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Study of stability and drug-excipient compatibility of estradiol and pharmaceutical excipients

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Abstract

Estradiol (E2) is the main drug used in menopause therapy. This study aimed to evaluate the drug-excipient compatibility of binary mixtures (BMs) (1:1 BMs, w/w), initially by differential scanning calorimetry (DSC), and subsequently, by complementary techniques such as X-ray powder diffraction (XRPD) and high performance liquid chromatography (HPLC) if there was any evidence of interaction. The samples were stored under accelerated stability conditions (40 °C at 75 % relative humidity). The DSC curves of estradiol and the BMs with excipients (corn starch, lactose, xanthan gum, microcrystalline cellulose, magnesium stearate, dibasic calcium phosphate, and talc) were obtained. The results show that estradiol was compatible with all the selected excipients. XRPD and HPLC analysis were instrumental in interpreting the DSC results and excluding relevant pharmaceutical incompatibilities in all cases. Overall, the compatibility of the selected excipients with estradiol was successfully evaluated using a combination of thermal and spectroscopic methods, and the formulations developed using the compatible excipients were found to be stable.

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Acknowledgements

This work has been supported by the Program for Changjiang Scholars and Innovative Research Team in University (IRT13095), and prospective joint research project of Jiangsu province (BY2012193).

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Authors and Affiliations

  1. School of Chemical Science and Technology, Yunnan University, Kunming, 650031, People’s Republic of China

    Rui Gao, Yi Jin, Qing-Yi Yang & Jun Lin

  2. College of Chemistry and Chemical Engineering, Southeast University, Nanjing, 211189, People’s Republic of China

    Rui Gao & Bai-Wang Sun

Authors
  1. Rui Gao
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  2. Yi Jin
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  3. Qing-Yi Yang
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  4. Bai-Wang Sun
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  5. Jun Lin
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Corresponding authors

Correspondence to Bai-Wang Sun or Jun Lin.

Additional information

Rui Gao and Yi Jin have contributed equally to this study.

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Gao, R., Jin, Y., Yang, QY. et al. Study of stability and drug-excipient compatibility of estradiol and pharmaceutical excipients. J Therm Anal Calorim 120, 839–845 (2015). https://doi.org/10.1007/s10973-014-4234-0

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  • DOI: https://doi.org/10.1007/s10973-014-4234-0

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