径尺寸(1-2毫米)的主体,以研究其对药物释放的影响。对其形态、重量变化、体外和体内漂浮时间以及药物释放特性进行了研究。结果表明,增加装置的帽厚度(从1.2毫米增加到1.3毫米)可增加总漂浮时间(TFT)。在含吗丁啉-M的CFD3-5(帽壁厚1.3毫米)中观察到最大TFT为10小时,漂浮滞后时间(FLT)<5秒。减小装置上孔的尺寸导致DOM的持续释放。CFD5(帽厚度1.3毫米,孔宽1.5毫米)在10小时内释放约98%,释放动力学与零级动力学拟合良好(R>0.95)。在兔体内的漂浮研究表明,CFD5的漂浮时间超过10小时。这些结果表明,CFD被成功设计用于提供胃滞留药物递送,具有漂浮和持续药物释放的能力。