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Aging in co-amorphous systems: Dissolution decrease and non-negligible dissolution increase during storage without recrystallization
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DOI：10.1016/j.ijpharm.2024.124943.png)
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Abstract
En 中文
Developing co-amorphous systems is a promising strategy to improve the water solubility of poorly water-soluble drugs. Most of the studies focused on the initial dissolution rate of the fresh co-amorphous systems, and only physical stability was investigated after storage. However, the maintenance of the enhanced dissolution rate of co-amorphous systems after storage is necessary for further product development. The maintenance of amorphous forms after storage does not always mean the maintenance of the dissolution rate. In this study, indomethacin, arginine, tryptophan, and phenylalanine were used as the model drug and the co-formers to prepare co-amorphous systems and then stored under dry condition and RH 60 +/- 5 % condition. No recrystallization was observed after the storage for 40 d and 80 d. Interestingly, both intrinsic dissolution rate (IDR) decrease and unexpected increase after storage were confirmed. The further mixing of IND and the co-former at a molecular level and the moisture changes of the co-amorphous systems during storage were supposed to play important roles in the aging. This study reminds us that the possible dissolution changes (both dissolution decrease and increase) of co-amorphous systems during storage should be carefully considered, though these samples maintained amorphous forms.
Keywords:
Co-amorphous systems
Poorly water-soluble drugs
Aging
Intrinsic dissolution rate (IDR)
Physical stability
Journal
IF:
5.2
Papers:
2.2W
Citations:
7.5W
Organization
Cited Papers
Co-Amorphous Drug Formulations in Numbers: Recent Advances in Co-Amorphous Drug Formulations with Focus on Co-Formability, Molar Ratio, Preparation Methods, Physical Stability, In Vitro and In Vivo Performance, and New Formulation Strategies.png)
PHARMACEUTICS
OAAI
PHARMACEUTICSIF5.5
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