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

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.

Atazanavir sulphate is a drug used for treatment of AIDS in which the patients are infected with HIV. Presently, it is available as a capsule. The amount of the drug reaching the blood after oral delivery is less due to the poor solubility of the drug. Compared with capsules, tablets are more preferred dosage forms due to its ease of manufacturing and tamper proof nature. In the present research work, we have developed a tablet formulation of the drug, which has improved solubility. The higher solubility leads to greater absorption after oral delivery. Thus the formulation is beneficial to the patients as the dose can be reduced and the treatment can be made more economic.