Yoneda Saki, Torisu Tetsuo, Uchiyama Susumu
Department of Biotechnology, Graduate School of Engineering, Osaka University, Osaka, Japan.
Exploratory Research Center on Life and Living Systems, National Institutes of Natural Sciences, Okazaki, Aichi, Japan.
Expert Opin Drug Deliv. 2021 Apr;18(4):459-470. doi: 10.1080/17425247.2021.1853699. Epub 2021 Jan 25.
Several new biopharmaceutical dosage forms have developed over time, such as lyophilized vial, liquid vial, and liquid prefilled syringe formulations. This review summarizes major pharmaceutical dosage forms and their advantages, disadvantages, and countermeasures against the shortcomings of each formulation. The appropriate combination of active pharmaceutical ingredients, excipients, and containers should be selected for the safe and less burdensome administration to the patients. Finally, we note certain opinions on the future development of not only therapeutic proteins but also gene therapeutics.
This review is to discuss the challenges of the development of dosage forms to improve pharmaceutical stability and how they can be overcome.
Silicone oil-free syringes are highly preferable for minimizing subvisible particles in the drug. It can be proposed that materials with less protein adsorption property are preferable for the suppression of protein aggregation. It is required to minimize adverse effects of biopharmaceuticals through proper quality control of the drug in a container, based on the understating of physicochemical stability of the protein in solution, the physicochemical properties of the container, and their combinations.
随着时间的推移，已经开发出几种新的生物制药剂型，如冻干瓶、液体瓶和液体预填充注射器制剂。本综述总结了主要的药物剂型及其优缺点，以及针对每种制剂缺点的应对措施。应选择活性药物成分、辅料和容器的适当组合，以便为患者提供安全且负担较小的给药方式。最后，我们对治疗性蛋白质以及基因治疗的未来发展提出了一些看法。
本综述旨在讨论剂型开发中提高药物稳定性的挑战以及如何克服这些挑战。
无硅油注射器对于最大限度减少药物中的亚可见颗粒非常可取。可以提出，具有较低蛋白质吸附特性的材料对于抑制蛋白质聚集更可取。基于对溶液中蛋白质的物理化学稳定性、容器的物理化学性质及其组合的理解，需要通过对容器中药物进行适当的质量控制，将生物制药的不良反应降至最低。
