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

研究成果: 雜誌貢獻文章

13 引文 斯高帕斯(Scopus)

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.
原文英語
頁(從 - 到)458-468
頁數11
期刊International Journal of Pharmaceutics
473
發行號1-2
DOIs
出版狀態已發佈 - 十月 1 2014

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Medicine(all)

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