In vivo supersaturation explained
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 (pKa 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]
Notes and 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. en. 29. 10. 2738–2753. 10.1007/s11095-012-0759-8. 22580905. 15502736. 0724-8741.
- 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. 10.1016/j.ijpharm.2003.07.010. 14602386. 0378-5173.