Exploring the Impact of Intestinal Fluid Components on the Solubility and Supersaturation of Danazol

Cecilie Maria Madsen, Jakob Plum, Bart Hens, Patrick Augustijns, Anette Müllertz, Thomas Rades
In: Journal of Pharmaceutical Sciences · 2021 · vol. 110(6) , pp. 2479–2488 · doi:10.1016/j.xphs.2020.12.039 · PMID:33428916 · W3120230554
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This study investigated how components within intestinal fluid affect the solubility and supersaturation of danazol, a medication used to treat endometriosis and fibroids.

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Abstract

Eleven simulated intestinal fluids (SIF) were designed using a Design of Experiment (DoE) approach. The DoE SIF covered a range of compositions of fasted state human intestinal fluid (FaHIF) with regard to pH, bile salt (BS), and phospholipid (PL). Using the model compound danazol, the apparent crystalline solubility (aCS) and apparent amorphous solubility (aAS), as well as the supersaturation propensity was determined in the DoE SIF media. The aCS of danazol was dependent on the composition of the SIF, with PL as the main factor, and a small effect from BS and an interaction between BS and PL. From the DoE solubility data a model was derived, which could predict aCS in commercially available SIF (FaSSIF-V1 and -V2) and in a range of FaHIF. The aAS of danazol was differently affected by the SIF composition than the aCS; PL was again the main factor influencing the aAS, but interactions between BS and pH, as well as pH and PL were also important. The supersaturation propensities of danazol in the DoE SIF media were affected by the same factors as the aCS. Hence, the supersaturation behaviour and aCS of danazol, were found to be closely related.

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References (66)

SciLite annotations

chemicals 6
danazol bile salt phospholipid danazol danazol danazol
organisms 1
human

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