Enhancement of wettability and dissolution properties of cilostazol using the supercritical antisolvent process: Effect of various additives

Min Soo Kim, Jeong Soo Kim, Sung Joo Hwang

Research output: Contribution to journalArticle

18 Citations (Scopus)

Abstract

The aim of this study was to improve wettability and dissolution rate of a poorly water-soluble drug, cilostazol, using the supercritical antisolvent (SAS) process. The solid state of particles precipitated from dichloromethane containing additives, including poloxamer 188, poloxamer 407, TPGS 1000, Gelucire® 44/14 and Gelucire® 50/13, in supercritical CO2 medium were characterized by differential scanning calorimetry DSC), powder X-ray diffraction (PXRD), FT-IR, particle size analysis, contact angle, and dissolution. Interestingly, the morphology of SAS particles processed with TPGS 1000, Gelucire® 44/14 and Gelucire® 50/13 changed plate- or leaflet-shaped. Furthermore, the particle sizes of cilostazol processed with Gelucire® 44/14 and Gelucire® 50/13 were increased compared to cilostazol processed without additives. Poloxamer 188 and poloxamer 407 were superior in increasing the dissolution rate due to decreased particle size, the resulting increased surface area, and improved wettability. Micronization with the supercritical antisolvent process resulted in a significant decrease in mean particle size, and wettability of cilostazol was increased by using small amounts of hydrophilic additives.

Original languageEnglish
Pages (from-to)230-233
Number of pages4
JournalChemical and Pharmaceutical Bulletin
Volume58
Issue number2
DOIs
Publication statusPublished - 2010 Feb 1

Fingerprint

Wettability
Poloxamer
Particle Size
Wetting
Dissolution
Particle size
Methylene Chloride
Differential Scanning Calorimetry
X-Ray Diffraction
Particle size analysis
Powders
X ray powder diffraction
Contact angle
Differential scanning calorimetry
cilostazol
Water
Pharmaceutical Preparations
gelucire 44-14
Gelucire 50-13
alpha-tocopheryl polyethylene glycol succinate

All Science Journal Classification (ASJC) codes

  • Drug Discovery
  • Chemistry(all)

Cite this

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abstract = "The aim of this study was to improve wettability and dissolution rate of a poorly water-soluble drug, cilostazol, using the supercritical antisolvent (SAS) process. The solid state of particles precipitated from dichloromethane containing additives, including poloxamer 188, poloxamer 407, TPGS 1000, Gelucire{\circledR} 44/14 and Gelucire{\circledR} 50/13, in supercritical CO2 medium were characterized by differential scanning calorimetry DSC), powder X-ray diffraction (PXRD), FT-IR, particle size analysis, contact angle, and dissolution. Interestingly, the morphology of SAS particles processed with TPGS 1000, Gelucire{\circledR} 44/14 and Gelucire{\circledR} 50/13 changed plate- or leaflet-shaped. Furthermore, the particle sizes of cilostazol processed with Gelucire{\circledR} 44/14 and Gelucire{\circledR} 50/13 were increased compared to cilostazol processed without additives. Poloxamer 188 and poloxamer 407 were superior in increasing the dissolution rate due to decreased particle size, the resulting increased surface area, and improved wettability. Micronization with the supercritical antisolvent process resulted in a significant decrease in mean particle size, and wettability of cilostazol was increased by using small amounts of hydrophilic additives.",
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Enhancement of wettability and dissolution properties of cilostazol using the supercritical antisolvent process : Effect of various additives. / Kim, Min Soo; Kim, Jeong Soo; Hwang, Sung Joo.

In: Chemical and Pharmaceutical Bulletin, Vol. 58, No. 2, 01.02.2010, p. 230-233.

Research output: Contribution to journalArticle

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