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Morphology control of eprosartan crystals via polymer-directed crystallization

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Abstract

Improving the stability, processability and bioavailability of drug crystals is important during the development of most drugs. In traditional crystal engineering, different crystallization conditions are used to tailor the properties of crystals, often improving one property at the cost of another, or simply optimizing both properties. The influence of soluble polymers on the particle morphology of crystals during the crystallization of eprosartan was investigated to explore the possibility of improving the properties of the drug crystals. The presence of polyethylenimine (PEI) during the crystallization of eprosartan induced the self-assembly of small primary crystals into larger aggregates without changing the crystal polymorph. In particular, spherical aggregates of an ordered structure were obtained when eprosartan was crystallized by changing the pH from 12 to 4.2 in the presence of PEI. This technique of polymer-directed crystallization is promising for the property engineering of drug crystals, which has been limited by a few crystallization variables to date.

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Acknowledgments

This article does not contain any studies with human and animal subjects performed by any of the authors. All authors (H. Bae, J. Lee) declare that they have no conflict of interest. This research was supported by a National Research Foundation grant from the Korea Ministry of Science, ICT and Future Planning (NRF-2014R1A2A1A11054206, NRF-2013R1A1A2021573 & Engineering Research Center 2014-009799).

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Authors and Affiliations

  1. Department of Chemical Engineering and Materials Science, Chung-Ang University, 221, Heukseok-dong, Dongjak-gu, Seoul, 156-756, Republic of Korea

    Harim Bae & Jonghwi Lee

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  1. Harim Bae
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  2. Jonghwi Lee
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Correspondence to Jonghwi Lee.

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Bae, H., Lee, J. Morphology control of eprosartan crystals via polymer-directed crystallization. Journal of Pharmaceutical Investigation 45, 367–374 (2015). https://doi.org/10.1007/s40005-015-0186-z

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  • DOI: https://doi.org/10.1007/s40005-015-0186-z

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