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Development of extended release matrix tablets of Ranolazine containing polyacrylic and ethylcellulose polymers | Abstract
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Abstract

Development of extended release matrix tablets of Ranolazine containing polyacrylic and ethylcellulose polymers

Author(s): Jagdish Bidada, Indrajeet Gonjari, Akshay Bhusari, Chandrakant Raut, Amar Dhule

Ranolazine is an anti-anginal drug with extensive and highly variable hepatic first pass metabolism following oral administration, with systemic bio-availability of 76% and ranolazine also has a relatively short plasma half-life of 2.5+0.5 hours. Ranolazine, used in management therapy of anginal disorders, has been incorporated into monolithic matrices whose excipients were mixtures at different ratios of a acrylic resin (Carbopol 971 P) hydrophilic & pHdependent nature and an ethylcellulose (Ethocel N20/N50), water-insoluble and pH-independent polymers. Technological characterization (drug particle morphology, mean weight, diameter, thickness, hardness and friability of tablets) was carried out and in vitro drug release behaviour was measured using the USP Type II (Paddle) apparatus. The effect of varying the Carbopol– Ethocel ratio, as well as the drug–polymeric matrix ratio, was evaluated by simple factorial design using two independent factors. The results showed the suitability of Carbopol–Ethocel mixtures as matrix-forming material for ranolazine Extended release formulations. Combination of the swelling properties of Carbopol 971 P with the plastic properties of the more hydrophobic Ethocel N20/N50 allowed suitable modulation of ranolazine release. Mathematical analysis of the release kinetics indicated that the nature of drug release from the matrix tablets was dependent on drug diffusion and polymer relaxation and therefore followed non-Fickian or anomalous release. The developed extended release matrix tablets of Ranolazine prepared with monolithic matrices release up to 12 hours. The factorial study indicates a good correlation coefficient (0.98317). The effect was dependent on both the independent factors of hydrophilic and hydrophilic polymer.