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

Research output: Contribution to journalArticle

11 Citations (Scopus)

Abstract

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.

Original languageEnglish
Pages (from-to)458-468
Number of pages11
JournalInternational Journal of Pharmaceutics
Volume473
Issue number1-2
DOIs
Publication statusPublished - Oct 1 2014

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Vitamin E
Hot Temperature
Hardness
Excipients
Pharmaceutical Preparations
Solubility
Biological Availability
Adsorption
cilostazol
poly(ethylene succinate)
Water
fujicalin

Keywords

  • Cilostazol
  • Solid dispersion
  • Thermal adhesion granulation
  • Tocopheryl polyethylene glycol succinate (TPGS)

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Medicine(all)

Cite this

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title = "Physical and dissolution characterization of cilostazol solid dispersions prepared by hot melt granulation (HMG) and thermal adhesion granulation (TAG) methods",
abstract = "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{\circledR} VA64, tocopheryl polyethylene glycol succinate (TPGS), vitamine E) with hot-melt and thermal adhesion granulation (TAG) method to adsorb Fujicalin{\circledR} and Microcel{\circledR} were characterized. Results demonstrate the angle of repose in formulations with Fujicalin{\circledR} was improved than those with Microcel{\circledR}, 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{\circledR} had lower hardness than those with Fujicalin{\circledR}, because Microcel{\circledR} 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{\circledR} (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.",
keywords = "Cilostazol, Solid dispersion, Thermal adhesion granulation, Tocopheryl polyethylene glycol succinate (TPGS)",
author = "Chen, {Ying Chen} and Ho, {Hsiu O.} and Chiou, {Jiun Da} and Sheu, {Ming Thau}",
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T1 - Physical and dissolution characterization of cilostazol solid dispersions prepared by hot melt granulation (HMG) and thermal adhesion granulation (TAG) methods

AU - Chen, Ying Chen

AU - Ho, Hsiu O.

AU - Chiou, Jiun Da

AU - Sheu, Ming Thau

PY - 2014/10/1

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N2 - 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.

AB - 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.

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