In vitro evaluation of the impact of gastrointestinal transfer on luminal performance of commercially available products of posaconazole and itraconazole using BioGIT
| Autor: | Mira Symillides, Alexandros Kourentas, Christos Reppas, Patrick Augustijns, Joachim Brouwers, Bart Hens, Maria Vertzoni |
|---|---|
| Rok vydání: | 2016 |
| Předmět: |
medicine.medical_specialty
Posaconazole Duodenum Itraconazole Pharmaceutical Science Capsules 02 engineering and technology Absorption (skin) Pharmacology 030226 pharmacology & pharmacy Gastroenterology Intestinal absorption 03 medical and health sciences 0302 clinical medicine Internal medicine Gastric mucosa medicine Humans Gastrointestinal Transit Chemistry Stomach Fasting Triazoles 021001 nanoscience & nanotechnology Small intestine medicine.anatomical_structure Intestinal Absorption Solubility Gastric Mucosa Phenobarbital 0210 nano-technology medicine.drug |
| Zdroj: | International Journal of Pharmaceutics. 515:352-358 |
| ISSN: | 0378-5173 |
| DOI: | 10.1016/j.ijpharm.2016.10.018 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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