in-vitro characterization and oral bioavailability of organic solvent-free solid dispersions containing telmisartan

poorly water-soluble drugs often suffer from limited or irreproducible clinical response due to their low solubility and dissolution rate. in this study, organic solvent-free solid dispersions (osf-sds) containing telmisartan (tel) were prepared using polyvinylpyrrolidone k30 (pvp k30) and polyethylene glycol 6000 (peg 6000) as hydrophilic polymers, sodium hydroxide (naoh) as an alkalizer, and poloxamer 188 as a surfactant by a lyophilization method. in vitro dissolution rate and physicochemical properties of the osf-sds were characterized using the usp i basket method, differential scanning calorimetry (dsc), x-ray diffractometry (xrd) and fourier transform-infrared (ft-ir) spectroscopy. in addition, the oral bioavailability of osf-sds in rats was evaluated by using tel bulk powder as a reference. the dissolution rates of the osf-sds were significantly enhanced as compared to tel bulk powder. the results from dsc, xrd showed that tel was molecularly dispersed in the osf-sds as an amorphous form. the ft-ir results suggested that intermolecular hydrogen bonding had formed between tel and its carriers. the osf-sds exhibited significantly higher auc0–24 h and cmax, but similar tmax as compared to the reference. this study demonstrated that osf-sds can be a promising method to enhance the dissolution rate and oral bioavailability of tel.