Formulation and in-vitro evaluation of directly compressed controlled release matrices of Losartan Potassium using Ethocel Grade 100 as rate retarding agent

Int J Pharm. 2015 Dec 30;496(2):759-65. doi: 10.1016/j.ijpharm.2015.10.051. Epub 2015 Nov 3.

Abstract

Current study was aimed to develop 200mg controlled release matrix tablets of Losartan Potassium using Ethocel 100 Premium and Ethocel 100 FP Premium as rate controlling polymer. In-vitro studies were performed according to USP Method-I in phosphate buffer (PH 6.8) using pharma test dissolution apparatus. The temperature of the dissolution medium was kept constant at 37±0.5°C at 100rpm. Flow properties, physical quality control tests, effect of polymer size and drug-to-polymers ratios were studied using different kinetics models such as 1st-order, zero-order, Hixon Crowell model, Highuchi model and Power law. Difference factor f1 and similarity factor f2 were applied for dissolution profiles against Cardaktin® tablets used as a reference formulation. The matrices with polymer ethocel 100 FP Premiums have prolonged the drug release rate as compared to polymer ethocel 100 Premiums. The n values matrices with polymer ethocel grade 100 ranged from 0.603 to 0.857 indicating that the drug release occurred by anomalous non fickian diffusion kinetics while then value of reference Cardaktin® tablet was measured as 0.125 indicating that these tablets do not follow power law. The dissolution profiles of test formulations were different than that of reference Cardaktin®. This suggests the polymer Ethocel grade 100 can be proficiently incorporated in fabrication and development of once a day controlled release matrix tablets.

Keywords: Controlled release; Ethocel grade 100; Losartan Potassium; Matrix tablets.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cellulose / analogs & derivatives*
  • Chemistry, Pharmaceutical
  • Delayed-Action Preparations
  • Losartan / chemistry*
  • Solubility
  • Tablets

Substances

  • Delayed-Action Preparations
  • Tablets
  • Cellulose
  • Losartan