School of Energy and Environment, Southeast University, Nanjing, PR China.
Jiangsu Industrial Technology Research Institute for Process and Optimization, Suzhou, PR China.
Pharm Dev Technol. 2022 Jul;27(6):635-645. doi: 10.1080/10837450.2022.2098975. Epub 2022 Jul 15.
Remdesivir is one of the effective drugs proposed for the treatment of coronavirus disease 2019 (COVID-19). However, the study on inhalable regimen is currently limited though COVID-19 is respiratory diseases and infects lung area. This work aims to prepare inhalable remdesivir formulations and verify their effectiveness through evaluations. Formulations containing different ratios of jet-milled inhalable remdesivir (5, 10, 20,40, and 70%) with excipients were produced and characterized in terms of the particle size distribution, particle morphology, flowability, water content, crystallinity, the water sorption and desorption capabilities, and the aerodynamic performance. Results indicating that drug loading are a vital factor in facilitating the dispersion of remdesivir dry powder, and the ternary excipient plays a negligible role in improving aerosol performance. Besides, the 70% remdesivir with lactose carrier (70% RD-Lac) was physically stable and retain high aerosol performance after conditioned at 40 °C and 75% RH for a month. Therefore, formulation 70% RD-Lac might be recommended as a candidate product for the potential treatment of COVID-19.
瑞德西韦是治疗 2019 年冠状病毒病(COVID-19)的有效药物之一。然而,尽管 COVID-19 是呼吸道疾病并感染肺部,但目前关于可吸入方案的研究仍很有限。本工作旨在通过评估来制备可吸入的瑞德西韦制剂并验证其效果。制备了含有不同比例(5%、10%、20%、40%和 70%)经气流粉碎的可吸入瑞德西韦与赋形剂的制剂,并从粒径分布、颗粒形态、流动性、含水量、结晶度、水吸附和解吸能力以及空气动力学性能等方面对其进行了表征。结果表明,载药量是促进瑞德西韦干粉分散的一个重要因素,而三元赋形剂在改善气溶胶性能方面作用不大。此外,含有乳糖载体的 70%瑞德西韦(70%RD-Lac)在 40°C 和 75%相对湿度下放置一个月后仍保持物理稳定性和高气溶胶性能。因此,制剂 70%RD-Lac 可能被推荐为治疗 COVID-19 的候选产品。