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Role of Cyclodextrins and Drug Solid State Properties on Flufenamic Acid Dissolution Performance from Tablets.
Francesca Maestrelli1, Marzia Cirri1, Enrico De Luca1
1Department of Chemistry "U. Schiff", University of Florence, Via Schiff 6, Sesto Fiorentino, 50019 Florence, Italy.
Pharmaceutics
|February 26, 2022
Summary
Flufenamic acid (FFA) solubility and dissolution issues were overcome using randomly methylated-β-cyclodextrin (RAMEB) complexation. This resulted in reproducible tablet dissolution, independent of the drug supplier.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Physical Pharmacy
Background:
- Flufenamic acid (FFA), a non-steroidal anti-inflammatory drug, exhibits poor solubility and variable dissolution rates, leading to bio-inequivalence.
- Variations in FFA powder characteristics from different suppliers impact its dissolution behavior in solid dosage forms.
Purpose of the Study:
- To enhance the solubility and dissolution rate of flufenamic acid (FFA).
- To develop an effective and reproducible tablet formulation for FFA using direct compression.
- To mitigate issues related to FFA batch variability and supplier differences.
Main Methods:
- Screening of various cyclodextrins (CDs) including randomly methylated-β-cyclodextrin (RAMEB) for complexation with FFA.
- Utilizing different techniques, such as grinding, to prepare binary drug-CD systems.
- Formulating conventional and immediate-release tablets via direct compression using the optimized FFA-RAMEB system.
- Comprehensive characterization of the prepared tablets for technological properties and dissolution performance.
Main Results:
- The grinding technique with RAMEB was the most effective method, achieving complete amorphization of FFA.
- Significant improvement in FFA dissolution rate was observed with the FFA-RAMEB system.
- Tablets formulated with the FFA-RAMEB complex exhibited improved and highly reproducible dissolution profiles.
- The dissolution performance of the formulated tablets was independent of the original FFA supplier, overcoming batch variability.
Conclusions:
- Complexation with RAMEB, particularly via grinding, effectively enhances FFA solubility and dissolution.
- Direct compression of FFA-RAMEB complexes yields robust and reproducible immediate-release and conventional tablets.
- The developed formulation strategy successfully addresses the bio-inequivalence issues associated with FFA by ensuring consistent drug release.
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