Effect of operating parameters on PVP/tadalafil solid dispersions prepared using supercritical anti-solvent process

Junsung Park, Wonkyung Cho, Han Kang, Benjamin Byung Jun Lee, Taek Sun Kim, Sung Joo Hwang

Research output: Contribution to journalArticle

21 Citations (Scopus)

Abstract

Supercritical anti-solvent (SAS) process was employed to produce tadalafil solid dispersion sub-micron particles. Three independent variables for the SAS process (temperature, pressure, and drug concentration) were varied in order to investigate the effects on particle size and morphology of PVP/tadalafil solid dispersion (drug to polymer ratio 1:4). The mean particle size decreased with decreasing temperature (50 → 40 °C) and concentration (15 → 5 mg/mL) and increasing pressure (90 → 150 bar). Depending on the experimental variable, the mean particle size varied from 200 nm to 900 nm, and the dominant experimental variable was determined to be the drug concentration. Moreover, at a concentration of 15 mg/mL with any other process conditions, tadalafil tended to partially aggregate in crystalline form with irregular particle shapes. The results of in vitro dissolution experiments showed good correlation with mean particle size and crystallinity of the SAS-processed particles, in that the highest drug concentration showed the least dissolution rate and vice versa. Therefore, among the three variables studied, the drug concentration is the major factor that produces sub-micron particles in the SAS process.

Original languageEnglish
Pages (from-to)126-133
Number of pages8
JournalJournal of Supercritical Fluids
Volume90
DOIs
Publication statusPublished - 2014 Jan 1

Fingerprint

Dispersions
Particle size
drugs
Pharmaceutical Preparations
Dissolution
dissolving
Crystalline materials
Polymers
Temperature
Tadalafil
crystallinity
Experiments
temperature
polymers

All Science Journal Classification (ASJC) codes

  • Chemical Engineering(all)
  • Condensed Matter Physics
  • Physical and Theoretical Chemistry

Cite this

Park, Junsung ; Cho, Wonkyung ; Kang, Han ; Lee, Benjamin Byung Jun ; Kim, Taek Sun ; Hwang, Sung Joo. / Effect of operating parameters on PVP/tadalafil solid dispersions prepared using supercritical anti-solvent process. In: Journal of Supercritical Fluids. 2014 ; Vol. 90. pp. 126-133.
@article{a3f142ae701d4083814d7ae7541f7036,
title = "Effect of operating parameters on PVP/tadalafil solid dispersions prepared using supercritical anti-solvent process",
abstract = "Supercritical anti-solvent (SAS) process was employed to produce tadalafil solid dispersion sub-micron particles. Three independent variables for the SAS process (temperature, pressure, and drug concentration) were varied in order to investigate the effects on particle size and morphology of PVP/tadalafil solid dispersion (drug to polymer ratio 1:4). The mean particle size decreased with decreasing temperature (50 → 40 °C) and concentration (15 → 5 mg/mL) and increasing pressure (90 → 150 bar). Depending on the experimental variable, the mean particle size varied from 200 nm to 900 nm, and the dominant experimental variable was determined to be the drug concentration. Moreover, at a concentration of 15 mg/mL with any other process conditions, tadalafil tended to partially aggregate in crystalline form with irregular particle shapes. The results of in vitro dissolution experiments showed good correlation with mean particle size and crystallinity of the SAS-processed particles, in that the highest drug concentration showed the least dissolution rate and vice versa. Therefore, among the three variables studied, the drug concentration is the major factor that produces sub-micron particles in the SAS process.",
author = "Junsung Park and Wonkyung Cho and Han Kang and Lee, {Benjamin Byung Jun} and Kim, {Taek Sun} and Hwang, {Sung Joo}",
year = "2014",
month = "1",
day = "1",
doi = "10.1016/j.supflu.2014.04.001",
language = "English",
volume = "90",
pages = "126--133",
journal = "Journal of Supercritical Fluids",
issn = "0896-8446",
publisher = "Elsevier",

}

Effect of operating parameters on PVP/tadalafil solid dispersions prepared using supercritical anti-solvent process. / Park, Junsung; Cho, Wonkyung; Kang, Han; Lee, Benjamin Byung Jun; Kim, Taek Sun; Hwang, Sung Joo.

In: Journal of Supercritical Fluids, Vol. 90, 01.01.2014, p. 126-133.

Research output: Contribution to journalArticle

TY - JOUR

T1 - Effect of operating parameters on PVP/tadalafil solid dispersions prepared using supercritical anti-solvent process

AU - Park, Junsung

AU - Cho, Wonkyung

AU - Kang, Han

AU - Lee, Benjamin Byung Jun

AU - Kim, Taek Sun

AU - Hwang, Sung Joo

PY - 2014/1/1

Y1 - 2014/1/1

N2 - Supercritical anti-solvent (SAS) process was employed to produce tadalafil solid dispersion sub-micron particles. Three independent variables for the SAS process (temperature, pressure, and drug concentration) were varied in order to investigate the effects on particle size and morphology of PVP/tadalafil solid dispersion (drug to polymer ratio 1:4). The mean particle size decreased with decreasing temperature (50 → 40 °C) and concentration (15 → 5 mg/mL) and increasing pressure (90 → 150 bar). Depending on the experimental variable, the mean particle size varied from 200 nm to 900 nm, and the dominant experimental variable was determined to be the drug concentration. Moreover, at a concentration of 15 mg/mL with any other process conditions, tadalafil tended to partially aggregate in crystalline form with irregular particle shapes. The results of in vitro dissolution experiments showed good correlation with mean particle size and crystallinity of the SAS-processed particles, in that the highest drug concentration showed the least dissolution rate and vice versa. Therefore, among the three variables studied, the drug concentration is the major factor that produces sub-micron particles in the SAS process.

AB - Supercritical anti-solvent (SAS) process was employed to produce tadalafil solid dispersion sub-micron particles. Three independent variables for the SAS process (temperature, pressure, and drug concentration) were varied in order to investigate the effects on particle size and morphology of PVP/tadalafil solid dispersion (drug to polymer ratio 1:4). The mean particle size decreased with decreasing temperature (50 → 40 °C) and concentration (15 → 5 mg/mL) and increasing pressure (90 → 150 bar). Depending on the experimental variable, the mean particle size varied from 200 nm to 900 nm, and the dominant experimental variable was determined to be the drug concentration. Moreover, at a concentration of 15 mg/mL with any other process conditions, tadalafil tended to partially aggregate in crystalline form with irregular particle shapes. The results of in vitro dissolution experiments showed good correlation with mean particle size and crystallinity of the SAS-processed particles, in that the highest drug concentration showed the least dissolution rate and vice versa. Therefore, among the three variables studied, the drug concentration is the major factor that produces sub-micron particles in the SAS process.

UR - http://www.scopus.com/inward/record.url?scp=84899649687&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=84899649687&partnerID=8YFLogxK

U2 - 10.1016/j.supflu.2014.04.001

DO - 10.1016/j.supflu.2014.04.001

M3 - Article

AN - SCOPUS:84899649687

VL - 90

SP - 126

EP - 133

JO - Journal of Supercritical Fluids

JF - Journal of Supercritical Fluids

SN - 0896-8446

ER -