Journal
MOLECULAR PHARMACEUTICS
Volume 16, Issue 10, Pages 4121-4130Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.molpharmaceut.9b00406
Keywords
BioFLUX; dissolution-permeation; membrane transport; absorption; itraconazole; supersaturation; kinetic solubility; in vivo; in vitro; prediction; fraction of dose absorbed
Funding
- New National Excellence Program of the Ministry of Human Capacities [UNKP-18-3-I, UNKP-18-4-BME-213]
- Gedeon Richter Talentum Foundation
- Pro Progressio Foundation
- Hungarian Scientific Research Fund [OTKA PD121143]
- National Research, Development and Innovation Fund of Hungary under the FIEK_16 funding scheme [FIEK_16-1-2016-0007]
- Janos Bolyai Research Scholarship of the Hungarian Academy of Sciences
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In this work, two different approaches have been developed to predict the food effect and the bioequivalence of marketed itraconazole (ITRA) formulations. Kinetic solubility and simultaneous dissolution-permeation tests of three (ITRA) formulations (Sporanox capsules and solution and SUBA-ITRA capsules) were carried out in simulated fasted and fed states. Fraction of dose absorbed ratios estimating food effect and bioequivalence were calculated based on these results and were compared to the in vivo study results published by Medicines Agencies. The comparison demonstrated that kinetic solubility and flux values could be used as input parameters for biopharmaceutics modeling and simulations to estimate food effect and bioequivalence. Both prediction methods were able to determine a slightly negative food effect in the case of the Sporanox solution and also a pronounced positive food effect for the Sporanox capsule. Superior bioavailability was predicted when the Sporanox solution was compared to the Sporanox capsule (in agreement with in vivo data).
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