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Revaprazan-loaded surface-modified solid dispersion: Physicochemical characterization and in vivo evaluation

Title
Revaprazan-loaded surface-modified solid dispersion: Physicochemical characterization and in vivo evaluation
Author
최한곤
Keywords
Revaprazan; surface-modified solid dispersion; unchanged crystalline; drug solubility; oral bioavailability
Issue Date
2019-05
Publisher
TAYLOR & FRANCIS LTD
Citation
PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY, v. 24, No. 6, Page. 788-793
Abstract
The purpose of this research was to develop a novel revaprazan-loaded surface-modified solid dispersion (SMSD) with improved drug solubility and oral bioavailability. The impact of carriers on aqueous solubility of revaprazan was investigated. HPMC and Cremophor A25 were selected as an appropriate polymer and surfactant, respectively, due to their high drug solubility. Numerous SMSDs were prepared with various concentrations of carriers, using distilled water, and the drug solubility of each was assessed. Moreover, the physicochemical properties, dissolution and pharmacokinetics of selected SMSD in rats were assessed in comparison to revaprazan powder. Of the SMSDs assessed, the SMSD composed of revaprazan/HPMC/Cremophor A25 at the weight ratio of 1:0.28:1.12 had the most enhanced drug solubility (approximate to 6000-fold). It was characterized by particles with a relatively rough surface, suggesting that the carriers were attached onto the surface of the unchanged crystalline revaprazan powder. It had a significantly higher dissolution rate, AUC and C-max, and a faster T-max value in comparison to revaprazan powder, with a 5.3-fold improvement in oral bioavailability of revaprazan. Therefore, from an environmental perspective, this SMSD system prepared with water, and without organic solvents, should be recommended as a revaprazan-loaded oral pharmaceutical alternative.
URI
https://www.tandfonline.com/doi/full/10.1080/10837450.2019.1597114https://repository.hanyang.ac.kr/handle/20.500.11754/114465
ISSN
1083-7450; 1097-9867
DOI
10.1080/10837450.2019.1597114
Appears in Collections:
COLLEGE OF PHARMACY[E](약학대학) > PHARMACY(약학과) > Articles
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