Dissolution of poorly water-soluble drugs in biphasic media using USP 4 and fiber optic system

Evolution of a mini-scale biphasic dissolution model: Impact of model parameters on partitioning of dissolved API and modelling of in vivo-relevant kinetics

“…Mudie et al [11] illustrated that rotation speeds higher than 75 rpm should be avoided causing a vortex in the dissolution vessel. Paddle speeds less than 60 rpm, however, generated insufficient hydrodynamics [13]. Therefore, in agreement with our results, the optimal rotation speed of 75 rpm for establishing IVIVC with human models was reported by Shi et al [24].…”

“…All experiments with the dual paddle showed that the interface between the aqueous and the octanol phase was robust for this model. A second adjustable paddle was used by Vangani et al [13]. In their proposed model setup the smaller octanol paddle was mounted perpendicular to the regular paddle to guarantee sufficient hydrodynamics.…”

“…Various biphasic dissolution models are described in the literature [10][11][12] which are regarded as advantageous as they implement sink conditions by introducing a partitioning process of the non-protonated base into a second lipophilic phase [13]. The implementation of a lipophilic phase mimics the absorption step, which is an alternative process to precipitation of a weak base at elevated pH in the GIT, showing superior predictive power for APIs with dissolution-limited absorption [14].…”

Toward Biorelevant Dissolution: Application of a Biphasic Dissolution Model as a Discriminating Tool for HPMC Matrices Containing a Model BCS Class II Drug

“…In accordance with this, water and octanol were selected as the aqueous and organic solvents used in the biphasic dissolution medium throughout this study, respectively. It should be noted that previous studies have reported biphasic media comprising a variety of alternative aqueous (SIF, HCl, SDS, and sodium phosphate-buffered water) and organic (chloroform, ethyl acetate, cyclohexene/octanol, and nonanol/octanol) solvents (34)(35)(36)(37)(38)(39)(40)(41).…”

“…There are several examples of the use of a biphasic dissolution system as a means of maintaining sink conditions, some of which look at CR formulations of poorly soluble drugs (34)(35)(36)(37)(38)(39)(40)(41). However, there does not appear to be any example illustrating the use of a biphasic dissolution model to discriminate between CR formulations designed to release the API with different rates based on the matrix polymer content.…”