In vivo supersaturation

In vivo supersaturation is the behavior of orally administered compounds that undergo supersaturation as they pass through the gastrointestinal (GI) tract. Typically these compounds have a weakly basic nature (pK_a in the range of 5 to 8)^[1] and a relatively low solubility in aqueous solutions. In vivo supersaturation is a recent phenomenon that was first observed by Yamashita et al. in 2003.^[2]

References

^ Hsieh, Yi-Ling; Ilevbare, Grace A.; Van Eerdenbrugh, Bernard; Box, Karl J.; Sanchez-Felix, Manuel Vincente; Taylor, Lynne S. (2012-05-12). "pH-Induced Precipitation Behavior of Weakly Basic Compounds: Determination of Extent and Duration of Supersaturation Using Potentiometric Titration and Correlation to Solid State Properties". Pharmaceutical Research. 29 (10): 2738–2753. doi:10.1007/s11095-012-0759-8. ISSN 0724-8741. PMID 22580905. S2CID 15502736.
^ Yamashita, Kazunari; Nakate, Toshiomi; Okimoto, Kazuto; Ohike, Atsuo; Tokunaga, Yuji; Ibuki, Rinta; Higaki, Kazutaka; Kimura, Toshikiro (November 2003). "Establishment of new preparation method for solid dispersion formulation of tacrolimus". International Journal of Pharmaceutics. 267 (1–2): 79–91. doi:10.1016/j.ijpharm.2003.07.010. ISSN 0378-5173. PMID 14602386.

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[1] Hsieh, Yi-Ling; Ilevbare, Grace A.; Van Eerdenbrugh, Bernard; Box, Karl J.; Sanchez-Felix, Manuel Vincente; Taylor, Lynne S. (2012-05-12). "pH-Induced Precipitation Behavior of Weakly Basic Compounds: Determination of Extent and Duration of Supersaturation Using Potentiometric Titration and Correlation to Solid State Properties". Pharmaceutical Research. 29 (10): 2738–2753. doi:10.1007/s11095-012-0759-8. ISSN 0724-8741. PMID 22580905. S2CID 15502736.

[2] Yamashita, Kazunari; Nakate, Toshiomi; Okimoto, Kazuto; Ohike, Atsuo; Tokunaga, Yuji; Ibuki, Rinta; Higaki, Kazutaka; Kimura, Toshikiro (November 2003). "Establishment of new preparation method for solid dispersion formulation of tacrolimus". International Journal of Pharmaceutics. 267 (1–2): 79–91. doi:10.1016/j.ijpharm.2003.07.010. ISSN 0378-5173. PMID 14602386.

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