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


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.


bioavailability coamorphous loratadine-citric acid systems loratadine physical stability 



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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