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AAPS PharmSciTech

, Volume 18, Issue 7, pp 2541–2550 | Cite as

Coamorphous Loratadine-Citric Acid System with Enhanced Physical Stability and Bioavailability

  • Jin Wang
  • Ruimiao Chang
  • Yanan Zhao
  • Jiye Zhang
  • Ting Zhang
  • Qiang Fu
  • Chun Chang
  • Aiguo ZengEmail author
Research Article

Abstract

Coamorphous systems using citric acid as a small molecular excipient were studied for improving physical stability and bioavailability of loratadine, a BCS class II drug with low water solubility and high permeability. Coamorphous loratadine-citric acid systems were prepared by solvent evaporation technique and characterized by differential scanning calorimetry, X-ray powder diffraction, and Fourier transform infrared spectroscopy. Solid-state analysis proofed that coamorphous loratadine-citric acid system (1:1) was amorphous and homogeneous, had a higher T g over amorphous loratadine, and the intermolecular hydrogen bond interactions between loratadine and citric acid exist. The solubility and dissolution of coamorphous loratadine-citric acid system (1:1) were found to be significantly greater than those of crystalline and amorphous form. The pharmacokinetic study in rats proved that coamorphous loratadine-citric acid system (1:1) could significantly improve absorption and bioavailability of loratadine. Coamorphous loratadine-citric acid system (1:1) showed excellently physical stability over a period of 3 months at 25°C under 0% RH and 25°C under 60% RH conditions. The improved stability of coamorphous loratadine-citric acid system (1:1) could be related to an elevated T g over amorphous form and the intermolecular hydrogen bond interactions between loratadine and citric acid. These studies demonstrate that the developed coamorphous loratadine-citric acid system might be a promising oral formulation for improving solubility and bioavailability of loratadine.

KEY WORDS

bioavailability coamorphous loratadine-citric acid systems loratadine physical stability 

Notes

Acknowledgements

This study was supported by the Natural Science Foundation of Shaanxi Province (grant number 2016JM8050) and the Fundamental Research Funds for the Central Universities.

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Copyright information

© American Association of Pharmaceutical Scientists 2017

Authors and Affiliations

  • Jin Wang
    • 1
  • Ruimiao Chang
    • 1
  • Yanan Zhao
    • 1
  • Jiye Zhang
    • 1
  • Ting Zhang
    • 1
  • Qiang Fu
    • 1
  • Chun Chang
    • 1
  • Aiguo Zeng
    • 1
    Email author
  1. 1.School of Pharmacy, Health Science CenterXi’an Jiaotong UniversityXi’anChina

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