Evaluation of in vitro release rate and in vivo absorption characteristics of four metoprolol tartrate immediate-release tablet formulations

Pharmaceutical Development and Technology
G S RekhiL L Augsburger

Abstract

The purpose of this investigation was to examine the impact of formulation and process changes on dissolution and bioavailability/bioequivalency of metoprolol tartrate tablets manufactured using a high-shear granulation process. A half-factorial (2(4-1), Res IV) design was undertaken to study the selected formulation and processing variables during scale-up. Levels and ranges for excipients and processing changes studied represented level 2 or greater changes as indicated by the SUPAC-IR Guidance. Blend and tableting properties were evaluated. Changes in sodium starch glycolate and magnesium stearate levels, and the order of addition microcrystalline cellulose (intra- vs. extragranular) were significant only in affecting percent drug released (Q) in 5, 10, and 15 min. Statistical analysis of data showed no significant curvature. No interaction effects were found to be statistically significant. To examine the impact of formulation and processing variables on in vivo absorption, three batches were selected for a bioavailability study based on their dissolution profiles. Subjects received four metoprolol treatments (Lopressor, slow-, medium-, and fast-dissolving formulations) separated by 1 week according to a randomized crossove...Continue Reading

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Citations

Apr 10, 2013·Drug Design, Development and Therapy·Aleksander MendykRenata Jachowicz
May 17, 2011·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Zi-qiang LiShu-jun Sun
Apr 6, 2005·The Journal of Pharmacy and Pharmacology·Hans Lennernäs, Bertil Abrahamsson
Jun 18, 2002·Pharmaceutical Development and Technology·Paul R SeoJames E Polli
Feb 23, 1999·Pharmaceutical Development and Technology·J E Polli
Dec 19, 2013·Langmuir : the ACS Journal of Surfaces and Colloids·Samantha J HeidlebaughSachin S Velankar
Jun 5, 2002·Journal of Clinical Pharmacology·Marilyn N Martinez, Gordon L Amidon

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