DEVELOPMENT AND EVALUATION OF CANDESARTAN CILEXETIL TABLETS USING CRYSTAL AGGREGATES PREPARED BY POLYMER ENRICHED BRIDGING LIQUIDAbstract
The main objective of the study was to formulate tablets of Candesartan cilexetil using the crystal agglomerates for the enhancement in flow properties and solubility. The crystal agglomerates were prepared by polymer enriched bridging liquid (PEBL) technique. The process requires three solvent systems, the good solvent for the drug, the bad solvent and the bridging liquid. The hydrophilic polymer PVP K30 was incorporated in the bridging liquid. The addition of hydrophilic polymer increased the hydrophilicity and wettability of Candesartan cilexetil. The saturation solubility analysis, percentage yield, drug content, micromeritic properties, FTIR, DSC, XRD, SEM were carried out for the evaluation of crystal agglomerates. The tablets were prepared by direct compression using the formulated crystal agglomerates and were subjected to various in-vitro evaluations. The crystal agglomerates prepared by the PEBL technique showed 25 folds enhancement in the solubility. The FTIR analysis revealed the absence of incompatibility. The DSC analysis and XRD pattern showed a reduction in crystallinity. The SEM analysis revealed the porous and sphericity of the agglomerates. The tablets showed a hardness of 7 kg/cm2, friability (0.56%), weight variation (2.2%). The drug content found was 99.03% ± 0.33% and the disintegration time was 2 min. The tablets showed a % CDR of 99.99 ± 0.15 at the end of 30 min which was comparable with the marketed formulation. The release of pure drug observed was 28.08 ± 1.85 in 30 min. The PEBL technique provided a single step process for enhancing the flow characteristics, solubility and dissolution of Candesartan cilexetil for the development of Candesartan cilexetil tablets.
K. Manoj, P. Seenivasan *, K. Arul and M. S. Kumar
Faculty of Pharmacy, Sri Ramachandra Institute of Higher Education and Research, Porur, Tamil Nadu, India.
22 September 2019
11 November 2019
17 November 2019
01 December 2019