Design, Development, Optimization and Evaluation of Ranolazine Extended Release Tablets

The objective of the current study was to develop an extended release (XR) tablet formulation for ranolazine using Eudragit L 100-55 and hydroxypropylmethylcellulose (HPMC) K100M in an appropriate composition. Ranolazine, an anti-anginal agent, is mainly used for treating chronic stable angina pectoris. The main advantage of this drug that it exhibits anti-ischemic effect, which was not influenced by either blood pressure or heart rate.

XR tablets of ranolazine were prepared using variable amounts of Eudragit L 100-55 and HPMC K100M in various proportions as per 3² factorial design by direct compression technique. The amount of polymers with desired sustained drug release was labeled as factors. On other hand, time taken for drug dissolution was labeled as responses (t_10%, t_50%, t_75%, t_90%).

Nine formulations were obtained as per design, developed, and evaluated for quality control parameters. The obtained results clear that all formulations pass the compendial limits. Data obtained from the dissolution study fitted well to kinetic modeling and kinetic parameters were determined. Polynomial equations were derived for responses and checked for validity.

RF₅ composed of 31.25 mg of Eudragit L 100-55 and 31.25 mg of HPMC K100M, is the best formulation showing similarity f₂: 85.78, f₁: 2.32 with the marketed product (RANEXA). Formulation RF₅ follows zero order, whereas the release mechanism was found to be non-fickian type (n= 0.65).