Preparation and intestinal absorption studies of tacrolimus cyclodextrin inclusion complexes
HUO Tao-tao
CHEN Xu
ZHANG Qian
SUN Kai-hui
ZHANG Min-xin
TAO Chun
SONG Hong-tao
Abstract：Objective: To prepare tacrolimus ( FK506) cyclodextrin inclusion complexes for improving the dissolution and intestinal absorption efficiency of drug. Methods: Hydroxypropyl-beta-cyclodextrin ( HP-β-CD), Dimethyl-beta-cyclodextrin ( DM-β-CD) and Sulfobutylether-beta-cyclodextrin ( SBE-β-CD) were used as carriers respectively to prepare tacrolimus inclusion complexes by saturated aqueous solution method, and the optimal prescription was screened out by the dissolution in vitro and the influence factors study, meanwhile, the reaction temperature in the preparation of inclusion complex was also investigated. The scanning electronic microscopy ( SEM), differential scanning calorimetry ( DSC) and fourier-transform infrared spectroscopy ( FT-IR) were used to characterize the optimal prescription. Then, raw tacrolimus and the Prografwere used as control to study the intestinal absorption of tacrolimus inclusion complex. Results: The three different cyclodextrins inclusion complexes can improve the dissolution of tacrolimus, and the DM-β-CD inclusion complexes ( FK 506-DM-β-CD) improved the absorption of drug in the duodenum and jejunum. Conclusion: FK 506 DM-β-CD inclusion complexes improved the dissolution in vitro and the intestinal absorption of tacrolimus.
Keywords：tacrolimuscyclodextrin inclusion complexthe dissolution in vitrothe study of intestinal absorption in rats
Publication Date：2018-01-01
Online Publishing Date：2026-08-14(First online date of this platform, not the publication date of the document)
Pages：9( 1918-1926 )