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Abstract <p>The production of prodrugs aimed at enhancing various properties of pharmaceuticals is a remains one of the most relevant and dynamic fields in modern pharmaceutical chemistry. While attaching a hydrophobic fragment can enhance cell wall permeability in drug design, it often comes at the cost of reduced solubility and bioavailability. One effective strategy to address this issue is to convert the drug into an amorphous form. However, the practical application of amorphous forms is hindered by the complexities involved in their preparation and their low kinetic and thermodynamic stability. In this study, we synthesized prodrugs based on sulfapyridine and sulfamethizole. We propose methods for producing an amorphous state and assess its stability using both non-isothermal and isothermal kinetics approaches. Our findings indicate that the amorphous forms of studied compounds are stable at room temperature for over 10 years. The results of the study can be used in the development of approaches to obtaining stable amorphous forms of drugs.</p>

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Kinetic Stability of Amorphous Glasses of New Sulfonamide-Based Prodrugs According to Differential Scanning Calorimetry Data

  • 期刊论文

  • 发表日期：

    2025年5月21日

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  • S. E. Lapuk,
  • I. O. Nasibullin,
  • L. S. Zubaidullina,
  • R. A. Larionov,
  • V. A. Burilov,
  • Kh. R. Khayarov,
  • R. N. Nagrimanov,
  • A. V. Gerasimov

摘要

Abstract

The production of prodrugs aimed at enhancing various properties of pharmaceuticals is a remains one of the most relevant and dynamic fields in modern pharmaceutical chemistry. While attaching a hydrophobic fragment can enhance cell wall permeability in drug design, it often comes at the cost of reduced solubility and bioavailability. One effective strategy to address this issue is to convert the drug into an amorphous form. However, the practical application of amorphous forms is hindered by the complexities involved in their preparation and their low kinetic and thermodynamic stability. In this study, we synthesized prodrugs based on sulfapyridine and sulfamethizole. We propose methods for producing an amorphous state and assess its stability using both non-isothermal and isothermal kinetics approaches. Our findings indicate that the amorphous forms of studied compounds are stable at room temperature for over 10 years. The results of the study can be used in the development of approaches to obtaining stable amorphous forms of drugs.