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

Turkish Journal of Pharmaceutical Sciences

article

Raghavendra Kumar GUNDA¹  Prasada Rao MANCHINENI²  Dhachinamoorthi DURAISWAMY³  Koteswara Rao GSN⁴ 

[1] Vignan’s Foundation for Science, Technology and Research ,(Deemed to be University), Faculty of Pharmacy, Department of Pharmaceutical Sciences;M.A.M College of Pharmacy, Department of Pharmaceutical Analysis;QIS College of Pharmacy, Department of Pharmaceutics;KL College of Pharmacy, Koneru Lakshmaiah Education Foundation ,(Deemed to be University), Department of Pharmaceutics

关键词: Ranolazine;    extended release;    Eudragit L 100-55;    HPMC K100M;    32 factorial design;    non-fickian diffusion;   

DOI  :  10.4274/tjps.galenos.2021.58047

来源: Galenos Yayinevi

【 摘 要 】

Objectives: 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. Materials and Methods: 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 (t10%, t50%, t75%, t90%). Results: 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. Conclusion: 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).

【 授权许可】

Unknown