Optimization of Dissolution Compartments in a Biorelevant Dissolution Apparatus Golem v2, Supported by Multivariate Analysis

Abstract

Biorelevant dissolution instruments represent an important tool for pharmaceutical research and development. These instruments are designed to simulate the dissolution of drug formulations in conditions most closely mimicking the gastrointestinal tract. In this work, we focused on the optimization of dissolution compartments/vessels for an updated version of the biorelevant dissolution apparatus—Golem v2. We designed eight compartments of uniform size but different inner geometry. The dissolution performance of the compartments was tested using immediate release caffeine tablets and evaluated by standard statistical methods and principal component analysis. Based on two phases of dissolution testing (using 250 and 100 mL of dissolution medium), we selected two compartment types yielding the highest measurement reproducibility. We also confirmed a statistically ssignificant effect of agitation rate and dissolution volume on the extent of drug dissolved and measurement reproducibility.

Exploration of Neusilin® US2 as an Acceptable Filler in HPMC Matrix Systems—Comparison of Pharmacopoeial and Dynamic Biorelevant Dissolution Study

“…It consists of a heated plate, where the following four compartments are placed: stomach, duodenum, jejunum, and ileum. Each compartment is made from two-layer (polyolefin/polyamide) intravenous bags (Baxter Viaflo, Baxter Healthcare Ltd., Thetford, UK) that were modified by welding to provide a specific inner geometry and incorporated a pH probe [26]. Compartments are connected through peristaltic pumps, which enable the movement of predetermined volumes between consecutive compartments.…”

“…Other measurement conditions were as follows: a flow rate of 1.5 mL/min, an injection volume of 10 µL, and a column temperature of 40 • C. The spectra were recorded in the wavelength range between 190 and 400 nm. The chromatogram was acquired at 294 nm [26].…”

“…The spectra were recorded in the wavelength range between 190 and 400 nm. The chromatogram was acquired at 294 nm [26]. on a template created explicitly for Golem v2 software.…”

An In Vitro Dissolution Method for Testing Extended-Release Tablets Under Mechanical Compression and Sample Friction

“…Recently, scientists have developed several non-compendial dissolution methods for drug release and dissolution that try to mimic GI physiological conditions. 4,[6][7][8][9][10][11][12][13][14][15][16][17][18][19][20][21] The mechanical compression force (the grinding or crushing of the GI contents), the friction between formulation, food and the GI wall resulting from antral contractions may impact the drug release mechanism from ER formulations. 22 Some non-compendial apparatuses that apply an external stress to the dosage form have been used to explore the impact of contractile forces during transit along the GI tract.…”