Development and Evaluation of Poorly Water-Soluble Celecoxib as Solid Dispersions Containing Nonionic Surfactants Using Fluidized-Bed Granulation

Development and Evaluation of Poorly Water-Soluble Celecoxib as Solid Dispersions Containing Nonionic Surfactants Using Fluidized-Bed Granulation

The purpose of this study is to develop a solid dispersion system with improved dissolution, absorption, and patient compliance of poorly water-soluble celecoxib (CXB). Instead of sodium lauryl sulfate (SLS), an anionic surfactant used in the marketed product (Celebrex ), solubilization was performe...

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Published in:Pharmaceutics Vol. 11; no. 3; p. 136
Main Authors: Kwon, Hyeok Jin, Heo, Eun-Ji, Kim, Young-Hwan, Kim, Sarah, Hwang, Young-Ha, Byun, Ji-Mi, Cheon, Se Hyeop, Park, Sang Yeob, Kim, Dong Yun, Cho, Kwan Hyung, Maeng, Han-Joo, Jang, Dong-Jin
Format: Journal Article
Language:English
Published: Switzerland MDPI AG 20-03-2019
MDPI
Subjects:
Arthritis
Bioavailability
celecoxib
Cellulose
Cremophor RH40
Drug dosages
fluid-bed granulation
Lactose
nonionic surfactants
Pharmaceuticals
Pharmacokinetics
Scanning electron microscopy
solid dispersion
Surfactants
tableting
United States > US
Japan
Germany
nonionic surfactants
fluid-bed granulation
celecoxib
solid dispersion
pharmacokinetics
tableting
Cremophor RH40
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Summary:The purpose of this study is to develop a solid dispersion system with improved dissolution, absorption, and patient compliance of poorly water-soluble celecoxib (CXB). Instead of sodium lauryl sulfate (SLS), an anionic surfactant used in the marketed product (Celebrex ), solubilization was performed using non-ionic surfactants with low toxicity. Cremophor RH40 (Cre-RH) was selected as the optimal solubilizer. Granules and tablets containing CXB and Cre-RH were prepared via fluid-bed and tableting processes, respectively. The morphology, crystallinity, flowability, dissolution, and pharmacokinetics for CXB-solid dispersion granules (SDGs) and the hardness and friability for CXB-solid dispersion tablets (SDTs) were evaluated. The solubility of CXB was found to be increased by about 717-fold when using Cre-RH. The dissolution of granules containing Cre-RH was found to be increased greatly compared with CXB API and Celebrex (66.9% versus 2.3% and 37.2% at 120 min). The improvement of the dissolution was confirmed to be the same as that of granules in tablets. The CXB formulation resulted in 4.6- and 4.9-fold higher AUC and of CXB compared with those of an oral dose of CXB powder in rats. In short, these data suggest that the solid dispersion based on Cre-RH-a non-toxic solubilizer, non-ionic surfactant- may be an effective formulation for CXB to enhance its oral bioavailability and safety.
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content type line 23
ISSN:1999-4923
1999-4923
DOI:10.3390/pharmaceutics11030136