Design and Development of Crystallo-co-agglomerates of Ritonavir for the Improvement of Physicochemical Properties

[摘要] Objectives: The aim of the present study was to obtain CCA of ritonavir to improve the solubility, dissolution rate, and other physicochemical properties. Materials and Methods: Ritonavir agglomerates were prepared using the CCA technique. Acetone-water containing HPMC K-15, PEG-6000, PVP K-30 was used as the crystallization medium. The agglomerates were evaluated for saturation solubility, micromeritic properties, yield, and drug content. The agglomerates were also characterized using FTIR, DSC, XRPD and SEM. Results: The growth of particle size and the spherical form of the agglomerates resulted in the formation of products with good flow and packing properties. The improved compaction properties of the agglomerated crystals were due to the fragmentation that occurred during compression. DSC and XRD studies showed that ritonavir particles crystallized in the presence of HPMC, PEG-6000, PVP K-30 and diluents did not undergo structural modifications. The solubility and dissolution rate of ritonavir agglomerates were improve compare to pure ritonavir.Conclusion: CCA was successfully applied to improve the physicochemical properties of ritonavir.

[关键词] Crystallo-co-agglomeration;solubility;dissolution;ritonavir