Development and Assessment of Trandolapril Immediate Release Tablets Employing Various Super-disintegrating Agents

Abstract

Trandolapril is a powerful prodrug that does not contain sulfur and is converted into its active form, trandolaprilat, in the liver. Trandolapril has demonstrated efficacy and safety in treating mild-to-moderate essential hypertension in obese persons. The half-life of trandolapril and trandolaprilate is roughly 6 hours and 16-24 hours, respectively. This refers to the duration it takes for the concentration of these compounds to reduce by half due to elimination mechanisms. The aim of this study is to improve the composition of the Trandolapril immediate release tablet by integrating various types of supersintegrants. The optimization procedure utilized Crospovidone, sodium starch glycolate, and croscarmellose sodium as superdisintegrating agents. These agents were used at concentrations of 2%, 4%, and 6%. Nine formulations (IRTR 1 to IRTR 9) were created using the direct compression approach. The precompression parameters of all batches were assessed in relation to the set thresholds, and it was concluded that the powder blend had outstanding flow and compressibility characteristics. The tablets were assessed for post-compression properties, including hardness, drug content, and Disintegration Time (DT). A drug dissolution test was performed in a laboratory setting using 900 ml of hydrochloric acid (HCl) with a concentration of 0.1N. The test was completed at a controlled temperature of 37 ± 0.5°C. When formulating IRTR1-IRTR9, the disintegration time varied between 30.23 and 71.67 seconds. Additionally, over 70% of the medication was released during a 30-minute period. Therefore, after assessing many characteristics, it was concluded that the formulation of immediate release tablets of Trandolapril was successfully developed. The tablet designated IRTR3 demonstrated a disintegration time of 30.23, which is the shortest time it took to break down. Additionally, it achieved a drug release of 90.56% within a 30- minute period.