The Biopharmaceutics Classification System: subclasses for in vivo predictive dissolution (IPD) methodology and IVIVC.
- Y. Tsume, Deanna M. Mudie, P. Langguth, G. Amidon, G. Amidon
- BiologyEuropean Journal of Pharmaceutical Sciences
- 16 June 2014
Low Buffer Capacity and Alternating Motility along the Human Gastrointestinal Tract: Implications for in Vivo Dissolution and Absorption of Ionizable Drugs.
The results clearly demonstrated the dynamic change in pH as a function of time and the extremely low buffer capacity along the GI tract, which is profound for the oral delivery of both acidic and basic active pharmaceutical ingredients (APIs).
Sulforaphane enhances the anticancer activity of taxanes against triple negative breast cancer by killing cancer stem cells.
- J. Burnett, G. Lim, Tao Zhang
- Biology, ChemistryCancer Letters
- 28 May 2017
The suitability of an in situ perfusion model for permeability determinations: utility for BCS class I biowaiver requests.
- Jae-Seung Kim, S. Mitchell, P. Kijek, Y. Tsume, J. Hilfinger, G. Amidon
- BiologyMolecular Pharmaceutics
- 4 October 2006
A method using the 90% confidence interval of the permeability ratio of the test to internal reference standard in order to differentiate between high and low permeability compounds is developed and suggests a robust means for assessing drug permeability classification.
In vitro dissolution methodology, mini-Gastrointestinal Simulator (mGIS), predicts better in vivo dissolution of a weak base drug, dasatinib.
- Y. Tsume, Susumu Takeuchi, K. Matsui, Gregory E Amidon, Gordon L Amidon
- Biology, ChemistryEuropean Journal of Pharmaceutical Sciences
- 30 August 2015
Quantitative evaluation of the gastrointestinal absorption of protein into the blood and lymph circulation.
- Y. Tsume, Y. Taki, S. Yamashita
- Medicine, BiologyBiological and Pharmaceutical Bulletin
- 15 October 1996
It was demonstrated that not only the small intestine but also the stomach can absorb OVA, and the liposomes suppressed the enzymatic degradation of OVA and released it slowly in the gastrointestinal tract.
The Dipeptide Monoester Prodrugs of Floxuridine and Gemcitabine—Feasibility of Orally Administrable Nucleoside Analogs
- Y. Tsume, B. Bermejo, G. Amidon
- Biology, ChemistryPharmaceuticals
- 27 January 2014
Cell proliferation assays in ductal pancreatic cancer cells indicated that dipeptide prodrugs of floxuridine and gemcitabine were more potent than their parent drugs and enhanced potency of nucleoside analogs was attributed to their improved membrane permeability.
The biowaiver extension for BCS class III drugs: the effect of dissolution rate on the bioequivalence of BCS class III immediate-release drugs predicted by computer simulation.
The results of GastroPlus simulations indicate that the dissolution rate of BCS class III drugs could be prolonged to the point where dissolution, rather than permeability, would control the overall absorption.
Enhanced Cancer Cell Growth Inhibition by Dipeptide Prodrugs of Floxuridine: Increased Transporter Affinity and Metabolic Stability
- Y. Tsume, J. Hilfinger, G. Amidon
- Biology, ChemistryMolecular Pharmaceutics
- 25 July 2008
Dipeptide monoester prodrugs of floxuridine suggest their potential for increased oral uptake, delayed enzymatic bioconversion and enhanced resistance to metabolism to 5-fluorouracil, as well as enhanced uptake and cytotoxic activity in cancer cells, attributes that would facilitate prolonged systemic circulation for enhanced therapeutic action.
Comparison of the permeability of metoprolol and labetalol in rat, mouse, and Caco-2 cells: use as a reference standard for BCS classification.
- T. Incecayir, Y. Tsume, G. Amidon
- Biology, MedicineMolecular Pharmaceutics
- 4 March 2013
Overall, labetalol showed high Peff in rat and mouse intestinal perfusion models similar to metoprolol at a concentration based on HDS, however, the concentration-dependent permeability of labetAlol in mice due to P-gp and the inhibition study with verapamil in Caco-2 cells indicated that labet alol is not an ideal reference standard for BCS classification.