Review & Monography

In vitro dynamic dissolution models for oral drugs

Expand
  • College of Pharmaceutical Science, Zhejiang University of Technology, Hangzhou 310014, China

Received date: 2022-01-22

  Online published: 2024-06-24

Abstract

Dissolution test is an important way to evaluate the quality of oral solid dosage forms. The dissolution and absorption of drugs in gastrointestinal tract are continuous and dynamic progress. Due to the lack of chemical components and fluid dynamics conditions which are similar to in vivo enviroment, the traditional dissolution methods are extremely limited in the evaluation of drug in vivo. Therefore, in vitro non-biological dynamic dissolution methods based on physiological state of gastrointestinal tract have been constructed, including multi-compartment dissolution models, dissolution-absorption systems, and in vitro digestion models. These novel in vitro dissolution models could be supplements or substitutes of traditional dissolution models, so that researchers can comprehensively understand the drug dissolution behavior in vivo. This paper reviewed recent advances of non-compendial dissolution models, and summarized the applicable scopes and relative merits, aiming to provide a reference for the evaluation of dissolution degree of oral drugs.

Cite this article

ZHANG Ya-qi, TU Lu-ping, RAO Ze-peng, JIN He-xiang, WANG Wen-xi . In vitro dynamic dissolution models for oral drugs[J]. Chinese Journal of Pharmaceutical Analysis, 2023 , 43(3) : 366 -374 . DOI: 10.16155/j.0254-1793.2023.03.02

References

[1] 李伊娜, 张娜, 刘万卉, 等. 往复筒法在药物溶出度研究中的应用进展[J].药物分析杂志, 2021, 41(2):185
LI YN, ZHANG N, LIU WH, et al. Progress in applications of the reciprocating cylinder apparatus in dissolution testing of drug formulations[J].Chin J Pharm Anal, 2021, 41(2):185
[2] 张春晓, 彭玉帅, 许卉, 等. 流池法的研究进展及应用[J].药物分析杂志, 2021, 41(2):195
ZHANG CX, PENG YS, XU H, et al. Development and application of flow through cell method[J].Chin J Pharm Anal, 2021, 41(2):195
[3] O’FARRELL C, STAMATOPOULOS K, SIMMONS M, et al. In vitro models to evaluate ingestible devices: present status and current trends[J].Adv Drug Deliv Rev, 2021(178): 113924
[4] GRIGNARD E, TAYLOR R, MCALLISTER M, et al. Considerations for the development of in vitro dissolution tests to reduce or replace preclinical oral absorption studies[J].Eur J Pharm Sci, 2017, 99: 193
[5] MUDIE D M, STEWART A M, ROSALES J A, et al. Amorphous solid dispersion tablets overcome acalabrutinib pH effect in dogs[J].Pharmaceutics, 2021, 13(4):557
[6] LI C, YU W, WU P, et al. Current in vitro digestion systems for understanding food digestion in human upper gastrointestinal tract[J].Trends Food Sci Technol, 2020, 96: 114
[7] VATIER J, MALIKOVA-SEKERA E, VITRE MT, et al. An artificial stomach-duodenum model for the in vitro evaluation of antacids[J].Aliment Pharmacol Ther, 2007, 6(4):447
[8] CARINO SR, SPERRY DC, HAWLEY M. Relative bioavailability estimation of carbamazepine crystal forms using an artificial stomach-duodenum model[J].J Pharm Sci, 2006, 95(1):116
[9] CARINO SR, SPERRY DC, HAWLEY M. Relative bioavailability of three different solid forms of PNU-141659 as determined with the artificial stomach-duodenum model[J].J Pharm Sci, 2010, 99(9):3923
[10] LEE CM, LUNER PE, LOCKE K, et al. Application of an artificial stomach-duodenum reduced gastric pH dog model for formulation principle assessment and mechanistic performance understanding[J].J Pharm Sci, 2017, 106(8):1987
[11] BHATTACHAR SN, PERKINS EJ, TAN JS, et al. Effect of gastric pH on the pharmacokinetics of a BCS class Ⅱ compound in dogs: utilization of an artificial stomach and duodenum dissolution model and gastroplus,TM simulations to predict absorption[J].J Pharm Sci, 2011, 100(11):4756
[12] POLSTER CS, ATASSI F, WU SJ, et al. Use of artificial stomach-duodenum model for investigation of dosing fluid effect on clinical trial variability[J].Mol Pharm, 2010, 7(5):1533
[13] POLSTER CS, WU SJ, GUEORGUIEVA I, et al. Mechanism for enhanced absorption of a solid dispersion formulation of ly2300559 using the artificial stomach duodenum model[J].Mol Pharm, 2015, 12(4):1131
[14] 缪慧, 阮昊, 陈悦, 等. 生物相关性溶出度方法研究进展[J].中国现代应用药学, 2018, 35(1):138
MIU H, RUAN H, CHEN Y, et al. Research advances of bio-relevance dissolution method[J].Chin J Mod Appl Pharm, 2018, 35(1):138
[15] TAKEUCHI S, TSUME Y, AMIDON G E, et al. Evaluation of a three compartment in vitro gastrointestinal simulator dissolution apparatus to predict in vivo dissolution[J].J Pharm Sci, 2014, 103(11):3416
[16] HENS B, KATAOKA M, UEDA K, et al. Biopredictive in vitro testing methods to assess intestinal drug absorption from supersaturating dosage forms[J].J Drug Deliv Sci Technol, 2020, 56: 101275
[17] MUDIE DM, BUCHANAN S, STEWART AM, et al. A novel architecture for achieving high drug loading in amorphous spray dried dispersion tablets[J].Int J Pharm, 2020, 578: 100042
[18] TSUME Y, MATSUI K, SEARLS AL, et al. 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)[J].Eur J Pharm Sci, 2017, 102: 126
[19] MATSUI K, TSUME Y, AMIDON GE, et al. In vitro dissolution of fluconazole and dipyridamole in gastrointestinal simulator (GIS), predicting in vivo dissolution and drug-drug interaction caused by acid-reducing agents[J].Mol Pharm, 2015, 12(7):2418
[20] MATSUI K, TSUME Y, AMIDON GE, et al. The evaluation of in vitro drug dissolution of commercially available oral dosage forms for itraconazole in gastrointestinal simulator with biorelevant media[J].J Pharm Sci, 2016, 105(9):2804
[21] AMIDON GL, TSUME Y. Oral product input to the GI tract: GIS an oral product performance technology[J].Front Chem Sci Eng, 2017, 11(4):516
[22] GAN Y, ZHANG X, XU D, et al. Evaluating supersaturation in vitro and predicting its performance in vivo with biphasic gastrointestinal simulator: a case study of a BCS ⅡB drug[J].Int J Pharm, 2020, 578: 119043
[23] DOLUISIO JT, SWINTOSKY JV. Drug partitioning Ⅱ[J].J Pharm Sci, 1964, 53(6):597
[24] HEIGOLDT U, SOMMER F, DANIELS R, et al. Predicting in vivo absorption behavior of oral modified release dosage forms containing pH-dependent poorly soluble drugs using a novel pH-adjusted biphasic in vitro dissolution test[J].Eur J Pharm Biopharm, 2010, 76(1):105
[25] VANGANI S, LI X, ZHOU P, et al. Dissolution of poorly water-soluble drugs in biphasic media using USP 4 and fiber optic system[J].Clin Res Regul Aff, 2009, 26(1-2):8
[26] PESTIEAU A, EVRARD B. In vitro biphasic dissolution tests and their suitability for establishing in vitro-in vivo correlations: a historical review[J].Eur J Pharm Sci, 2017, 102: 203
[27] DENG J, STAUFENBIEL S, BODMEIER R. Evaluation of a biphasic in vitro dissolution test for estimating the bioavailability of carbamazepine polymorphic forms[J].Eur J Pharm Sci, 2017, 105: 64
[28] THIRY J, BROZE G, PESTIEAU A, et al. Investigation of a suitable in vitro dissolution test for itraconazole-based solid dispersions[J].Eur J Pharm Sci, 2016, 85: 94
[29] JANKOVIC S, O’DWYER PJ, BOX KJ, et al. Biphasic drug release testing coupled with diffusing wave spectroscopy for mechanistic understanding of solid dispersion performance[J].Eur J Pharm Sci, 2019, 137: 105001
[30] SARODE AL, WANG P, OBARA S, et al. Supersaturation, nucleation, and crystal growth during single-and biphasic dissolution of amorphous solid dispersions: polymer effects and implications for oral bioavailability enhancement of poorly water soluble drugs[J].Eur J Pharm Biopharm, 2014, 86(3):351
[31] XU H, KRAKOW S, SHI Y, et al. In vitro characterization of ritonavir formulations and correlation to in vivo performance in dogs[J].Eur J Pharm Sci, 2018, 115: 286
[32] GINSKI M. Prediction of dissolution-absorption relationships from a dissolution/Caco-2 system[J].Int J Pharm, 1999, 177(1):117
[33] MOTZ SA, SCHAEFER UF, BALBACH S, et al. Permeability assessment for solid oral drug formulations based on Caco-2 monolayer in combination with a flow through dissolution cell[J].Eur J Pharm Biopharm, 2007, 66(2):286
[34] LAMBERTI G, CASCONE S, IANNACCONE M, et al. In vitro simulation of drug intestinal absorption[J].Int J Pharm, 2012, 439(1-2):165
[35] HATE SS, REUTZEL-EDENS SM, TAYLOR LS. Absorptive dissolution testing of supersaturating systems: impact of absorptive sink conditions on solution phase behavior and mass transport[J].Mol Pharm, 2017, 14(11):4052
[36] HATE SS, REUTZEL-EDENS SM, TAYLOR LS. Insight into amorphous solid dispersion performance by coupled dissolution and membrane mass transfer measurements[J].Mol Pharm, 2019, 16(1):448
[37] ZHONG C, LANGRISH T. A comparison of different physical stomach models and an analysis of shear stresses and strains in these system[J].Food Res Int, 2020, 135: 109296
[38] SENSOY I. A review on the food digestion in the digestive tract and the used in vitro models[J].Curr Res Food Sci, 2021(4): 308
[39] MERCURI A, PASSALACQUA A, WICKHAM MSJ, et al. The effect of composition and gastric conditions on the self-emulsification process of ibuprofen-loaded self-emulsifying drug delivery systems: a microscopic and dynamic gastric model study[J].Pharm Res, 2011, 28(7):1540
[40] VARDAKOU M, MERCURI A, BARKER SA, et al. Achieving antral grinding forces in biorelevant in vitro models: comparing the usp dissolution apparatus Ⅱ and the dynamic gastric model with human in vivo data[J].AAPS Pharm Sci Tech, 2011, 12(2):620
[41] VARDAKOU M, MERCURI A, NAYLOR TA, et al. Predicting the human in vivo performance of different oral capsule shell types using a novel in vitro dynamic gastric model[J].Int J Pharm, 2011, 419(1-2):192
[42] MANN JC, PYGALL SR. A formulation case study comparing the dynamic gastric model with conventional dissolution methods[J].Dissol Technol, 2012, 19(4):14
[43] MASON LM, CHESSA S, HUATAN H, et al. Use of the dynamic gastric model as a tool for investigating fed and fasted sensitivities of low polymer content hydrophilic matrix formulations[J].Int J Pharm, 2016, 510(1):210
[44] ABRAHAMSSON B, PAL A, SJÖBERG M, et al. A novel in vitro and numerical analysis of shear-induced drug release from extended-release tablets in the fed stomach[J].Pharm Res, 2005, 22(8):1215
[45] GARBACZ G, WEDEMEYER RS, NAGEL S, et al. Irregular absorption profiles observed from diclofenac extended release tablets can be predicted using a dissolution test apparatus that mimics in vivo physical stresses[J].Eur J Pharm Biopharm, 2008, 70(2):421
[46] WEITSCHIES W, KOSCH O, MONNIKES H, et al. Magnetic marker monitoring: an application of biomagnetic measurement instrumentation and principles for the determination of the gastrointestinal behavior of magnetically marked solid dosage forms[J].Adv Drug Deliv Rev, 2005, 57(8):1210
[47] SCHNEIDER F, BEECK R, HOPPE M, et al. In vitro simulation of realistic gastric pressure profiles[J].Eur J Pharm Sci, 2017, 107: 71
[48] GARBACZ G, WEITSCHIES W. Investigation of dissolution behavior of diclofenac sodium extended release formulations under standard and biorelevant test conditions[J].Drug Dev Ind Pharm, 2010, 36(5):518
Outlines

/