Co-Amorphous Telmisartan-Pimelic Acid with Improved Solubility

Abstract

Telmisartan (TEL), a type of antihypertensive drug, has poor solubility. To improve its solubility, the co-amorphous telmisartan with pimelic acid (PA) in molar ratio of 1:1 and 2:1, respectively, were obtained using a liquid-assisted grinding method. The co-amorphous system was characterized by the powder X-ray diffraction and differential scanning calorimetry. The molecular interactions of the co-amorphous were studied by the infrared spectra. After the formation of co-amorphous, the solubility of TELwas much improved, and the apparent solubility values were approximately 9-15 times as high as that of crystalline TEL. Moreover, the co-amorphous TEL-PA was stored under 25 °C/20% RH for a month without any evidence of conversion by powder X-ray diffraction analysis.

New Perspectives for Antihypertensive Sartans as Components of Co-crystals and Co-amorphous Solids with Improved Properties and Multipurpose Activity

“…The TEL/HCT 1:3 formulation showed the greatest improvement in properties, both apparent solubility and the in vitro dissolution rate. Co-amophous solid dispersions of TEL with PI were synthesized by liquid-assisted grinding using pestle and mortar in molar ratios of 1:1 and 2:1 . It was shown that the carboxyl groups of both TEL and PA participated in the formation of intermolecular interactions.…”

“…Telmisartan was co-amorphized with HCT and pimelic acid (PI) . The formulations with HCT were used in two-component preparations together with TEL, hence, the synthesis of these co-amorphous products was deeply justified.…”

“…193 Telmisartan was co-amorphized with HCT 194 and pimelic acid (PI). 195 The formulations with HCT were used in twocomponent preparations together with TEL, hence, the synthesis of these co-amorphous products was deeply justified. The authors synthesized TEL/HCT co-amorphous formulations by solvent evaporation in molar ratios of 1:1, 2:3, 1:2, and 1:3, taking 1:3 as the dose equivalent ratio.…”

“…Co-amophous solid dispersions of TEL with PI were synthesized by liquid-assisted grinding using pestle and mortar in molar ratios of 1:1 and 2:1. 195 It was shown that the carboxyl groups of both TEL and PA participated in the formation of intermolecular interactions. It was possible to increase the solubility of TEL by 9−15 times by using PI as a co-former.…”