Solubility enhancement of rosiglitazone by using melt sonocrystallization technique

Abstract

The poor solubility and low dissolution rate in gastro-intestinal fluid, especially for class-II drugs according to Biopharmaceutics Classification System (BCS) the bioavailability enhanced by increasing the solubility and dissolution rate. A novel melt sonocrystallization technique of particle engineering to enhance solubility as well as dissolution of hydrophobic drug and to study its effect on crystal properties of drug. The present study leads to use investigate solubility of melt sonocrystallization technique to modify the undesirable properties of Rosiglitazone is antidiabetic drug in thiozolidione category with (BCS II) to forms agglomerates with number of shallow circular pits on the surface leads to increase solubility. Melt sonocrystallization process was developed for Rosiglitazone in which Rosiglitazone melt was poured in deionized water and simultaneously subjected to ultrasonic energy for 20min at amplitude 80%. The product obtained was evaluated using scanning electron microscopy, differential scanning calorimetry, X-ray powder diffractometry (XPRD), Fourier transformed infrared spectroscopy (FTIR), solubility and dissolution rate. The irregular agglomerates with porous surface were obtained having different crystal habit which increases solubility and dissolution rate. FTIR shows thermal behavior of untreated Rosiglitazone and treated Rosiglitazone have no significant difference low intensity peaks in XPRD of treated Rosiglitazone were noticed crystals habit changes and lattice defects during processing have causes favorable changes in the physicochemical properties of Rosiglitazone. The use of melt sonocrystallization technique is promising technique that may affords powder with improved flow as well as improved solubility and dissolution.