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Amorphism and physicochemical stability of spray-dried frusemide
1Department of Pharmaceutical Technology, Kobe Women's College of Pharmacy, Japan.
The Journal of Pharmacy and Pharmacology
|August 1, 1992
Summary
Investigating amorphous frusemide (a diuretic drug) forms revealed distinct glass transition temperatures and varying hygroscopic stability. Form B exhibited greater stability at low humidity, while both forms showed similar stability at high humidity.
Area of Science:
- Pharmaceutical Sciences
- Materials Science
- Physical Chemistry
Background:
- Amorphous forms of drugs can offer improved bioavailability compared to crystalline counterparts.
- Understanding the physicochemical properties and stability of amorphous drug forms is crucial for formulation development.
- Frusemide is a widely used loop diuretic.
Purpose of the Study:
- To investigate the physicochemical properties of spray-dried amorphous frusemide.
- To evaluate the hygroscopic stability of amorphous frusemide forms under various temperature and humidity conditions.
- To compare the stability profiles of two different amorphous forms (A and B).
Main Methods:
- Preparation of amorphous frusemide forms via spray-drying at 50°C (Form A) and 150°C (Form B).
- Differential Scanning Calorimetry (DSC) to determine glass transition temperatures and activation energies.
- X-ray Diffraction (XRD) to assess physical stability under controlled temperature (25°C, 40°C) and relative humidity (0%, 75%) conditions.
Main Results:
- Amorphous Form A exhibited a glass transition temperature (Tg) of 44.2°C, while Form B had a Tg of 54.4°C.
- Activation energies for glass transition and crystallization were calculated for both forms.
- Form B demonstrated higher stability than Form A at 0% relative humidity across tested temperatures.
- At 75% relative humidity, both Form A and Form B showed comparable stability at 25°C and 40°C.
Conclusions:
- Spray-drying conditions significantly influence the physicochemical properties and stability of amorphous frusemide.
- Amorphous Form B offers superior stability at low humidity, suggesting potential advantages in certain storage conditions.
- Both amorphous forms exhibit similar hygroscopic stability profiles at high humidity, indicating potential challenges for formulation in humid environments.