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INFLUENCE OF PROCESS PARAMETERS ON COMPRESSIBILITY, SOLUBILITY AND RELEASE CHARACTERISTICS OF MELT SONOCRYSTALLIZED FENOFIBRATE

SACHINKUMAR PATIL^*, SHITALKUMAR PATIL, GEETA KAVATHEKAR

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The aim of the present study was to investigate the suitability of the melt sonocrystallization (MSC) technique in order to modify the processability properties along with solubility and drug release of anti-hyperlipidemic drug fenofibrate (FNO) as a Biopharmaceutical Classification System (BCS) Class II drug candidate. Melted sonocrystallized fenofibrate agglomerates (MSC-FNO) were prepared by probe ultrasonicator by varying the sonication time (1, 2 and 3 min) and the level of amplitude (60, 70 and 80%) by 32 factorial design. Stable MSC-FNO agglomerates were successfully prepared with an adequate percentage yield and drug content, having porous surface and different crystal habits such as needles, plates, and some hollow tubes. MSC-FNO has shown improved micrometric properties consequently compressibility and flowability than FNO. Also MSC-FNO has shown an increase in the solubility and the drug release may be due to formation of porous agglomerates witnessed in Scanning Electron Microscopic photographs. These results were well supported by Differential Scanning Calorimetry and X-ray Powder Diffraction (XRPD), which has indicated the decrease in drug crystallinity. As sonication time and amplitude increased, MSC-FNO properties were proportionally improved. Study of Fourier Transform Infrared Spectroscopy revealed that no chemical transition of FNO has occurred during MSC. Thus MSC is a promising cost-effective technique that may give a powder with improved required processability properties with better improvement in solubility and drug release much needed for BCS class II drugs.