Diabetes and Obesity Drug Discovery & Therapy (Track)
FORMULATION AND IN VITRO, IN VIVO EVALUATION OF SPHERICAL AGGLOMERATES OF PIOGLITAZONE HYDROCHLORIDE WITH β CYCLODEXTRIN
Sachinkumar Patil, Shitalkumar Patil and Sunitkumar Sahoo
PAshokarao Mane College of Pharmacy, Pethvadgaon, Maharashtra, 416112, India.
Present work deals with preparation and evaluation of spherical agglomerates of Pioglitazone hydrochloride (PGH) with improved physicochemical properties. The use of spherical crystallization technique appears to be efficient alternative for obtaining suitable particles for direct compression for drugs having compressibility problems.
PGH plane agglomerates and agglomerates with β cyclodextrin (β-CD) [1% and 2%] were prepared by emulsion solvent diffusion method using methanol, chloroform and water as good solvent, bridging liquid and poor solvent respectively. Prepared agglomerates were evaluated for micromeritics properties, flowability, compactibility, packability, solubility, in vitro drug release and in vivo bioavailability. Also drug and agglomerates were characterized by X-ray powder diffraction, differential scanning calorimetry and fourier transforms infrared spectroscopy.
Flowability, compactibility and packability were dramatically improved for all agglomerates compared with raw crystals of PGH, resulting in successful direct tabletting without capping. These improved properties of spherically agglomerated crystals were due to their large and spherical shape and enhanced fragmentation during compaction well supported less elastic recovery of its compact. Also agglomerates comparative enhancement in solubility, dissolution and bioavailability has shown their improved wettability. X-ray powder diffraction and differential scanning calorimetry study were indicated polymorphic transition of PGH from form II to I during recrystallization but not associated with chemical transition indicated by fourier transforms infrared spectra. No significant difference was observed in all properties of agglomerates with different concentration of β-CD.