FORMULATION AND IN-VIVO EVALUATION OF ACTARIT TABLETS USING CARBOXYMETHYL TAMARIND SEED GUM AND CYCLODEXTRIN NANOSPONGES

Abstract

Actarit tablets of interpenetrating polymer networks were prepared using carboxy methyl tamarind gum and cyclodextrin nanosponges for increasing oral bioavailability. Formulations with different carboxymethyl tamarind gum concentrations were freeze dried to create actarit-loaded interpenetration polymer networks, which were then analysed for drug loading equilibrium swelling and characterised using FTIR, DSC, and XRD. Actarit loaded IPN tablets were prepared and evaluated for in-vitro and in-vivo studies. The drug loading in the IPNs ranged from 59.36 to 65.72%, and swelling in the presence of 0.1N HCl in the IPNs was substantially lower (P 0.05) than in the presence of phosphate buffer pH 6.8. Studies using FTIR, DSC, and XRD confirmed that Actarit and IPNs formed a molecular combination. Actarit loaded IPN tablets' average weight, thickness, hardness, friability, and percentage of drug content were all within acceptable ranges. The drug release was highest for F3 (99.86%) and for marketed 98.67%. From in vivo bioavailability studies, the pure drug's Cmax was 404.34±12.87 ng/ml, significantly higher when compare with marketed product and optimized IPN actarit tablets of 385.21±9.43 and 342.76±13.56 ng/ml respectively. The Tmax of pure drug, marketed and optimized formulation were 1.5±0.05, 2.0±0.06 and 4.0±0.04 h respectively. The formulation of the marketed and optimized formulation exhibited a higher AUC0- ∞ (815±14.23 and 915±28.33 ng.h/ml) than the pure drug (800.76±15.76 ng.h/ml). The optimized tablet formulation showed a significantly higher AUC0-t and MRT than the pure drug and marketed product. The bioavailability of Actarit's cyclodextrin nanosponges based IPNs tablets were significantly improved when compared to the pure drug.