Solubility Profiling of HIV Protease Inhibitors in Human Intestinal Fluids
Journal of Pharmaceutical Sciences, ISSN: 0022-3549, Vol: 102, Issue: 10, Page: 3800-3807
2013
- 30Citations
- 42Captures
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Example: if you select the 1-year option for an article published in 2019 and a metric category shows 90%, that means that the article or review is performing better than 90% of the other articles/reviews published in that journal in 2019. If you select the 3-year option for the same article published in 2019 and the metric category shows 90%, that means that the article or review is performing better than 90% of the other articles/reviews published in that journal in 2019, 2018 and 2017.
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Metrics Details
- Citations30
- Citation Indexes30
- 30
- CrossRef24
- Captures42
- Readers42
- 42
Article Description
The present study pursued to profile the intestinal solubility of nine HIV protease inhibitors (PIs) in fasted- and fed-state human intestinal fluids (FaHIF, FeHIF) aspirated from four volunteers. In addition, the ability of fasted- and fed-state simulated intestinal fluids (FaSSIF, FeSSIF) to predict the intestinal solubility was evaluated. All PIs were poorly soluble in FaHIF (from 7-μM for ritonavir to 327-μM for darunavir) and FeHIF (from 15-μM for atazanavir to 409μM for darunavir). For four of nine PIs, food intake significantly enhanced the solubilizing capacity of intestinal fluids (up to 18.4-fold increase for ritonavir). The intersubject variability (average coefficient of variance CV fed = 60.6%, CV fasted = 40.4%) was higher as compared with the intrasubject variability ( CV fed = 41.3%, CV fasted = 20.5%). PI solubilities correlated reasonably well between FaSSIF and FaHIF ( R = 0.817), but not between FeSSIF and FeHIF ( R = 0.617). To conclude, postprandial conditions increased the inter- and intrasubject variability of the PIs. The inability of FeSSIF to accurately predict the FeHIF solubility emphasizes the need for a multivariate approach to determine solubility profiles, taking into account solid-state characteristics, pH, mixed bile acid/phospholipid micelles, and digestive products. © 2013 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 102:3800–3807, 2013
Bibliographic Details
http://www.sciencedirect.com/science/article/pii/S0022354915309011; http://dx.doi.org/10.1002/jps.23698; http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=84883767546&origin=inward; http://www.ncbi.nlm.nih.gov/pubmed/23939880; https://linkinghub.elsevier.com/retrieve/pii/S0022354915309011; https://dx.doi.org/10.1002/jps.23698
Elsevier BV
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