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Int J Pharm. 2016 Dec 30;515(1-2):352-358. doi: 10.1016/j.ijpharm.2016.10.018. Epub 2016 Oct 11.

In vitro evaluation of the impact of gastrointestinal transfer on luminal performance of commercially available products of posaconazole and itraconazole using BioGIT.

Author information

1
Department of Pharmacy, National and Kapodistrian University of Athens, Zografou, Greece.
2
Drug Delivery & Disposition, KU Leuven, Leuven, Belgium.
3
Department of Pharmacy, National and Kapodistrian University of Athens, Zografou, Greece. Electronic address: reppas@pharm.uoa.gr.

Abstract

Biorelevant Gastrointestinal Transfer system (BioGIT) has been shown to be useful in reproducing concentrations of drugs in the fasted upper small intestine after their administration in the stomach. In the present investigation, we evaluated the impact of gastrointestinal transfer on luminal performance of commercially available products of two highly lipophilic weak bases, posaconazole (Noxafil® suspension) and itraconazole (Sporanox® hard gelatin capsules and Sporanox® oral solution) by comparing % solid fraction, concentrations and supersaturation in the duodenal compartment of BioGIT with recently reported data in the upper small intestine of healthy adults. BioGIT was useful for estimating the % solid fraction in the upper small intestine, in cases where dissolution during gastric residence was incomplete, i.e. after administration of Noxafil® and Sporanox® capsules, and the precipitated fraction of itraconazole in the upper small intestine after administration of Sporanox® solution; median values in vitro were similar to the luminal values. Based on the values for the area under the concentration vs. time data estimated up to 45min post initiation of the experiment, concentrations in the duodenal compartment of BioGIT were similar to previously measured concentrations in the upper small intestine of healthy adults or they overestimated them by up to 2.5 times. In most cases, supersaturation of contents in the upper small intestine was overestimated, partly due to underestimation of luminal solubility.

KEYWORDS:

BioGIT; Dissolution; Itraconazole; Posaconazole; Precipitation; Supersaturation

PMID:
27732895
DOI:
10.1016/j.ijpharm.2016.10.018
[Indexed for MEDLINE]

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