Design of telmisartan-weak acid solid dispersion to improve its solubility and stability

摘要

Telmisartan (TEL), an angiotensin II receptor antagonist, is widely used for the treatment of hypertension. However, low solubility of TEL has resulted in solubilized commercial products with alkalizers. On the contrary, our study aims to improve the solubility and dissolution rate by preparing a new TEL-solid dispersion (SD) using a weak acid. The SD formulations (SD1-0, TEL-tartaric acid-Aerosil®300 in a 1:5:3 wt ratio; SD1-6, TEL-tartaric acid-Aerosil®300: IR® in a 1:5:3:1 wt ratio) showed improved dissolution (%) by 1.19-/1.08-/1.16-fold and 1.15-/1.06-/1.11-fold compared to that of Micardis® in pH 1.2/distilled water/pH 6.8, respectively. The physical properties of the SD formulations were changed, including melting points, crystallization, and chemical interaction. Moreover, these SD formulations well maintained their stability for 12 months. In conclusion, the improved solubility and dissolution (%) of TEL in the SD formulations may result in improved bioavailability and efficacy as an anti-hypertensive substance in animals.