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Aim <p>In the present study, matrices of metoprolol tartrate (200&#xa0;mg) were developed with two individual polymers (Ethocel 7 premium and Ethocel 7FP premium) at various w/w drug-to-polymer ratios (10:3, 10:4, and 10:5), with a filler (spray-dried lactose) and lubricant (magnesium stearate).</p> Methodology <p>The direct compression method was used to prepare the matrices, and their diameter, thickness, friability, hardness, weight variation, in vitro dissolution tests (24-h drug release profiles), and uniformity of content were used to evaluate them.</p> Results <p>The matrices comprising Ethocel 10 FP at a 10:3 ratio showed pseudo-zero-order kinetics (n-value of 0.989), but the dissolving data from the test matrices and reference tablets did not match. The following pharmacokinetic characteristics were studied: Cmax (196.0 ± 0.025&#xa0;µg/mL), half-life (11.210 ± 0.169), Tmax (4.11 ± 0.091&#xa0;h), AUCo (2121.23 ± 0.215&#xa0;µg.mL), AUCo-inf (4234.46 ± 0.105&#xa0;µg.h/mL), Cl (0.013 ± 0.011&#xa0;mL/min), and MRTo-48&#xa0;h (11.48 ± 0.391). A correlation value of 0.9836 was found between the in vitro and in vivo results for the test-optimized matrices, showing a level-A relationship (point-to-point correlation between the percentages of drug released in vitro and the percentage of drug absorbed in vivo<i>).</i></p> Conclusion <p>The matrices may increase patient adherence to once-a-day drug and therapy effects.</p>

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Fabrication, Preparation and In-Vitro and In-Vivo Evaluation of Metoprolol Tartrate Controlled-Release Matrices to Establish a Correlation

  • 期刊论文

  • 发表日期：

    2026年2月27日

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  • Kamran Ahmad Khan,
  • Ashfaq Ahmad,
  • Muhammad Israr,
  • Saima Mahmood,
  • Sami-ul-Huq,
  • Naveed Ullah,
  • Anam Adil,
  • Fida Muhammad

摘要

Aim

In the present study, matrices of metoprolol tartrate (200 mg) were developed with two individual polymers (Ethocel 7 premium and Ethocel 7FP premium) at various w/w drug-to-polymer ratios (10:3, 10:4, and 10:5), with a filler (spray-dried lactose) and lubricant (magnesium stearate).

Methodology

The direct compression method was used to prepare the matrices, and their diameter, thickness, friability, hardness, weight variation, in vitro dissolution tests (24-h drug release profiles), and uniformity of content were used to evaluate them.

Results

The matrices comprising Ethocel 10 FP at a 10:3 ratio showed pseudo-zero-order kinetics (n-value of 0.989), but the dissolving data from the test matrices and reference tablets did not match. The following pharmacokinetic characteristics were studied: Cmax (196.0 ± 0.025 µg/mL), half-life (11.210 ± 0.169), Tmax (4.11 ± 0.091 h), AUCo (2121.23 ± 0.215 µg.mL), AUCo-inf (4234.46 ± 0.105 µg.h/mL), Cl (0.013 ± 0.011 mL/min), and MRTo-48 h (11.48 ± 0.391). A correlation value of 0.9836 was found between the in vitro and in vivo results for the test-optimized matrices, showing a level-A relationship (point-to-point correlation between the percentages of drug released in vitro and the percentage of drug absorbed in vivo).

Conclusion

The matrices may increase patient adherence to once-a-day drug and therapy effects.