Citation: Xiao-Feng CHEN, Peng LI, Hui-Ping WANG, Juan XU, Li-Feng NING. Polymorphic Characterization and Bioavailability of Nomegestrol Acetate[J]. Chinese Journal of Structural Chemistry, ;2020, 39(4): 662-672. doi: 10.14102/j.cnki.0254-5861.2011-2514 shu

Polymorphic Characterization and Bioavailability of Nomegestrol Acetate

National Research Institute for Family Planning, Beijing 100081, China

Corresponding author: Li-Feng NING, saintcxf2017@163.com
Received Date: 27 June 2019
Accepted Date: 7 January 2020

Fund Project: the National Key R&D Program of China 2016YFC1000901the innovation fund of National Research Institute for Family Planning KYS [2019] GJM02

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Polymorph screening is currently one of the most important strategies of innovators and generic companies from both pharmaceutical and intellectual property rights perspectives. Different polymorphs may have varying physicochemical properties which influence the bioavailability. The purpose of this study was to investigate the crystal structures and physicochemical properties of Nomegestrol acetate (NOMAC) polymorphs. Forms Ⅰ and Ⅱ (dioxane solvate) were isolated and prepared by systemic crystallization screening in this study, and the forms are reported for the first time. A structural analysis and comparison of all the forms are presented. This study was also the first time to apply a rapid and feasible ultra-high-performance-liquid chromatography (UHPLC)-electrospray ionization (ESI)-tandem mass spectrometry (MS) method to determine plasma levels of NOMAC within 3.0 mins. And this study demonstrated that the optimal crystal Form Ⅰ displayed higher bioavailability than API indicating that Form Ⅰ could be an alternative solid form that needs further research.
- nomegestrol acetate,
- crystalline structure,
- solubility,
- bioavailability
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