Physical and dissolution characterization of cilostazol solid dispersions prepared by hot melt granulation (HMG) and thermal adhesion granulation (TAG) methods

摘要

A growing number of poorly water-soluble drug have been discovered, but the poor bioavailability is a critical problem. In this study, physical properties and dissolution profiles of cilostazol solid dispersions prepared by hydrophilic/lipophilic excipients (Kollidon齎A64, tocopheryl polyethylene glycol succinate (TPGS), vitamine E) with hot-melt and thermal adhesion granulation (TAG) method to adsorb Fujicalin齛nd Microcel齱ere characterized. Results demonstrate the angle of repose in formulations with Fujicalin齱as improved than those with Microcel?but the difference disappeared when more TPGS or vitamin E was added. Compared the formulation made by hot-melt and TAG method, both improved flowability. The hardness decreased with the increased amount of TPGS and vitamin E. The formulations with Microcel齢ad lower hardness than those with Fujicalin?because Microcel齢as weaker adsorption ability and cannot afford much TPGS and vitamin E, leading to lower hardness. Furthermore, the solubility was almost three-fold higher than that of Pletaal?7.68 ?.20 ?mL) in compositions containing TPGS and vitamin E made by hot-melt or TAG method, in which a controlled drug release pattern was demonstrated. There is no significant difference on dissolution profile between hot-melt and TAG method. However, the procedure of TAG is easier, indicating its potential pharmaceutical use.