Itraconazole formation using supercritical carbon dioxide

Ali Hassan, Yi Min Tang, James W. Ayres

Research output: Contribution to journalArticlepeer-review

18 Citations (Scopus)

Abstract

A new method of preparing Itraconazole (C35H38Cl 2N8O4), a synthetic triazole antifungal agent, was developed using supercritical carbon dioxide (SC CO2) while eliminating the use of toxic solvents. Dissolution amounts of the product were measured in gastric fluid and compared to those of conventional drug formulations. Different operating conditions (five levels of treatment temperature ranging between 110-140°C, four levels of treatment pressure ranging between 30-400 atm, and four different treatment times ranging from 10-60 minutes) were tested in order to produce a desired Itraconazole product, which does not degrade during the product formation and has the highest extent of dissolution in gastric fluid after one hour. Itraconazole dissolution of 100% at one-hour was achieved for the drug produced at the optimum treatment condition: 135°C, 300 atm, and 30 minutes. Extent of dissolution obtained from this solvent and detergent-free process is 10% higher than that of the conventional method involving toxic organic solvents. Itraconazole produced using SC CO2 should provide minimal side effects in human body.

Original languageEnglish
Pages (from-to)1029-1035
Number of pages7
JournalDrug Development and Industrial Pharmacy
Volume30
Issue number10
DOIs
Publication statusPublished - 2004

Keywords

  • CO
  • Dissolution rate
  • Itraconazole
  • Supercritical fluids

ASJC Scopus subject areas

  • Pharmacology
  • Pharmaceutical Science
  • Drug Discovery
  • Organic Chemistry

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