期刊
MOLECULAR PHARMACEUTICS
卷 11, 期 7, 页码 2294-2304出版社
AMER CHEMICAL SOC
DOI: 10.1021/mp400729x
关键词
poorly soluble pharmaceutical; phase behavior; molecular weight of polymer; indomethacin; artemisinin; thermodynamic model; PC-SAFT
资金
- CLIB-Graduate Cluster Industrial Biotechnology
- Alexander von Humboldt-Foundation
To improve the bioavailability of poorly soluble active pharmaceutical ingredients (APIs), these materials are often integrated into a polymer matrix that acts as a carrier. The resulting mixture is called a solid dispersion. In this work, the phase behaviors of solid dispersions were investigated as a function of the API as well as of the type and molecular weight of the carrier polymer. Specifically, the solubility of artemisinin and indomethacin was measured in different poly(ethylene glycol)s (PEG 400, PEG 6000, and PEG 35000). The measured solubility data and the solubility of sulfonamides in poly(vinylpyrrolidone) (PVP) K10 and PEG 35000 were modeled using the perturbed-chain statistical associating fluid theory (PC-SAFT). The results show that PC-SAFT predictions are in a good accordance with the experimental data, and PC-SAFT can be used to predict the whole phase diagram of an API/polymer solid dispersion as a function of the kind of API and polymer and of the polymer's molecular weight. This remarkably simplifies the screening process for suitable API/polymer combinations.
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