Objective: To study the formulation optimization of epimedium flavonoids self-emulsifying drug delivery system and evaluate its effect in vitro and in vivo.
Methods: Based on the degree of emulsification and emulsifying time, the formulation optimization (i.e., screening of suitable oil phases, nonionic surfactants and co-surfactants) was made by the use of determination of the solubility, orthogonal design and construction of tertiary phase diagram. The dissolution of SEDDS was measured and its pharmacokinetic in rats was measured.
Results: The experimental results revealed the optimized formulation of the self-emulsifying drug delivery system which consisted of oleic acid as oil phase, Tween-80 as nonionic surfactant, and PEG400 as co-surfactant in the proportion of 2:4:4. The dissolution of SEDDS in water was more than 85% in 25 minutes, while that of the epimedium flavonoids capsule was less than 50% in 60 minutes.
Conclusion: Application of the optimized formulation of epimedium flavonoids self-emulsifying drug delivery system could significantly increase the solubility of epimedium flavonoids in water and improve its bioavailability.
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