Dissolution-Hollow Fiber Membrane (D-HFM) System to Anticipate Biopharmaceutics Risk of Tablets and Capsules

A dissolution-hollow fiber membrane (D-HFM) system with relatively high area/volume ratio was previously characterized and showed favorably high percent drug absorption. Also, it's in vitro permeation constant (K0p) was close to in vivo human permeation constant (kp). The objective of the current study was to predict the in vivo human absorption profile and biopharmaceutic performance of five drug products using the D-HFM system. Four immediate-release (IR) and one extended-release (ER) solid oral dosage form were sub-jected to the D-HFM system. Tablets and capsule dissolution were also measured using USP apparatus II. Drug solutions were also subjected to D-HFM testing. Predicted and observed absorption profiles in D-HFM system showed close agreement for each solid oral dosage form. Levy-Polli plots from D-HFM system suc-cessfully predicted the four IR products to be low biopharmaceutic risk due to permeation rate limited or mixed dissolution/permeation rate limited absorption, and successfully predicted metoprolol ER product to be high biopharmaceutic risk due to dissolution rate limited absorption. These observations showed poten-tial of the in vitro D-HFM system to be utilized in biopharmaceutics risk assessment of in vivo tablet and cap-sule performance. (c) 2022 The Authors. Published by Elsevier Inc. on behalf of American Pharmacists Association. This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/)

Automated summary

The study successfully predicted the in vivo absorption profile and biopharmaceutic performance of five drug products using a dissolution-hollow fiber membrane (D-HFM) system. The results demonstrated the potential of the D-HFM system in accurately predicting the absorption characteristics of solid oral dosage forms and assessing their biopharmaceutic risk.