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Publications

This is a listing of the numerous papers, books, posters and invited reviews authored by Pion's scientists and other researchers using our instruments.  Several publications are from collaborations with pharmaceutical companies and academic institutions.  Pion participates in pharmaceutical and drug development conferences world wide. 

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Drug Absorption

Avdeef, A. Absorption and Drug Development. Wiley-Interscience: New York. 2003. Amazon

Avdeef A. Drug ionization and physicochemical profiling. In: Mannhold, R. (Ed.), Drug Properties: Measurement and Computation, Wiley-VCH, 2007, pp. 55-83. Amazon

 Avdeef, A.; Testa, B. Physicochemical profiling in drug research: a brief survey of the state-of-the-art of experimental techniques. Cell. Molec. Life Sci., 2003, 59, 1681-1689. Available on-line through SpringerLink.

Avdeef, A. Physicochemical Profiling (Permeability, Solubility, Charge State). Curr. Topics Med. Chem., 2001, 1, 277-351.

Prediction

Žmuidinavicius, D.; Didžiapetris, R.; Japertas, P.; Avdeef, A.; Petrauskas, A. Classification structure-activity relations (C-SAR) in prediction of human intestinal absorption. J. Pharm. Sci.,2003, 92, 621-633.

McFarland, J.W.; Avdeef, A.; Berger, C.M.; Raevsky, O.A. Estimating the water solubilities of crystalline compounds from their chemical structure alone. J. Chem. Inf. Comput. Sci., 2001, 41, 1355-1359. (Part 5 in pSOL series). Available on-line through ACS.

Didžiapetris, R.; Japertas, P.; Avdeef, A.; Petrauskas, A. Classification analysis of P-glycoprotein substrate specificity. J. Drug Target, 2003, 11, 391-406.   Bergström, C.A.S.; Strafford, M.; Lazarova, L.; Avdeef, A.; Luthman, K.; Artursson, P. Absorption classification of oral drugs based on molecular surface properties. J. Med. Chem.,2003, 46, 558-570. (Part 4 in pSOL series)  Available online through ACS  

Permeability/PAMPA

Tsinman O, Tsinman K, Sun N, Avdeef A, Physicochemical selectivity of the BBB microenvironment governing passive diffusion--matching with a porcine brain lipid extract artificial membrane permeability model. Pharm Res. 2011 Feb;28(2):337-63. Epub 2010 Oct 14.

Sugano K, Kansy M, Artursson P, Avdeef A, Bendels S, Di L, Ecker GF, Faller B, Fischer H, Gerebtzoff G, Lennernaes H, Senner F., Coexistence of passive and carrier-mediated processes in drug transport.  Nat. Rev. Drug Discov., 2010 8, 597-614.

 K. Y. Tam; A. Avdeef; O. Tsinman; N. Sun, The Permeation of Amphoteric Drugs through Artificial Membranes − An in Combo Absorption Model Based on Paracellular and Transmembrane Permeability, J. Med. Chem., 2010, 53 (1), pp 392–401. Available through ACS. 

Dagenais C, Avdeef A, Tsinman O, Dudley A, Beliveau R. P-Glycoprotein Deficient Mouse in situ Blood-Brain Barrier Permeability and its Prediction using an in combo PAMPA Model.  Eur J Pharm Sci. 2009. Available online for FREE through NIH. (a followup paper in Pharm. Res. is due out soon!)

Escher BI, Berger C, Bramaz N, Kwon J-H, Richter M, Tsinman O, Avdeef A. Membrane-water partitioning, membrane permeability and non-target modes of action in aquatic organisms of the parasiticides ivermectin, ablendazole and morantel. Envir. Tox. Chem. 2008, 27, in press. (Part 25 PAMPA series)

Avdeef A, Bendels S, Di L, Faller B, Kansy M, Sugano K, Yamauchi Y. PAMPA - a useful tool in drug discovery. J. Pharm. Sci. 2007, 96, 2893-2909. (Part 24 in PAMPA Series)

Avdeef A, Kansy M, Bendels S, Tsinman K. Absorption-excipient-pH classification gradient maps: sparingly-soluble drugs and the pH partition hypothesis. Eur. J. Pharm. Sci. 2008, 33, 29-41. (Part 23 PAMPA Series)

Bendels, S.; Tsinman, O.; Wagner, B.; Lipp, D.; Parilla, I.; Kansy, M.; Avdeef, A. PAMPA-Excipient Classification Gradient Map. Pharm. Res., 2006, 23, 2525-2535. (Part 21 in PAMPA series). Available on-line through SpringerLink.

Fischer, H.; Kansy, M., Avdeef, A.; Senner, F. Permeation of permanently charged molecules through artificial membranes – influence of physico-chemical properties. Eur. J. Pharm. Sci. 2007, 31, 32-42. (Part 20 in PAMPA series). Available on-line through ScienceDirect.

Avdeef, A. The Rise of PAMPA. Expert Opinion on Drug Metab. Tox., 2005, 1, 325-342. (Part 17 in PAMPA series)

Kansy, M.; Avdeef, A.; Fischer, H. Advances in Screening for Membrane Permeability: High-Resolution PAMPA for Medicinal Chemists. Drug Discovery Today: Technologies, 2005, 1, 349-355. (Part 16 in PAMPA series)

Ruell, J.A.; Avdeef, A. Absorption using the PAMPA Approach. In: Yan, Z.; Caldwell, G.W. (Eds.), Optimization in Drug Discovery: In Vitro Methods. The Humana Press: Totowa, NJ, 2004, pp. 37-64. (Part 15 in PAMPA series)

Avdeef, A. HT Solubility and Permeability: MAD-PAMPA Analysis. In: Krämer, S.D.; Folkers, G.; Testa, B. (Eds.), Physicochemical and Biological Profiling in Drug Research. Wiley-VCH: Weinheim, 2004, pp. 221-241. (Part 14 in PAMPA series)

Avdeef, A.; Tsinman, O. PAMPA – a Drug Absorption in vitro Model. 13. Chemical Selectivity due to Membrane Hydrogen Bonding: in combo Comparisons of HDM-, DOPC-, and DS-PAMPA. Eur. J. Pharm. Sci., 2006, 28(1-2), 43-50. (Part 13 in PAMPA series). Available on-line through ScienceDirect.

Ruell, J.A.; Tsinman, O.; Avdeef, A. Acid-Base Cosolvent Method for Determining Aqueous Permeability of Amiodarone, Itraconazole, Tamoxifen, Terfenadine and Other Very Insoluble Molecules. Chem. Pharm. Bull., 2004, 52, 561-565. (Part 12 in PAMPA series)

Rated #12 on the List of ScienceDirect TOP25 Hottest Articles - Jul-Sep 2004
Avdeef, A.; Nielsen, P.E.; Tsinman, O. PAMPA - a Drug Absorption in vitro Model. 11. Matching the in vivo Unstirred Water Layer Thickness by Individual-Well Stirring in Microtitre Plates. Eur. J. Pharm. Sci., 2004, 22, 365-374. (Part 11 in PAMPA series). Available on-line through ScienceDirect.

Caron, G.; Ermondi, G.; Damiano, A.; Novaroli, L.; Tsinman, O.; Ruell, J.A.; Avdeef, A. Ionization, lipophilicity, and molecular modeling to investigate permeability and other biological properties of amlodipine. Bioorg. Med. Chem., 2004, 23, 6107-6118. (Part 10 in PAMPA series)

Most Cited Paper Award 2005 from European Journal of Pharmaceutical Sciences. Rated #15 on the List of ScienceDirect TOP25 Hottest Articles - Apr-Jun 2005
Avdeef, A.; Artursson, P.; Neuhoff, S.; Lazarova, L.; Gråsjö, J.; Tavelin, S. Caco-2 Permeability of Weakly Basic Drugs Predicted with the Double-Sink PAMPA pKaflux Method. Eur. J. Pharm. Sci., 2005, 24, 333-349. (Part 9 in PAMPA series). Available on-line through ScienceDirect.

Nielsen, P.; Avdeef, A. PAMPA - a Drug Absorption in vitro Model. 8. Apparent Filter Porosity and the Unstirred Water Layer. Eur. J. Pharm. Sci., 2004, 22, 33-41. (Part 8 in PAMPA series). Available on-line through ScienceDirect.

Most Cited Paper Award 2004 from European Journal of Pharmaceutical Sciences. Bermejo, M.; Avdeef, A.; Ruiz, A.; Nalda, R.; Ruell, J.A.; Tsinman, O.; González, I.; Fernández, C.; Sánchez, G.; Garrigues, T.M.; Merino, V. PAMPA - a drug absorption in vitro model. 7. Comparing rat in situ, Caco-2, and PAMPA permeability of fluoroquinolones. Eur. J. Pharm. Sci., 2004, 21,429-441. (Part 7 in PAMPA series). Available on-line through ScienceDirect.

Youdim, K.A.; Avdeef, A.; Abbott, N.J. In vitro trans-monolayer permeability calculations: often forgotten assumptions. Drug Disc. Today, 2003, 8, 997-1003. (Part 6 in PAMPA series)

Ruell, J.A.; Tsinman, K.L.; Avdeef, A. PAMPA - a drug absorption in vitro model. 5. Unstirred water layer in iso-pH mapping assays and pKaflux - optimized design (pOD-PAMPA). Eur. J. Pharm. Sci., 2003, 20, 393-402 (Part 5 in PAMPA series). Available on-line through ScienceDirect.

Liu, H.; Sabus, C.; Carter, G.T; Du, C.; Avdeef, A.; Tischler, M. In Vitro Permeability of Poorly Aqueous Soluble Compounds Using Different Solubilizers in the PAMPA Assay with Liquid Chromatography/Mass Spectrometry Detection. Pharm. Res., 2003, 20, 1820-1826. (Part 4 in PAMPA series). Available on-line through SpringerLink.

Avdeef, A. High-throughput Measurement of Membrane Permeability. In: H. van de Waterbeemd, H. Lennernäs, P. Artursson (Eds.). Drug Bioavailability/Estimation of Solubility, Permeability, Absorption and Bioavailability. Wiley-VCH: Weinheim, 2003, pp. 46-71. (Part 3 in PAMPA series)

Avdeef, A.; Strafford, M.; Block, E.; Balogh, M.P.; Chambliss, W.; Khan, I. Drug Absorption In Vitro Model: Filter-Immobilized Artificial Membranes. 2. Studies of the Permeability Properties of Lactones in Piper methysticum Forst. Eur. J. Pharm. Sci., 2001, 14, 271-280. (Part 2 in PAMPA series). Available on-line through ScienceDirect.

Ruell, J. Membrane-based Drug Assays. Modern Drug Disc., 2003, January issue, 28-30.

Avdeef A. Solubility of sparingly-soluble drugs. Dressman J, Reppas C. (Eds., special issue: The Importance of Drug Solubility). Adv. Drug Deliv. Rev. 2007, 59, 568-590. (Part 8 in pSOL series)

Avdeef A, Bendels S, Tsinman O, Kansy M. Solubility-excipient classification gradient maps. Pharm. Res., 2007, 24, 530-545.

Avdeef, A.; Testa, B. Physicochemical profiling in drug research: a brief state-of-the-art of experimental techniques. Cell. Molec. Life Sci., 2003, 59, 1681-1689.

Avdeef, A. Physicochemical Profiling (Permeability, Solubility, Charge State). Curr. Topics Med. Chem., 2001, 1, 277-351.

Solubility

Avdeef, A.; Bendels, S.; Tsinman, O.; Tsinman, K.; Kansy, M. Solubility-Excipient Classification Gradient Maps. Pharm. Res., 2007, 24, 530-545. (Part 22 in PAMPA series). Available on-line through SpringerLink.

Avdeef, A. High-throughput measurements of solubility profiles. In: Testa, B., van de Waterbeemd, H., Folkers, G., Guy, R. (Eds.), Pharmacokinetic Optimization in Drug Research, Verlag Helvetica Chimica Acta: Zürich and Wiley - VCH: Weinheim, 2001, pp. 305-326. (Part 1 in PAMPA series)

 Avdeef, A. Drug ionization and physicochemical profiling. In: Mannhold, R. (Ed.), Drug Properties: Measurement and Computation, Wiley-VCH, 2007, pp. 55-83. (Part 1 in pKa series)

Avdeef, A.; Voloboy, D.; Foreman, A. Dissolution – Solubility of Multiprotic Drugs: pH, Buffer, Salt, Dual-Solid, and Aggregation Effects. In: Testa, B.; van de Waterbeemd, H. (Eds.).Comprehensive Medicinal Chemistry II, Vol. 5 ADME-TOX Approaches. Elsevier: Oxford, UK, 2006, pp. 399-423. (Part 7 in pSOL series)

McFarland, J.W.; Du, C.M.; Avdeef, A. Factors influencing the water solubility of crystalline drugs. In: van de Waterbeemd, H.; Lennernäs, H.; Artursson, P.(Eds.). Drug Bioavailability. Estimation of Solubility, Permeability, Absorption and Bioavailability. Wiley - VCH: Weinheim, 2003, pp. 232-242. (Part 6 in pSOL series)

Avdeef, A.; Berger, C.M.; Brownell, C. pH-Metric Solubility. 2. Correlation Between the Acid-Base Titration and the Saturation Shake-Flask Solubility-pH Methods. Pharm. Res., 2000, 17, 85-89. (Part 2 in pSOL series). Available on-line through SpringerLink.

Avdeef, A.; Berger, C.M. pH-Metric Solubility. 3. Dissolution Titration Template Method for Solubility Determination. Eur. J. Pharm. Sci., 2001, 14, 271-280. (Part 3 in pSOL series). Available on-line through ScienceDirect.

Avdeef, A., . pH-Metric Solubility. 1. Solubility-pH Profiles from Bjerrum Plots. Gibbs Buffer and pKa in the Solid State. Pharm. Pharmacol. Commun., 1998, 4, 165-178. (Part 1 in pSOL series)

Ruell, J.; Avdeef, A. A measured solution. Modern Drug Disc., 2003, June issue, 47-49.

Dissolution 

Fagerberg JH, Tsinman O,  Sun N, Tsinman K, Avdeef A, Bergstrom C, Dissolution Rate and Apparent Solubility of Poorly Soluble Drugs in Biorelevant Dissolution Media, Mol. Pharmaceutics, 2010 May, 7 (5), 1419–1430.

Alonzo DE, Zhang GG, Zhou D, Gao Y, Taylor LS. Understanding the behavior of amorphous pharmaceutical systems during dissolution, Pharm Res. 2010 Apr;27(4):608-18. Epub 2010 Feb 12.  Available through SpringerLink.

Berger CM, Tsinman O., Voloboy D, Lipp D, Stones S, Avdeef A. Miniaturized intrinsic dissolution rate (Mini-IDR™) measurement of griseofulvin and carbamazepine. Dissolut. Tech.2007, 14, 39-41. (Part 9 in the pSOL Series). Available from Dissolution Tech.

Avdeef A., Tsinman O., Miniaturized rotating disk intrinsic dissolution rate measurement: effects of buffer capacity in comparisons to traditional wood's apparatus. Pharm Res. 2008 Nov;25(11):2613-27. Epub 2008 Jul 22. Available from SpringerLink.

Tsinman K, Avdeef A., Tsinman O., Voloboy, D., Powder dissolution method for estimating rotating disk intrinsic dissolution rates of low solubility drugs. Pharm Res. 2009 Sep;26(9):2093-100. Epub 2009 Jun 19. Available from SpringerLink.

Avdeef A., Tsinman K, Tsinman O., Sun, N., Voloboy, D., Miniaturization of Powder Dissolution Measurement and Estimation of Particle Size, Chem Biodivers. 2009  Nov;6(11):1796-811. Available from Wiley InterScience.

B. S. Zolnik, J-L. Raton, D. UJ. Burgess, Application of USP Apparatus 4 and In Situ Fiber Optic Analysis to Microsphere Release Testing.  Diss. Tech. May: 11-14 (2005). Available from Dissolution Tech.

C. J. Toher, P. E. Nielsen, A. S. Foreman, and A. Avdeef. In situ fiber optic dissolution monitoring of vitamin B12 solid dosage formulation. Diss. Tech. Nov: 20–25 (2003). Available from Dissolution Tech.

Vishal Bijlani, Domotiere Yuonayel, Sabitha Katpally, Beatrice Nkem Chukwumezie, and M. C. Adeyeye, Monitoring Ibuprofen Release from (Avicel-based) Multi-particulates: In-situ Fiber Optic Technique versus the HPLC Method. A Technical Note. AAPS PharmSciTech, 2007; 8 (3) Article 52.  Available from AAPS PharmSciTech