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. © 2016 by school of pharmacy.