International Journal of Pharmaceutics 2014-10-01

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

Ying-Chen Chen, Hsiu-O Ho, Jiun-Da Chiou, Ming-Thau Sheu

文献索引：Int. J. Pharm. 473(1-2) , 458-68, (2014)

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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(®) VA64, tocopheryl polyethylene glycol succinate (TPGS), vitamine E) with hot-melt and thermal adhesion granulation (TAG) method to adsorb Fujicalin(®) and Microcel(®) were characterized. Results demonstrate the angle of repose in formulations with Fujicalin(®) was 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(®) had lower hardness than those with Fujicalin(®), because Microcel(®) has 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 ± 0.20 μg/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.Copyright © 2014 Elsevier B.V. All rights reserved.