Abstract
The aim of this present study was to develop and formulate sustained release coated metoprolol tartrate matrix granules and to design an in-vitro in-vivo correlation (IVIVC) tool based on bioavailability data available from human volunteers. USP apparatus II, paddle type was used for generation of in-vitro drug release data for each formulation. The similarity factor (f2) was determined using dissolution data parameters of the formulations. Twenty-four healthy male volunteers participated in the two-way crossover bioequivalent study where the volunteers were treated in a completely randomized fashion. The percent drug dissolved in the dissolution test and percent absorbed data shows a ‘level A’ IVIVC was achieved with a good linear regression relation. Different release rate formulation including Fast, Moderate and Slow release formulations exhibited an excellent covenant between the three dosage forms. Key words: Sustained-release capsules, metoprolol tartrate, bioavailability, in-vitro in-vivo correlation (IVIVC), humans.
Highlights
An in-vitro in-vivo correlation (IVIVC) has been distinctly explained by United States Pharmacopoeia (USP, 1998) and the Food and Drug Administration (FDA)
The in-vitro dissolution curve is usually produced by an appropriate dissolution test and in-vivo absorption parameters are frequently measured by deconvolution technique using various established model (e.g. Wagner-Nelson or Loo Regelman) or model-independent (e.g. DeMons) methods (USP Subcommittee on Biopharmaceutics, 1988; Gibaldi et al, 1982)
AUC0- 879.12 ± 34.76 1086.38 ± 44.32 1164.07 ± 25.89 1214.81 ± 45.52 chromatographic method for quantification of metoprolol tartrate in human plasma is used according to method described in literature (Aqil et al, 2007)
Summary
An in-vitro in-vivo correlation (IVIVC) has been distinctly explained by United States Pharmacopoeia (USP, 1998) and the Food and Drug Administration (FDA). The formulation can be used to predict in-vivo absorption (that is, bioavailability) of the drug after minor modification in formulation development processes (Jerome et al, 1990). Different types of IVIVC levels correlation have been explained by the FDA (FDA, 2017). The most important and useful of these is Level A correlation. The FDA guidance explains the various procedures of assessment of prediction error internally and externally. Internal validation indicates how well the model can be used to determine the correlation. In case of External validation, IVIVC model can be used for the formulation which was not used in the development of that particular model (CDER, 1997; Mandal et al, 2007)
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