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New Sodium Mefenamate - Nicotinamide Multicomponent Crystal Development to Modulate Solubility and Dissolution:
Ilma Nugrahani1, Felicia Fisandra1, Ayano Horikawa2
1School of Pharmacy, Bandung Institute of Technology, Indonesia.
Journal of Pharmaceutical Sciences
|June 6, 2021
Summary
New sodium mefenamate (SM) - nicotinamide (NA) salt cocrystals (SMN) were developed. The SMN hemihydrate demonstrated superior solubility and dissolution properties, indicating potential for improved drug formulation.
Area of Science:
- Pharmaceutical Science
- Crystal Engineering
- Materials Science
Background:
- Mefenamic acid (MA) solubility is limited, and while MA-nicotinamide (NA) cocrystals improve it, they don't surpass sodium mefenamate (SM) solubility.
- Development of novel solid forms is crucial for enhancing the bioavailability of poorly soluble drugs like MA.
Purpose of the Study:
- To synthesize and characterize novel salt cocrystals of sodium mefenamate (SM) and nicotinamide (NA).
- To evaluate the pharmaceutical properties, including solubility and dissolution, of the newly formed SM-NA salt cocrystals.
Main Methods:
- Cocrystal screening using solvent drop grinding and slow evaporation techniques.
- Single crystal X-ray diffraction for structural analysis.
- Investigation of hydrate stability, solubility, and intrinsic dissolution rates.
Main Results:
- Two new SM-NA salt cocrystals were successfully prepared as hemihydrate (SMN-HH) and monohydrate (SMN-MH).
- SMN-MH transformed into the more stable SMN-HH under ambient conditions.
- Both SMN-HH and SMN-MH exhibited enhanced solubility and intrinsic dissolution compared to SM, with SMN-HH showing superior performance.
Conclusions:
- SM-NA salt cocrystals effectively combine the benefits of salt formation and cocrystallization.
- The SMN-HH form presents significant potential for developing improved dosage forms of mefenamic acid due to its enhanced solubility and dissolution characteristics.
Keywords:
HydrateIntrinsic dissolutionMulticomponent crystalNicotinamideSalt cocrystalSodium mefenamateSolubilityStabilityMore Related Videos
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