In Vivo Predictive Dissolution and Simulation Workshop Report: Facilitating the Development of Oral Drug Formulation and the Prediction of Oral Bioperformance

Overview

Journal AAPS J

Specialty Pharmacology

Date 2018 Sep 8

PMID 30191341

Citations 2

Authors

Yasuhiro Tsume

SanjayKumar Patel

Nikoletta Fotaki

Christel Bergstrm

Gordon L Amidon

James G Brasseur

Deanna M Mudie

Duxin Sun

Marival Bermejo

Ping Gao

Wei Zhu

David C Sperry

Maria Vertzoni

Neil Parrott

Robert Lionberger

Atsushi Kambayashi

Andre Hermans

Xujin Lu

Gregory E Amidon

Affiliations

Soon will be listed here.

Citing Articles

Focusing on First Cycle Approval in ANDA Submission: Understanding Common Deficiencies & Case Study Insights.

Pawar J, Hegde N, Sharma S Ther Innov Regul Sci. 2025; .

PMID: 39922964 DOI: 10.1007/s43441-025-00755-5.

Quantification of Fluid Volume and Distribution in the Paediatric Colon via Magnetic Resonance Imaging.

Goelen J, Alexander B, Wijesinghe H, Evans E, Pawar G, Horniblow R Pharmaceutics. 2021; 13(10).

PMID: 34684022 PMC: 8540766. DOI: 10.3390/pharmaceutics13101729.

Current trends in drug metabolism and pharmacokinetics.

Li Y, Meng Q, Yang M, Liu D, Hou X, Tang L Acta Pharm Sin B. 2019; 9(6):1113-1144.

PMID: 31867160 PMC: 6900561. DOI: 10.1016/j.apsb.2019.10.001.

References

Litou C, Vertzoni M, Xu W, Kesisoglou F, Reppas C . The impact of reduced gastric acid secretion on dissolution of salts of weak bases in the fasted upper gastrointestinal lumen: Data in biorelevant media and in human aspirates. Eur J Pharm Biopharm. 2017; 115:94-101. DOI: 10.1016/j.ejpb.2017.02.009. View

Tomaszewska I, Karki S, Shur J, Price R, Fotaki N . Pharmaceutical characterisation and evaluation of cocrystals: Importance of in vitro dissolution conditions and type of coformer. Int J Pharm. 2013; 453(2):380-8. DOI: 10.1016/j.ijpharm.2013.05.048. View

Krieg B, Taghavi S, Amidon G, Amidon G . In vivo predictive dissolution: transport analysis of the CO2 , bicarbonate in vivo buffer system. J Pharm Sci. 2014; 103(11):3473-3490. DOI: 10.1002/jps.24108. View

Tsume Y, Matsui K, Searls A, Takeuchi S, Amidon G, Sun D . The impact of supersaturation level for oral absorption of BCS class IIb drugs, dipyridamole and ketoconazole, using in vivo predictive dissolution system: Gastrointestinal Simulator (GIS). Eur J Pharm Sci. 2017; 102:126-139. DOI: 10.1016/j.ejps.2017.02.042. View

Tsume Y, Langguth P, Garcia-Arieta A, Amidon G . In silico prediction of drug dissolution and absorption with variation in intestinal pH for BCS class II weak acid drugs: ibuprofen and ketoprofen. Biopharm Drug Dispos. 2012; 33(7):366-77. PMC: 3466597. DOI: 10.1002/bdd.1800. View

Cristofoletti R, Dressman J . Matching phosphate and maleate buffer systems for dissolution of weak acids: Equivalence in terms of buffer capacity of bulk solution or surface pH?. Eur J Pharm Biopharm. 2016; 103:104-108. DOI: 10.1016/j.ejpb.2016.03.024. View

Hens B, Tsume Y, Bermejo M, Paixao P, Koenigsknecht M, Baker J . Low Buffer Capacity and Alternating Motility along the Human Gastrointestinal Tract: Implications for in Vivo Dissolution and Absorption of Ionizable Drugs. Mol Pharm. 2017; 14(12):4281-4294. DOI: 10.1021/acs.molpharmaceut.7b00426. View

Amidon G, Lennernas H, Shah V, Crison J . A theoretical basis for a biopharmaceutic drug classification: the correlation of in vitro drug product dissolution and in vivo bioavailability. Pharm Res. 1995; 12(3):413-20. DOI: 10.1023/a:1016212804288. View

Reppas C, Karatza E, Goumas C, Markopoulos C, Vertzoni M . Characterization of Contents of Distal Ileum and Cecum to Which Drugs/Drug Products are Exposed During Bioavailability/Bioequivalence Studies in Healthy Adults. Pharm Res. 2015; 32(10):3338-49. DOI: 10.1007/s11095-015-1710-6. View

10.

Stewart A, Grass M, Brodeur T, Goodwin A, Morgen M, Friesen D . Impact of Drug-Rich Colloids of Itraconazole and HPMCAS on Membrane Flux in Vitro and Oral Bioavailability in Rats. Mol Pharm. 2017; 14(7):2437-2449. DOI: 10.1021/acs.molpharmaceut.7b00338. View

11.

Xu H, Shi Y, Vela S, Marroum P, Gao P . Developing Quantitative In Vitro-In Vivo Correlation for Fenofibrate Immediate-Release Formulations With the Biphasic Dissolution-Partition Test Method. J Pharm Sci. 2017; 107(1):476-487. DOI: 10.1016/j.xphs.2017.06.018. View

12.

Tsume Y, Takeuchi S, Matsui K, Amidon G, Amidon G . In vitro dissolution methodology, mini-Gastrointestinal Simulator (mGIS), predicts better in vivo dissolution of a weak base drug, dasatinib. Eur J Pharm Sci. 2015; 76:203-12. DOI: 10.1016/j.ejps.2015.05.013. View

13.

Markopoulos C, Andreas C, Vertzoni M, Dressman J, Reppas C . In-vitro simulation of luminal conditions for evaluation of performance of oral drug products: Choosing the appropriate test media. Eur J Pharm Biopharm. 2015; 93:173-82. DOI: 10.1016/j.ejpb.2015.03.009. View

14.

Bittner B, McIntyre C, Tian H, Tang K, Shah N, Phuapradit W . Phase I clinical study to select a novel oral formulation for ibandronate containing the excipient sodium N-[8-(2-hydroxybenzoyl) amino] caprylate (SNAC). Pharmazie. 2012; 67(3):233-41. View

15.

Fotaki N, Aivaliotis A, Butler J, Dressman J, Fischbach M, Hempenstall J . A comparative study of different release apparatus in generating in vitro-in vivo correlations for extended release formulations. Eur J Pharm Biopharm. 2009; 73(1):115-20. DOI: 10.1016/j.ejpb.2009.04.012. View

16.

Matsui K, Tsume Y, Takeuchi S, Searls A, Amidon G . Utilization of Gastrointestinal Simulator, an in Vivo Predictive Dissolution Methodology, Coupled with Computational Approach To Forecast Oral Absorption of Dipyridamole. Mol Pharm. 2017; 14(4):1181-1189. DOI: 10.1021/acs.molpharmaceut.6b01063. View

17.

Takeuchi S, Tsume Y, Amidon G, Amidon G . Evaluation of a three compartment in vitro gastrointestinal simulator dissolution apparatus to predict in vivo dissolution. J Pharm Sci. 2014; 103(11):3416-3422. DOI: 10.1002/jps.24112. View

18.

Xu H, Vela S, Shi Y, Marroum P, Gao P . In Vitro Characterization of Ritonavir Drug Products and Correlation to Human in Vivo Performance. Mol Pharm. 2017; 14(11):3801-3814. DOI: 10.1021/acs.molpharmaceut.7b00552. View

19.

Tsume Y, Igawa N, Drelich A, Amidon G, Amidon G . The Combination of GIS and Biphasic to Better Predict In Vivo Dissolution of BCS Class IIb Drugs, Ketoconazole and Raloxifene. J Pharm Sci. 2017; 107(1):307-316. DOI: 10.1016/j.xphs.2017.09.002. View

20.

Yu A, Baker J, Fioritto A, Wang Y, Luo R, Li S . Measurement of in vivo Gastrointestinal Release and Dissolution of Three Locally Acting Mesalamine Formulations in Regions of the Human Gastrointestinal Tract. Mol Pharm. 2016; 14(2):345-358. DOI: 10.1021/acs.molpharmaceut.6b00641. View