Enhancing Telmisartan Bioavailability via Advanced Co-Processing Techniques with Excipients

Abstract

Hypertension, a widespread medical condition, necessitates effective pharmaceutical interventions like Telmisartan, an angiotensin II receptor blocker (ARB), to manage blood pressure. Despite its efficacy, Telmisartan's poor solubility and dissolution rate hinder its optimal bioavailability and therapeutic effectiveness. This study aimed to enhance Telmisartan's physicochemical properties through co-processing with various excipients, specifically focusing on improving solubility, dissolution rate, and stability. Micromeritic properties of different formulations were evaluated, revealing that bulk density ranged from 0.36 to 0.53 gm/cm³ and tapped density from 0.58 to 0.79 gm/cm³. The Hausner ratio varied between 0.85 and 1.23, with formulations F1 and F2 indicating good flowability, while others showed moderate to poor flow properties. Carr’s index values ranged from 11.20% to 17.20%, with formulation F1 exhibiting the lowest index, signifying excellent flow and compressibility. The angle of repose ranged from 24°.8' to 29°.8', with formulation F8 showing the lowest angle, indicating superior flow properties. Additionally, solubility tests showed the highest solubility in 0.1N HCl (80 µg/ml), succeeded by phosphate buffer solution of pH 6.8 (70 µg/ml), and the lowest in distilled water (50 µg/ml). The partition coefficient of Telmisartan was 2.22± 0.10. Overall, formulations F1 and F8 demonstrated the best flow properties, suggesting improved processability during tablet manufacturing. These findings highlight the potential of co-processing to overcome Telmisartan's inherent limitations, enhancing its pharmaceutical performance and therapeutic efficacy.