| Autor: |
Sawittree Sahakijpijarn, Chaeho Moon, Zachary N. Warnken, Esther Y. Maier, Jennie E. DeVore, Dale J. Christensen, John J. Koleng, Robert O. Williams, III |
| Jazyk: |
angličtina |
| Rok vydání: |
2021 |
| Předmět: |
|
| Zdroj: |
International Journal of Pharmaceutics: X, Vol 3, Iss , Pp 100073- (2021) |
| Druh dokumentu: |
article |
| ISSN: |
2590-1567 |
| DOI: |
10.1016/j.ijpx.2021.100073 |
| Popis: |
Remdesivir dry powder for inhalation was previously developed using thin film freezing (TFF). A single-dose 24-h pharmacokinetic study in hamsters demonstrated that pulmonary delivery of TFF remdesivir can achieve plasma remdesivir and GS-441524 levels higher than the reported EC50s of both remdesivir and GS-441524 (in human epithelial cells) over 20 h. The half-life of GS-4412524 following dry powder insufflation was about 7 h, suggesting the dosing regimen would be twice-daily administration. Although the remdesivir-Captisol® (80/20 w/w) formulation showed faster and greater absorption of remdesivir and GS-4412524 in the lung, remdesivir-leucine (80/20 w/w) exhibited a greater Cmax with shorter Tmax and lower AUC of GS-441524, indicating lower total drug exposure is required to achieve a high effective concentration against SAR-CoV-2. In conclusion, remdesivir dry powder for inhalation would be a promising alternative dosage form for the treatment of COVID-19 disease. |
| Databáze: |
Directory of Open Access Journals |
| Externí odkaz: |
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