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Development and in vitro evaluation of a buccoadhesive pindolol tablet formulation
1Department of Pharmaceutical Technology, Faculty of Pharmacy, Marmara University, Istanbul, Turkey.
Drug Development and Industrial Pharmacy
|January 7, 1999
Summary
New buccoadhesive tablets offer controlled release of pindolol for chronic hypertension. This approach improves drug bioavailability by bypassing liver metabolism, ensuring consistent plasma levels.
Area of Science:
- Pharmaceutical Technology
- Pharmacology
- Drug Delivery Systems
Background:
- Chronic hypertension management requires consistent drug plasma concentrations.
- Pindolol's bioavailability is limited by significant hepatic first-pass metabolism.
- Buccoadhesive drug delivery offers potential for sustained release and improved absorption.
Purpose of the Study:
- To develop and evaluate controlled-release buccoadhesive tablets of pindolol.
- To achieve constant plasma concentrations for chronic hypertension treatment.
- To enhance pindolol bioavailability by avoiding hepatic first-pass metabolism.
Main Methods:
- Formulation of buccoadhesive tablets using Carbopol 934 and NaCMC as bioadhesive polymers.
- Incorporation of Methocel K4M, Methocel K15M, and HPC as matrix-forming polymers.
- Evaluation of tablet properties including weight, hardness, friability, content uniformity, swelling rate, bioadhesive force, and drug release rate.
Main Results:
- Successfully prepared controlled-release buccoadhesive tablets containing pindolol.
- Characterization confirmed acceptable physical properties and swelling behavior.
- Drug release studies demonstrated sustained release profiles over the desired period.
Conclusions:
- Controlled-release buccoadhesive pindolol tablets are a viable formulation for chronic hypertension.
- This delivery system can improve pindolol bioavailability by reducing first-pass metabolism.
- Buccoadhesive technology offers a promising strategy for optimizing antihypertensive therapy.