School of Pharmaceutical Sciences, University of Shizuoka, 52-1 Yada, Suruga-ku, Shizuoka 422-8526, Japan.
Faculty of Pharmaceutical Sciences, Toho University, 2-2-1 Miyama, Funabashi, Chiba 274-8510, Japan.
Int J Pharm. 2018 Jan 15;535(1-2):371-378. doi: 10.1016/j.ijpharm.2017.11.029. Epub 2017 Nov 14.
A new scale-down methodology from commercial rotary die scale to laboratory scale was developed to optimize a plant-derived soft gel capsule formulation and eventually manufacture superior soft gel capsules on a commercial scale, in order to reduce the time and cost for formulation development. Animal-derived and plant-derived soft gel film sheets were prepared using an applicator on a laboratory scale and their physicochemical properties, such as tensile strength, Young's modulus, and adhesive strength, were evaluated. The tensile strength of the animal-derived and plant-derived soft gel film sheets was 11.7 MPa and 4.41 MPa, respectively. The Young's modulus of the animal-derived and plant-derived soft gel film sheets was 169 MPa and 17.8 MPa, respectively, and both sheets showed a similar adhesion strength of approximately 4.5-10 MPa. Using a D-optimal mixture design, plant-derived soft gel film sheets were prepared and optimized by varying their composition, including variations in the mass of κ-carrageenan, ι-carrageenan, oxidized starch and heat-treated starch. The physicochemical properties of the sheets were evaluated to determine the optimal formulation. Finally, plant-derived soft gel capsules were manufactured using the rotary die method and the prepared soft gel capsules showed equivalent or superior physical properties compared with pre-existing soft gel capsules. Therefore, we successfully developed a new scale-down methodology to optimize the formulation of plant-derived soft gel capsules on a commercial scale.
为了减少配方开发的时间和成本，开发了一种从商业旋转模头缩小到实验室规模的新方法，以优化植物源软胶囊配方，并最终在商业规模上制造出优质的软胶囊。在实验室规模上使用涂布机制备了动物源和植物源的软胶囊膜片，并评估了它们的物理化学性质，如拉伸强度、杨氏模量和粘合强度。动物源和植物源软胶囊膜片的拉伸强度分别为 11.7 MPa 和 4.41 MPa。动物源和植物源软胶囊膜片的杨氏模量分别为 169 MPa 和 17.8 MPa，且两种膜片的粘合强度均约为 4.5-10 MPa。使用 D-最优混合设计，通过改变 κ-卡拉胶、ι-卡拉胶、氧化淀粉和热处理淀粉的质量等因素来制备和优化植物源软胶囊膜片。评估膜片的物理化学性质以确定最佳配方。最后，使用旋转模头法制造了植物源软胶囊，并与现有的软胶囊进行了比较，结果表明，所制备的软胶囊具有相当或更优的物理性能。因此，我们成功地开发了一种新的方法，可在商业规模上优化植物源软胶囊的配方。
