Improvement of dissolution characteristics of 4-t-butyl-2′-car☐ymethoxy-4′-(3-methyl-2-butenyloxy)chalcone by β-cyclodextrin complexation

Add time:07/26/2019    Source:sciencedirect.com

The inclusion complexation of 4-t-butyl-2′-car☐ymethoxy-4′-(3-methyl-2-butenyloxy)chalcone (SU-740), a newly developed antiulcer agent, with β-cyclodextrin (β-CyD) in water and in solid state was investigated for the purpose of improving the low aqueous solubility and oral bioavailability. SU-740 formed 1:1 and 1:2 (guest:host) inclusion complexes in water and in the solid state and the 1:1 stability constant was much higher than the 1:2 stability constant. The dissolution rate of SU-740 was significantly improved by the complexation with β-CyD, suggesting the enhanced bioavailability.

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