MODIFICATION OF PHYSICOCHEMICAL PROPERTIES OF TELMISARTAN THROUGH SALT

• Main Author: G A Nadia Prasta Unique, I
• Format: Theses
• Language: Indonesia
• Online Access: https://digilib.itb.ac.id/gdl/view/70438
• Institution: Institut Teknologi Bandung

Telmisartan (TEL) is an Angiotensin Receptor Blockers (ARB) antihypertensive drug which is categorized in BCS (Biopharmaceutical Classification System) class II, due to its high permeability but low solubility, hence limiting its development. Therefore, efforts have been made to improve its physicochemical properties, including solubility and dissolution rate. This study aims to form the TEL raw material into its salt form using hydrochloric acid (HCl) as a counterion, and evaluate its solubility, intrinsic dissolution rate, particle size distribution, and flowability. The formation of TEL-HCl salt using solvent evaporation method was able to improve the physicochemical properties of TEL. The salt formation succeeded in increasing the solubility, intrinsic dissolution rate and improving the flowability of TEL. The obtained solids were characterized using thermogravimetric analysis (TGA), differential scanning calorimetry (DSC), and powder X-ray diffractometry (PXRD) to determine their characteristics. The results confirmed that TEL-HCl salt was obtained. This salt form was able to increase the solubility by 13-fold , increase the intrinsic dissolution rate by 18-fold, improve the particle size distribution, and improve the flowability of TEL. Based on these data, TEL-HCl salt has the potential to be further developed into raw material for pharmaceutical preparations.