Document Detail


Development, characterization and permeability assessment based on caco-2 monolayers of self-microemulsifying floating tablets of tetrahydrocurcumin.
MedLine Citation:
PMID:  23319299     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Novel self-microemulsifying floating tablets were developed to enhance the dissolution and oral absorption of the poorly water-soluble tetrahydrocurcumin (THC). Their physicochemical properties and THC permeability across Caco-2 cell monolayers were assessed. The self-microemulsifying liquid containing THC was adsorbed onto colloidal silicon dioxide, mixed with HPMC, gas-generating agents (sodium bicarbonate and tartaric acid), lactose and silicified-microcrystalline cellulose and transformed into tablets by direct compression. The use of different types/concentrations of HPMC and sodium bicarbonate in tablet formulations had different effects on the floating characteristics and in vitro THC release. The optimum tablet formulation (F2) provided a short floating lag time (∼23 s) together with a prolonged buoyancy (>12 h). About 72% of THC was released in 12 h with an emulsion droplet size in aqueous media of 33.9±1.0 nm while that of a self-microemulsifying liquid was 29.9±0.3 nm. The tablet formulation was stable under intermediate and accelerated storage conditions for up to 6 months. The THC released from the self-microemulsifying liquid and tablet formulations provided an approximately three- to fivefold greater permeability across the Caco-2 cell monolayers than the unformulated THC and indicated an enhanced absorption of THC by the formulations. The self-microemulsifying floating tablet could provide a dosage form with the potential to improve the oral bioavailability of THC and other hydrophobic compounds.
Authors:
Namfa Sermkaew; Kamonthip Wiwattanawongsa; Wichan Ketjinda; Ruedeekorn Wiwattanapatapee
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2013-01-15
Journal Detail:
Title:  AAPS PharmSciTech     Volume:  14     ISSN:  1530-9932     ISO Abbreviation:  AAPS PharmSciTech     Publication Date:  2013 Mar 
Date Detail:
Created Date:  2013-02-26     Completed Date:  2013-08-12     Revised Date:  2014-01-23    
Medline Journal Info:
Nlm Unique ID:  100960111     Medline TA:  AAPS PharmSciTech     Country:  United States    
Other Details:
Languages:  eng     Pagination:  321-31     Citation Subset:  IM    
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MeSH Terms
Descriptor/Qualifier:
Caco-2 Cells
Chromatography, High Pressure Liquid
Curcumin / analogs & derivatives*,  chemistry
Emulsions*
Humans
Kinetics
Microscopy, Electron, Scanning
Permeability
Tablets*
Chemical
Reg. No./Substance:
0/Emulsions; 0/Tablets; 00U0645U03/tetrahydrocurcumin; IT942ZTH98/Curcumin
Comments/Corrections

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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