Physicochemical characterization and evaluation of microemulsion system for parenteral deliveryof rutaecarpine

摘要

To develop a parenteral preparation containing poorlyrnwater-soluble rutaecarpine using O/W microemulsionrnsystem, the solubility of rutaecarpine in water, ethanol,rnvarious oils and surfactants were investigated. Among thernsurfactants and oils tested, Tween 20/PEG 400 and castor oilrnwere chosen as the surfactant system and oil phase of thernmicroemulsion, as rutaecarpine was most soluble in them,rnrespectively. Pseudoternary phase diagrams werernconstructed to obtain the concentration range of oil,rnsurfactant and cosurfactant for microemulsion formation,rnand the stability test and pharmacokinetics of rutaecarpinerndelivered by microemulsion formation were then evaluated.rnThe rutaecarpine (300rnμg/g)-loaded microemulsionrncomposed of 10.8 % PEG 400, 7.2% Tween 80, 20% casterrnoil and 72% water was stable for at least 6 months. It gavernsignificantly higher AUC of rutaecarpine than didrnsuspension, suggesting that the bioavailability ofrnrutaecarpine in this microemulsion system could bernenhanced. Thus, the microemulsion system composed ofrncastor oil, PEG 400, Tween 80 and water could be a morernstable and effective parenteral dosage form for rutaecarpine.rnKeywords: microemulsion; rutaecarpine; parenteralrndelivery; pharmacokinetics; stability