Enhancing Solubility of a BCS Class II Drug- Itraconazole by Developing and Optimizing Solid Lipid Nanoparticles using a Central Composite Design.

Background: Itraconazole (ICZ) has been approved by the FDA to treat many fungal infections including, blastomycosis, histoplasmosis, and aspergillosis. ICZ can be also used as prophylaxis in the population who are at high risk for developing systemic fungal infections, such as HIV patients, and chemotherapy patients.

Aim: However, since ICZ is a BCS Class II drug that has low solubility and high permeability, leads to low oral bioavailability.

Strategizing Spray Drying Process Optimization for the Manufacture of Redispersible Indomethacin Nanoparticles Using Quality-by-Design Principles.

The present study adopted a Quality by Design (QbD) approach to spray dry indomethacin nanosuspension (IMC-NS) consisting of HPC-SL, poloxamer 407, and lactose monohydrate. The Box-Behnken Design was used to systematically evaluate the effects of inlet temperature, aspiration rate, and feed rate on the critical quality attributes (CQAs) [redispersibility index (RDI; minimize), % yield (maximize), and % release at 15 min (maximize)] of the indomethacin spray dried nanosuspension (IMC-SD-NS). To identify significant main and quadratic effects, two-way interactions, and create a predictive model for the spray drying process, regression analysis and ANOVA were utilized.

4-Hy-droxy-6-(4-meth-oxy-phen-yl)-4-phenyl-1,3-diazinane-2-thione.

In the title compound, C(17)H(18)N(2)O(2)S, the 1,3-diazinane-2-thione ring system is not coplanar with the benzene ring and meth-oxy-phenyl ring system, the dihedral angle between the planes being 65.58 (13) and 89.18 (10)°, respectively.