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, C. Novák

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 2010

Fingerprint

Indinavir
Raw materials
dissolving
Pharmaceutical Preparations
quality control
diffraction
humidity
sulfates
manufacturing
fusion
curves
water
Dissolution
x rays
Assays

Keywords

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

ASJC Scopus subject areas

  • Physical and Theoretical Chemistry
  • Condensed Matter Physics

Cite this

Do Nascimento, T. G., Basílio Júnior, I. D., MacÊdo, R. O., Moura, E. A., Dornelas, C. B., Bernardo, V. B., ... Novák, 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

Characterization of the indinavir raw materials stability in some pharmaceutical processes. / Do Nascimento, Ticiano Gomes; Basílio Júnior, Irinaldo D.; MacÊdo, Rui O.; Moura, Elisana A.; Dornelas, Camila B.; Bernardo, Vanderson B.; Rocha, Vânia N.; Novák, C.

In: Journal of Thermal Analysis and Calorimetry, Vol. 102, No. 1, 10.2010, p. 269-275.

Research output: Contribution to journalArticle

Do Nascimento, TG, Basílio Júnior, ID, MacÊdo, RO, Moura, EA, Dornelas, CB, Bernardo, VB, Rocha, VN & Novák, C 2010, 'Characterization of the indinavir raw materials stability in some pharmaceutical processes', Journal of Thermal Analysis and Calorimetry, vol. 102, no. 1, pp. 269-275. https://doi.org/10.1007/s10973-009-0446-0
Do Nascimento TG, Basílio Júnior ID, MacÊdo RO, Moura EA, Dornelas CB, Bernardo VB et al. Characterization of the indinavir raw materials stability in some pharmaceutical processes. Journal of Thermal Analysis and Calorimetry. 2010 Oct;102(1):269-275. https://doi.org/10.1007/s10973-009-0446-0
Do Nascimento, Ticiano Gomes ; Basílio Júnior, Irinaldo D. ; MacÊdo, Rui O. ; Moura, Elisana A. ; Dornelas, Camila B. ; Bernardo, Vanderson B. ; Rocha, Vânia N. ; Novák, C. / Characterization of the indinavir raw materials stability in some pharmaceutical processes. In: Journal of Thermal Analysis and Calorimetry. 2010 ; Vol. 102, No. 1. pp. 269-275.
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