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Purpose <p>This work presents a study of the physical stability of a co-amorphous (CAM) combination of two drugs: Candesartan cilexetil (CDS) and Amlodipine besylate (AMB) and the polymer polyvinylpyrrolidone (PVP).</p> Methods <p>Two methods, milling and quench cooling, were used for the preparation of the co-amorphous drugs. Prepared samples were characterized by DSC, FTIR, LC-MS and XRD.</p> Results <p>AMB improved the amorphization propensity of CDS into co-milled CDS with AMB systems. Compared to the milling process, quench cooling generated a stabler amorphous dispersion reinforced by the integration of PVP; however, the heat treatment strongly affected candesartan cilexetil, causing decomposition. The optimal method to prepare amorphous CDS is milling with AMB in a 50/50 mixture. 20% PVP can be added to improve the amorphous state, although in the presence of PVP the sample becomes more sensitive to water.</p> Conclusion <p>The challenges related to the formulation of co-amorphous CDS-AMB will be discussed, focusing on the limitations associated with their physical and chemical stability.</p>

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The Physical Stability of Co-Amorphous Candesartan-Amlodipine

  • 期刊论文

  • 发表日期：

    2025年2月13日

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  • Rachel Torkhani,
  • Feriel El Kara,
  • Ivo Rietveld,
  • Rafik Kalfat,
  • Haykel Galai

摘要

Purpose

This work presents a study of the physical stability of a co-amorphous (CAM) combination of two drugs: Candesartan cilexetil (CDS) and Amlodipine besylate (AMB) and the polymer polyvinylpyrrolidone (PVP).

Methods

Two methods, milling and quench cooling, were used for the preparation of the co-amorphous drugs. Prepared samples were characterized by DSC, FTIR, LC-MS and XRD.

Results

AMB improved the amorphization propensity of CDS into co-milled CDS with AMB systems. Compared to the milling process, quench cooling generated a stabler amorphous dispersion reinforced by the integration of PVP; however, the heat treatment strongly affected candesartan cilexetil, causing decomposition. The optimal method to prepare amorphous CDS is milling with AMB in a 50/50 mixture. 20% PVP can be added to improve the amorphous state, although in the presence of PVP the sample becomes more sensitive to water.

Conclusion

The challenges related to the formulation of co-amorphous CDS-AMB will be discussed, focusing on the limitations associated with their physical and chemical stability.