Document Detail


PVP and surfactant combined carrier as an effective absorption enhancer of poorly soluble astilbin in vitro and in vivo.
MedLine Citation:
PMID:  23350723     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
Abstract Context: Astilbin is considered to be a new and promising immunosuppressant for immune related diseases, but limited in clinical application due to its poor water solubility, difficult oral absorption and low bioavailability. Objective: The present work studied the effect of PVP and surfactant combined carrier on its capability to improve drug absorption. Materials and methods: PVP K30-Tween 80 combined carries was applied into the astilbin solid dispersions, tested both in vivo in beagle dogs and in vitro in transport experiments across Caco-2 cell monolayers. Results and discussion: In the animal studies a many fold increase in plasma AUC was observed for the solid dispersions of drug in PVP K30-Tween 80 combined carries compared to active pharmaceutical ingredient (API). The applicability of Caco-2 monolayers as a tool for predicting the in vivo transport behavior of Astilbin in combination with a solubility enhancing carries was shown. In vitro transport studies confirmed the effect of combined carries on the absorption behavior of the astilbin. MTT studies showed the cell viability gradually decreased with the increase of the drug concentration in a dose dependent manner for astilbin and that in solid dispersions. The permeability and apparent permeability coefficients (P(app)) increased with drug in the Caco-2 cell. Conclusion: In this study, it was found that PVP K30 and Tween 80 promoted the permeability of drugs best within a certain amount. For astilbin PVP K30 and surfactant combined carrier had a strong potential to improve oral bioavailability.
Authors:
Yan He; Hongfei Liu; Zhiyong Xie; Qiongfeng Liao; Xiaoping Lai; Zhiyun Du
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2013-1-28
Journal Detail:
Title:  Drug development and industrial pharmacy     Volume:  -     ISSN:  1520-5762     ISO Abbreviation:  Drug Dev Ind Pharm     Publication Date:  2013 Jan 
Date Detail:
Created Date:  2013-1-28     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  7802620     Medline TA:  Drug Dev Ind Pharm     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Affiliation:
School of Chemical Engineering and Light Industry , Guangdong University of Technology, Guangzhou, Guangdong, PR China .
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