Development and Characterization of Orally Disintegrating Tablets Containing a Captopril-Cyclodextrin Complex

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems

Background:

• Captopril, an angiotensin-converting enzyme inhibitor, is a key hypertension treatment.
• Cyclodextrin inclusion complexes offer enhanced drug properties.
• Bitter taste and release kinetics are challenges for captopril formulations.

Purpose of the Study:

• To investigate the inclusion of captopril within β-cyclodextrin.
• To formulate captopril-β-cyclodextrin complexes into orally disintegrating tablets.
• To evaluate the dissolution and clinical performance of the new formulation.

Main Methods:

• Preparation of captopril-β-cyclodextrin inclusion complexes using the paste method (1:2 molar ratio).
• Characterization via Fourier-transform infrared spectroscopy, scanning electron microscopy, X-ray diffraction, and thermal analysis.
• Formulation into orally disintegrating tablets and dissolution studies in compendial and simulated saliva media.
• Clinical evaluation of taste and formulation compliance in healthy volunteers.

Main Results:

• Solid inclusion complexes of captopril with β-cyclodextrin were successfully prepared and characterized.
• The Noyes Whitney model accurately described captopril release kinetics.
• Orally disintegrating tablets demonstrated improved taste masking and acceptable release profiles.
• Clinical studies confirmed enhanced palatability compared to conventional captopril tablets.

Conclusions:

• β-cyclodextrin inclusion complexes offer a viable strategy for improving captopril formulation.
• Orally disintegrating tablets provide a patient-compliant dosage form with masked bitter taste.
• This approach enhances drug accessibility and therapeutic efficacy for hypertension management.