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Carbopol®-crospovidone interpolymer complex for pH-dependent desloratadine release
1Gedeon Richter Plc., Formulation R&D, Gyömrői Str. 19-21., 1103 Budapest, Hungary.
Journal of Pharmaceutical and Biomedical Analysis
|February 22, 2016
Summary
This study explores how drug molecule state affects release from polymer complexes. Desloratadine release was immediate at acidic pH but suppressed at higher pH due to interactions within the Carbopol-polyvinylpyrrolidone complex.
Area of Science:
- Polymer Science
- Pharmaceutical Sciences
- Drug Delivery Systems
Background:
- Hydrogen-bonded interpolymer complexes are formed by interactions between polymers.
- Drug molecules can intercalate into these complexes, influencing release patterns.
- Few studies have focused on the specific drug molecule state's impact on release.
Purpose of the Study:
- To investigate the dissolution and release profiles of desloratadine incorporated into a Carbopol-polyvinylpyrrolidone (PVP) complex.
- To understand the mediating interactions at different pH values.
- To elucidate the role of the drug molecule's state in its release mechanism.
Main Methods:
- Preparation of a Carbopol-PVP complex incorporating desloratadine using a novel method.
- Investigation of dissolution and release profiles at various pH values.
- Analysis of drug-polymer interactions influencing release.
Main Results:
- Desloratadine exhibited immediate release at acidic pH, indicating minimal dissolution retarding effect from the polymer complex.
- The protonated state of desloratadine at acidic pH enhanced its detachment and dissolution.
- Higher pH values suppressed desloratadine dissolution significantly, suggesting complex interactions.
Conclusions:
- Drug molecule state, particularly its protonation, critically influences release from polymer complexes.
- Hydrogen bonding interactions between the drug and polymer components play a significant role in modulating release.
- Understanding these pH-dependent interactions is crucial for designing effective drug delivery systems.
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