Spherical crystal agglomeration technique for improved flow properties and oral bioavailability of atazanavir sulphate.

Abstract

Aim: The current research focused on formulation of spherical crystal agglomerates (SCA) of atazanavir sulphatefor improving flow property and solubility. Materials & methods: SCA were formulated by quasi-emulsification solvent diffusion. Methanol, water and dichloromethane were employed as a good solvent, bad solvent and bridging liquid respectively. Results & conclusion: SCA with improved solubility and micromeritic properties were directly compressed into a tablet. The SCA tablets had higher dissolution rates compared with plain drug and marketed product. Invivo pharmacokinetic studies revealed higher Cmax and AUC0-t of the SCA than marketed product with relative bioavailability of 1.74. The formulation was stable for more than 3months, with insignificant difference in % drug content and % drug dissolution.