Related Experiment Video
Updated: Jul 24, 2025
A Package of Established Analytical Tools to Investigate the Solid-State Alteration of Lipid-Based Excipients
Published on: August 9, 2022
In vitro dissolution/permeation tools for amorphous solid dispersions bioavailability forecasting I: Experimental
Patrícia D Nunes1, João F Pinto2, Annette Bauer-Brandl3
1R&D Analytical Development, Hovione Farmaciência S.A., Campus do Lumiar, Building S, 1649-038 Lisboa, Portugal; R&D Oral Drug Product Development, Hovione Farmaciência S.A., Campus do Lumiar, Building S, 1649-038 Lisboa, Portugal; Research Institute for Medicines (iMed.Ulisboa), Faculty of Pharmacy, Universidade de Lisboa, 1649-003 Lisboa, Portugal.
This study optimized a dissolution/permeation assay for predicting drug bioavailability. The new method accurately forecasts how drug formulations perform in vivo, aiding in early drug development.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery
- Biopharmaceutics
Background:
- Accurate in vitro bioavailability forecasting is crucial for drug product development.
- Dissolution/permeation (D/P) systems offer a cost-effective method for predicting passive diffusion absorption, common for new chemical entities (NCEs).
Purpose of the Study:
- To establish and optimize a PermeaLoop™-based D/P assay for simultaneous drug release and permeation evaluation.
- To develop a standardized approach for predicting the bioavailability of poorly soluble, weakly basic drug formulations.
Main Methods:
- Screening of donor/acceptor media and permeation barriers (PermeaPad®, PermeaPlain®).
- Evaluation of solubilizers (Sodium Dodecyl Sulfate, Vitamin E-TPGS, hydroxypropyl-β-cyclodextrin) in the acceptor medium.
- Optimization of Itraconazole (ITZ) dose, selecting 100 mg for comparability with in vivo studies.
Main Results:
- Optimized method conditions for simultaneous drug release and permeation assessment.
- Identified suitable solubilizers and media for the assay.
- Established a standardized 100 mg Itraconazole dose for future comparative studies.
Conclusions:
- A standardized dissolution/permeation assay was successfully developed and optimized.
- This assay strengthens the in vitro analytical portfolio for pre-clinical drug product development.
- The method aids in predicting the bioavailability of challenging drug formulations.
More Related Videos
Related Concept Videos
01:27Factors Influencing Drug Absorption: Drug Dissolution
01:20Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry
01:21Factors Affecting Dissolution: Drug pKa, Lipophilicity and GI pH
A drug's pKa and the pH of the gastrointestinal (GI) tract play crucial roles...
01:15Theories of Dissolution: Diffusion Layer Model
This process starts with a thin layer, saturated with the drug, forming at the interface between the solid and liquid. The solute then diffuses from this layer into the main solution. The Noyes-Whitney equation suggests that the rate of dissolution relies on the diffusion...
01:16Methods for Studying Drug Absorption: In vitro
The diffusion cell method uses a two-compartment cell, including a donor compartment with the drug solution, which simulates the environment where the drug is applied, and a receptor compartment with a buffer solution, which simulates the environment...
01:09Methods for Studying Drug Absorption: In situ
The Doluisio method involves perfusing a prepared segment of a rat's small intestine with a solution of radiolabeled drug and a non-absorbable marker. This helps to differentiate between absorbed and non-absorbed drug concentrations. The intestinal segment is connected at both ends using tubing and syringes,...