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Supersaturation Theory and Supersaturating Drug Delivery System(SDDS)

Yifan Xue , Wenhui Meng , Runze Wang , Junjie Ren , Weili Heng , Jianjun Zhang

Progress in Chemistry ›› 2020, Vol. 32 ›› Issue (6) : 698 -712.

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Progress in Chemistry ›› 2020, Vol. 32 ›› Issue (6) : 698-712 DOI: 10.7536/PC19094
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Supersaturation Theory and Supersaturating Drug Delivery System(SDDS)
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Abstract

In drug research and development, it is a big challenge to effectively improve the solubility/dissolution and in vivo absorption of poorly water-soluble drugs. Currently, supersaturating drug delivery system(SDDS), taking advantage of the drug solution in a supersaturated state, can simultaneously improve the apparent solubility and permeability of drugs. The current article systematically reviews the theory of supersaturation and its application, including generation and maintenance of supersaturation, and the relationship with in vivo drug absorption. Commonly used approaches, especially amorphous solid dispersion, co-crystal, amorphous/co-amorphous systems, have been introduced.

Contents

1 Introduction
2 Synopsis of supersaturation 2.1 Generation2.2 Maintenance2.3 Stability2.4 The relationship between supersaturation and in vivo drug absorption
3 Supersaturating drug delivery system(SDDS) 3.1 Amorphous solid dispersion3.2 Co-amorphous3.3 Co-crystal3.4 Salts3.5 Nanocrystal3.6 Others
4 Conclusion and outlook

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Keywords

supersaturation / solubility / permeability / absorption / supersaturating drug delivery system(SDDS)

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Yifan Xue, Wenhui Meng, Runze Wang, Junjie Ren, Weili Heng, Jianjun Zhang. Supersaturation Theory and Supersaturating Drug Delivery System(SDDS). Progress in Chemistry, 2020, 32(6): 698-712 DOI:10.7536/PC19094

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Funding

the National Natural Science Foundation of China(81703712, 81773675, 81873012)

the “Double First-Class” University Project(CPU2018GY11, CPU2018GY27)

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