分子薬学および有機プロセス研究ジャーナル

抽象的な

Formulation, Characterization and Pharmacokinetic Evaluation of Telmisartan Solid Dispersions

Arno A Enose, Priya Dasan, Hariharan Sivaramakrishanan and Vandita Kakkar

Telmisartan (TEL), a BCS class II antihypertensive drug possesses poor aqueous solubility which results in poor bioavailability after oral administration. Solid dispersion approach has been widely and successfully used to improve the biopharmaceutical profiles of the poorly soluble drugs. Present study was an attempt to prepare and compare the solid dispersion (SD) of Telmisartan using a novel polymer soluplus® by employing spray drying and melt extrusion techniques. Results demonstrated an improvement in solubility of TEL by 44, 3.3, 11 and 99 times as compared to pure drug in water and buffers pH 1.2, 4.5 and 7.4 respectively, post preparation of solid dispersions. Further, similar improvement was observed in in vitro release studies highlighting the importance of formulating solid dispersion. DSC and PXRD study revealed the amorphous state of TEL in solid dispersion. The developed SD were found to be stable at 40°C/75% RH, 25°C/60% RH and 2-8°C in accordance to ICH guidelines. The pharmacokinetic study in rats revealed promising results which were correlated well with the in vitro dissolution and solubility study. Results indicated the usefulness of solid dispersions prepared using soluplus® by industrially viable techniques to improve not only the bioavailability of TEL but also their potential for commercialization.