PROGRESS UPDATES

 

Mechanistic understanding of food effects: water diffusivity in gastrointestinal tract is an important parameter for the prediction of disintegration of solid oral dosage forms.

Radwan A, Ebert S, Amar A, Münnemann K, Wagner M, Amidon GL, Langguth P.

Mol Pharm. 2013 Jun 3;10(6):2283-90. doi: 10.1021/mp3006209.


Mechanistic basis for unexpected bioavailability enhancement of polyelectrolyte complexes incorporating BCS class III drugs and carrageenans.

Heinen C, Reuss S,  Saaler-Reinhardt S, Langguth P

Eur. J. Pharm. Biopharm. 85 (1): 26-33 (2013). doi:10.1016/j.ejpb.2013.03.010


Ion pairing with bile salts modulates intestinal permeability and contributes to food-drug interaction of BCS class III compound trospium chloride.

Heinen CA, Reuss S, Amidon GL, Langguth P.

Mol Pharm. 2013 Nov 4;10(11):3989-96. doi: 10.1021/mp400179v.


In vitro – in vivo correlations. General Principles and Methodologies ( Part 1)

Hühn E, Langguth P

Pharm. Ind. 75(1) 143-152 (2013)


In vitro – in vivo correlations. General Principles and Methodologies ( Part 2)

Hühn E, Langguth P

Pharm. Ind. 75(2) 312-318 (2013)


The innovative medicines initiative OrBiTo project – developing the next generation predictive tools for oral biopharmaceutics.

McAllister M., Abrahamsson B., Lennernäs H. (2014)

European Industrial Pharmacy. December 2013, Issue 19: 9-11.


Intragastric volume changes after intake of a high-caloric, high-fat standard breakfast in healthy human subjects investigated by MRI.

Koziolek M, Grimm M, Garbacz G, Kühn JP, Weitschies W.

Mol Pharm. 2014 May 5;11(5):1632-9. doi: 10.1021/mp500022u.


Oral Biopharmceutics- Current status and identified gaps of understanding.

Lennernäs H , Abrahamsson B , Langguth P

EJ Pharm. Sci. (2014) doi: 10.1016/j.ejps.2014.02.001


Oral biopharmaceutics tools - Time for a new initiative - An introduction to the IMI project OrBiTo.

Lennernäs H, Aarons L, Augustijns P, Beato S, Bolger M, Box K, Brewster M, Butler J, Dressman J, Holm R, Julia Frank K, Kendall R, Langguth P, Sydor J, Lindahl A, McAllister M, Muenster U, Müllertz A, Ojala K, Pepin X, Reppas C, Rostami-Hodjegan A, Verwei M, Weitschies W, Wilson C, Karlsson C, Abrahamsson B.

Eur J Pharm Sci. 2014 Jun 16;57:292-9. doi: 10.1016/j.ejps.2013.10.012


Early pharmaceutical profiling to predict oral drug absorption: Current status and unmet needs.

Bergström CA, Holm R, Jørgensen SA, Andersson SB, Artursson P, Beato S, Borde A, Box K, Brewster M, Dressman J, Feng KI, Halbert G, Kostewicz E, McAllister M, Muenster U, Thinnes J, Taylor R, Mullertz A.

Eur J Pharm Sci. 2014 Jun 16;57:173-99. doi: 10.1016/j.ejps.2013.10.015.


In vitro models for the prediction of in vivo performance of oral dosage forms.

Kostewicz ES, Abrahamsson B, Brewster M, Brouwers J, Butler J, Carlert S, Dickinson PA, Dressman J, Holm R, Klein S, Mann J, McAllister M, Minekus M, Muenster U, Müllertz A, Verwei M, Vertzoni M, Weitschies W, Augustijns P.

Eur J Pharm Sci. 2014 Jun 16;57:342-66. doi: 10.1016/j.ejps.2013.08.024. Epub 2013 Aug 27.


PBPK models for the prediction of in vivo performance of oral dosage forms.

Kostewicz ES, Aarons L, Bergstrand M, Bolger MB, Galetin A, Hatley O, Jamei M, Lloyd R, Pepin X, Rostami-Hodjegan A, Sjögren E, Tannergren C, Turner DB, Wagner C, Weitschies W, Dressman J.

Eur J Pharm Sci. 2014 Jun 16;57:300-21. doi: 10.1016/j.ejps.2013.09.008. Epub 2013 Sep 21


In vivo methods for drug absorption - comparative physiologies, model selection, correlations with in vitro methods (IVIVC), and applications for formulation/API/excipient characterization including food effects.

Sjögren E, Abrahamsson B, Augustijns P, Becker D, Bolger MB, Brewster M, Brouwers J, Flanagan T, Harwood M, Heinen C, Holm R, Juretschke HP, Kubbinga M, Lindahl A, Lukacova V, Münster U, Neuhoff S, Nguyen MA, Peer Av, Reppas C, Hodjegan AR, Tannergren C, Weitschies W, Wilson C, Zane P, Lennernäs H, Langguth P.

Eur J Pharm Sci. 2014 Jun 16;57:99-151. doi: 10.1016/j.ejps.2014.02.010.


Use of the pentagastrin dog model to explore the food effects on formulations in early drug development.

Zane P, Guo Z, MacGerorge D, Vicat P, Ollier C.

Eur J Pharm Sci. 2014 Jun 16;57:207-13. doi: 10.1016/j.ejps.2013.09.018. Epub 2013 Oct 1


Bio-predictive tablet disintegration: effect of water diffusivity, fluid flow, food composition and test conditions.

Radwan A, Wagner M, Amidon GL, Langguth P

Eur J Pharm Sci. 2014 Jun 16;57:273-9. doi: 10.1016/j.ejps.2013.08.038.


The Biohharmaceutics classification system: Subclasses for in vivo predictive dissolution (IPD) methodology and IVIVC.

Tsume Y, Mudie D, Langguth P, Amidon G, Amidon G

E J Pharm Sci. 2014) doi: 10.1016/j.ejps.2014.01.009


Improvement of trospium-specific absorption models for fasted and fed states in humans.

Cvijić S, Langguth P.

Biopharm Drug Dispos. 2014 Jul 17. doi: 10.1002/bdd.1911. [Epub ahead of print]


Viscosity-mediated negative food effect on oral absorption of poorly-permeable drugs with an absorption window in the proximal intestine: In vitro experimental simulation and computational verification.

Cvijić S, Parojčić J, Langguth P.

Eur J Pharm Sci. 2014 Sep 30;61:40-53. doi: 10.1016/j.ejps.2014.04.008


Novel insights into excipient effects on the biopharmaceutics of APIs from different BCS classes: Lactose in solid oral dosage forms.

Kubbinga M, Moghani L, Langguth P.

Eur J Pharm Sci. 2014 Sep 30;61:27-31. doi: 10.1016/j.ejps.2014.03.008. Epub 2014 Apr 13


Resolving intraluminal drug and formulation behaviour: gastrointestinal concentration profiling in humans.

Brouwers J, Augustijns P

EJ Pharm Sci. 2014 Sept 30: Volume 61, Pages 2-10. doi:10.1016/j.ejps.2014.01.010


Gastrointestinal transfer: In vivo evaluation and implementation in in vitro and in silico predictive tools.

Hens B, Brouwers J, Anneveld B, Corsetti M, Symillides M, Vertzoni M, Reppas C, Turner DB, Augustijns P.

Eur J Pharm Sci. 2014 Oct 15;63:233-42. doi: 10.1016/j.ejps.2014.07.008.


Direct In Vivo Human Intestinal Permeability (Peff ) Determined with Different Clinical Perfusion and Intubation Methods.

Dahlgren D, Roos C, Sjögren E, Lennernäs H.

J Pharm Sci. 2014 Nov 19. doi: 10.1002/jps.24258. [Epub ahead of print]


Statistical investigation of simulated intestinal fluid composition on the equilibrium solubility of Biopharmaceutics Classification System Class II drugs

Khadra I, Zhou Z, Dunn C, Wilson CG, Halbert G.

Eur J Pharm Sci. 2015 Published online: 22-Nov-2014: 65-75 doi: 10.1016/j.ejps.2014.10.019


Gastrointestinal transfer: in vivo evaluation and implementation in in vitro and in silico predictive tools

Hens B, Brouwers J, Anneveld B, Corsetti M, Symillides M, Vertzoni M, Reppas C, Turner DB, Augustijns P.

Eur J Pharm Sci. 2014 Oct 15;63:233-42. doi: 10.1016/j.ejps.2014.07.008. Epub 2014 Jul 23.


Investigation of pH and Temperature Profiles in the GI Tract of Fasted Human Subjects Using the Intellicap(®) System

Koziolek M, Grimm M, Becker D, Iordanov V, Zou H, Shimizu J, Wanke C, Garbacz G, Weitschies W.

J Pharm Sci. 2014 Nov 19. doi: 10.1002/jps.24274. [Epub ahead of print]


Intragastric volume changes after intake of a high-caloric, high-fat standard breakfast in healthy human subjects investigated by MRI 

Koziolek M, Grimm M, Garbacz G, Kühn JP, Weitschies W.

Mol Pharm. 2014 May 5;11(5):1632-9. doi: 10.1021/mp500022u. Epub 2014 Apr 15


Oral solid dosage form disintegration – The forgotten test

J. Al-Gousous and P. Langguth

J Pharm Sci. 2014 Dec 24. doi: 10.1002/jps.24303. [Epub ahead of print]


Dissolution of mesalazine modified release tablets under standard and bio-relevant test conditions

Garbacz G, Rappen GM, Koziolek M, Weitschies W.

J Pharm Pharmacol. 2015 Feb;67(2):199-208. doi: 10.1111/jphp.12332. Epub 2014 Dec 31.


The Influence of Chitosan on the Oral Bioavailability of Acyclovir-a Comparative Bioavailability Study in Humans

Kubbinga M, Nguyen MA, Staubach P, Teerenstra S, Langguth P.

Pharm Res. 2015 Jan 22. [Epub ahead of print]


Human in vivo regional intestinal permeability: quantitation using site-specific drug absorption data.

Sjögren E, Dahlgren D, Roos C, Lennernäs H

Mol Pharm. 2015 Jun 1;12(6):2026-39. doi: 10.1021/mp500834v. Epub 2015 May 6.


In vitro simulation of luminal conditions of performance of oral drug products choosing the appropriate test media.

Markopoulos C, Andreas C, Vertzoni M, Dressman J, Reppas C

E J Pharm Bio. 2015 June: Volume 93, pp 173-182. doi:10.1016/j.ejpb.2015.03.009


European versus United States Pharmacopeia Disintegration Testing Methods for Enteric-Coated Soft Gelatin Capsules

Al-Gousous J, Langguth P.

Dissolution Technologies 2015 Aug.  dx.doi.org/10.14227/DT220315P6 


Development of a high-throughput in vitro lipolysis model for rapid screening of lipid-based drug delivery systems.

Mosgaard M, Sassene P, Mu H, Rades T, Müllertz A

E J Pharm. Bio. 2015 August: Volume 94, pp 493-500. doi:10.1016/j.ejpb.2015.06.028


Oral solid dosage form disintegration - The forgotten test

Al-Gousous J, Langguth P

J Pharm Sci. 2015 Sept: Volume 104, Issue 9, pp 2664-2675. DOI: 10.1002/jps.24303


Investigation of pH and temperature profiles in the GI-tract of fasted human subjects using the IntelliCap® system.

Koziolek M, Grimm M, Becker D, Iordanov V, Zou H, Shimizu J, Wanke C, Garbacz G, Weirschies W

J Pharm Sci. 2015 Sept: Volume 104, Issue 9, pp2855-2863. DOI: 10.1002/jps.24274


Computational fluid dynamics simulation of hydrodynamics and stresses in the PhEur/USP disintegration tester under fed and fasted fluid characteristics.

Kindgen S, Wachtet H, Abrahamsson B, Langguth P

J Pharm Sci. 2015 Sept: Volume 104, Issue 9, pp 2956-2968. DOI: 10.1002/jps.24511


Two-stage single-compartment models to evaluate dissolution in lower intestine.

Markopoulos C, Vertzoni M, Symillides M, Kesisoglou F, Reppas C

J Pharm Sci. 2015 September: Volume 104, Issue 9, pp 2986-2997. DOI: 10.1002/jps.24485


Gastrointestinal behavior of nano- and micronized fenofibrate: in vivo evaluation in man and in vitro assessment of the permeation potential.

Hens B, Brouwers J, Corsetti M, Augustijns P

E J  Pharm. Sci. 2015 Sept 18: Volume 77, Pages 40-47. doi:10.1016/j.ejps.2015.05.023


Characterization of contents of distal ileum and cecum to which drugs/drug products are exposed during BA/BE studies in healthy adults.

Reppas C, Karatza E, Goumas C, Markolpoulos C, Vertzoni

Pharm. Research. 2015 Oct, Volume 32, Issue 10, pp 3338-3349. 10.1007/s11095-015-1710-6


Drug disposition and modelling before and after gastric bypass: immediate and controlled-release metoprolol formulations.

Gesquiere I, Darwich A, Schueren B, Hoon J, Lannoo M, Matthys C, Rostami A, Foulon V, Augustijn P

BJCP. 2015 Nov: Volume 80, Issue 5, pp 1021-1030. DOI: 10.1111/bcp.12666


In vitro biorelevant models for evaluating modified release mesalamine products for forecasting effect of formulation and meal intake on drug release.

Andreas C, Chen Y, Markopoulos C, Reppas C, Dressman J

E J Pharm. & BioPharm. 2015 Nov: Volume 97, Part A, pp 39-50. doi:10.1016/j.ejpb.2015.09.002


Intragastric pH and pressure profiles after intake of the high-caloric, high-fat meal as used for food effect studies.

Koziolek M, Schneider F, Grimm M, Modeβ C, Seekamp A, Roustom T, Siegmund W,Weitschies W.​

2015 Dec 28;220(Pt A):71-8. doi: 10.1016/j.jconrel.2015.10.022.

Hens B, Corsetti M, Brouwers J, Augustijns P

J Pharm Sci. 2016 May 10. doi:10.1016/j.xphs.2016.03.027


Effectiveness of supersaturation promoting excipients on luminal albendazole concentrations following in complete gastric dissolution in fasted healthy adults.

Kourentas A, Vertzoni M, Symillides M, Goumas K, Gibbon R, Butler J, Reppas C

E J Pharm Sci. 2016 May 13. doi:10.1016/j.ejps.2016.05.013


An in vitro biorelevant gastrointestinal transfer (BioGIT) system for forecasting concentrations in the fasted upper small intestine: Design, implementation and evaluation.

Kourentas A, Vertzoni M, Stavrinoudakis N, Symillidis A, Brouwers J, Augustijns P, Reppas C, Symillides M

E J Pharm Sci. 2016 Jan 20. doi:10.1016/j.ejps.2015.11.012


Gastrointestinal behavior of weakly acidic BCS class II drugs in man - case study diclofenac potassium.

Abeele J, Brouwers J, Mattheus R, Tack J, Augustijns P

J Pharm Sci. 2015 Sept. DOI: 10.1002/jps.24647


Elucidating the Molecular Interactions Occurring during Drug Precipitation of Weak Bases from Lipid-Based Formulations: A Case Study with Cinnarizine and a Long Chain Self-Nanoemulsifying Drug Delivery System.

Sassene PJ, Mosgaard M, Löbmann K, Mu H, Larsen F, Rades T, Müllertz A

Mol. Pharmaceutics, 2015, 12 (11), pp 4067–4076. DOI: 10.1021/acs.molPharmaceut.5b00498


Supersaturation and precipitatioin of posaconazole upon entry in the upper small intestine in humans.

Hens B, Brouwers J, Corsetti M, Augustijns P

J Pharm Sci. 2015 Oct 27. doi: 10.1002/jps.24690


Evaluation of two dynamic in vitro models simulating fasted and fed state conditions in the upper GI tract (TIM-1 and tiny TIM) for investigating the bioaccessibility of Pharm.ceutical compounds from oral dosage forms.

Verwei M, Minekus M, Zeijdner E, Schilderink R, Havenaar R

Int J Pharm. 2016 Feb 10: Volume 498, Issues 1-2, pp 178-186. doi:10.1016/j.ijpharm.2015.11.048


Meta-Analysis of Magnetic Marker Monitoring data to characterize the movement of single unit dosage forms though the gastrointestinal tract under fed and fasting conditions.

Hénin E, Bergstrand M, Weitschies W, Karlsson M

Pharm. Research. 2016 March. Volume 33, Issue 3, pp 751-762. doi:10.​1007/​s11095-015-1824-x


Semi-mechanistic model describing gastric emptying and glucose absorption in healthy subjects and patients with type 2 diabetes.

Alskär O, Bagger J, Røge R, Knop F, Karlsson M, Visbøll, Kjellsson M

J Clin Pharmacol. 2016 Mar;56(3):340-8. doi: 10.1002/jcph.602. Epub 2015 Oct 12


Koziolek M, Grimm M, Schneider F, Jedamzik P, Sager M, Kühn JP, Siegmund W, Weitschies W.

Adv Drug Deliv Rev. 2016 Jun 1;101:75-88.doi: 10.1016/j.addr.2016.03.009.


Effectiveness of supersaturation promoting excipients on albendazole concentrations in upper gastrointestinal lumen of fasted healthy adults.

Kourentas A, Vertzoni M, Symillides M, Goumas K, Gibbon R, Butler J, Reppas C.

Eur J Pharm Sci. 2016 Aug 25;91:11-9. doi: 10.1016/j.ejps.2016.05.013.


Evaluation of the Impact of Excipients and an Albendazole Salt on Albendazole Concentrations in Upper Small Intestine Using an In Vitro Biorelevant Gastrointestinal Transfer (BioGIT) System.

Kourentas A, Vertzoni M, Khadra I, Symillides M, Clark H, Halbert G, Butler J,Reppas C.

J Pharm Sci. 2016 Sep;105(9):2896-903. doi: 10.1016/j.xphs.2016.04.037.


Regional Intestinal Permeability of Three Model Drugs in Human.

Dahlgren D, Roos C, Lundqvist A, Abrahamsson B, Tannergren C, Hellström PM, Sjögren E, Lennernäs H.

Mol Pharm. 2016 Sep 6;13(9):3013-21. doi: 10.1021/acs.molpharmaceut.6b00514.


The dynamic gastric environment and its impact on drug and formulation behaviour.

Van Den Abeele J, Rubbens J, Brouwers J, Augustijns P.

Eur J Pharm Sci. 2016 Sep 2. pii: S0928-0987(16)30349-9. doi: 10.1016/j.ejps.2016.08.060.


Gastrointestinal and Systemic Monitoring of Posaconazole in Humans After Fasted and Fed State Administration of a Solid Dispersion.

Hens B, Corsetti M, Brouwers J, Augustijns P.

J Pharm Sci. 2016 Sep;105(9):2904-12. doi: 10.1016/j.xphs.2016.03.027.


Resolving the physiological conditions in bioavailability and bioequivalence studies: comparison of fasted and fed state.

Schneider F, Grimm M, Koziolek M, Modeß C, Dokter A, Roustom T, Siegmund W, Weitschies W.

Eur J Pharm Biopharm. 2016 Sep 14. pii: S0939-6411(16)30558-6. doi: 10.1016/j.ejpb.2016.09.009.


Supersaturation and Precipitation of Posaconazole Upon Entry in the Upper Small Intestine in Humans.

Hens B, Brouwers J, Corsetti M, Augustijns P.

J Pharm Sci. 2016 Sep;105(9):2677-84. doi: 10.1002/jps.24690


Interlaboratory Validation of Small-Scale Solubility and Dissolution Measurements of Poorly Water-Soluble Drugs.

Andersson SB, Alvebratt C, Bevernage J, Bonneau D, da Costa Mathews C, Dattani R, Edueng K, He Y, Holm R, Madsen C, Müller T, Muenster U, Müllertz A, Ojala K, Rades T, Sieger P, Bergström CA.

J Pharm Sci. 2016 Sep;105(9):2864-72. doi: 10.1016/j.xphs.2016.03.010. Epub 2016 Apr 23.


In Vivo Precipitation of Poorly Soluble Drugs from Lipid-Based Drug Delivery Systems.

Sassene PJ, Michaelsen MH, Mosgaard MD, Jensen MK, Van Den Broek E, Wasan KM, Mu H, Rades T, Müllertz A.

Mol Pharm. 2016 Oct 3;13(10):3417-3426. Epub 2016 Aug 30.


High-Throughput Lipolysis in 96-Well Plates for Rapid Screening of Lipid-Based Drug Delivery Systems.

Mosgaard MD, Sassene PJ, Mu H, Rades T, Müllertz A.

J Pharm Sci. 2017 Apr;106(4):1183-1186. doi: 10.1016/j.xphs.2016.12.026. Epub 2017 Jan 3.


Studying the Propensity of Compounds to Supersaturate: A Practical and Broadly Applicable Approach.

Palmelund H, Madsen CM, Plum J, Müllertz A, Rades T.

J Pharm Sci. 2016 Oct;105(10):3021-3029. doi: 10.1016/j.xphs.2016.06.016. Epub 2016 Jul 31.


Use of physiologically relevant biopharmaceutics tools within the pharmaceutical industry and in regulatory sciences: Where are we now and what are the gaps?

Flanagan T, Van Peer A, Lindahl A.

Eur J Pharm Sci. 2016 Aug 25;91:84-90. doi: 10.1016/j.ejps.2016.06.006. Epub 2016 Jun 7.


Comparison of lipases for in vitro models of gastric digestion: lipolysis using two infant formulas as model substrates.

Sassene PJ, Fanø M, Mu H, Rades T, Aquistapace S, Schmitt B, Cruz-Hernandez C, Wooster TJ, Müllertz A.

Food Funct. 2016 Sep 14;7(9):3989-3998.


Can dosage form-dependent food effects be predicted using biorelevant dissolution tests? Case example extended release nifedipine.

Andreas CJ, Tomaszewska I, Muenster U, van der Mey D, Mueck W, Dressman JB.

Eur J Pharm Biopharm. 2016 Aug;105:193-202. doi: 10.1016/j.ejpb.2016.06.010. Epub 2016 Jun 15.


A Novel Disintegration Tester for Solid Dosage Forms Enabling Adjustable Hydrodynamics.

Kindgen S, Rach R, Nawroth T, Abrahamsson B, Langguth P.

J Pharm Sci. 2016 Aug;105(8):2402-9. doi: 10.1016/j.xphs.2016.05.028. Epub 2016 Jul 13.


Forecasting oral absorption across biopharmaceutics classification system classes with physiologically based pharmacokinetic models.

Hansmann S, Darwich A, Margolskee A, Aarons L, Dressman J.

J Pharm Pharmacol. 2016 Dec;68(12):1501-1515. doi: 10.1111/jphp.12618. Epub 2016 Oct 26.


IMI - oral biopharmaceutics tools project - evaluation of bottom-up PBPK prediction success part 1: Characterisation of the OrBiTo database of compounds.

Margolskee A, Darwich AS, Pepin X, Pathak SM, Bolger MB, Aarons L, Rostami-Hodjegan A, Angstenberger J, Graf F, Laplanche L, Müller T, Carlert S, Daga P, Murphy D, Tannergren C, Yasin M, Greschat-Schade S, Mück W, Muenster U, van der Mey D, Frank KJ, Lloyd R, Adriaenssen L, Bevernage J, De Zwart L, Swerts D, Tistaert C, Van Den Bergh A, Van Peer A, Beato S, Nguyen-Trung AT, Bennett J, McAllister M, Wong M, Zane P, Ollier C, Vicat P, Kolhmann M, Marker A, Brun P, Mazuir F, Beilles S, Venczel M, Boulenc X, Loos P, Lennernäs H, Abrahamsson B.

Eur J Pharm Sci. 2017 Jan 1;96:598-609. doi: 10.1016/j.ejps.2016.09.027. Epub 2016 Sep 23.

 

IMI - Oral biopharmaceutics tools project - Evaluation of bottom-up PBPK prediction success part 2: An introduction to the simulation exercise and overview of results.

Margolskee A, Darwich AS, Pepin X, Aarons L, Galetin A, Rostami-Hodjegan A, Carlert S, Hammarberg M, Hilgendorf C, Johansson P, Karlsson E, Murphy D, Tannergren C, Thörn H, Yasin M, Mazuir F, Nicolas O, Ramusovic S, Xu C, Pathak SM, Korjamo T, Laru J, Malkki J, Pappinen S, Tuunainen J, Dressman J, Hansmann S, Kostewicz E, He H, Heimbach T, Wu F, Hoft C, Laplanche L, Pang Y, Bolger MB, Huehn E, Lukacova V, Mullin JM, Szeto KX, Costales C, Lin J, McAllister M, Modi S, Rotter C, Varma M, Wong M, Mitra A, Bevernage J, Biewenga J, Van Peer A, Lloyd R, Shardlow C, Langguth P, Mishenzon I, Nguyen MA, Brown J, Lennernäs H, Abrahamsson B.

Eur J Pharm Sci. 2017 Jan 1;96:610-625. doi: 10.1016/j.ejps.2016.10.036. Epub 2016 Nov 2.

 

IMI - Oral biopharmaceutics tools project - Evaluation of bottom-up PBPK prediction success part 3: Identifying gaps in system parameters by analysing In Silico performance across different compound classes.

Darwich AS, Margolskee A, Pepin X, Aarons L, Galetin A, Rostami-Hodjegan A, Carlert S, Hammarberg M, Hilgendorf C, Johansson P, Karlsson E, Murphy D, Tannergren C, Thörn H, Yasin M, Mazuir F, Nicolas O, Ramusovic S, Xu C, Pathak SM, Korjamo T, Laru J, Malkki J, Pappinen S, Tuunainen J, Dressman J, Hansmann S, Kostewicz E, He H, Heimbach T, Wu F, Hoft C, Pang Y, Bolger MB, Huehn E, Lukacova V, Mullin JM, Szeto KX, Costales C, Lin J, McAllister M, Modi S, Rotter C, Varma M, Wong M, Mitra A, Bevernage J, Biewenga J, Van Peer A, Lloyd R, Shardlow C, Langguth P, Mishenzon I, Nguyen MA, Brown J, Lennernäs H, Abrahamsson B.

Eur J Pharm Sci. 2017 Jan 1;96:626-642. doi: 10.1016/j.ejps.2016.09.037. Epub 2016 Sep 28.


Biopharmaceutics data management system for anonymised data sharing and curation: First application with orbito IMI project.

Lacy-Jones K, Hayward P, Andrews S, Gledhill I, McAllister M, Abrahamsson B, Rostami-Hodjegan A, Pepin X.

Comput Methods Programs Biomed. 2017 Mar;140:29-44. doi: 10.1016/j.cmpb.2016.11.006. Epub 2016 Nov 18.


Statistical investigation of simulated fed intestinal media composition on the equilibrium solubility of oral drugs.

Zhou Z, Dunn C, Khadra I, Wilson CG, Halbert GW.

Eur J Pharm Sci. 2017 Mar 1;99:95-104. doi: 10.1016/j.ejps.2016.12.008. Epub 2016 Dec 7.


Mechanistic Oral Absorption Modeling and Simulation for Formulation Development and Bioequivalence Evaluation: Report of an FDA Public Workshop.

Zhang X, Duan J, Kesisoglou F, Novakovic J, Amidon GL, Jamei M, Lukacova V, Eissing T, Tsakalozou E, Zhao L, Lionberger R.

CPT Pharmacometrics Syst Pharmacol. 2017 Aug;6(8):492-495. doi: 10.1002/psp4.12204. Epub 2017 Jul 11.


Regional Intestinal Permeability in Dogs: Biopharmaceutical Aspects for Development of Oral Modified-Release Dosage Forms.

Dahlgren D, Roos C, Johansson P, Lundqvist A, Tannergren C, Abrahamsson B, Sjögren E, Lennernäs H.

Mol Pharm. 2016 Sep 6;13(9):3022-33. doi: 10.1021/acs.molpharmaceut.6b00515. Epub 2016 Aug 18.


Influence of Physiological Gastrointestinal Surfactant Ratio on the Equilibrium Solubility of BCS Class II Drugs Investigated Using a Four Component Mixture Design.

Zhou Z, Dunn C, Khadra I, Wilson CG, Halbert GW.

Mol Pharm. 2017 Aug 22. doi: 10.1021/acs.molpharmaceut.7b00354. [Epub ahead of print]


Gastrointestinal dissolution, supersaturation and precipitation of the weak base indinavir in healthy volunteers.

Rubbens J, Brouwers J, Tack J, Augustijns P.

Eur J Pharm Biopharm. 2016 Dec;109:122-129. doi: 10.1016/j.ejpb.2016.09.014. Epub 2016 Sep 28.


Gastrointestinal dissolution, supersaturation and precipitation of the weak base indinavir in healthy volunteers.

Rubbens J, Brouwers J, Tack J, Augustijns P.

Eur J Pharm Biopharm. 2016 Dec;109:122-129. doi: 10.1016/j.ejpb.2016.09.014. Epub 2016 Sep 28.


Optimization of the Ussing chamber setup with excised rat intestinal segments for dissolution/permeation experiments of poorly soluble drugs.

Forner K, Roos C, Dahlgren D, Kesisoglou F, Konerding MA, Mazur J, Lennernäs H, Langguth P.

Drug Dev Ind Pharm. 2017 Feb;43(2):338-346. doi: 10.1080/03639045.2016.1251449. Epub 2016 Nov 6.


Partitioning into Colloidal Structures of Fasted State Intestinal Fluid Studied by Molecular Dynamics Simulations.

Holmboe M, Larsson P, Anwar J, Bergström CA.

Langmuir. 2016 Dec 6;32(48):12732-12740. Epub 2016 Nov 28.


Development of a Video-Microscopic Tool To Evaluate the Precipitation Kinetics of Poorly Water Soluble Drugs: A Case Study with Tadalafil and HPMC.

Christfort JF, Plum J, Madsen CM, Nielsen LH, Sandau M, Andersen K, Müllertz A, Rades T.

Mol Pharm. 2017 Aug 16. doi: 10.1021/acs.molpharmaceut.7b00422. [Epub ahead of print].


Resolving the physiological conditions in bioavailability and bioequivalence studies: Comparison of fasted and fed state.

Schneider F, Grimm M, Koziolek M, Modeß C, Dokter A, Roustom T, Siegmund W, Weitschies W.

Eur J Pharm Biopharm. 2016 Nov;108:214-219. doi: 10.1016/j.ejpb.2016.09.009. Epub 2016 Sep 14.


Exploring the link between gastric motility and intragastric drug distribution in man.

Van Den Abeele J, Brouwers J, Tack J, Augustijns P.

Eur J Pharm Biopharm. 2017 Mar;112:75-84. doi: 10.1016/j.ejpb.2016.10.027. Epub 2016 Nov 16


In Vivo Predictive Dissolution (IPD) and Biopharmaceutical Modeling and Simulation: Future Use of Modern Approaches and Methodologies in a Regulatory Context.

Lennernäs H, Lindahl A, Van Peer A, Ollier C, Flanagan T, Lionberger R, Nordmark A, Yamashita S, Yu L, Amidon GL, Fischer V, Sjögren E, Zane P, McAllister M, Abrahamsson B.

Mol Pharm. 2017 Apr 3;14(4):1307-1314. doi: 10.1021/acs.molpharmaceut.6b00824. Epub 2017 Mar 1.


Effect of composition of simulated intestinal media on the solubility of poorly soluble compounds investigated by design of experiments.

Madsen CM, Feng KI, Leithead A, Canfield N, Jørgensen SA, Müllertz A, Rades T.

Eur J Pharm Sci. 2017 Oct 3. pii: S0928-0987(17)30547-X. doi: 10.1016/j.ejps.2017.10.003. [Epub ahead of print].


Exploring the link between gastric motility and intragastric drug distribution in man.

Van Den Abeele J, Brouwers J, Tack J, Augustijns P.

Eur J Pharm Biopharm. 2017 Mar;112:75-84. doi: 10.1016/j.ejpb.2016.10.027. Epub 2016 Nov 16.


A survey on IVIVC/IVIVR development in the pharmaceutical industry - Past experience and current perspectives.

Nguyen MA, Flanagan T, Brewster M, Kesisoglou F, Beato S, Biewenga J, Crison J, Holm R, Li R, Mannaert E, McAllister M, Mueller-Zsigmondy M, Muenster U, Ojala K, Page S, Parr A, Rossenu S, Timmins P, Van Peer A, Vermeulen A, Langguth P.

Eur J Pharm Sci. 2017 May 1;102:1-13. doi: 10.1016/j.ejps.2017.02.029. Epub 2017 Feb 21. Review.


The dynamic gastric environment and its impact on drug and formulation behaviour.

Van Den Abeele J, Rubbens J, Brouwers J, Augustijns P.

Eur J Pharm Sci. 2017 Jan 1;96:207-231. doi: 10.1016/j.ejps.2016.08.060. Epub 2016 Sep 3. Review.


Mapping the intermediate digestion phases of human healthy intestinal contents from distal ileum and caecum at fasted and fed state conditions.

Tran T, Fatouros DG, Vertzoni M, Reppas C, Müllertz A.

J Pharm Pharmacol. 2017 Mar;69(3):265-273. doi: 10.1111/jphp.12686. Epub 2017 Jan 20.


Mechanism-Based Modeling of Gastric Emptying Rate and Gallbladder Emptying in Response to Caloric Intake.

Guiastrennec B, Sonne DP, Hansen M, Bagger JI, Lund A, Rehfeld JF, Alskär O, Karlsson MO, Vilsbøll T, Knop FK, Bergstrand M.

CPT Pharmacometrics Syst Pharmacol. 2016 Dec;5(12):692-700. doi: 10.1002/psp4.12152.


Dissolution and dissolution/permeation experiments for predicting systemic exposure following oral administration of the BCS class II drug clarithromycin.

Kristin F, René H, Boontida M, Buraphacheep JV, Maximilian A, Johanna M, Peter L.

Eur J Pharm Sci. 2017 Apr 1;101:211-219. doi: 10.1016/j.ejps.2017.02.003. Epub 2017 Feb 4.


In vitro evaluation of the impact of gastrointestinal transfer on luminal performance of commercially available products of posaconazole and itraconazole using BioGIT.

Kourentas A, Vertzoni M, Symillides M, Hens B, Brouwers J, Augustijns P, Reppas C.

Int J Pharm. 2016 Dec 30;515(1-2):352-358. doi: 10.1016/j.ijpharm.2016.10.018. Epub 2016 Oct 11.


Prediction of Ketoconazole absorption using an updated in vitro transfer model coupled to physiologically based pharmacokinetic modelling.

Ruff A, Fiolka T, Kostewicz ES.

Eur J Pharm Sci. 2017 Mar 30;100:42-55. doi: 10.1016/j.ejps.2016.12.017. Epub 2016 Dec 21.


Exploring gastrointestinal variables affecting drug and formulation behavior: Methodologies, challenges and opportunities.

Hens B, Corsetti M, Spiller R, Marciani L, Vanuytsel T, Tack J, Talattof A, Amidon GL, Koziolek M, Weitschies W, Wilson CG, Bennink RJ, Brouwers J, Augustijns P.

Int J Pharm. 2017 Mar 15;519(1-2):79-97. doi: 10.1016/j.ijpharm.2016.11.063. Epub 2016 Nov 30. Review.


Gastric and Duodenal Ethanol Concentrations after Intake of Alcoholic Beverages in Postprandial Conditions.

Rubbens J, Riethorst D, Brouwers J, Wolfs K, Adams E, Tack J, Augustijns P.

Mol Pharm. 2017 Aug 11. doi: 10.1021/acs.molpharmaceut.7b00252. [Epub ahead of print].


Evaluation of Dissolution in the Lower Intestine and Its Impact on the Absorption Process of High Dose Low Solubility Drugs.

Georgaka D, Butler J, Kesisoglou F, Reppas C, Vertzoni M.

Mol Pharm. 2017 Apr 13. doi: 10.1021/acs.molpharmaceut.6b01129. [Epub ahead of print].


Validation of Dissolution Testing with Biorelevant Media: An OrBiTo Study.

Mann J, Dressman J, Rosenblatt K, Ashworth L, Muenster U, Frank K, Hutchins P, Williams J, Klumpp L, Wielockx K, Berben P, Augustijns P, Holm R, Hofmann M, Patel S, Beato S, Ojala K, Tomaszewska I, Bruel JL, Butler J.

Mol Pharm. 2017 Aug 23. doi: 10.1021/acs.molpharmaceut.7b00198. [Epub ahead of print].


Controlled Suspensions Enable Rapid Determinations of Intrinsic Dissolution Rate and Apparent Solubility of Poorly Water-Soluble Compounds.

Andersson SBE, Alvebratt C, Bergström CAS.

Pharm Res. 2017 Sep;34(9):1805-1816. doi: 10.1007/s11095-017-2188-1. Epub 2017 Jun 15.


Evaluating the predictability of the in vitro transfer model and in vivo rat studies as a surrogate to investigate the supersaturation and precipitation behaviour of different Albendazole formulations for humans.

Ruff A, Holm R, Kostewicz ES.

Eur J Pharm Sci. 2017 Jul 15;105:108-118. doi: 10.1016/j.ejps.2017.04.024. Epub 2017 May 1.


The Effect of Sparkling Water on Intraluminal Formulation Behavior and Systemic Drug Performance.

Van Den Abeele J, Brouwers J, Deloose E, Tack J, Augustijns P.

J Pharm Sci. 2017 Sep;106(9):2472-2482. doi: 10.1016/j.xphs.2017.03.039. Epub 2017 Apr 7.


Assessment of Passive Intestinal Permeability Using an Artificial Membrane Insert System.

Berben P, Brouwers J, Augustijns P.

J Pharm Sci. 2017 Aug 19. pii: S0022-3549(17)30566-X. doi: 10.1016/j.xphs.2017.08.002. [Epub ahead of print].


Gastrointestinal behavior of itraconazole in humans - Part 1: Supersaturation from a solid dispersion and a cyclodextrin-based solution.

Brouwers J, Geboers S, Mols R, Tack J, Augustijns P.

Int J Pharm. 2017 Jun 15;525(1):211-217. doi: 10.1016/j.ijpharm.2017.04.029. Epub 2017 Apr 13.


Preclinical Effect of Absorption Modifying Excipients on Rat Intestinal Transport of Model Compounds and the Mucosal Barrier Marker 51Cr-EDTA.

Dahlgren D, Roos C, Lundqvist A, Tannergren C, Langguth P, Sjöblom M, Sjögren E, Lennernäs H.

Mol Pharm. 2017 Aug 8. doi: 10.1021/acs.molpharmaceut.7b00353. [Epub ahead of print].


Regional Intestinal Permeability in Rats: A Comparison of Methods.

Roos C, Dahlgren D, Sjögren E, Tannergren C, Abrahamsson B, Lennernäs H.

Mol Pharm. 2017 Oct 5. doi: 10.1021/acs.molpharmaceut.7b00279. [Epub ahead of print].


In Vivo Mechanisms of Intestinal Drug Absorption from Aprepitant Nanoformulations.

Roos C, Dahlgren D, Berg S, Westergren J, Abrahamsson B, Tannergren C, Sjögren E, Lennernäs H.

Mol Pharm. 2017 Aug 10. doi: 10.1021/acs.molpharmaceut.7b00294. [Epub ahead of print].


Gastrointestinal and Systemic Disposition of Diclofenac under Fasted and Fed State Conditions Supporting the Evaluation of in Vitro Predictive Tools.

Van Den Abeele J, Schilderink R, Schneider F, Mols R, Minekus M, Weitschies W, Brouwers J, Tack J, Augustijns P.

Mol Pharm. 2017 Jul 7. doi: 10.1021/acs.molpharmaceut.7b00253. [Epub ahead of print].


Model-Based Analysis of Biopharmaceutic Experiments To Improve Mechanistic Oral Absorption Modeling: An Integrated in Vitro in Vivo Extrapolation Perspective Using Ketoconazole as a Model Drug.

Pathak SM, Ruff A, Kostewicz ES, Patel N, Turner DB, Jamei M.

Mol Pharm. 2017 Aug 25. doi: 10.1021/acs.molpharmaceut.7b00406. [Epub ahead of print].


Development of a Video-Microscopic Tool To Evaluate the Precipitation Kinetics of Poorly Water Soluble Drugs: A Case Study with Tadalafil and HPMC.

Christfort JF, Plum J, Madsen CM, Nielsen LH, Sandau M, Andersen K, Müllertz A, Rades T.

Mol Pharm. 2017 Aug 16. doi: 10.1021/acs.molpharmaceut.7b00422. [Epub ahead of print].


Molecular Structuring and Phase Transition of Lipid-Based Formulations upon Water Dispersion: A Coarse-Grained Molecular Dynamics Simulation Approach.

Larsson P, Alskär LC, Bergström CAS.

Mol Pharm. 2017 Aug 29. doi: 10.1021/acs.molpharmaceut.7b00397. [Epub ahead of print].


In Silico Modeling Approach for the Evaluation of Gastrointestinal Dissolution, Supersaturation, and Precipitation of Posaconazole.

Hens B, Pathak SM, Mitra A, Patel N, Liu B, Patel S, Jamei M, Brouwers J, Augustijns P, Turner DB.

Mol Pharm. 2017 Sep 5. doi: 10.1021/acs.molpharmaceut.7b00396. [Epub ahead of print].


Statistical investigation of the full concentration range of fasted and fed simulated intestinal fluid on the equilibrium solubility of oral drugs.

Perrier J, Zhou Z, Dunn C, Khadra I, Wilson CG, Halbert G.

Eur J Pharm Sci. 2017 Oct 5. pii: S0928-0987(17)30551-1. doi: 10.1016/j.ejps.2017.10.007. [Epub ahead of print].


Gastric Water Emptying under Fed State Clinical Trial Conditions Is as Fast as under Fasted Conditions.

Grimm M, Scholz E, Koziolek M, Kühn JP, Weitschies W.

Mol Pharm. 2017 Oct 5. doi: 10.1021/acs.molpharmaceut.7b00623. [Epub ahead of print].


In vitro simulation of realistic gastric pressure proles.

Schneider, F., Beeck, R., Hoppe, M., Koziolek, M., Weitschies, W.

European Journal of Pharmaceutical Sciences, 107, 71-77, 2017.