DSC, TGA-FTIR and FTIR Assisted by Chemometric Factor Analysis and PXRD in Assessing the Incompatibility of the Antiviral Drug Arbidol Hydrochloride with Pharmaceutical Excipients

Molecules. 2024 Jan 4;29(1):264. doi: 10.3390/molecules29010264.

Abstract

Arbidol hydrochloride is an antiviral product widely used in Russia and China for the treatment of, among other diseases, influenza. In recent years, it has turned out to be highly effective against COVID-19. However, there is little knowledge about its physicochemical properties and its behavior in the presence of various pharmaceutical excipients, which could be useful in the development of new preparations by increasing its solubility and bioavailability. For this reason, binary mixtures composed of arbidol hydrochloride and selected pharmaceutical excipients such as chitosan, polyvinylpyrrolione K-30 and magnesium stearate were prepared and subjected to differential scanning calorimetry (DSC), thermogravimetry combined with Fourier transform infrared spectrometry (TGA-FTIR) and Fourier transform infrared spectrometry (FTIR) analyses. In order to obtain clarity in the interpretation of the outcomes, chemometric calculations with factor analysis (FA) were used. Additionally, a powder X-ray diffraction (PXRD) and an intrinsic dissolution rate study were performed for arbidol hydrochloride itself and in the presence of excipients. As a result of the study, it was revealed that arbidol hydrochloride may undergo polymorphic transformations and be incompatible with chitosan and magnesium stearate. However, mixing arbidol hydrochloride with polyvinylpyrrolidone K-30 guarantees the obtaining of durable and safe pharmaceutical preparations.

Keywords: DSC; FTIR; PXRD; TGA-FTIR; arbidol hydrochloride; chemometric calculation; compatibility/incompatibility; excipients; intrinsic dissolution rate study.

MeSH terms

  • Antiviral Agents
  • Calorimetry, Differential Scanning
  • Chemometrics*
  • Chitosan*
  • Excipients
  • Factor Analysis, Statistical
  • Hydrochloric Acid
  • Indoles*
  • Spectroscopy, Fourier Transform Infrared
  • Sulfides*
  • X-Ray Diffraction

Substances

  • umifenovir
  • Chitosan
  • Excipients
  • Hydrochloric Acid
  • Antiviral Agents
  • Indoles
  • Sulfides