최한곤
2019-11-26T02:15:20Z
2019-11-26T02:15:20Z
2019-05
PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY, v. 24, No. 6, Page. 788-793
1083-7450
1097-9867
https://www.tandfonline.com/doi/full/10.1080/10837450.2019.1597114
https://repository.hanyang.ac.kr/handle/20.500.11754/114465
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.
This work was supported by National Research Foundation (NRF) of South Korea grants funded by the South Korea government (MEST) [no. 2018R1A2B2004668] and a grant [16173MFDS542] from the Ministry of Food and Drug Safety in 2016.
en_US
TAYLOR & FRANCIS LTD
Revaprazan
surface-modified solid dispersion
unchanged crystalline
drug solubility
oral bioavailability
Revaprazan-loaded surface-modified solid dispersion: Physicochemical characterization and in vivo evaluation
Article
6
24
10.1080/10837450.2019.1597114
788-793
PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY
Park, Jong Hyuck
Cho, Jung Hyun
Kim, Dong Shik
Kim, Jung Suk
Din, Fakhar Ud
Kim, Jong Oh
Yong, Chul Soon
Youn, Yu Seok
Oh, Kyung Taek
Kim, Dong Wuk
Choi, Han-Gon
2019045019
E
COLLEGE OF PHARMACY[E]
DEPARTMENT OF PHARMACY
hangon