T. Ramchandar1*, J. Bhaskar2, V.L. Narasaiah3
1Dept. of Pharmaceutics, Mother Teresa college of Pharmacy, Ghatkesar, Hyderabad, Telangana India.
2Dept. of Pharmaceutics, Princeton Institute of Pharmaceutical Sciences, Hyderabad, Telangana, India.
3Dept. of Pharmaceutics, Dr Samuel George Institute of Pharmaceutical Sciences, Markapur, A.P, India.
A B S T R A C T
The main objective of this study was to formulate and evaluate the rapidly disintegrating technology makes tablets to disintegrate in the mouth without chewing and additional water intakes have drawn a great deal of attention. Rizatriptan benzoate is a potent anti-migraine drug with a bitter taste. Thus the taste has to be masked in order to reduce its bitterness, to increase its palatability and also to improve patient compliance. Therefore, attempts were undertaken to mask the bitter taste by using ion exchange resin Tulsion 339 and to formulate into RDT by adopting direct compression method by incorporating superdisintegrants Indion 234, CCS and SSG in various concentrations. The loading process was optimized for resin solubility, concentration, swelling, stirring and pH of loading solution and drug: resin ratio. The powder complex was evaluated for bulk density, angle of repose, drug release and drug-polymer complex’s interactions. Precompressional studies revealed good micromeritic properties of powder blend for direct compression. The hardness (2.8 to 3.6 kg/cm2), friability (0.42 to 0.66), weight variation (0.94 – 1.28%), drug content (98.32 to 99.82 %) and disintegration time (21-39 sec) were found uniform and reproducible for all formulations. The process variables played a vital role resulting in maximum drug loading. Tulsion 339 complex (1:1) with 40 min swelling time at pH 3, stirred for 150 min showed maximum drug loading. Optimized formulation (R4) containing Indion 234 exhibited quicker disintegration than CCS, SSG and were also found to be superior to marketed tablet with respect to disintegration and dissolution. Release was proportional to superdisintegrant concentration irrespective of polymer complex. Selected tablets were found stable and followed diffusion controlled first order kinetics. The results revealed that Rizatriptan benzoate was successfully taste masked and formulated into a RDT as an alternative method to conventional tablets.
Keywords: Tulsion, Indion, Rapid-disintegrating tablets, Rizatriptan benzoate, Superdisintegrants