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An In Vitro Dissolution Determination of Multi-Index Components in Tibetan Medicine Rhodiola Granules
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Investigation of a suitable in vitro dissolution test for itraconazole-based solid dispersions
Justine Thiry1, Guy Broze2, Aude Pestieau1
1Laboratory of Pharmaceutical Technology and Biopharmacy, Department of Pharmacy, Center for Interdisciplinary Research on Medicines (CIRM), University of Liege, 4000, Liege, Belgium.
Summary
Finding effective in vitro dissolution tests for amorphous solid dispersions is challenging. Excipient interactions significantly impact drug release, complicating in vivo behavior prediction for poorly soluble drugs like itraconazole.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Physical Pharmacy
Background:
- Evaluating poorly soluble drugs in vitro is difficult.
- Amorphous solid dispersions enhance drug solubility but pose formulation challenges.
- It is crucial to develop relevant dissolution tests for these advanced formulations.
Purpose of the Study:
- To investigate the in vitro dissolution behavior of itraconazole amorphous solid dispersions.
- To compare the performance of a marketed product (Sporanox®) with a hot-melt extruded formulation (Soluplus®/ITZ).
- To identify the impact of dissolution media and excipient interactions on drug release.
Main Methods:
- Tested three itraconazole formulations (Sporanox®, Soluplus®/ITZ extrudates, crystalline ITZ) in seven USP apparatus conditions.
- Utilized disintegration, dynamic light scattering, and nuclear magnetic resonance.
- Analyzed drug release profiles in various dissolution media (sink, non-sink, biphasic, simulated gastric).
Main Results:
- Amorphous solid dispersions showed variable release profiles dependent on the dissolution medium.
- Extrudates performed better in non-sink and biphasic conditions; Sporanox® excelled in sink and simulated gastric conditions.
- Excipient interactions (surfactants, Soluplus®) and micelle formation influenced drug release and matrix erosion.
Conclusions:
- Standard in vitro dissolution tests are insufficient for predicting the in vivo performance of amorphous solid dispersions.
- Excipient-drug and excipient-excipient interactions significantly complicate dissolution testing.
- Further research is needed to develop more predictive dissolution methodologies for complex formulations.
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