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Characterization of Multi-Sourced Diclofenac Sodium Extended-Release Tablet Dissolution Profiles: A New Approach to Establish an In vitro-In vivo Correlation Based on Multiple Integral Response Surface

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Abstract

Purpose

In this study, a new parameter, volume under response surface (VURS), based on the multiple integrals response surface (MIRS) was applied to establish in vitro-in vivo correlations (IVIVC) refer to in vitro dissolution data and in vivo pharmacokinetic data.

Materials and methods

The in vivo predictive capacity of f2 factor, dissolution efficiency (DE), and VURS were compared by investigating the multi-sourced diclofenac sodium extended-release tablets. In vitro dissolution tests were investigated under various conditions. Beagle dogs were used for in vivo pharmacokinetic study as a preliminary investigation of the new approach. In vivo pharmacokinetic experiments were conducted based on the crossed-over design principle, and the blood concentration was determined by LC-MS/MS method.

Results

Data indicated both DE value and f2 factor were unable to discriminate the significant difference in relative bioavailability among the test formulations, although they could suggest in vivo bio-inequivalent risk to some extent. VURS is successfully explored to establish an IVIVC in beagle dogs with diclofenac sodium extended-release formulations with similar release mechanism.

Conclusions

Compared with DE value and f2 factor, the advantage of VURS was demonstrated to predict in vivo parameters of test formulation with a similar or dissimilar release mechanism.

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Correspondence to Jiasheng Tu or Chunmeng Sun.

Additional information

Baoming Ning and Xi Liu contributed equally to this work.

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Ning, B., Liu, X., Luan, H. et al. Characterization of Multi-Sourced Diclofenac Sodium Extended-Release Tablet Dissolution Profiles: A New Approach to Establish an In vitro-In vivo Correlation Based on Multiple Integral Response Surface. J Pharm Innov 10, 302–312 (2015). https://doi.org/10.1007/s12247-015-9227-4

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