Phase I clinical study to select a novel oral formulation for ibandronate containing the excipient sodium N-[8-(2-hydroxybenzoyl) amino] caprylate (SNAC)

B. Bittner, C. McIntyre, H. Tian, K. Tang, N. Shah, W. Phuapradit, H. Ahmed, H. Chokshi, M. Infeld, Nikoletta Fotaki, H. Ma, A. Portron, P. Jordan, J. Schmidt

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Abstract

The aim of this study was to select a novel oral formulation for ibandronate (IBN, CAS number: 13892619). In four cohorts of 28, 21, 19 and 29 healthy volunteers, the impact of the carrier molecule sodium N-[8-(2-hydroxybenzoyl) amino] caprylate (SNAC, CAS number: 203787-91-1) on the bioavailability of IBN was investigated. Within each cohort different oral formulations with one dose of ibandronate (30 mg) and three different ratios of IBN:SNAC (1:5, 1:10 and 1:20) were compared to the approved oral IBN tablet formulations (150 and 50 mg IBN) in a 4-way cross-over design and a one week washout between the administrations. The highest mean IBN exposure was achieved with a capsule formulation containing drug-coated beadlets and an IBN:SNAC ratio of 1:5. AUClast and Cmax of IBN were approximately 1.3- and 2.2-fold higher compared to the reference treatment (150 mg IBN without SNAC). Increasing the post-dose fasting duration from 15 to 30 min resulted in a more than 2-fold increase in AUClast, while superimposable IBN serum concentration-time profiles were achieved after a 30 and 60 min fast. The tolerability of the IBN/SNAC treatments in all cohorts was similar to that in the IBN reference groups and most adverse events (AEs) were of mild to moderate intensity.

Original languageEnglish
Pages (from-to)233-241
JournalDie Pharmazie - An International Journal of Pharmaceutical Sciences
Volume67
Issue number3
DOIs
Publication statusPublished - Mar 2012

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    Bittner, B., McIntyre, C., Tian, H., Tang, K., Shah, N., Phuapradit, W., Ahmed, H., Chokshi, H., Infeld, M., Fotaki, N., Ma, H., Portron, A., Jordan, P., & Schmidt, J. (2012). Phase I clinical study to select a novel oral formulation for ibandronate containing the excipient sodium N-[8-(2-hydroxybenzoyl) amino] caprylate (SNAC). Die Pharmazie - An International Journal of Pharmaceutical Sciences, 67(3), 233-241. https://doi.org/10.1691/ph.2012.1648