The preparation and characterization of solid dispersions on pellets using a fluidized-bed system

Hsiu O. Ho, Huei Lin Su, Tsuimin Tsai, Ming Thau Sheu

Research output: Contribution to journalArticle

42 Citations (Scopus)

Abstract

In this study, solid dispersions of a poorly water-soluble drug, nifedipine, were prepared in hydroxypropylmethylcellulose (HPMC) on sugar spheres using a fluidized-bed coating system and characterized by differential scanning calorimetry (DSC) and dissolution measurements. A mixture of acetone and water (7:3) was found to be suitable as a spraying solution for simultaneous application of nifedipine and HPMC. DSC studies showed that the peak corresponding to the melting point of nifedipine became broadened when nifedipine was incorporated in a solid dispersion with HPMC at both ratios of 1:1 and 1:3. The results demonstrated that dissolution rates were fastest at the lowest nifedipine loading. Furthermore, the dissolution rate of nifedipine increased as more HPMC was added to the solid dispersions. The enhancement in the dissolution rate of nifedipine upon addition of Tween 80 in simulated gastric acid was attributed to the solubilizing effect of Tween 80 on nifedipine. Tween 80 had less influence when nifedipine was incorporated in solid dispersions containing higher fractions of HPMC.

Original languageEnglish
Pages (from-to)223-229
Number of pages7
JournalInternational Journal of Pharmaceutics
Volume139
Issue number1-2
DOIs
Publication statusPublished - Aug 9 1996

Fingerprint

Nifedipine
Polysorbates
Differential Scanning Calorimetry
Water
Gastric Acid
Acetone
Freezing
Hypromellose Derivatives
Pharmaceutical Preparations

Keywords

  • Fluidized-bed system
  • Hydroxypropylmethylcellulose (HPMC)
  • Nifedipine
  • Solid dispersions

ASJC Scopus subject areas

  • Pharmaceutical Science

Cite this

The preparation and characterization of solid dispersions on pellets using a fluidized-bed system. / Ho, Hsiu O.; Su, Huei Lin; Tsai, Tsuimin; Sheu, Ming Thau.

In: International Journal of Pharmaceutics, Vol. 139, No. 1-2, 09.08.1996, p. 223-229.

Research output: Contribution to journalArticle

@article{fccfbe5795de4a7ab3536890a54a3907,
title = "The preparation and characterization of solid dispersions on pellets using a fluidized-bed system",
abstract = "In this study, solid dispersions of a poorly water-soluble drug, nifedipine, were prepared in hydroxypropylmethylcellulose (HPMC) on sugar spheres using a fluidized-bed coating system and characterized by differential scanning calorimetry (DSC) and dissolution measurements. A mixture of acetone and water (7:3) was found to be suitable as a spraying solution for simultaneous application of nifedipine and HPMC. DSC studies showed that the peak corresponding to the melting point of nifedipine became broadened when nifedipine was incorporated in a solid dispersion with HPMC at both ratios of 1:1 and 1:3. The results demonstrated that dissolution rates were fastest at the lowest nifedipine loading. Furthermore, the dissolution rate of nifedipine increased as more HPMC was added to the solid dispersions. The enhancement in the dissolution rate of nifedipine upon addition of Tween 80 in simulated gastric acid was attributed to the solubilizing effect of Tween 80 on nifedipine. Tween 80 had less influence when nifedipine was incorporated in solid dispersions containing higher fractions of HPMC.",
keywords = "Fluidized-bed system, Hydroxypropylmethylcellulose (HPMC), Nifedipine, Solid dispersions",
author = "Ho, {Hsiu O.} and Su, {Huei Lin} and Tsuimin Tsai and Sheu, {Ming Thau}",
year = "1996",
month = "8",
day = "9",
doi = "10.1016/0378-5173(96)04594-2",
language = "English",
volume = "139",
pages = "223--229",
journal = "International Journal of Pharmaceutics",
issn = "0378-5173",
publisher = "Elsevier",
number = "1-2",

}

TY - JOUR

T1 - The preparation and characterization of solid dispersions on pellets using a fluidized-bed system

AU - Ho, Hsiu O.

AU - Su, Huei Lin

AU - Tsai, Tsuimin

AU - Sheu, Ming Thau

PY - 1996/8/9

Y1 - 1996/8/9

N2 - In this study, solid dispersions of a poorly water-soluble drug, nifedipine, were prepared in hydroxypropylmethylcellulose (HPMC) on sugar spheres using a fluidized-bed coating system and characterized by differential scanning calorimetry (DSC) and dissolution measurements. A mixture of acetone and water (7:3) was found to be suitable as a spraying solution for simultaneous application of nifedipine and HPMC. DSC studies showed that the peak corresponding to the melting point of nifedipine became broadened when nifedipine was incorporated in a solid dispersion with HPMC at both ratios of 1:1 and 1:3. The results demonstrated that dissolution rates were fastest at the lowest nifedipine loading. Furthermore, the dissolution rate of nifedipine increased as more HPMC was added to the solid dispersions. The enhancement in the dissolution rate of nifedipine upon addition of Tween 80 in simulated gastric acid was attributed to the solubilizing effect of Tween 80 on nifedipine. Tween 80 had less influence when nifedipine was incorporated in solid dispersions containing higher fractions of HPMC.

AB - In this study, solid dispersions of a poorly water-soluble drug, nifedipine, were prepared in hydroxypropylmethylcellulose (HPMC) on sugar spheres using a fluidized-bed coating system and characterized by differential scanning calorimetry (DSC) and dissolution measurements. A mixture of acetone and water (7:3) was found to be suitable as a spraying solution for simultaneous application of nifedipine and HPMC. DSC studies showed that the peak corresponding to the melting point of nifedipine became broadened when nifedipine was incorporated in a solid dispersion with HPMC at both ratios of 1:1 and 1:3. The results demonstrated that dissolution rates were fastest at the lowest nifedipine loading. Furthermore, the dissolution rate of nifedipine increased as more HPMC was added to the solid dispersions. The enhancement in the dissolution rate of nifedipine upon addition of Tween 80 in simulated gastric acid was attributed to the solubilizing effect of Tween 80 on nifedipine. Tween 80 had less influence when nifedipine was incorporated in solid dispersions containing higher fractions of HPMC.

KW - Fluidized-bed system

KW - Hydroxypropylmethylcellulose (HPMC)

KW - Nifedipine

KW - Solid dispersions

UR - http://www.scopus.com/inward/record.url?scp=0030576575&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0030576575&partnerID=8YFLogxK

U2 - 10.1016/0378-5173(96)04594-2

DO - 10.1016/0378-5173(96)04594-2

M3 - Article

AN - SCOPUS:0030576575

VL - 139

SP - 223

EP - 229

JO - International Journal of Pharmaceutics

JF - International Journal of Pharmaceutics

SN - 0378-5173

IS - 1-2

ER -