FORMULATION AND EVALUATION OF EXTENDED RELEASE GASTRO RETENTIVE TABLETS OF METOPROLOL SUCCINATE

Background: Metoprolol succinate, a cardioselective 1-adrenergic receptor antagonist, exhibits suboptimal bioavailability due to its short gastric residence time and preferential absorption in the upper gastrointestinal tract.This study aimed to develop and evaluate gastro-retentive extended-release tablets of metoprolol succinate using hydroxypropyl methylcellulose (HPMC) as the primary matrix-forming polymer to enhance therapeutic efficacy and patient compliance.Methods: Seven formulations (F1-F7) were developed using wet granulation technique with varying concentrations of HPMC (100-170 mg), sodium bicarbonate (80-150 mg), and microcrystalline cellulose as primary excipients.Comprehensive pre-formulation studies included organoleptic evaluation, melting point determination, solubility profiling, and Fourier transform infrared spectroscopy for drug-excipient compatibility assessment.Post-compression parameters including hardness, friability, weight variation, and thickness were evaluated according to pharmacopoeial standards. Results:The optimized formulation F4, containing 170 mg HPMC and 90 mg sodium bicarbonate, demonstrated superior physical characteristics with hardness of 6.0 kg/cm, friability of 0.25%, and sustained drug release achieving 98% cumulative release over 12 hours.Pre-formulation studies confirmed excellent drug-excipient compatibility with melting point of 121-124C and partition coefficient of 4.0, indicating favorable lipophilic characteristics for oral absorption. Conclusion:The developed gastro-retentive tablets successfully provided controlled release of metoprolol succinate over an extended period, demonstrating potential for once-daily administration with enhanced patient compliance and therapeutic outcomes in cardiovascular disease management.

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Publication Details

Journal
Indian Journal of Health Care Medical & Pharmacy Practice
Published
2025-05-06
DOI
https://doi.org/10.59551/ijhmp/25832069/2025.6.1.114
Primary Topic
Drug Solubulity and Delivery Systems
Type
article
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article

FORMULATION AND EVALUATION OF EXTENDED RELEASE GASTRO RETENTIVE TABLETS OF METOPROLOL SUCCINATE

Rohit Ghoshi
Indian Journal of Health Care Medical & Pharmacy Practice
Drug Solubulity and Delivery Systems
article

FORMULATION AND EVALUATION OF EXTENDED RELEASE GASTRO RETENTIVE TABLETS OF METOPROLOL SUCCINATE

Rohit Ghoshi
article en

Abstract

Background: Metoprolol succinate, a cardioselective 1-adrenergic receptor antagonist, exhibits suboptimal bioavailability due to its short gastric residence time and preferential absorption in the upper gastrointestinal tract.This study aimed to develop and evaluate gastro-retentive extended-release tablets of metoprolol succinate using hydroxypropyl methylcellulose (HPMC) as the primary matrix-forming polymer to enhance therapeutic efficacy and patient compliance.Methods: Seven formulations (F1-F7) were developed using wet granulation technique with varying concentrations of HPMC (100-170 mg), sodium bicarbonate (80-150 mg), and microcrystalline cellulose as primary excipients.Comprehensive pre-formulation studies included organoleptic evaluation, melting point determination, solubility profiling, and Fourier transform infrared spectroscopy for drug-excipient compatibility assessment.Post-compression parameters including hardness, friability, weight variation, and thickness were evaluated according to pharmacopoeial standards. Results:The optimized formulation F4, containing 170 mg HPMC and 90 mg sodium bicarbonate, demonstrated superior physical characteristics with hardness of 6.0 kg/cm, friability of 0.25%, and sustained drug release achieving 98% cumulative release over 12 hours.Pre-formulation studies confirmed excellent drug-excipient compatibility with melting point of 121-124C and partition coefficient of 4.0, indicating favorable lipophilic characteristics for oral absorption. Conclusion:The developed gastro-retentive tablets successfully provided controlled release of metoprolol succinate over an extended period, demonstrating potential for once-daily administration with enhanced patient compliance and therapeutic outcomes in cardiovascular disease management.

Indian Journal of Health Care Medical & Pharmacy PracticeVol. 06(01)
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FORMULATION AND EVALUATION OF EXTENDED RELEASE GASTRO RETENTIVE TABLETS OF METOPROLOL SUCCINATE — Rohit Ghoshi · Indian Journal of Health Care Medical & Pharmacy Practice (2025) | TGRS Research Map | TGRS