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Studies on the characterization and polymorphic stability of Fosamprenavir
Cleydson F Cordeiro1, Ingrid Bettio1, Marcello G Trevisan1
1Institute of Chemistry, Federal University of Alfenas, Alfenas, MG, Brazil.
Anais Da Academia Brasileira De Ciencias
|May 14, 2020
Summary
Fosamprenavir calcium Form I, crucial for treating AIDS, maintains its crystalline structure and chemical integrity under various conditions. This study confirms its suitability for pharmaceutical applications.
Area of Science:
- Pharmaceutical Sciences
- Solid-State Chemistry
- Drug Development
Background:
- Fosamprenavir calcium, an amprenavir prodrug, is vital in treating Acquired Immunodeficiency Syndrome (AIDS).
- Understanding the physico-chemical properties and stability of different solid forms is essential for selecting optimal drug formulations.
- Patents describe various solid forms, necessitating detailed characterization.
Purpose of the Study:
- To characterize Form I (commercial) and amorphous fosamprenavir calcium.
- To evaluate the chemical and polymorphic stability of the commercial form (Form I).
- To determine the suitability of fosamprenavir calcium Form I for pharmaceutical use.
Main Methods:
- Differential Scanning Calorimetry (DSC)
- Thermogravimetry (TGA)
- Powder X-ray Diffraction (PXRD)
- Fourier-Transform Infrared Spectroscopy (FTIR)
- Scanning Electron Microscopy (SEM)
- High-Performance Liquid Chromatography (HPLC)
Main Results:
- Water presence is critical for maintaining Form I crystallinity, as shown by thermal and spectroscopic analyses.
- Form I exhibited no phase changes under accelerated stability testing (controlled temperature and humidity).
- HPLC and FTIR confirmed the chemical stability of Form I under tested conditions.
Conclusions:
- Fosamprenavir calcium Form I is stable both polymorphically and chemically.
- The presence of water is essential for the crystalline integrity of Form I.
- Form I demonstrates suitability for pharmaceutical development and application.
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