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

Prediction of the Oral Pharmacokinetics and Food Effects of Gabapentin Enacarbil Extended-Release Tablets Using Biorelevant Dissolution Tests

“…The experimental conditions in the dissolution test, including the dip rate, flow rate, and duration for each dissolution medium, were slightly modified from those of previous reports, [8][9][10] which were used to predict the in vivo performance of nifedipine ER tablets, two prototypes of colon-targeting tablets containing caffeine, and the diclofenac sodium oral modified-release pellet dosage form. In the present study, the hydrodynamic forces in these apparatuses had little effect on the dissolution rate of the drug up to a 1.7-fold dip rate and 2-fold flow rate (data not shown), while the paddle revolution rate strongly affected the dissolution profiles of the drug product.…”

“…The detailed experimental procedures were performed according to previously reported methods. [8][9][10] However, FeSSCoF, instead of FaSSCoF (Fasted State Simulated Colonic Fluid), was used as a colonic biorelevant medium for dissolution testing under both the fasted and fed states because the FaSSCoF medium was designed from human colonic contents after using bowel cleansing agent. 16) We therefore concluded that it was reasonable to use FeSSCoF under the standard fasting condition in clinical trials.…”

“…The detailed experimental procedures were performed according to previously reported methods. [8][9][10] The dissolution tests were performed using an open-loop configuration with manual sample collection. For the fasted state, samples were taken at 20, 40, 60, 75, 90, 120, 165, 210, 240, 285, 320, 370, 420 and 480 min.…”

“…Fotaki et al 7) reported the importance of in vitro hydrodynamics when using the dissolution apparatus 2 (paddle), 3 and 4 to determine the IVIVC of two monolithic ER products, a hydrophilic matrix formulation containing carbomer and an osmotic pump formulation. Andreas et al 8) developed in vitro biorelevant test setups by using the USP dissolution apparatus 3 and 4 to predict the food effects of several ER formulations of 5-aminosalicylic acid which were pH-dependent coating formulations, a Multi-Matrix system, and ethylcellulosecoated microgranules. Further, Andreas et al 9,10) predicted the food effects of two nifedipine ER formulations (an osmotic pump and a matrix-type coat-core) and ER zolpidem (Ambien ® CR).…”

Potential prediction of formulation performance in paediatric patients using biopharmaceutical tools and simulation of clinically relevant administration scenarios of nifedipine and lorazepam

“…During recent decades, the purpose of dissolution testing of drugs has expanded from pure quality control to prediction of in vivo drug performance and identifying potential bioavailability problems of pharmaceutical formulations. With development of biorelevant dissolution media (reflecting the main properties of gastrointestinal [GI] fluids), simulation of GI residence times, and simulation of GI hydrodynamics, successful in vitro–in vivo relations and correlations (IVIVRs/IVIVCs) have been established for oral immediate and modified release formulations in adults, using compendial dissolution apparatus . Furthermore, in vitro dissolution data are used as input in physiologically based pharmacokinetic (PBPK) prediction models in which different factors influencing drug absorption are integrated.…”