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Review
. 2010 Sep;12(3):397-406.
doi: 10.1208/s12248-010-9203-3. Epub 2010 May 11.

The use of biorelevant dissolution media to forecast the in vivo performance of a drug

Sandra Klein  1
Affiliations
Review

The use of biorelevant dissolution media to forecast the in vivo performance of a drug

Sandra Klein. AAPS J. 2010 Sep.

Abstract

Simulation of gastrointestinal conditions is essential to adequately predict the in vivo behavior of drug formulations. To reduce the size and number of human studies required to identify a drug product with appropriate performance in both the fed and fasted states, it is advantageous to be able to pre-screen formulations in vitro. The choice of appropriate media for such in vitro tests is crucial to their ability to correctly forecast the food effect in pharmacokinetic studies. The present paper gives an overview of the development and composition of biorelevant dissolution media that can be used for the in vitro simulation of different dosing conditions (fasted and fed states). In addition, the application of these media to predicting food effects is described in several case examples.

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Figures

Fig. 1
Fig. 1
Dissolution profiles of Danatrol® tablets obtained in media simulating the intralumenal composition of the small intestine before and after a meal (n = 3 ± SD; adapted from Galia (30))
Fig. 2
Fig. 2
Dissolution profiles of Phenhydan® tablets obtained in compendial and biorelevant media simulating the intralumenal composition of stomach and small intestine before and after a meal (n = 3 ± SD)
Fig. 3
Fig. 3
Solubility data of itraconazole formulated with HBenBCD in compendial and biorelevant media
Fig. 4
Fig. 4
Dissolution profiles of a itraconazole–HBenBCD complex obtained in compendial and biorelevant media simulating the intralumenal composition of stomach and small intestine before and after a meal (n = 3 ± SD)
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References

    1. Dressman JB, Reppas C. In vitro–in vivo correlations for lipophilic, poorly water-soluble drugs. Eur J Pharm Sci. 2000;11(Suppl 2):73–80. doi: 10.1016/S0928-0987(00)00181-0. - DOI - PubMed
    1. Noyes AA, Whitney WR. The rate of solution of solid substances in their own solutions. J Am Chem Soc. 1897;19:930–934. doi: 10.1021/ja02086a003. - DOI
    1. Nernst W. Theorie der Reaktionsgeschwindigkeit in heterogenen Systemen. Z Physikal Chemie. 1904;47:52–55.
    1. Horter D, Dressman JB. Influence of physicochemical properties on dissolution of drugs in the gastrointestinal tract. Adv Drug Del Rev. 1997;25(April):3–14. doi: 10.1016/S0169-409X(96)00487-5. - DOI - PubMed
    1. Dressman JB, Amidon GL, Reppas C, Shah VP. Dissolution testing as a prognostic tool for oral drug absorption: immediate release dosage forms. Pharm Res. 1998;15(1):11–22. doi: 10.1023/A:1011984216775. - DOI - PubMed

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