Metoprolol succ vs tartrate
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Comparison of Metoprolol Succinate vs. Metoprolol Tartrate
Hemodynamic Effects in Congestive Heart Failure
Hemodynamic Benefits and Adverse Effects
Both metoprolol succinate (MS) and metoprolol tartrate (MT) have been shown to produce significant hemodynamic benefits in patients with congestive heart failure. A study comparing the two formulations found that long-term therapy with either drug resulted in similar improvements in functional, exercise, and hemodynamic parameters1. However, upon readministration during chronic therapy, both drugs exhibited parallel adverse hemodynamic effects, such as a decrease in cardiac index and stroke volume index, and an increase in systemic vascular resistance1.
Heart Rate Reduction
In another study, metoprolol succinate sustained-release tablets were found to be more effective in reducing the average heart rate in patients with chronic congestive heart failure compared to metoprolol tartrate tablets2. Despite this difference, both formulations showed no significant differences in other cardiac and renal function parameters, such as left ventricular end-diastolic dimension (LVDd), ejection fraction (EF), blood urea nitrogen (BUN), and creatinine (Crea) levels2.
Structural and Bioavailability Differences
Solid-State Structure and Behavior
The solid-state structures of metoprolol tartrate and metoprolol succinate exhibit notable differences. Metoprolol succinate has a slightly greater cohesive energy and undergoes reversible anisotropic lattice expansion/contraction upon temperature changes. In contrast, metoprolol tartrate expands/contracts isotropically and forms an amorphous solid upon cooling from the melt, which takes several days to revert to its original crystal form3. These differences are significant for pharmaceutical manufacturing and storage.
Bioavailability
A study comparing the bioavailability of metoprolol tartrate administered orally and via a transdermal drug delivery system (TDDS) found that the TDDS form had a threefold improvement in bioavailability over the oral form4. The TDDS maintained therapeutically effective plasma concentrations for up to 48 hours, which could enhance patient compliance by reducing the frequency of administration4.
Extended-Release Formulations
Development and Manufacturing
Research on developing extended-release (ER) matrix tablet formulations for metoprolol tartrate has shown that the choice of polymer and granulation process significantly affects drug release rates. Higher viscosity grades of hydroxypropyl methylcellulose (HPMC) resulted in slower drug release, and fluid-bed granulation was identified as the most satisfactory process for ensuring good flow and tableting performance5. These findings are crucial for regulatory policy development concerning the scale-up and post-approval changes for modified-release dosage forms5.
Conclusion
Both metoprolol succinate and metoprolol tartrate are effective in managing congestive heart failure, with similar hemodynamic benefits and adverse effects. Metoprolol succinate may offer advantages in heart rate reduction and structural stability, while metoprolol tartrate has shown improved bioavailability when administered via TDDS. The development of extended-release formulations for metoprolol tartrate highlights the importance of manufacturing processes in achieving consistent drug release profiles.
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