As a widely prescribed anti diabetic drug, pioglitazone belongs to class II under BCS and exhibits low and variable oral bioavailability due to its poor aqueous solubility. Its oral absorption is dissolution rate limi...As a widely prescribed anti diabetic drug, pioglitazone belongs to class II under BCS and exhibits low and variable oral bioavailability due to its poor aqueous solubility. Its oral absorption is dissolution rate limited, and its solubility and dissolution rate need to be enhanced in order to increase its oral bioavailability. In the present study, we aimed to screen various oils, surfactants and cosolvents. The highest solubility was observed in Labrafac, Tween-80 and propylene glycol. Then the feasibility of formulating pioglitazone SEDDS was evaluated, and the effect of dilution on the dissolution rate and dissolution efficiency of pioglitazone was also analyzed. A comparative evaluation of pioglitazone from SEDDS was made in SGF and 1% SLS. Dissolution of pioglitazone from SEDDS was rapid and higher compared with pure drug. The rate and extent of release of pioglitazone hydrochloride from stable SEDDS （F1） were higher in 1% SLS compared with SGF. The FTIR spectra proved that there was on chemical interaction between excipients and drug. SEM studies confirmed that the size was small and spherical.展开更多
文摘As a widely prescribed anti diabetic drug, pioglitazone belongs to class II under BCS and exhibits low and variable oral bioavailability due to its poor aqueous solubility. Its oral absorption is dissolution rate limited, and its solubility and dissolution rate need to be enhanced in order to increase its oral bioavailability. In the present study, we aimed to screen various oils, surfactants and cosolvents. The highest solubility was observed in Labrafac, Tween-80 and propylene glycol. Then the feasibility of formulating pioglitazone SEDDS was evaluated, and the effect of dilution on the dissolution rate and dissolution efficiency of pioglitazone was also analyzed. A comparative evaluation of pioglitazone from SEDDS was made in SGF and 1% SLS. Dissolution of pioglitazone from SEDDS was rapid and higher compared with pure drug. The rate and extent of release of pioglitazone hydrochloride from stable SEDDS （F1） were higher in 1% SLS compared with SGF. The FTIR spectra proved that there was on chemical interaction between excipients and drug. SEM studies confirmed that the size was small and spherical.
