Characterization of the indinavir raw materials stability in some pharmaceutical processes

Ticiano Gomes Do Nascimento, Irinaldo D. Basílio Júnior, Rui O. MacÊdo, Elisana A. Moura, Camila B. Dornelas, Vanderson B. Bernardo, Vânia N. Rocha, Csaba Nóvak

Research output: Contribution to journalArticle

7 Citations (Scopus)

Abstract

This article characterizes the stability of indinavir sulfate using different analytical techniques of quality control to evaluate important steps in the manufacturing process of indinavir, specifically involving storage and compression. Indinavir A, B, and C were obtained from different suppliers and submitted to DSC, Karl Fisher, NIR, XRPD analyses and dissolution assay. DSC curves of indinavir presented endothermic peaks of fusion at 149-150 °C for indinavir A and B (form I) and 139-143 °C for indinavir C (form II). When indinavir A and B were submitted to high Relative Humidity (RH) pseudo-polymorphic form II was formed. Indinavir C converted into an amorphous substance when submitted to compression. Near infrared and Karl Fisher assays detected high values of water for indinavir C in relation to indinavir A and B. X-ray powder diffraction of indinavir B and C showed displacement of 0.05-0.10 θ in the peaks and higher angle of diffraction in relation to indinavir A. Amorphous indinavir C demonstrated a higher intrinsic dissolution rate than indinavir A and B. Indinavir form I should be monitored during the pharmaceutical process to avoid its conversion to indinavir form II or an amorphous substance which can alter the dissolution rate.

Original languageEnglish
Pages (from-to)269-275
Number of pages7
JournalJournal of Thermal Analysis and Calorimetry
Volume102
Issue number1
DOIs
Publication statusPublished - Oct 1 2010

Keywords

  • DSC
  • Indinavir sulfate
  • Intrinsic dissolution
  • Raw materials
  • Stability of hydrates

ASJC Scopus subject areas

  • Condensed Matter Physics
  • Physical and Theoretical Chemistry

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  • Cite this

    Do Nascimento, T. G., Basílio Júnior, I. D., MacÊdo, R. O., Moura, E. A., Dornelas, C. B., Bernardo, V. B., Rocha, V. N., & Nóvak, C. (2010). Characterization of the indinavir raw materials stability in some pharmaceutical processes. Journal of Thermal Analysis and Calorimetry, 102(1), 269-275. https://doi.org/10.1007/s10973-009-0446-0