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Issue 19, 2016
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Solid-state characterization of 17β-estradiol co-crystals presenting improved dissolution and bioavailability

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Abstract

17β-estradiol (E2) is a steroid hormone with low oral bioavailability due to its low aqueous solubility (0.2–5 μg mL−1). To improve its solubility and thus bioavailability, two co-crystals of E2 with isonicotinamide (INA) (1) and piperazine (PIP) (2) were successfully designed and synthesized and their structures were successfully determined. In vivo PK studies revealed that 1 possesses improved bioavailability in an animal model.

Graphical abstract: Solid-state characterization of 17β-estradiol co-crystals presenting improved dissolution and bioavailability

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Publication details

The article was received on 24 Feb 2016, accepted on 16 Apr 2016 and first published on 18 Apr 2016


Article type: Paper
DOI: 10.1039/C6CE00433D
Citation: CrystEngComm, 2016,18, 3498-3505

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    Solid-state characterization of 17β-estradiol co-crystals presenting improved dissolution and bioavailability

    J. Wang, X. Wang, Y. Yang, X. Chen and X. Mei, CrystEngComm, 2016, 18, 3498
    DOI: 10.1039/C6CE00433D

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