Evaluation of different in vitro dissolution tests based on level A in vitro–in vivo correlations for fenofibrate self-emulsifying lipid-based formulations

A Rational Design of a Biphasic Dissolution Setup—Modelling of Biorelevant Kinetics for a Ritonavir Hot-Melt Extruded Amorphous Solid Dispersion

“…A general purpose of the present study was to combine the advantages of a small-scale one-vessel method as a useful tool in formulation screening [13,14,34] and the proven biorelevance of the USP II and USP IV model [12,35,36]. All experiments were conducted in triplicate.…”

Developing Quantitative In Vitro–In Vivo Correlation for Fenofibrate Immediate-Release Formulations With the Biphasic Dissolution-Partition Test Method

“…4,5 Recently, the dissolution-partition systems, referred to as the biphasic test in this article, have been applied for characterization of both immediate-release and modified-release formulations. [6][7][8][9][10][11][12][13][14][15][16][17] The biphasic test involves both aqueous and organic phases and is designed to evaluate dissolution and precipitation of the drug formulations in aqueous phase under a nonsink condition accompanied by a simultaneous partition of the drug from the aqueous phase into the organic phase under a sink condition. The organic phase acts as an "absorptive compartment," and the amount of drug partitioned into this phase is dictated by the free drug concentration in the aqueous phase.…”

“…), discriminating capacity, and opportunity for in vitroein vivo relationship. [6][7][8][10][11][12][13][14][15][16] Amidon et al developed a mechanistic model to describe the drug transport phenomenon associated with the 2-phase dissolution system. 9 This approach assumes first-order absorption kinetics and a relatively high fraction absorbed in vivo (Fa).…”

Characterization of the Partition Rate of Ibuprofen Across the Water-Octanol Interface and the Influence of Common Pharmaceutical Excipients

“…Drug concentration-time profiles observed in both the aqueous and octanol phases from the biphasic test reflect an interplay among 3 kinetic processes including dissolution, precipitation, and partition, and may closely resemble the dissolution-absorption processes in vivo. [7][8][9][10][11] It is worth noting that, for several decades, the transfer of a drug molecule through the water-oil, in particular, the water-octanol (W/ O) interface has been adopted as a simple model for permeation of biological membranes. [12][13][14] Typically, the distribution coefficient, log D o/w , a ratio of the drug concentrations between octanol and water, is considered a highly important biopharmaceutical attribute of a drug, representing its driving forces for permeation into the biological membrane.…”

“…When designed properly, the rate of appearance of drug in the octanol phase is expected to be similar to the rate of absorption in vivo as illustrated by establishment of a level A in vitro and in vivo correlation. [7][8][9][10][11] It is highly desirable to quantitatively measure the partition rate of drugs and gain a fundamental understanding of the drug molecular attribute and the L-L interface resistance as a barrier. It would also be beneficial to obtain knowledge of the interfacial Figure 1.…”