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Published on: December 9, 2010
Spherical crystal agglomeration technique for improved flow properties and oral bioavailability of atazanavir
Darpan Shah1, Jatin Rawat1, Hetal Thakkar1
1Center for Post-Graduate Studies & Research in Pharmaceutical Sciences, Shri GH Patel Pharmacy building, Faculty of Pharmacy, The Maharaja Sayajirao University of Baroda, Vadodara, Gujarat, 390002, India.
Abstract:
Aim: The current research focused on formulation of spherical crystal agglomerates (SCA) of atazanavir sulphate for 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. In vivo 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 3 months, with insignificant difference in % drug content and % drug dissolution.
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