期刊
INTERNATIONAL JOURNAL OF PHARMACEUTICS
卷 602, 期 -, 页码 -出版社
ELSEVIER
DOI: 10.1016/j.ijpharm.2021.120649
关键词
Co-amorphous system; Co-former; Miscibility; Glass forming ability; LLPS; GLPS; Supersaturation
资金
- Manipal Academy of Higher Education
Co-amorphous drug delivery systems, utilizing small molecular weight compounds called co-formers to stabilize drugs in amorphous form, have shown potential as an alternative to amorphous solid dispersions technology. The stability and supersaturation potential of co-amorphous phases largely depend on the type of co-former employed, but the rationality behind co-former selection is poorly understood. Various factors affecting co-former selection in co-amorphous systems have been compiled, including thermodynamic, kinetic, and pharmacokinetic-pharmacologically relevant parameters.
Co-amorphous drug delivery systems are evolving as a credible alternative to amorphous solid dispersions technology. In Co-amorphous systems (CAMs), a drug is stabilized in amorphous form using small molecular weight compounds called as co-formers. A wide variety of small molecular weight co-formers have been leveraged in the preparation of CAMs. The stability and supersaturation potential of prepared co-amorphous phases largely depend on the type of co-former employed in the CAMs. However, the rationality behind the co-former selection in co-amorphous systems is poorly understood and scarcely compiled in the literature. There are various facets to the rational selection of co-former for CAMs. In this context, the present review compiles various factors affecting the co-former selection. The factors have been broadly classified under Thermodynamic, Kinetic and Pharmacokinetic-Pharmacologically relevant parameters. In particular, the importance of Glass transition, Miscibility, Liquid-Liquid phase separation (LLPS), Crystallization inhibition has been deliberated in detail.
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