Preparation and characterization of triamterene complex with ascorbic acid derivatives

Area of Science:

• Pharmaceutical Sciences
• Materials Science

Background:

• Triamterene (TRT) is a diuretic drug with poor aqueous solubility, limiting its bioavailability.
• Developing effective drug delivery systems is crucial for improving the therapeutic efficacy of poorly soluble compounds like TRT.

Purpose of the Study:

• To prepare solid dispersions of triamterene (TRT) using ascorbic acid (AA) or ascorbic acid 2 glucoside (AA2G).
• To characterize the physical properties of these solid dispersions.
• To evaluate the impact of these solid dispersions on the dissolution rate of TRT.

Main Methods:

• Solid dispersions were prepared using the evaporation (EVP) method.
• Physical characterization involved Powder X-ray Diffraction (PXRD), Differential Scanning Calorimetry (DSC), Fourier Transform Infrared (FT-IR) spectroscopy, and Near-Infrared Absorption (NIR) spectroscopy.
• Dissolution tests were conducted to assess the drug release profiles.

Main Results:

• PXRD and DSC indicated the formation of amorphous solid dispersions with the disappearance of characteristic melting peaks for TRT and the co-formers.
• FT-IR and NIR spectroscopy provided evidence of molecular interactions between TRT and AA/AA2G, suggesting complex formation.
• Dissolution tests showed a significant enhancement in the dissolved fraction of TRT from the solid dispersions, reaching approximately 90% within 3 minutes compared to 30% for TRT alone.

Conclusions:

• Solid dispersions of TRT with AA or AA2G can be successfully prepared using the evaporation method.
• The prepared solid dispersions exhibit improved physical properties and molecular interactions conducive to enhanced drug release.
• The study confirms that these solid dispersions significantly improve the dissolution properties of triamterene, offering a promising approach for enhancing its bioavailability.