Effect of β-sitosterol on precipitation of cholesterol from non-aqueous and aqueous solutions

L. Christiansen (Corresponding Author), M. Karjalainen, Tuulikki Seppänen-Laakso, R. Hiltunen, T. Yliruusi

Research output: Contribution to journalArticleScientificpeer-review

27 Citations (Scopus)

Abstract

The aim of the present work was to study the solubility and phase behaviour of the β-sitosterol–cholesterol mixed crystals in the presence and absence of water. Cholesterol, β-sitosterol and 3:1, 1:1 and 1:3 mixtures of these were co-precipitated from acetone and acetone–water solutions. Precipitated crystals were analysed using powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), optical microscopy and Karl–Fischer titrimetry. The quantification of the sterols in solutions was preformed using GC–MS. The solubility of the sterols was mutually limiting. In the aqueous system, the solubility of both the sterols were significantly lower than in the absence of water, but the decrease in the solubility was considerably greater with the more hydrophobic β-sitosterol. In the aqueous system, the total sterol solubility decreased with the increasing proportion of β-sitosterol. The formation of new crystal structures, solid solutions of cholesterol and β-sitosterol, was observed in non-aqueous as well as in aqueous environments except with the lowest cholesterol proportion in the system, in which case mixed crystals with eutectic behaviour were formed.
Original languageEnglish
Pages (from-to)155-166
Number of pages12
JournalInternational Journal of Pharmaceutics
Volume254
Issue number2
DOIs
Publication statusPublished - 2003
MoE publication typeA1 Journal article-refereed

Fingerprint

Solubility
Sterols
Cholesterol
Titrimetry
Water
Differential Scanning Calorimetry
Acetone
X-Ray Diffraction
Powders
Gas Chromatography-Mass Spectrometry
Microscopy
gamma-sitosterol

Keywords

  • Cholesterol
  • beta-Sitosterol
  • Co-precipitation
  • Solubility

Cite this

Christiansen, L. ; Karjalainen, M. ; Seppänen-Laakso, Tuulikki ; Hiltunen, R. ; Yliruusi, T. / Effect of β-sitosterol on precipitation of cholesterol from non-aqueous and aqueous solutions. In: International Journal of Pharmaceutics. 2003 ; Vol. 254, No. 2. pp. 155-166.
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abstract = "The aim of the present work was to study the solubility and phase behaviour of the β-sitosterol–cholesterol mixed crystals in the presence and absence of water. Cholesterol, β-sitosterol and 3:1, 1:1 and 1:3 mixtures of these were co-precipitated from acetone and acetone–water solutions. Precipitated crystals were analysed using powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), optical microscopy and Karl–Fischer titrimetry. The quantification of the sterols in solutions was preformed using GC–MS. The solubility of the sterols was mutually limiting. In the aqueous system, the solubility of both the sterols were significantly lower than in the absence of water, but the decrease in the solubility was considerably greater with the more hydrophobic β-sitosterol. In the aqueous system, the total sterol solubility decreased with the increasing proportion of β-sitosterol. The formation of new crystal structures, solid solutions of cholesterol and β-sitosterol, was observed in non-aqueous as well as in aqueous environments except with the lowest cholesterol proportion in the system, in which case mixed crystals with eutectic behaviour were formed.",
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Effect of β-sitosterol on precipitation of cholesterol from non-aqueous and aqueous solutions. / Christiansen, L. (Corresponding Author); Karjalainen, M.; Seppänen-Laakso, Tuulikki; Hiltunen, R.; Yliruusi, T.

In: International Journal of Pharmaceutics, Vol. 254, No. 2, 2003, p. 155-166.

Research output: Contribution to journalArticleScientificpeer-review

TY - JOUR

T1 - Effect of β-sitosterol on precipitation of cholesterol from non-aqueous and aqueous solutions

AU - Christiansen, L.

AU - Karjalainen, M.

AU - Seppänen-Laakso, Tuulikki

AU - Hiltunen, R.

AU - Yliruusi, T.

PY - 2003

Y1 - 2003

N2 - The aim of the present work was to study the solubility and phase behaviour of the β-sitosterol–cholesterol mixed crystals in the presence and absence of water. Cholesterol, β-sitosterol and 3:1, 1:1 and 1:3 mixtures of these were co-precipitated from acetone and acetone–water solutions. Precipitated crystals were analysed using powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), optical microscopy and Karl–Fischer titrimetry. The quantification of the sterols in solutions was preformed using GC–MS. The solubility of the sterols was mutually limiting. In the aqueous system, the solubility of both the sterols were significantly lower than in the absence of water, but the decrease in the solubility was considerably greater with the more hydrophobic β-sitosterol. In the aqueous system, the total sterol solubility decreased with the increasing proportion of β-sitosterol. The formation of new crystal structures, solid solutions of cholesterol and β-sitosterol, was observed in non-aqueous as well as in aqueous environments except with the lowest cholesterol proportion in the system, in which case mixed crystals with eutectic behaviour were formed.

AB - The aim of the present work was to study the solubility and phase behaviour of the β-sitosterol–cholesterol mixed crystals in the presence and absence of water. Cholesterol, β-sitosterol and 3:1, 1:1 and 1:3 mixtures of these were co-precipitated from acetone and acetone–water solutions. Precipitated crystals were analysed using powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), optical microscopy and Karl–Fischer titrimetry. The quantification of the sterols in solutions was preformed using GC–MS. The solubility of the sterols was mutually limiting. In the aqueous system, the solubility of both the sterols were significantly lower than in the absence of water, but the decrease in the solubility was considerably greater with the more hydrophobic β-sitosterol. In the aqueous system, the total sterol solubility decreased with the increasing proportion of β-sitosterol. The formation of new crystal structures, solid solutions of cholesterol and β-sitosterol, was observed in non-aqueous as well as in aqueous environments except with the lowest cholesterol proportion in the system, in which case mixed crystals with eutectic behaviour were formed.

KW - Cholesterol

KW - beta-Sitosterol

KW - Co-precipitation

KW - Solubility

U2 - 10.1016/S0378-5173(03)00007-3

DO - 10.1016/S0378-5173(03)00007-3

M3 - Article

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JO - International Journal of Pharmaceutics

JF - International Journal of Pharmaceutics

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