Is metoprolol tartrate extended release
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Metoprolol Tartrate Extended-Release Formulations: A Comprehensive Overview
Introduction to Metoprolol Tartrate Extended-Release
Metoprolol tartrate is a beta-1 selective adrenergic blocking agent commonly used to treat hypertension, angina, and heart failure. Extended-release (ER) formulations of metoprolol tartrate are designed to provide a controlled release of the drug over an extended period, improving patient compliance and maintaining therapeutic drug levels.
Development and Evaluation of ER Matrix Tablets
Formulation Techniques and Challenges
Several studies have focused on developing ER matrix tablets for metoprolol tartrate using various formulation techniques. One study explored the use of different grades of hydroxypropyl methylcellulose (HPMC) and granulation processes, finding that fluid-bed granulation with Methocel K100LV provided the best balance of flow and tableting performance1. Another study highlighted the robustness of barrier membrane (BM) coated matrix tablets, which eliminated the initial burst release and provided controlled drug release under various gastrointestinal conditions2.
Critical Formulation Variables
The influence of critical formulation and processing variables on drug release has been extensively studied. Factors such as polymer level, filler type, and compression force significantly affect the drug release profile. For instance, increasing the polymer level or changing the filler from lactose to dicalcium phosphate can decrease the amount of metoprolol released over 12 hours1 3. Additionally, the viscosity of ethylcellulose used in the barrier membrane coating plays a crucial role in ensuring consistent drug release5.
In Vitro-In Vivo Correlation (IVIVC)
Predictability and Scale-Up
The predictability of in vitro-in vivo correlation (IVIVC) for metoprolol tartrate ER formulations has been validated across different scales and processing methods. Studies have shown that IVIVC can accurately predict plasma profiles for various formulations, making it a valuable tool for regulatory approval and ensuring consistent therapeutic outcomes6.
Novel Delivery Systems
Chronotherapeutic Formulations
Innovative approaches have been explored to optimize the timing of drug release. A novel chronotherapeutic formulation designed for nighttime dosing was developed to provide maximum effect during morning hours when the risk of cardiovascular events is higher. This formulation used a combination of HPMC and Eudragit® coatings to control the release rate and ensure stability across different pH levels and agitation rates4.
Ophthalmic Gels
Metoprolol tartrate has also been formulated into ophthalmic gels to increase contact time with the cornea and provide a sustained release. Studies have shown that gels using Carbopol 934 and Pluronic F127 polymers can effectively extend the duration of drug action, making them a promising alternative for ocular applications9.
Clinical Efficacy and Tolerability
Comparison of ER Preparations
Clinical trials comparing different ER preparations of metoprolol tartrate have demonstrated significant reductions in blood pressure with both hydrophilic and insoluble matrix formulations. These studies found no significant differences in antihypertensive efficacy between the two types of formulations, indicating that both are effective and well-tolerated options for managing hypertension8.
Conclusion
The development of metoprolol tartrate extended-release formulations has advanced significantly, with various studies highlighting the importance of formulation techniques, critical variables, and innovative delivery systems. These advancements ensure consistent drug release, improved patient compliance, and better therapeutic outcomes. As research continues, new formulations and delivery methods will likely emerge, further enhancing the clinical utility of metoprolol tartrate.
Sources and full results
Most relevant research papers on this topic
Development of metoprolol tartrate extended-release matrix tablet formulations for regulatory policy consideration.
Metoprolol tartrate extended-release matrix tablet formulations using Methocel K100LV and fluid-bed granulation show satisfactory flow and tableting performance, with fluid-bed granulation being the most suitable process for regulatory policy development.
In Vitro Study
Highly CitedRobustness of barrier membrane coated metoprolol tartrate matrix tablets: Drug release evaluation under physiologically relevant in vitro conditions
Barrier membrane-coated hydrophilic matrix tablets show robust drug release without initial burst in vitro, demonstrating a promising approach for highly controlled and robust drug release in oral extended release formulations.
In Vitro StudyIdentification of critical formulation and processing variables for metoprolol tartrate extended-release (ER) matrix tablets.
Changes in polymer level significantly affect drug release in metoprolol tartrate extended-release matrix tablets, with dicalcium phosphate and compression force also affecting dissolution profiles.
Highly CitedDesign and in vitro evaluation of a novel controlled onset extended-release delivery system of metoprolol tartrate
The developed controlled onset extended-release formulation of metoprolol tartrate provides maximum blood pressure reduction in the morning hours, independent of pH, rotational speed, and gastric motility.
In Vitro StudyInvestigation into the Effect of Ethylcellulose Viscosity Variation on the Drug Release of Metoprolol Tartrate and Acetaminophen Extended Release Multiparticulates—Part I
Ethylcellulose viscosity variation within manufacturers' specifications does not impact drug release in extended release multiparticulate dosage forms for metoprolol tartrate and acetaminophen, highlighting consistent and robust drug release performance.
Evaluation of "external" predictability of an in vitro-in vivo correlation for an extended-release formulation containing metoprolol tartrate.
The metoprolol IVIVC is externally valid and predictive of alternate processing methods, scale-up, and in vitro dissolution data, but not for formulation V.
In Vitro StudyMetoprolol CR/XL in the Treatment of Chronic Heart Failure
Metoprolol CR/XL improves survival and reduces hospitalization in patients with chronic heart failure when individualized therapy is designed.
Efficacy and Tolerability of Metoprolol Tartrate in Patients with Mild- to- Moderate Essential Hypertension
Both Meto HM and Meto IM, 100mg and 200mg once daily, effectively reduce blood pressure in patients with mild-to-moderate hypertension, with no significant differences in efficacy or tolerability.
RCTFormulation and evaluation of new long acting metoprolol tartrate ophthalmic gels
Carbopol 934 gel formulations with Carbopol 934 polymer extend the duration of pressure reducing effect of metoprolol tartrate to more than 5 hours compared to Pluronic F127 gel formulations.
In Vitro StudyDevelopment of Sustained Release Capsules Containing “Coated Matrix Granules of Metoprolol Tartrate”
Wet granulation with subsequent coating by fluidized bed technique is a suitable method to formulate sustained release capsules of metoprolol tartrate, providing therapeutic benefits over conventional immediate release dosage forms.
In Vitro Study