Applying Biopharmaceutical Classification System Criteria to Predict the Potential Effect of Cremophor^® RH 40 on Fexofenadine Bioavailability at Higher Doses

Abstract

Aim: To study the impact of various permeability enhancers on fexofenadine bioavailability. Furthermore, to predict the potential effect of Cremophor^® RH 40 on fexofenadine pharmacokinetics at higher doses using Biopharmaceutical Classification System criteria. Experimental methods: The effect of the dose increase (60–360 mg) on the dissolution and permeability behavior of fexofenadine-Cremophor RH 40 formulations was studied in humans. The Biopharmaceutical Classification System criteria of the drug was determined. Results & conclusion: Cremophor RH 40 improved the dissolution and bioavailability of fexofenadine. The pharmacokinetics increased linearly with the dose increase. Absorption number (A_n) was significantly increased after addition of Cremophor RH 40 in comparison to an unprocessed drug. Similar A_n values were observed throughout the same dose range. The dose number (D₀) values were <1 whereas, all the dissolution number (D_n) values were >1 at the same dose level.

Keywords:

• BSC
• Cremophor^® RH 40
• dissolution
• fexofenadine
• permeability
• pharmacokinetics

Supplementary data

To view the supplementary data that accompany this paper please visit the journal website at:www.tandfonline.com/doi/suppl/10.4155/tde-2020-0042

Financial & competing interests disclosure

The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.

Writing assistance (free of charge) was utilized in the production of this manuscript.

Ethical conduct of research

The authors state that they have obtained a ClinicalTrials.gov Identifier NCT 01767272 and have followed the principles outlined in the Declaration of Helsinki for human experimental investigations. In addition, for investigations involving human subjects, informed consent has been obtained from all the participants involved.

Data sharing statement

The authors certify that this manuscript reports original clinical trial data, NCT 01767272. Individual participant data that underlies the results reported in the article, after de-identification (text, tables, figures and supplement) are available along with the study protocol. The data will be available from the date of online article publication. Proposals to access data will be available to anyone who wishes to access the data, for any purpose by any mechanism.