Discovery, characterization, and pharmaceutical applications of two loratadine–oxalic acid cocrystals

Zhengxuan Liang, Hongbo Chen, Chenguang Wang, Changquan Calvin Sun

Research output: Contribution to journalArticlepeer-review

Abstract

Loratadine (Lor) is an antihistamine drug commonly used to relieve the symptoms of allergy. It has high permeability but low solubility under physiological conditions. To overcome the problem of low solubility, we synthesized and characterized two Loratadine multi-component crystalline phases with oxalic acid (Oxa), i.e., a 1:1 Lor-Oxa conjugate acid-base (CAB) cocrystal (Lor-Oxa CAB) and a 2:1 Lor-Oxa cocrystal monohydrate (Lor-Oxa hydrate). Both cocrystals exhibited an enhanced solubility and intrinsic dissolution rate (IDR) compared to Lor and adequate physical stability. The intrinsic dissolution rate of Lor-Oxa CAB is 95 times that of Lor, which makes it a promising candidate for tablet formulation development.

Original languageEnglish (US)
Article number996
Pages (from-to)1-15
Number of pages15
JournalCrystals
Volume10
Issue number11
DOIs
StatePublished - Nov 2020

Bibliographical note

Funding Information:
We thank the Minnesota Supercomputing Institute (MSI) at the University of Minnesota for providing the resources that contributed to the research results reported within this paper (http://www.msi. umn.edu). The Bruker-AXS D8 Venture diffractometer was purchased through a grant from NSF/MRI (#1229400) and the University of Minnesota.

Funding Information:
Acknowledgments: We thank the Minnesota Supercomputing Institute (MSI) at the University of Minnesota for providing the resources that contributed to the research results reported within this paper (http://www.msi. umn.edu). The Bruker-AXS D8 Venture diffractometer was purchased through a grant from NSF/MRI (#1229400) and the University of Minnesota.

Publisher Copyright:
© 2020 by the authors. Licensee MDPI, Basel, Switzerland.

Keywords

  • Cocrystal
  • Compression
  • Intrinsic dissolution rate
  • Loratadine
  • Solubility

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